第7号(2017/02/16公開) 220件 [WO] [US] [EP] [JP]

医薬品特許データベース配信メールサービス

WO

WO2017024406

N-SUBSTITUTED BICYCLIC LACTAMS, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

N-SUBSTITUTED BICYCLIC LACTAMS, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

  • Cpd. 13 を例示
  • NEOMED INST [CA]

ブロモドメイン阻害剤。増殖疾患、自己免疫疾患、炎症疾患、等処置/予防 This application relates to N-substituted bicyclic lactams of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to the N-substituted bicyclic lactams of formula (I) and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.

WO2017024408

ARYL-SUBSTITUTED DIHYDROQUINOLINONES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

ARYL-SUBSTITUTED DIHYDROQUINOLINONES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

  • Cpd. 12 を例示
  • NEOMED INST [CA]

ブロモドメイン阻害剤。増殖疾患、自己免疫疾患、炎症疾患、等処置/予防 This application relates to aryl-substituted dihydroquinolinones of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to aryl-substituted dihydroquinolinones and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.

WO2017024412

SUBSTITUTED BENZIMIDAZOLES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

SUBSTITUTED BENZIMIDAZOLES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

  • Cpd. 6 を例示
  • NEOMED INST [CA]

ブロモドメイン阻害剤。増殖疾患、自己免疫疾患、炎症疾患、等処置/予防 This application relates to substituted benzimidazoles of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted benzimidazoles and to their use as bromodomain inhibitors. The present application also relates to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasm, including tumors and/or cancers.

WO2017024589

IRAK4 INHIBITOR AND USE THEREOF

IRAK4 INHIBITOR AND USE THEREOF

  • Claim 6 下図化合物等
  • BEIJING HANMI PHARMACEUTICAL CO LTD [CN]

IRAK4阻害剤。自己免疫疾患、炎症疾患、血栓塞栓症、ガン等処置 The present invention relates to a compound inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (particularly humans). The compound has a structural formula I.

WO2017024968

VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS

VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS

  • Claim 10 下図を例示
  • MEDSHINE DISCOVERY INC [CN]

FGFR /VEGFR阻害剤。ガン処置 FGFR and VEGFR inhibitors are provided, and compounds represented by formula (I) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.

WO2017024996

HYDROXY AMIDINE DERIVATIVE, PREPARATION METHOD AND USE IN MEDICINE THEREOF

HYDROXY AMIDINE DERIVATIVE, PREPARATION METHOD AND USE IN MEDICINE THEREOF

  • Claim 12 下図化合物等
  • JIANGSU HENGRUI MEDICINE CO [CN] SHANGHAI HENGRUI PHARMACEUTICAL CO LTD [CN]

IDO介在トリプトファン代謝経路関連疾患(AD、免疫疾患、うつ、AIDS等)処置 Provided are a hydroxy amidine derivative, a preparation method and a use in medicine thereof. In particular, provided are the hydroxy amidine derivative as shown by general formula (I), the preparation method thereof and a pharmaceutical composition containing the derivative, and the use thereof for treating diseases having a pathological feature of an IDO-mediated tryptophan metabolic pathway, with these diseases comprising cancer, Alzheimer's disease, immunological diseases, depression, anxiety disorders, cataracts, psychological obstacles and AIDS.

WO2017025031

DIAZAOXA HETEROCYCLIC SPIRO-DIONE PIPERAZINE ALKALOID DERIVATIVE HAVING ANTIVIRAL ACTIVITY AND PREPARATION METHOD THEREOF

DIAZAOXA HETEROCYCLIC SPIRO-DIONE PIPERAZINE ALKALOID DERIVATIVE HAVING ANTIVIRAL ACTIVITY AND PREPARATION METHOD THEREOF

  • Claim 12 下図化合物等
  • YU YUE [CN]

抗ウイルス(RSV, HSV-1,EV71)剤 Disclosed is a diazaoxa heterocyclic spiro-dione piperazine alkaloid derivative having an antiviral activity and a preparation method thereof. The compound is a compound of formula (I), has anti-RSV, HSV-1 and EV71 activities and has the following structure.

WO2017025058

SUBSTITUTED INDOLE COMPOUNDS AND THEIR USING METHODS AND USES

SUBSTITUTED INDOLE COMPOUNDS AND THEIR USING METHODS AND USES

  • Claim 6 下図を例示
  • SUNSHINE LAKE PHARMA CO LTD [CN]

5-HT再吸収阻害薬/5-HT1A受容体作動薬。CNS疾患処置 Provided are substituted indole compounds and their using methods and uses. In particular, disclosed are indole compounds for 5-hydroxytryptamine reuptake inhibition and/or 5-HT1A receptor agonists, and their pharmaceutical compositions. Also provided are preparation methods of the compounds and the pharmaceutical compositions, and their uses in treating central nervous system disorder

WO2017025064

IRAK4 INHIBITOR AND USE THEREOF

IRAK4 INHIBITOR AND USE THEREOF

  • Claim 6 下図化合物等
  • BEIJING HANMI PHARMACEUTICAL CO LTD [CN]

IRAK4阻害剤。自己免疫疾患、炎症疾患、血栓塞栓症、ガン等処置 Disclosed are a compound related to inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (especially humans). The compound has a structural formula I.

WO2017025368

INDANYLAMINOPYRIDYLCYCLOPROPANECARBOXYLIC ACIDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

INDANYLAMINOPYRIDYLCYCLOPROPANECARBOXYLIC ACIDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

  • Claim 9 下図化合物等
  • BOEHRINGER INGELHEIM INT [DE]

GPR40受容体に結合、活性をモジュレート。2型糖尿病、等代謝疾患処置/予防 The present invention relates to compounds of general formula, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

WO2017025416

COMPOUNDS

COMPOUNDS

  • Claim 7
  • GLAXOSMITHKLINE IP DEV LTD [GB] UNIV OF DUNDEE [GB]

寄生生物病処置 A compound of Formula (I), or a salt thereof, compositions comprising the compound, processes for its preparation and its use in therapy, for example in the treatment of parasitic diseases such as Chagas disease, Human African Trypanosomiasis (HAT), Animal African trypanosomiasis (AAT) and leishmaniasis, particularly visceral leishmaniasis (VL).

WO2017025491

BACE1 INHIBITORS

BACE1 INHIBITORS

  • Claim 16 Ex. 1AB 下図を例示
  • F HOFFMANN-LA ROCHE AG [CH] HOFFMANN-LA ROCHE INC [US]

BACE1阻害剤。AD等治療/予防 The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

WO2017025493

QUINOLINE EZH2 INHIBITORS

QUINOLINE EZH2 INHIBITORS

  • Ex. 3 を例示
  • BAYER PHARMA AG [DE] THE BROAD INST OF MIT AND HARVARD INC [US]

EZH2 阻害剤。ガン処置 The present invention relates to quinolines of general formula (I) to methods for their preparation, to intermediates for their preparation, to pharmaceutical compositions comprising at least one of those compounds, and to the use thereof, for use in the treatment of cancer..

WO2017025523

PYRIDINE AND PYRIMIDINE DERIVATIVES

PYRIDINE AND PYRIMIDINE DERIVATIVES

  • Claim 16 Ex. 13 を例示
  • F HOFFMANN-LA ROCHE AG [CH] HOFFMANN-LA ROCHE INC [US]

精神疾患(統合失調症、双極性障害、強迫性障害、自閉症等)処置 The present invention relates to compounds of formula (I); or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

WO2017025559

2-AMINO-3-FLUORO-3-(FLUOROMETHYL)-6-METHYL-6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINS AS BACE1 INHIBITORS

2-AMINO-3-FLUORO-3-(FLUOROMETHYL)-6-METHYL-6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINS AS BACE1 INHIBITORS

  • Claim 17. N-(3-((2S,5S)-6-amino-5-fluoro-5-(fluoromethyl)-2-methyl-2,3,4,5-tetrahyd- ropyridin-2-yl)-4-fluorophenyl)-5-methoxypicolinamide; Ex. 1 を例示
  • H LUNDBECK AS [DK]

BACE1阻害剤。神経変性疾患、認知障害処置 The present invention provides compounds of Formula (I) for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula (I).

WO2017025562

SUBSTITUTED 1,2-DIHYDRO-3H PYRROLO[1,2-c]IMIDAZOL-3 ONE ANTIBACTERIALS

SUBSTITUTED 1,2-DIHYDRO-3H PYRROLO[1,2-c]IMIDAZOL-3 ONE ANTIBACTERIALS

  • Claim 11 Ex. 1 を例示
  • ACTELION PHARMACEUTICALS LTD [CH]

抗細菌剤 The invention relates to antibacterial compounds of formula (I).

WO2017025565

2-AMINO-7A-PHENYL-3,4,4A,5,7,7A-HEXAHYDROFURO[3,4-B]PYRIDINES AS BACE1 INHIBITORS

2-AMINO-7A-PHENYL-3,4,4A,5,7,7A-HEXAHYDROFURO[3,4-B]PYRIDINES AS BACE1 INHIBITORS

  • Claim 13 EX. 6 を例示
  • H LUNDBECK AS [DK]

BACE1阻害剤。AD 等処置 Compounds of the Formula (I) are provided which compounds are inhibitors of BACE. A method for the treatment of a disease selected from Alzheimer's disease etc.

WO2017025695

AZETIDINE CARBOXYLIC COMPOUNDS FOR TREATING DISEASES INVOLVING THE NURR1 NUCLEAR RECEPTORS

AZETIDINE CARBOXYLIC COMPOUNDS FOR TREATING DISEASES INVOLVING THE NURR1 NUCLEAR RECEPTORS

  • Claim 7 Ex. 1 を例示
  • INVENTIVA [FR]

NURR1受容体モジュレーター。タウオパシー予防/処置 The invention concerns the compounds of formula (l) in which W, X, Y, Z and Het are as defined in the description. The compounds of formula (I) are modulators of the NURR1 receptor.

WO2017025802

DPEP-1 BINDING COMPOSITIONS AND METHODS OF USE

DPEP-1 BINDING COMPOSITIONS AND METHODS OF USE

  • 小分子例
  • ARCH BIOPARTNERS INC [CA]

DPEP-1結合性化合物。炎症軽減、腫瘍転移阻止、急性腎障害阻止/軽減、等 Pharmaceutical compositions and methods of their use are provided for reducing inflammation in a subject, blocking leukocyte recruitment, inhibiting tumor metastasis, treating sepsis and preventing/reducing acute kidney injury.

WO2017025849

BICYCLIC-FUSED HETEROARYL OR ARYL COMPOUNDS

BICYCLIC-FUSED HETEROARYL OR ARYL COMPOUNDS

  • Claim 10 Ex. 28 を例示
  • PFIZER [US]

IRAK4阻害剤。自己免疫疾患、炎症疾患、疼痛、等処置 Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of lnterleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification. A method of treating a disease or condition selected from the group consisting of autoimmune diseases, inflammatory diseases, pain conditions, etc.

WO2017025864

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

  • Ex. 55 を例示
  • VIIV HEALTHCARE UK (NO 5) LTD [GB]

HIVインテグラーゼ阻害剤。HIV感染/AIDS、処置 Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

WO2017025868

3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE

3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE

  • Claim 12 Ex. 167 を例示
  • PFIZER [US] ITEOS THERAPEUTICS [BE]

TD02阻害剤。ガン、(PD、AD、等)神経変性疾患、(HCV、HIV、等)慢性ウイルス感染、うつ、肥満、等処置/予防 A compound of Formula (I) is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula (I) as TD02 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula (I).

WO2017025899

NOVEL C28-AMIDES WITH C3-MODIFICATIONS OF TRITERPENE DERIVATIVES AS HIV INHIBITORS

NOVEL C28-AMIDES WITH C3-MODIFICATIONS OF TRITERPENE DERIVATIVES AS HIV INHIBITORS

  • Claim 3 Ex. 1 を例示
  • HETERO RES FOUND [IN]

HIV阻害剤。HIV介在疾患処置 Formula (I) The present invention relates to novel C28-amides with C3-modifications of triterpene compounds of formula (I); or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, tautomers, stereoisomers, prodrugs or combination thereof. The present invention also relates to pharmaceutical compositions comprising compounds of formula (I) useful for the therapeutic treatment of viral mediated diseases and particularly HIV mediated diseases.

WO2017025901

NOVEL C28-ANALOGUES WITH C3-MODIFICATIONS OF TRITERPENE DERIVATIVES AS HIV INHIBITORS

NOVEL C28-ANALOGUES WITH C3-MODIFICATIONS OF TRITERPENE DERIVATIVES AS HIV INHIBITORS

  • Claim 7 Ex. 1 を例示
  • HETERO RES FOUND [IN]

HIV介在疾患処置 The present invention relates to compounds of novel C28-analogues with C3- modifications of triterpene derivatives of formula (I); or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, tautomers, stereoisomers, prodrugs, compositions or combination thereof. The present invention also relates to pharmaceutical compositions comprising compounds of formula (I) useful for the treatment of viral diseases and particularly HIV mediated diseases.

WO2017025913

IMIDAZOPYRIDINE MACROCYCLES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

IMIDAZOPYRIDINE MACROCYCLES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

  • Ex. 1 を例示
  • VIIV HEALTHCARE UK (NO 5) LTD [GB]

HIVインテグラーゼ阻害剤。HIV感染/AIDS、処置 Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

WO2017025914

5-(N-FUSED TRICYCLIC ARYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3- YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

5-(N-FUSED TRICYCLIC ARYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3- YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

  • Cpd. 1 を例示
  • VIIV HEALTHCARE UK (NO 5) LTD [GB]

HIVインテグラーゼ阻害剤。HIV感染/AIDS、処置 Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

WO2017025915

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

  • Ex. 24 を例示
  • VIIV HEALTHCARE UK (NO 5) LTD [GB]

HIVインテグラーゼ阻害剤。HIV感染/AIDS、処置 Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

WO2017025916

5-(N-[6,5]-FUSED BICYCLIC ARYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

5-(N-[6,5]-FUSED BICYCLIC ARYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

  • Cpd. 2 を例示
  • VIIV HEALTHCARE UK (NO 5) LTD [GB]

HIVインテグラーゼ阻害剤。HIV感染/AIDS、処置 Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

WO2017025917

5-(N-BENZYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

5-(N-BENZYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

  • Cpd. 116 を例示
  • VIIV HEALTHCARE UK (NO 5) LTD [GB]

HIVインテグラーゼ阻害剤。HIV感染/AIDS、処置 Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

WO2017025918

5-BROMO-2,6-DI-(LH-PYRAZOL-L-YL)PYRIMIDIN-4-AMINE FOR USE IN THE TREATMENT OF CANCER

5-BROMO-2,6-DI-(LH-PYRAZOL-L-YL)PYRIMIDIN-4-AMINE FOR USE IN THE TREATMENT OF CANCER

  • Claim 1
  • NOVARTIS AG [CH] PALOBIOFARMA SL [ES] (+5)

A2A拮抗剤。ガン処置 The present invention relates to 5-bromo-2,6-di-(1 H-pyrazol-1-yl)pyrimidin-4-amine, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compounds for use in the treatment of cancer. A2A antonist.

WO2017025951

PILLARARENES AND USES THEREOF

PILLARARENES AND USES THEREOF

  • Cpd. 30 を例示
  • RAMOT AT TEL-AVIV UNIVERSITY LTD. [IL/IL];

バイオフィルム形成阻害剤 The present invention provides cationic pillar[n]arenes, e.g., positively charged poly-ammonium, poly-phosphonium and poly-imidazolium pillar[5-6]arene derivatives, capable of inhibiting or preventing biofilm formation, and facilitating existing biofilm decomposition; as well as compositions thereof and methods of use.

WO2017026516

イソチアゾール誘導体

イソチアゾール誘導体

  • 実施例2を例示
  • MOCHIDA PHARM CO LTD [JP]

本発明は、式(I)で表される化合物、又は製薬学的に許容されるその塩又はそれらの溶媒和物を提供する。本発明によりNrf2活性化能を有する化合物が提供される。Nrf2が関与する疾患、例えば多発性硬化症、乾癬等の予防及び/又は治療剤

WO2017026718

NOVEL 3-(ISOXAZOL-3-YL)-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE COMPOUND, WHICH IS RET KINASE INHIBITOR

NOVEL 3-(ISOXAZOL-3-YL)-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE COMPOUND, WHICH IS RET KINASE INHIBITOR

  • Ex. 1 を例示
  • KOREA INST SCI & TECH [KR]

RETキナーゼ阻害剤。ガン予防/処置 The present invention relates to a novel 3-(isoxazol-3-yl)-pyrazolo[3,4-d]pyrimidin-4-amine compound, a preparation method for the compound, and a pharmaceutical use of the compound to be used in the prevention and treatment of various cancer diseases caused by the activity of RET kinases.

WO2017027064

8-HYDROXYQUINOLINE DERIVATIVES AS DIAGNOSTIC AND THERAPEUTIC AGENTS

8-HYDROXYQUINOLINE DERIVATIVES AS DIAGNOSTIC AND THERAPEUTIC AGENTS

  • Claim 64 下図化合物等
  • MASSACHUSETTS GEN HOSPITAL [US]

メタルキレート化合物。診断/処置薬。AD等神経疾患、ガン、処置 The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single- photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.

WO2017027136

THERAPEUTIC AGENTS CONTAINING CANNABIS FLAVONOID DERIVATIVES FOR THE PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISORDERS

THERAPEUTIC AGENTS CONTAINING CANNABIS FLAVONOID DERIVATIVES FOR THE PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISORDERS

  • Claim 2
  • FLAVOCURE BIOTECH LLC [US] LOWE HENRY IC [JM] (+1)

PD、AD、等神経変性疾患、予防/処置 The present invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected from the group of Apigenin, Cannflavin A, Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin, (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain diseases of the CNS system and related disorders.

WO2017027309

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

  • Cpd. 1 を例示
  • JANSSEN PHARMACEUTICA NV [BE] HUANG HUI [US]

GPR40受容体作動薬。2型糖尿病、処置 Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I), as follows: wherein R1, R2, R4, W, X, Y, and G, are defined herein.

WO2017027310

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

  • Cpd. 53 を例示
  • JANSSEN PHARMACEUTICA NV [BE] HUANG HUI [US]

GPR40受容体作動薬。2型糖尿病、処置 Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula II.

WO2017027312

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

  • Cpd. 44 を例示
  • JANSSEN PHARMACEUTICA NV [BE] HUANG HUI [US]

GPR40受容体作動薬。2型糖尿病、処置 Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (III).

WO2017027343

CGRP RECEPTOR ANTAGONISTS

CGRP RECEPTOR ANTAGONISTS

  • Claim 10
  • LILLY CO ELI [US]

CGRP受容体拮抗薬。片頭痛処置 The present invention provides a compound of Formula II: (II) or a pharmaceutically acceptable salt thereof, for use in the treatment of .migraine.

WO2017027345

CGRP RECEPTOR ANTAGONISTS

CGRP RECEPTOR ANTAGONISTS

  • Claim 10
  • LILLY CO ELI [US]

CGRP受容体拮抗薬。片頭痛処置 The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof, for use in the treatment of .migraine.

WO2017027357

PYRIDAZINONES AND THEIR USE IN THE TREATMENT OF CANCER

PYRIDAZINONES AND THEIR USE IN THE TREATMENT OF CANCER

  • Ex. 1
  • ARNÉR ELIAS SET JENÖ [SE] US HEALTH [US]

ガン処置 There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cancers.

WO2017027358

TRICYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER

TRICYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER

  • Ex. 58 を例示
  • ARNER ELIAS SET JENÖ [SE] THE UNITED STATES OF AMERICA AS REPESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES [US]

ガン処置。チオレドキシンレダクターゼ 阻害剤 There is provided compounds of formula (I), or pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cancers, through specific and potent inhibition of thioredoxin reductase.without targeting of glutathione reductase.

WO2017027359

PYRIDINES AND THEIR USE IN THE TREATMENT OF CANCER

PYRIDINES AND THEIR USE IN THE TREATMENT OF CANCER

  • Ex. 1 を例示
  • ARNÉR ELIAS SET JENÖ [SE] THE USA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES [US]

ガン処置 There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cancers.

WO2017027434

ANTIVIRAL BETA-AMINO ACID ESTER PHOSPHODIAMIDE COMPOUNDS

ANTIVIRAL BETA-AMINO ACID ESTER PHOSPHODIAMIDE COMPOUNDS

  • Ex. 24A を例示
  • MERCK SHARP & DOHME [US] VACHAL PETR [US] (+3)

HIV感染予防/処置 Compounds of Formula (I) and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

WO2017027512

USE OF LAQUINIMOD TO TREAT TRAUMATIC BRAIN INJURY

USE OF LAQUINIMOD TO TREAT TRAUMATIC BRAIN INJURY

  • ラキニモド
  • TEVA PHARMA [IL] LAMB BRUCE [US] (+1)

ラキニモドによる外傷性脳損傷処置 This application provides for a method of treating a subject suffering from traumatic brain injury, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application also provides use of laquinimod in the manufacture of a medicament for treating a subject suffering from traumatic brain injury. This application also provides laquinimod for use in treating a subject suffering from traumatic brain injury. This application also provides use of laquinimod in treating a subject suffering from traumatic brain injury. This application also provides a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from traumatic brain injury. This application also provides a pharmaceutical oral unit dosage form of laquinimod for use in treating a subject suffering from traumatic brain injury.

WO2017027544

COMBINATION THERAPY FOR CANCER

COMBINATION THERAPY FOR CANCER

  • N-(3-fluoro-4-(1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yloxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide
  • IMCLONE LLC [US]

ヒトVEGFR2 に結合する抗体と右図化合物ガン併用療法 The present invention relates to a combination of an anti-human VEGFR2 antibody, preferably ramucirumab, and N-(3-fluoro-4-(1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yloxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide, and to methods of using the combination to treat certain disorders, such as gastric cancer.

WO2017027564

COMPOSITIONS AND METHODS FOR TREATING ALOPECIA

COMPOSITIONS AND METHODS FOR TREATING ALOPECIA

  • Claim 7
  • RIVER TOWN THERAPEUTICS INC [US]

脱毛症処置。ミノキシジル、シクロスポリンA、FK506結合タンパク質4に結合する化合物(右図)を用いる The present invention is directed to a composition for treating alopecia containing minoxidil, cyclosporine A and a compound that binds FK506 binding protein 4 suitable for administration to humans. The present invention is further directed to treating alopecia in humans by administering a composition of the invention.

WO2017027571

MECHANISM OF RESISTANCE TO BET BROMODOMAIN INHIBITORS

MECHANISM OF RESISTANCE TO BET BROMODOMAIN INHIBITORS

  • Claim 6 BET inhibitor is JQ1, Claim 8 PP2A activator is FTY720
  • DANA-FARBER CANCER INSTITUTE, INC. [US/US];

BET阻害剤とPP2A活性化剤等による、ガン相乗併用療法 The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MEDl) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal

WO2017027582

COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS

COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS

  • Claim 23
  • ALZHEON INC [US]

Aβに結合、AD等神経変性疾患処置/予防 Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease. Compounds of the present invention have been found to bind Aβ, and therefore may be useful for the treatment and/or prevntion of neurodegenerative disorders.

WO2017027600

GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF α7-NICOTINIC ACETYLCHOLINE RECEPTORS

GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF α7-NICOTINIC ACETYLCHOLINE RECEPTORS

  • Cpd. (R)-20 Ex. 20 を例示
  • FORUM PHARMACEUTICALS INC [US]

α7- nAChR作動薬。認知機能、維持/処置/改善 The present invention relates to novel geminal substituted aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

WO2017027645

CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS

CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS

  • Claim 12 下図を例示
  • MERCK SHARP & DOHME [US] ALTMAN MICHAEL D [US] (+13)

1型インターフェロン産生誘導。STING作動薬 A class of polycyclic compounds of general formula (II), of general formula (II'), or of general formula (II"), that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

WO2017027651

METHOD AND COMPOSITION FOR TREATING CACHEXIA AND EATING DISORDERS

METHOD AND COMPOSITION FOR TREATING CACHEXIA AND EATING DISORDERS

  • cyproheptadine (CYP)、 cannabidiol (CBD)
  • INDIA GLOBALIZATION CAPITAL INC [US]

カヘキシー/摂食障害、処置。CYP、CBDを処方 The invention provides treating cachexia and eating disorders in humans and veterinary animals by administering a composition including: (i) cyproheptadine (CYP); and (ii) a cannabis compound selected from the group of cannabidiol (CBD) and mixtures of CBD and up to 50% tetrahydrocannabinol (THC).

WO2017027678

SALTS OF AN LSD1 INHIBITOR

SALTS OF AN LSD1 INHIBITOR

  • 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2- phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid,
  • INCYTE CORP [US]

LSD1阻害剤。ガン処置。結晶特許 The present disclosure relates to tosylate salts 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2- phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the LSD1-associated or mediated diseases such as cancer.

WO2017027684

FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME

FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME

  • Ex. 103 を例示
  • ZAFGEN INC [US]

フマギロール化合物。肥満処置 Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

WO2017027687

FUMAGILLOL SPIROCYCLIC COMPOUNDS AND FUSED BICYCLIC COMPOUNDS AND THEIR USE AS METAP2 INHIBITORS

FUMAGILLOL SPIROCYCLIC COMPOUNDS AND FUSED BICYCLIC COMPOUNDS AND THEIR USE AS METAP2 INHIBITORS

  • Ex. 1 を例示
  • ZAFGEN INC [US]

フマギロール化合物。肥満処置 Disclosed herein are fumagillol compounds of Formula (I) or Formula (Ia); and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

WO2017027717

BICYCLIC FUSED PYRIMIDINE COMPOUNDS AS TAM INHIBITORS

BICYCLIC FUSED PYRIMIDINE COMPOUNDS AS TAM INHIBITORS

  • Claim 55 Ex. 1 を例示
  • INCYTE CORP [US]

TAM阻害剤。ガン等処置 This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.

WO2017027768

COMPOSITIONS AND METHODS FOR TREATING TUBERCULOSIS

COMPOSITIONS AND METHODS FOR TREATING TUBERCULOSIS

  • Cpd. 97 を例示
  • THE BROAD INST INC [US]

細菌(結核菌)感染処置 The present invention provides compounds for the treatment of a bacterial infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the treatment of a bacterial infection in a subject.

WO2017027845

PHENYLSULFONAMIDO-BENZOFURAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF PROLIFERATIVE DISEASES

PHENYLSULFONAMIDO-BENZOFURAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF PROLIFERATIVE DISEASES

  • Claim 67 下図化合物等
  • MEMORIAL SLOAN-KETTERING CANCER CENTER [US] ALBERT EINSTEIN COLLEGE OF MEDICINE INC [US] (+3)

BCL-2ファミリープロテイン阻害剤。増殖疾患(ガン、炎症疾患、自己免疫疾患)処置/予防 Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and/or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and/or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.

WO2017027883

ATROPISOMERISM FOR INCREASED KINASE INHIBITOR SELECTIVITY

ATROPISOMERISM FOR INCREASED KINASE INHIBITOR SELECTIVITY

  • Claim 9
  • SAN DIEGO STATE UNIV RES FOUND [US]

キナーゼ阻害剤アトロプ異性体。ガン増殖阻止 The invention provides a series of conformationally stable kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds. A method of inhibiting the growth of cancer cells.

US

20170042889

AMINO PYRAZINE DERIVATIVES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

AMINO PYRAZINE DERIVATIVES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

  • Ex.8 を例示
  • NOVARTIS AG [CH]

PI 3-キナーゼガンマイソフォーム阻害剤。呼吸器疾患、アレルギー、RA、ガン、アテローム性動脈硬化症、糖尿病、等処置 The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform, for use in the treatment of respiratory diseases, allergies, rheumatoid arthritis, osteoarthritis, rheumatic disorders, psoriasis, ulcerative colitis, Crohn's disease, septic shock, proliferative disorders such as cancer, atherosclerosis, allograft rejection following transplantation, diabetes, stroke, obesity and restenosis. .

20170042897

TRIAZOLE AGONISTS OF THE APJ RECEPTOR 20170044131 同様特許

TRIAZOLE AGONISTS OF THE APJ RECEPTOR 

20170044131 同様特許

  • Ex. 772.0 を例示
  • AMGEN INC. [US]

APJ 受容体作動薬。心血管疾患、等処置 Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions.

20170042907

PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY

PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY

  • Claim 46
  • Galera Labs, LLC [US]

酸化損傷阻止、抗炎症作用 Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula --OC(O)X1each of the two axial ligands has the formula --OC(O)X1. Certain of these compounds have also been shown to possess potent anti-inflammatory activity and prevent oxidative damage in vivo.

20170043029

AMPHOTERICIN B DERIVATIVES

AMPHOTERICIN B DERIVATIVES

  • Fig. 3A を例示
  • Ramot at Tel-Aviv University Ltd. [IL] Technion Research & Development Foundation Ltd. [IL]

アムホテリシンB誘導体。抗真菌作用を保ち、溶解性向上、毒性軽減 Embodiments of the invention provide derivatives of Amphotericin B having increased solubility and reduced toxicity relative to AMB, while retaining antifungal activity against multiple clinical fungal isolates. Derivatives of AMB are provided comprising a polymer group having an amine group, the polymer linked to mycosamine via a relatively stable linker such as an amide linker. The derivatives may be of the general formula [I]:, and pharmaceutically acceptable salts, solvates, hydrates, diastereomers, and prodrugs of the compound of Formula [I].

20170044092

NOVEL CANNABIDIOL QUINONE DERIVATIVES

NOVEL CANNABIDIOL QUINONE DERIVATIVES

  • Clai 4 下図を例示
  • VIVACELL BIOTECHNOLOGY ESPANA S.L. Cordoba ES]

カンナビジオールキノン誘導体。PPARgモジュレーター。アテローム性動脈硬化症、IBD、RA、神経変性疾患、ガン、2型糖尿病、等処置 The present invention relates to novel cannabidiol quinone derivatives of formula (I) (I). The invention also relates to the use of any of the compounds of formula (I) as medicamentsin therapy, particularly for treating diseases and conditions responsive to PPARg modulation due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds, wherein the PPARg mediated disease is selected from: atherosclerosis, inflammatory bowel diseases, rheumatoid arthritis, liver fibrosis, nephropathy, psoriasis, skin wound healing, skin regeneration, pancreatitis, gastritis, neurodegenerative disorders, neuroinflammatory disorders scleroderma, cancer, hypertension, obesity, or type II diabetes.

20170044095

COMPOUNDS FOR THE TREATMENT OF SEIZURES AND OTHER CENTRAL NERVOUS SYSTEM DISORDERS AND CONDITIONS

COMPOUNDS FOR THE TREATMENT OF SEIZURES AND OTHER CENTRAL NERVOUS SYSTEM DISORDERS AND CONDITIONS

  • Claim 17 下図化合物等
  • Ketogen, Inc. [CA]

てんかん発作等CNS疾患処置 The present application relates to novel compounds comprising a moiety that leads to the metabolic production of ketones bonded to a ketone-potentiated anti-epileptic drug, compositions comprising these compounds, and their use, for example for the treatment of epilepsy, and other CNS diseases, disorders or conditions. In particular, the present application includes compounds of Formula I, and compositions and uses thereof:

20170044096

Augmenting Moieties for Anti-Inflammatory Compounds

Augmenting Moieties for Anti-Inflammatory Compounds

  • Claim 44 下図化合物等 
  • Rutgers, The State University of New Jersey [US] Lehigh University [US]

効力増強された抗炎症剤。アミノ酸コンジュゲート Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

20170044097

ANTIBACTERIALS AND/OR MODULATORS OF BIOFILM FORMATION AND METHODS OF USING THE SAME

ANTIBACTERIALS AND/OR MODULATORS OF BIOFILM FORMATION AND METHODS OF USING THE SAME

  • Claim 17 下図化合物等
  • INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION [US]

抗細菌作用。バイオフィルム形成阻害 Amides substituted with aromatic groups were synthesized and some were purified to create enantiomer pure compounds. The compounds were tested to determine their ability to inhibit the growth of bacteria and the formation of biofilms created by bacteria. Some of these compounds were found to be effective antibacterials and to effectively inhibit the formation of biofilms.

20170044098

Heterodimers of Glutamic Acid

Heterodimers of Glutamic Acid

  • Claim 72 下図を例示
  • Molecular Insight Pharmaceuticals, Inc. [US]

NAALADase阻害関連疾患(前立腺ガン等)、処置/管理 Compounds of Formula (Ia), which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

20170044100

INHIBITORS OF DRUG-RESISTANT MYCOBACTERIUM TUBERCULOSIS

INHIBITORS OF DRUG-RESISTANT MYCOBACTERIUM TUBERCULOSIS

  • Claim 18
  • THE JOHNS HOPKINS UNIVERSITY [US] UNIVERSITY OF ILLINOIS AT CHICAGO [US]

抗(薬剤抵抗性)結核菌薬 The present invention provides novel indoleamide compounds for treating tuberculosis, including drug-resistant M-tuberculosis, compositions comprising the indoleamides and methods of using the indoleamides in conjunction with other biologically active agents for the treatment of tuberculosis in a subject in need thereof.

20170044101

SALTS OF AN LSD1 INHIBITOR

SALTS OF AN LSD1 INHIBITOR

  • 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid Cpd. 1
  • WANG; Guangdi [US] Zheng; Shilong [US] Zhong; Qui [US] Zheng; Qiang [US]

LSD1阻害剤。ガン処置。結晶特許 Combretastatins analog compounds and their pharmaceutically acceptable salts are presented, as well as pharmaceutical compositions comprising the combretastatin analog compounds and uses of the combretastatin analog compounds, either alone or in combination with at least one additional therapeutic agent, in the treatment of cancer, and in particular cancer presenting as metastatic tumors.

20170044103

ANTI-VASCULATURE AND ANTI-TUBULIN COMBRETASTATIN ANALOGS FOR TREATMENT OF CANCER

ANTI-VASCULATURE AND ANTI-TUBULIN COMBRETASTATIN ANALOGS FOR TREATMENT OF CANCER

  • Claim 4. 2-bromo-6-(3,4,5-trimethoxyphenyl)pyridine Cpd. 2a を例示
  • WANG; Guangdi [US] Zheng; Shilong [US] Zhong; Qui [US] Zheng; Qiang [US]

コンブレタスタチンアナログ。抗血管新生/抗チューブリン活性。抗ガン剤 Combretastatins analog compounds and their pharmaceutically acceptable salts are presented, as well as pharmaceutical compositions comprising the combretastatin analog compounds and uses of the combretastatin analog compounds, either alone or in combination with at least one additional therapeutic agent, in the treatment of cancer, and in particular cancer presenting as metastatic tumors.

20170044107

Inhibitors of JMJD2C as Anticancer Agents

Inhibitors of JMJD2C as Anticancer Agents

  • Claim 14. 5-((2-morpholinoethylamino)methyl)quinolin-8-ol (Cpd.d SD70-17)
  • The J. David Gladstone Institutes [US]

ヒストン脱メチル化酵素JMJD2阻害剤。CRPC等処置 The present disclosure provides compounds, pharmaceutical compositions and related methods for the treatment of cancer, e.g., castration-resistant prostate cancer (CRPC). Specifically, the present disclosure provides a series of 8-hydroxyquinoline derivatives which show cytotoxic effects on androgen-independent prostate cancer cells. A method of inhibiting histone demethylase JMJD2C.

20170044110

Pyrimidine Compounds and Use as Anti-Cervical Cancer Thereof

Pyrimidine Compounds and Use as Anti-Cervical Cancer Thereof

  • Claim 16. 4-(4-tert-butylbenzylamino)-5-formaldoxime-6-chloropyrimidine
  • SICHUAN UNIVERSITY [CN]

抗子宮頸がん剤。抗ヒトパピローマウイルス活性 Provided is use of a pyrimidine compound or a pharmaceutically acceptable salt thereof in preparation of an anti-cervical cancer medicament. Research of the present invention has found that the above-mentioned pyrimidine compound can be effective against cervical cancer, and has a good inhibition effect on E6 and E7 of HPV16, and indicates that the above-mentioned pyrimidine compound also has a good anti-human papilloma virus effect, providing a new choice for clinical medication.

20170044111

JANUS KINASE INHIBITORS AND USES THEREOF

JANUS KINASE INHIBITORS AND USES THEREOF

  • Claim 51 下図を例示
  • Dana-Farber Cancer Institute, Inc. [US]

JAK3等に共有結合/非共有結合で結合、阻害。増殖疾患、炎症疾患、自己免疫疾患、疼痛、ウイルス感染、処置/予防 The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection). (I) (II)

20170044112

HYDROPHOBICALLY TAGGED JANUS KINASE INHIBITORS AND USES THEREOF

HYDROPHOBICALLY TAGGED JANUS KINASE INHIBITORS AND USES THEREOF

  • Claim 38 下図化合物等
  • Dana-Farber Cancer Institute, Inc. [US]

疎水性基を付けたヤヌスキナーゼ阻害剤。共有結合/非共有結合で結合。増殖疾患、炎症疾患、自己免疫疾患、疼痛、ウイルス感染、処置/予防 The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety R.sup.H may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).

20170044115

NOVEL DISUBSTITUTED 1, 2, 4-TRIAZINE COMPOUND

NOVEL DISUBSTITUTED 1, 2, 4-TRIAZINE COMPOUND

  • Ex. 86 を例示
  • MITSUBISHI TANABE PHARMA CORPORATION [JP]

アルドステロン生合成酵素阻害剤。高血圧等アルドステロン関連疾患処置 This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I], or a pharmaceutically acceptable salt thereof.

20170044117

SEMICARBAZIDE-SENSITIVE AMINE OXIDASE INHIBITORS FOR USE AS ANALGESICS IN TRAUMATIC NEUROPATHY AND NEUROGENIC INFLAMMATION

SEMICARBAZIDE-SENSITIVE AMINE OXIDASE INHIBITORS FOR USE AS ANALGESICS IN TRAUMATIC NEUROPATHY AND NEUROGENIC INFLAMMATION

  • Claim 4. 3-(4,5-diphenyl-1,3-oxazol-2-yl)propanal oxime.
  • PECSI TUDOM NYEGYETEM [HU]

SSAO/VAP-1阻害剤。外傷性神経障害/炎症由来の痛覚過敏、異痛症処置 The invention relates to a compound having SSAO/VAP-1 inhibitor activity for use in the treatment of hyperalgesia and allodynia implicated in traumatic neuropathy or neurogenic inflammation. Accordingly, the invention relates to a compound having SSAO/VAP-1 inhibitor activity for use in the inhibition of pathological activation and dysfunctions of peptidergic sensory nerves caused by mechanical damage or chemical activation of peptidergic sensory nerves in neurogenic inflammation.

20170044118

SALT COMPOUND

SALT COMPOUND

  • Claim 1
  • SGC PHARMA, INC. [CA]

神経変性疾患軽減、神経保護作用、認知機能増強 A salt compound, and methods for mitigating neurodegeneration, effecting, neuroprotection and/or effecting cognition enhancement in a subject using the salt compound are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic salt compound comprising, a nitrate ester.

20170044119

2,2'-TANDEM DITHIAZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF

2,2'-TANDEM DITHIAZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF

  • Claim 51 下図を例示
  • SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN]

ヒストンデアセチレース阻害剤。抗腫瘍剤。自己免疫疾患/2型糖尿病、/神経変性疾患、処置剤 The present invention relates to a thiazole-based compound, a preparation method therefor, and a use thereof. More specifically, the present invention relates to a 2,2'-bis-thiazole-based compound, a preparation method therefor, and a use of 2,2'-bis-thiazole-based compound a histone deacetylase inhibitor in the preparation of an antitumor medicament, a medicament for treating autoimmune diseases, a medicament for treating type II diabetes mellitus and complication thereof, or a medicament for treating neurodegenerative diseases.

20170044121

TETRA-O-SUBSTITUTED BUTANE-BRIDGE MODIFIED NDGA DERIVATIVES, THEIR SYNTHESIS AND PHARMAECUTICAL USE

TETRA-O-SUBSTITUTED BUTANE-BRIDGE MODIFIED NDGA DERIVATIVES, THEIR SYNTHESIS AND PHARMAECUTICAL USE

  • Ex. 4 Cpd. D を例示
  • Erimos Pharmaceuticals LLC

ノルジヒドログアイヤレチン酸(NDGA) 誘導体。HIV/HPV/HSVウイルス感染由来疾患、炎症疾患、糖尿病等の代謝疾患、高血圧、ガン、等処置 The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.

20170044122

Oxaspiro[2.5]Octane Derivatives and Analogs

Oxaspiro[2.5]Octane Derivatives and Analogs

  • Claim 7
  • Zafgen, Inc. [US]

MetAP2モジュレーター。過剰体重等処置 The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity. The disclosure provides, for example, compounds which may be modulators of MetAP2.

20170044127

ICARIIN DERIVATIVES

ICARIIN DERIVATIVES

  • Claim 17 およびICARIIN
  • H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. [US]

イカリイン誘導体。ガン、炎症疾患処置 Disclosed are derivatives of icariin. Disclosed are compounds having Formula I-VIII as defined herein. Methods of using these compounds for the treatment of cancer and inflammation are also disclosed.

20170044130

AGONISTS THAT ENHANCE BINDING OF INTEGRIN-EXPRESSING CELLS TO INTEGRIN RECEPTORS

AGONISTS THAT ENHANCE BINDING OF INTEGRIN-EXPRESSING CELLS TO INTEGRIN RECEPTORS

  • Ex. 2-5 (Ex. 10)を例示
  • TEXAS HEART INSTITUTE [US]

インテグリン発現細胞をインテグリン受容体に結合作動薬。損傷/疾患血管、処置 A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of .alpha.4.beta.1, .alpha.5.beta.1, .alpha.4.beta.7, .alpha.v.beta.3 and .alpha.L.beta.2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal. A method of treating damaged or diseased vascular tissue.

20170044132

HETEROCYCLIC COMPOUND

HETEROCYCLIC COMPOUND

  • Claim 9. (2E)-3-(4-(1-Methyl-1H-pyrazol-4-yl)pyridin-3-yl)-N-(2-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-isoindol-5-yl)acrylamide Ex. 289
  • Takeda Pharmaceutical Company Limited [JP]

CDK8/ CDK19阻害効果。ガン予防/処置 The present invention provides a heterocyclic compound having a CDK8 and/or CDK19 inhibitory effect. The present invention provides a compound represented by formula (I) or a salt thereof. A method for preventing or treating cancer.

20170044133

NOVEL 2-AMINO-PYRIDINE AND 2-AMINO-PYRIMIDINE DERIVATIVES AND MEDICINAL USE THEREOF

NOVEL 2-AMINO-PYRIDINE AND 2-AMINO-PYRIMIDINE DERIVATIVES AND MEDICINAL USE THEREOF

  • Claim 14: 2-[6-(3-trifluoromethoxy-benzylamino)-pyridin-3-yl]-3H-benzimidazole-4-carboxylic acid Ex. 2 を例示
  • MITSUBISHI TANABE PHARMA CORPORATION [JP]

ATX阻害剤。ガン/腫瘍予防/処置 Provided is a compound superior in an autotaxin inhibitory action and the like, effective as a prophylactic or therapeutic drug for diseases involving ATX. The present invention relates to a compound represented by the following formula (I), which has a superior autotaxin inhibitory action and is useful as a prophylactic or therapeutic drug for diseases involving ATX, wherein the disease involving ATX is cancer or tumor. .

20170044136

Pyridinoylpiperidines As 5-HT1F Agonists

Pyridinoylpiperidines As 5-HT1F Agonists

  • Ex. 1 4-Fluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide
  • Eli Lilly and Company [US]

5-HT1F作動薬/神経タンパク質管外漏出阻止薬。片頭痛処置/予防 The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

20170044138

CGRP RECEPTOR ANTAGONISTS

CGRP RECEPTOR ANTAGONISTS

  • Claim 9
  • Eli Lilly and Company [US]

CGRP受容体拮抗薬。片頭痛処置/予防 The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof. A method of preventing migraine. A method of treating migraine.

20170044139

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE

  • Claim 20 から Cpd. 409
  • Agios Pharmaceuticals, Inc. Cambridge [US]

変異IDH2阻害剤。ガン処置 Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein. The compound of Formula I or II or as described in any one of the embodiments herein inhibits mutant IDH2, particularly mutant IDH2.

20170044140

BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

  • Claim 5 下図を例示
  • SUNSHINE LAKE PHARMA CO., LTD. [CN]

HCV阻害剤。HCV感染処置 Provided herein is a bridged bring compound of formula (I) or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore provided herein are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions thereof in the treatment of HCV infection or hepatitis C.

20170044141

ALKYNE-, AZIDE- AND TRIAZOLE-CONTAINING FLAVONOIDS AS MODULATORS FOR MULTIDRUG RESISTANCE IN CANCERS

ALKYNE-, AZIDE- AND TRIAZOLE-CONTAINING FLAVONOIDS AS MODULATORS FOR MULTIDRUG RESISTANCE IN CANCERS

  • Ac13Az12 を例示
  • The Hong Kong Polytechnic University [CN] McGill University [CA]

フラボノイド2量体ライブラリーをスクリーニング。MDRガンに有効 A triazole bridged flavonoid dimer compound library was efficiently constructed via the cycloaddition reaction of a series of flavonoid-containing azides (Az 1-15) and alkynes (Ac 1-17). These triazole bridged flavonoid dimers and their precursor alkyne- and azide-containing flavonoids were screened for their ability to modulate multidrug resistance (MDR) in P-gp-overexpressed cell line (LCC6MDR), MRP1-overexpressed cell line (2008/MRP1) and BCRP-overexpressed cell line (HEK293/R2 and MCF7-MX100). Generally, they displayed very promising MDR reversal activity against P-gp-, MRP1- and BCRP-mediated drug resistance. Moreover, they showed different levels of selectivity for various transporters. Overall, they can be divided into mono-selective, dual-selective and multi-selective modulators for the P-gp, MRP1 and BCRP transporters. The EC.sub.50 values for reversing paclitaxel resistance (141-340 nM) of LCC6MDR cells, DOX (78-590 nM) and vincristine (82-550 nM) resistance of 2008/MRP1 cells and topotecan resistance (0.9-135 nM) of HEK293/R2 and MCF7-MX100 cells were at nanomolar range. Importantly, a number of compounds displayed EC.sub.50 at or below 10 nM in BCRP-overexpressed cell lines, indicating that these bivalent triazoles more selectively inhibit BCRP transporter than the P-gp and MRP1 transporters. Most of the dimers are notably safe MDR chemosensitizers as indicated by their high therapeutic index values.

20170044143

ISOINDOLINE-1-ONE DERIVATIVES AS CHOLINERGIC MUSCARINIC M1 RECEPTOR POSITIVE ALLOESTERIC MODULATOR ACTIVITY FOR THE TREATMENT OF ALZHEIMERS DISEASE

ISOINDOLINE-1-ONE DERIVATIVES AS CHOLINERGIC MUSCARINIC M1 RECEPTOR POSITIVE ALLOESTERIC MODULATOR ACTIVITY FOR THE TREATMENT OF ALZHEIMERS DISEASE

  • Claim 14. 2-[(3S,4S)-4-Hydroxytetrahydro-2H-pyran-3-yl]-6-(4-methoxybenzyl)-4,5-dimethyl-2,3-dihydro-1H-isoindol-1-one Ex. 18-1
  • Takeda Pharmaceutical Company Limited [JP]

コリン作動性ムスカリンM1受容体陽性アロステリックモジュレーター。AD、統合失調症、疼痛、睡眠障害、等予防/処置 The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. (I) wherein each symbol is as described in the specification, or a salt thereof.

20170044144

SELECTIVE HDAC1 AND HDAC2 INHIBITORS

SELECTIVE HDAC1 AND HDAC2 INHIBITORS

  • Claim 25 下図を例示
  • Acetylon Pharmaceuticals, Inc. [US]

HDAC2阻害剤。ガン、HIV、等処置/予防 Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.

20170044145

MORPHOLIN-PYRIDINE DERIVATIVES

MORPHOLIN-PYRIDINE DERIVATIVES

  • Claim 8. (RS)-1-(3-Chlorophenyl)-3-(6-morpholin-2-yl-3-pyridyl)urea Ex. 8 を例示
  • Hoffmann-La Roche Inc. [US]

TAAR1に親和性。精神疾患処置 The present invention relates to compounds of formula of formula I, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. It has been found that the compounds of the present invention have a good affinity to the trace amine associated receptors (TAARs), especially TAAR1.

20170044146

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

  • Claim 22 Cpd 10, (3S)-3-Cyclopropyl-3-(3-((4-(5, 5-dimethylcyclopent-1-enyl)-5-(6-methoxybenzo[b]thiophen-4-yl)thiophen-3-- yl)methoxy)phenyl)propanoic acid  Ex. 12を例示
  • Janssen Pharmaceutica NV [BE]

GPR40受容体作動薬。2型糖尿病、処置 Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I).

20170044147

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

  • Claim 20 Cpd 56 (S,E)-3-Cyclopropyl-3-(3-(2-(4-(5, 5-dimethylcyclopent-1-en-1-yl)-3-(2-fluoro-5-methoxyphenyl)isoxazol-5-yl)- vinyl)phenyl)propanoic acid Ex. 35 を例示
  • Janssen Pharmaceutica NV [BE]

GPR40受容体作動薬。2型糖尿病、処置 Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (II).

20170044148

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

  • Claim 21 (3S)-3-Cyclopropyl-3-(3-((1-(2-fluoro-5-methoxyphenyl)-5-(piperidin-1-yl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)propanoic (Cpd 44) Ex. 25 を例示
  • Janssen Pharmaceutica NV[BE]

GPR40受容体作動薬。2型糖尿病、処置 Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (III).

20170044149

PHARMACEUTICAL SALTS OF AN OREXIN RECEPTOR ANTAGONIST

PHARMACEUTICAL SALTS OF AN OREXIN RECEPTOR ANTAGONIST

  • suvorexant
  • MERCK SHARP &DOHME CORP. [US]

オレキシン受容体拮抗剤。神経/精神疾患処置/予防。結晶特許 The invention is directed to pharmaceutically acceptable salts of suvorexant, which is an antagonist of orexin receptors. The pharmaceutically acceptable salts of suvorexant are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is further directed to pharmaceutical compositions comprising pharmaceutically acceptable salts of suvorexant.

20170044150

IDENTIFICATION OF COMPOUNDS WHICH INHIBIT ATG8-ATG3 PROTEIN-PROTEIN INTERACTION AND THEIR USE AS ANTIPARASITICAL AGENTS

IDENTIFICATION OF COMPOUNDS WHICH INHIBIT ATG8-ATG3 PROTEIN-PROTEIN INTERACTION AND THEIR USE AS ANTIPARASITICAL AGENTS

  • Claim 16 下図化合物等
  • THE JOHNS HOPKINS UNIVERSITY [US]

Atg8-Atg3蛋白-蛋白相互作用阻害剤。寄生生物疾患抑制/処置 The present invention provides compounds or a pharmaceutically acceptable salts, solvates, stereoisomers, or prodrugs thereof which can block the Atg8-Atg3 protein-protein interaction, which is associated with autophagy in apicomplexan organisms. Pharmaceutical compositions comprising these compounds and their use for the suppression and treatment of various parasitical diseases are also provided.

20170044151

2-Amino-3-Fluoro-3-(Fluoromethyl)-6-Methyl-6-Phenyl-3,4,5,6-Tetrahydropyri- dines as BACE1 Inhibitors

2-Amino-3-Fluoro-3-(Fluoromethyl)-6-Methyl-6-Phenyl-3,4,5,6-Tetrahydropyri- dines as BACE1 Inhibitors

  • Claim 17. N-(3-((2S,5S)-6-amino-5-fluoro-5-(fluoromethyl)-2-methyl-2,3,4,5-tetrahyd- ropyridin-2-yl)-4-fluorophenyl)-5-methoxypicolinamide; Ex. 1 を例示
  • H. Lundbeck A/S [DK]

BACE1阻害剤。神経変性疾患、認知疾患処置 The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.

20170044152

COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM

COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM

  • Claim 16. 2,6-difluoro-N-(5-(1-methyl-3-(pyridin-2-yl)-1H-pyrazol-5-yl)thiophen-2-yl)benzamide Ex. 23 を例示
  • CalciMedica, Inc. [US]

SOCチャネルモジュレーター。自己免疫疾患、炎症疾患、等処置 Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. In one aspect is a method for treating an autoimmune disease, heteroimmune disease or condition, or inflammatory disease.

20170044155

Geminal Substituted Aminobenzisoxazole Compounds as Agonists of Alpha7-Nicotinic Acetylcholine Receptors

Geminal Substituted Aminobenzisoxazole Compounds as Agonists of Alpha7-Nicotinic Acetylcholine Receptors

  • Claim 51. 6-chloro-N-(2,2-dimethylquinuclidin-3-yl)benzo[d]isoxazol-3-amine Ex. 1 を例示
  • Forum Pharmaceuticals, Inc. [US]

α7-nAChR作動薬/部分作動薬。認知機能維持/処置/改善 The present invention relates to novel geminal substituted aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

20170044156

SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND MEDICINAL USE THEREOF AS HIV INTEGRASE INHIBITOR

SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND MEDICINAL USE THEREOF AS HIV INTEGRASE INHIBITOR

  • Ex. 24 を例示
  • JAPAN TOBACCO INC. [JP]

HIVインテグラーゼ阻害剤。抗HIV薬 Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof.

20170044157

NEW COMPOUNDS I

NEW COMPOUNDS I

  • Claim 5. 2,2,2-Trichloroethyl 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate Ex. 1 を例示
  • Proximagen Limited [GB]

SSAO活性阻害剤。炎症疾患、免疫疾患、処置 The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

20170044158

DIFLUOROMETHYLENE COMPOUND

DIFLUOROMETHYLENE COMPOUND

  • EX. 71 を例示
  • SATO PHARMACEUTICAL CO., LTD. [JP]

URAT1阻害剤。血中尿酸値低下剤 A compound having an URAT1 inhibitory activity, and an URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition containing the compound. More specifically, a compound represented by the formula (I).

20170044159

7-OXO-1,6-DIAZABICYCLO[3.2.1 ]OCTANE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS

7-OXO-1,6-DIAZABICYCLO[3.2.1 ]OCTANE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS

  • Claim 27. (2S,5R)-sulfuric acid mono-{2-[N'-(2-(S)-pyrrolidin-2-yl-acetyl)-hydrazinocarbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1] oct-6-yl} ester Ex. 1 を例示
  • WOCKHARDT LIMITED [IN]

抗細菌剤。細菌感染処置 Compounds of Formula (I), their preparation, and use in preventing or treating a bacterial infection are disclosed.

20170044160

TETRACYCLINE COMPOUNDS

TETRACYCLINE COMPOUNDS

  • Claim 31
  • Tetraphase Pharmaceuticals, Inc. [US]

テトラサイクリン化合物。抗ガン剤 The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use. A method for treating cancer.

20170044161

TRICYCLIC COMPOUND AND JAK INHIBITOR

TRICYCLIC COMPOUND AND JAK INHIBITOR

  • Ex. 6 を例示
  • NISSAN CHEMICAL INDUSTRIES, LTD. [JP]

JAK阻害剤。自己免疫疾患、炎症疾患、アレルギー、予防/処置 Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided. Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.

20170044162

Fused Pyrimidine-Based Hydroxamate Derivatives

Fused Pyrimidine-Based Hydroxamate Derivatives

  • Claim 36 Ex. 1 を例示
  • Agency for Science, Technology and Research [SG]

HDAC/キナーゼ阻害剤。ガン、炎症疾患、神経変性疾患、自己免疫疾患、等処置 The present invention relates to fused R1 pyrimidine-based hydroxamate compounds of formula (I), comprising a hydroxamate group, that are inhibitors of histone deacetylase (HDAC) and kinases. More particularly, the present invention relates to hydroxamate substituted purine or 5H-pyrrolo[3,2-d]pyrimidine derivatives, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having histone deacetylase, non-histone deacetylase and kinase activities/functions and/or via unspecified/multi-targeted mechanisms, wherein the disorder is cancer, angiogenic disorder or pathological angiogenesis, fibrosis, inflammatory conditions, asthma, neurological disorders, neurodegenerative disorders, muscle degenerative disorders, autoimmune disorders, disorders of the blood or disorders of the bone marrow, or is lymphoma, cutaneous T-cell lymphoma, follicular lymphoma, or Hodgkin lymphoma, cervical cancer, ovarian cancer, breast cancer, lung cancer, prostate cancer, colorectal cancer, sarcoma, hepatocellular carcinoma, leukemia or myeloma, retinal angiogenic disease, liver fibrosis, kidney fibrosis, Alzheimer's disease or Huntington's disease, spinal muscular atrophy, HIV/AIDS, polycythemia vera or essential thrombocythemia or myelofibrosis. .

20170044163

CGRP RECEPTOR ANTAGONISTS

CGRP RECEPTOR ANTAGONISTS

  • Claim 10
  • Eli Lilly and Company [US]

CGRP受容体拮抗剤。片頭痛処置 The present invention provides a compound of Formula II or a pharmaceutically acceptable salt thereof. A method of treating migraine.

20170044164

BICYCLIC FUSED PYRIMIDINE COMPOUNDS AS TAM INHIBITORS

BICYCLIC FUSED PYRIMIDINE COMPOUNDS AS TAM INHIBITORS

  • Claim 55. 4-(2-(Butylamino)-5-{4-[(4-methylpiperazin-1-yl)methyl]phenyl}imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanol; Ex. 1 を例示
  • Incyte Corporation [US]

TAMキナーゼ阻害剤。ガン等処置 This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.

20170044165

PENTYLENETETRAZOLE DERIVATIVES

PENTYLENETETRAZOLE DERIVATIVES

  • Claim 3 PTZのD化体 下図を例示
  • Balance Therapeutics, Inc. [US]

ペンチレンテトラゾール (PTZ) 誘導体。老化、動脈硬化、不安、行動障害等処置 Provided are compounds having formula I:, or a pharmaceutically salt thereof. Pharmaceutical compositions comprising the compounds and methods of their use, for instance in treating senility, senile confusion, psychoses, psychoneuroses when anxiety and nervous tension were present, cerebral arteriosclerosis, nausea, depression, fatigue, debilitation, mild behavioral disorders, irritability, emotional instability, antisocial attitudes, anxiety, vertigo or incontinence, or symptom thereof, or in improving cognitive function in individuals, for instance, in individuals with Down syndrome and other conditions, are also provided.

20170044167

SUBSTITUTED 2,4,5,6-TETRAHYDROPYRROLO[3,4-C]PYRAZOLE AND 4,5,6,7-TETRAHYDRO-2H-PYRAZOLO[4,3-C]PYRIDINE COMPOUNDS AS GLYT1 INHIBITORS

SUBSTITUTED 2,4,5,6-TETRAHYDROPYRROLO[3,4-C]PYRAZOLE AND 4,5,6,7-TETRAHYDRO-2H-PYRAZOLO[4,3-C]PYRIDINE COMPOUNDS AS GLYT1 INHIBITORS

  • Claim 114. (2-(4-Fluorophenyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)(2-isopropoxy-5-(methylsulfonyl)phenyl)methanone Ex. 1 を例示
  • DART NEUROSCIENCE (CAYMAN) LTD. [KY]

GLYT1阻害剤。神経/CNS疾患、神経変性疾患、疼痛、依存症等処置 The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence.

20170044168

COMPOUNDS AND COMPOSITIONS AS TOLL-LIKE RECEPTOR 7 AGONISTS

COMPOUNDS AND COMPOSITIONS AS TOLL-LIKE RECEPTOR 7 AGONISTS

  • Claim 13. 2-(dimethylamino)ethyl 4-((2-amino-4-(pentylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl)-3-methoxybenzoate Ex. 2 を例示
  • NOVARTIS AG [CH]

TLR7受容体作動薬。感染症、炎症疾患、呼吸器疾患、自己免疫疾患、ガン等処置 The invention provides a compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat diseases or disorders associated with Toll-Like Receptor 7 activity, wherein the disease is an infectious disease, a viral infectious disease, an inflammatory disease, a respiratory disease, a dermatological disease, an autoimmune disease, a cell-proliferative disease or cancer. .

20170044169

Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases

Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases

  • Claim 16 下図化合物等
  • JANSSEN SCIENCES IRELAND UC [IE]

TLR7/TLR8活性化剤。ウイルス感染等処置 This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and/or therapy of diseases. A method of activating human TLR7 or TLR8.

20170044170

SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYR- AZINO[2,3-b]PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF

SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYR- AZINO[2,3-b]PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF

  • 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyr- azino[2,3-b]pyrazin-2(1H)-one
  • Signal Pharmaceuticals, LLC [US]

mTOR/PI3K/Akt 経路阻害剤。ガン等処置/予防。結晶特許 Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyr- azino[2,3-b]pyrazin-2(1H)-one. In certain embodiments, solid forms of Compound 1 are useful for treating or preventing cancer and conditions treatable or preventable by inhibition of a kinase pathway, for example, the mTOR/PI3K/Akt pathway.

20170044172

SPIRO UREA COMPOUNDS AS RSV ANTIVIRAL COMPOUNDS

SPIRO UREA COMPOUNDS AS RSV ANTIVIRAL COMPOUNDS

  • Cpd. 18 を例示
  • Janssen Sciences Ireland UC [IE]

抗ウイルス剤。特にRSV複製阻害剤。RSY感染処置 The invention concerns novel substituted spiro urea azetidinyl or piperidinyl compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.

20170044173

Orvinol and Thevinol Derivatives Useful in the Treatment of Drug and Alcohol Abuse, Depression, Anxiety, or a Compulsive Disorder

Orvinol and Thevinol Derivatives Useful in the Treatment of Drug and Alcohol Abuse, Depression, Anxiety, or a Compulsive Disorder

  • No. 22 を例示
  • The University of Bath Bath and North East [GB]

オルビノール、テビノール誘導体。依存症、うつ、不安、強迫性障害、処置 The invention provides a method of treating drug and alcohol abuse, depression, anxiety, or a compulsive disorder in a subject comprising administering to the subject a compound having formula 2 or a pharmaceutically acceptable salt or solvate thereof.

20170044174

HETEROCYCLIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS

HETEROCYCLIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS

  • Claim 21. 4-[4-(4,6-dimethylpyrimidin-5-yl)-3-methylphenoxy]-2,3-dihydrofuro[3,2-c]- pyridine Ex. 1 を例示
  • PFIZER INC. NEW YORK [US]

ドーパミンD1リガンド。統合失調症、認知障害(統合失調症、AD、PD等関連)、ADHD、不安、うつ、等処置 The present invention provides, in part, compounds of Formula (I): and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

20170044175

INHIBITORS OF LATE SV40 FACTOR (LSF) AS CANCER CHEMOTHERAPEUTICS F

INHIBITORS OF LATE SV40 FACTOR (LSF) AS CANCER CHEMOTHERAPEUTICS  F

  • Claim 7
  • TRUSTEES OF BOSTON UNIVERSITY [US]

LSF阻害剤。ガン処置 The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formula (I)-(XXVI) and (III') as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.

20170044180

Sesquiterpenoids

Sesquiterpenoids

  • Claim 9 下図を例示
  • National Institute of Biological Sciences, Beijing [CN]

IKKα/β阻害剤。ガン、自己免疫疾患、炎症疾患、等処置 The invention provides novel compounds and compositions for inhibiting IKKα/β including treating disorders associated with IKKα/β activity, including cancer, autoimmune and inflammatory disorders, with a compound of structure:

20170044181

COMPOUNDS FOR TREATING VIRAL INFECTIONS

COMPOUNDS FOR TREATING VIRAL INFECTIONS

  • No. 2 を例示
  • INSTITUT PASTEUR KOREA [KR]

ウイルス疾患、特にHCV感染処置 The present invention relates to small molecule compounds and their use in the treatment of diseases, in particular viral diseases, in particular hepatitis C virus (HCV).

20170044182

FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF

FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF

  • Claim 47. (S)-N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-8-methyl-7-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-2-amine Ex. 21A を例示
  • FORUM Pharmaceuticals Inc. [US]

Aβ42濃度を低下。神経変性疾患、処置 The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine. In some embodiments, the invention provides a method for lowering Aβ42 concentration in a subject.

20170044183

FACTOR XIa INHIBITORS

FACTOR XIa INHIBITORS

  • Claim 10. methyl (4-(((S)-1-((S)-6-chloro-2-oxo-1,2-dihydrospiro[pyrido[2,3-d][1,3]oxazine- -4,3'-pyrrolidin]-1'-yl)-1-oxo-3-phenylpropan-2-yl)carbamoyl)phenyl)carbamate; Ex. 1a を例示
  • Merck Sharp & Dohme Corp. [US]

FXIa/プラズマカリクレイン阻害剤。血栓塞栓症、等処置/予防 The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

20170044185

Histone Deacetylase Inhibitors and Methods for Use Thereof

Histone Deacetylase Inhibitors and Methods for Use Thereof

  • Claim 7. RBC-1002a-A (N-(2-amino-4-(thiophen-2-yl)phenyl)-4-((3-oxoisothiazolo[5,4-b]pyridin-2- (3H)-yl)methyl)benzamide),
  • Reaction Biology Corp. [US]

HDAC阻害剤。ガン、炎症疾患、神経変性疾患、等処置 The present invention relates to methods of modulating (for example inhibiting) activity of histone deacetylases (HDACs) and/or treating HDACs--associated diseases including, for example, cancers, inflammatory disorders, neurodegenerative disorders, etc. The invention also provides novel compounds and compositions thereof, methods of preparation of the same, as well as methods of use of the same for inhibition of HDACs and/or treatment of HDAC-associated diseases.

20170044186

HISTONE DEACETYLASE INHIBITORS

HISTONE DEACETYLASE INHIBITORS

  • Cpd. D1 を例示
  • BIOMARIN PHARMACEUTICAL INC. [US]

HDAC阻害剤。神経疾患、ALS、AD、ガン、炎症疾患、記憶障害、薬物依存症、等処置 This invention relates to generally inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3). A method of treating a neurological disorder such as Friedreich's ataxia, myotonic dystrophy, spinal muscular atrophy, fragile X syndrome, Huntington's disease, spinocerebellar ataxia, Kennedy's disease, amyotrophic lateral sclerosis, Niemann Pick, Pitt Hopkins, spinal and bulbar muscular atrophy, and Alzheimer's disease; a cancer; an inflammatory disease; a memory impairment condition or a drug addiction.

20170044187

1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

  • Claim 5 下図を例示
  • SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN]

CCR 5拮抗剤。HIV 感染処置 Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

20170044189

COMPOSITIONS AND METHODS FOR IMPROVING GLUCOSE UPTAKE

COMPOSITIONS AND METHODS FOR IMPROVING GLUCOSE UPTAKE

  • Cpd. 5 を例示
  • BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY AND AGRICULTURAL AND Baton Rouge [US]

脂肪生成 増加なしに、細胞のブドウ糖取り込み増加 A compound includes the structure of general Formula II, pharmaceutically acceptable salts thereof, and/or solvates thereof. Such compounds can increase glucose uptake by cells and preferably do not substantially increase adipogenesis.

20170044191

Novel Prodrugs And Methods Of Use Thereof

Novel Prodrugs And Methods Of Use Thereof

  • Claim 21 下図を例示
  • Health Innovation Ventures B.V. [NL]

抗がん剤プロドラッグ The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds.

20170044192

ANTIVIRAL BETA-AMINO ACID ESTER PHOSPHODIAMIDE COMPOUNDS

ANTIVIRAL BETA-AMINO ACID ESTER PHOSPHODIAMIDE COMPOUNDS

  • Claim 13. 1-methylethyl N-[(S)-{[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl} {[(2S)-2-methyl-3-(1-methylethoxy)-3-oxopropyl]amino}phosphoryl]-L-alaninate Ex. 7A,7B を例示
  • Merck Sharp & Dohme Corp. [US]

HIV逆転写酵素阻害剤。HIV感染予防/処置 Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

20170044193

PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY

PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY

  • Claim 39
  • Galera Labs, LLC [US]

酸化損傷阻止、抗炎症作用 Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands.. Certain of these compounds have also been shown to possess potent anti-inflammatory activity and prevent oxidative damage in vivo.

20170044202

PYRROLOPYRIMIDINE NUCLEOSIDES AND ANALOGS THEREOF

PYRROLOPYRIMIDINE NUCLEOSIDES AND ANALOGS THEREOF

  • Cpd. 1 を例示
  • Chimerix, Inc. [US] The Regents of the University of Michigan [US]

ノロウイルス感染/感染症、処置 The present disclosure provides pyrrolopyrimidine nucleoside analogs of the Formula I, Formula IA, Formula IB, or Formula II and phospholipid conjugates and pharmaceutical compositions thereof. Also presented are methods of treating and/or preventing viral infection and/or viral infection-associated disease or disorder with one or more compounds of Formula I, Formula IA, Formula IB, or Formula II. A method of treating a viral infection or a viral infection-associated disease or disorder, wherein the viral infection is norovirus infection.

20170044203

PURINE DERIVATIVES AS CD73 INHIBITORS FOR THE TREATMENT OF CANCER

PURINE DERIVATIVES AS CD73 INHIBITORS FOR THE TREATMENT OF CANCER

  • Claim 60. (2-(((2R,3S,4R,5R)-5-(2-chloro-6-(methylamino)-9H-purin-9-yl)-3,4-dihydro- xytetrahydrofuran-2-yl)methoxy)-2-methylmalonic acid) Ex. 2 を例示
  • Vitae Pharmaceuticals, Inc. [US]

CD73阻害剤。ガン処置 Provided are novel compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.

20170044205

3'-SUBSTITUTED METHYL OR ALKYNYL NUCLEOSIDES NUCLEOTIDES FOR THE TREATMENT OF HCV

3'-SUBSTITUTED METHYL OR ALKYNYL NUCLEOSIDES NUCLEOTIDES FOR THE TREATMENT OF HCV

  • Claim 21 下図を例示
  • IDENIX PHARMACEUTICALS LLC [US]

HCVを含むフラビウイルス感染処置 Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3'-substituted methyl or alkynyl nucleosides of Formula I: (I); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof.

20170044206

CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS

CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS

  • Claim 22 下図を例示
  • Merck Sharp & Dohme Corp. [US]

STING作動薬。I型インターフェロン産生誘導 A class of polycyclic compounds of general formula (I), of general formula (I'), or of general formula (I''), that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

20170044208

SELECTIVE GLUCOCORTICOID RECEPTOR LIGANDS

SELECTIVE GLUCOCORTICOID RECEPTOR LIGANDS

  • Claim 10 下図を例示
  • The University of Manchester [GB]

グルココルチコイド受容体選択的リガンド。炎症疾患、特にRA、処置 Described herein are certain steroid derivative compounds, for example of formula (I), pharmaceutical compositions comprising such compounds, the use of such compounds and compositions to specifically target glucocorticoid action, and the use of such compounds and compositions in the treatment of acute and chronic inflammatory conditions, in particular rheumatoid arthritis, haematological and other malignancies, and for causing immunosuppression in the prevention or treatment of transplant rejection, as well as methods of preparing such compounds.

20170044266

CYTOTOXIC BENZODIAZEPINE DERIVATIVES

CYTOTOXIC BENZODIAZEPINE DERIVATIVES

  • Fig. 1から例示
  • ImmunoGen, Inc. [US]

細胞毒化合物。抗増殖性疾患活性 The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

EP

EP3130582

NOVEL COMPOUND HAVING IMMUNE DISEASE TREATMENT EFFECT AND USE THEREOF

NOVEL COMPOUND HAVING IMMUNE DISEASE TREATMENT EFFECT AND USE THEREOF

  • SD-282 を例示
  • THE CATHOLIC UNIV OF KOREA INDUSTRY-ACADEMIC [KR]

炎症誘発性サイトカイン生成抑制。免疫疾患処置 The present invention relates to a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present invention has effects of inhibiting the formation of proinflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of autoantibodies to regulate excessive immune responses, and inhibiting the differentiation to osteoclasts, and thus can be used for treating immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune responses.

EP3130583

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

  • Ex. 34 から (1S,2S)-2-[(3,4-Dichlorophenyl)carbonyl]cyclopropane-1-carboxylic acid を例示
  • CHDI FOUND INC [US]

キヌレニン-3-モノオキシゲナーゼ阻害剤。HD等神経変性疾患症状軽減 Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising the same and methods of treating patients suffering from certain diseases and disorders response to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof described herein, effective to reduce signs or symptoms of the disease or disorder. These diseases include neurodegenerative disorders such as Huntington's disease.

EP3130585

PYRROLO[3,2-D]PYRIMIDINE-4-AMINE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER

PYRROLO[3,2-D]PYRIMIDINE-4-AMINE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER

  • AAG1 を例示
  • DUQUESNE UNIV OF THE HOLY SPIRIT [US]

抗腫瘍剤 The present invention relates to 4-amino, 4-oxy, 4-thio or 4-alkyl substituted pyrrolo[3,2d]pyrimidines, furo[3,2d]pyrimidines, cyclopenta[d]pyridines, pyrrolo[2,3d]pyrimidines and furo[2,3d]pyrimidines, pharmaceutically acceptable salts, solvates and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also disclosed are these compounds for use in a method of treating tumor cells and inhibiting mitosis of cancerous cells.

EP3130589

HETEROCYCLIC AZA COMPOUNDS

HETEROCYCLIC AZA COMPOUNDS

  • Cpd. 11  2-(5-hydroxy-1-methyl-1H-indol-3-yl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)acetamide を例示
  • GRÜNENTHAL GMBH [DE]

バニロイド受容体リガンド。疼痛等処置/予防 The invention relates to heterocyclic aza compounds as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

EP3130590

AROMATIC AZA COMPOUNDS AS VR1/TRPV1 LIGANDS

AROMATIC AZA COMPOUNDS AS VR1/TRPV1 LIGANDS

  • Claim 11. 1-(2,3-dihydro-1H-inden-1-yl)-3-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)urea を例示
  • GRÜNENTHAL GMBH [DE]

バニロイド受容体リガンド。疼痛等処置/予防 The invention relates to aromatic aza compounds of formula (I) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

EP3130592

ANALOGUES OF 4H-PYRAZOLO[1,5- ]BENZIMIDAZOLE COMPOUND AS PARP INHIBITORS

ANALOGUES OF 4H-PYRAZOLO[1,5- ]BENZIMIDAZOLE COMPOUND AS PARP INHIBITORS

  • Claim 14. 6-fluoro-3-(piperidin-4-yl)-4H-benzo[4,5]imidazo[1,2-b]pyrazole-8-carboxamide Ex. 1 を例示
  • HUBEI BIO-PHARMACEUTICAL IND TECH INST INC [CN] HUMANWELL HEALTHCARE (GROUP) CO LTD [CN] (+1)

PARP阻害剤。ガン、心血管疾患、炎症疾患、糖尿病、等処置可能性 Disclosed is a series of analogues of 4H-pyrazolo[1,5-a]benzimidazole compound as PARP inhibitors. In particular, disclosed in the invention is a compound as shown by formula (I) or a pharmaceutically acceptable salt thereof as a PARP inhibitor. The PARP-1 inhibitors provided herein can be used for the treatment of wide rages of diseases comprising cancer, stroke, cardiac ischemia, inflammation, and diabetes.

EP3130593

PHENANTHROLINE PHOSPHONIC ACID DERIVATIVE AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

PHENANTHROLINE PHOSPHONIC ACID DERIVATIVE AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

  • Claim 18
  • BERYL THERAPEUTICS INC [CN]

コラーゲンプロリルヒドロキシラーゼ阻害剤。肝線維症等予防/処置 The present invention relates to a novel phenanthroline phosphonic acid compound and a pharmaceutical salt thereof, as well as an application of the compound and the pharmaceutical salt thereof as collagen prolyl hydroxylase inhibitors in the preparation of drugs for preventing or treating collagen prolyl-4-hydroxylase related disease. A method for preventing or treating fibro proliferative disease, for preventing or treating liver fibrosis.

EP3130594

PHOSPHONATES OF ACETYLENIC BETULIN DERIVATIVES WITH ANTICANCER ACTIVITY, METHOD FOR THEIR PRODUCTION AND THEIR APPLICATION

PHOSPHONATES OF ACETYLENIC BETULIN DERIVATIVES WITH ANTICANCER ACTIVITY, METHOD FOR THEIR PRODUCTION AND THEIR APPLICATION

  • ベツリン誘導体例
  • SLASKI UNIV MEDYCZNY W KATOWICACH [PL]

ベツリン誘導体。抗がん剤 The invention describes phosphonates of acetylenic betulin derivatives with anticancer activity, with Formula 2 method for their production and application.

EP3130599

AROMATIC-CATIONIC PEPTIDES AND USES OF SAME

AROMATIC-CATIONIC PEPTIDES AND USES OF SAME

  • Claim 1下図を例示
  • STEALTH PEPTIDES INT INC [MC]

芳香属カチオン性ペプチド。酸化損傷低下させ、ATP産生増強 The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant. A pharmaceutical composition for reducing oxidative damage A pharmaceutical composition for increasing the ATP synthesis rate.

EP3130600

A COMPOUND FOR TREATING SEQUELAE OF ISCHEMIC CEREBRAL STROKE

A COMPOUND FOR TREATING SEQUELAE OF ISCHEMIC CEREBRAL STROKE

  • Claim 7
  • WANG JINGYI [CN]

虚血性脳卒中の後遺症を治療するための化合物 The present invention provides a compound (I) for treating sequelae of ischemic cerebral stroke: H-(NH-CHR 1 -CO)-(NH-CHR 2 -CO)-(NH-CHR 3 -CO)-(NH-CHR 4 -CO) -(NH-CHR 5 -CO)-(NH-CHR 6 -CO)-(NH-CHR 7 -CO)-OH (I) or a pharmaceutically acceptable salt thereof. The present invention also provides a pharmaceutical composition comprising said compound and use of the same in the manufacture of a medicament for treating sequelae of ischemic cerebral stroke. The compound and pharmaceutical composition according to the present invention have good pharmacological activities so that they are able to improve significantly the symptom of sequelae of ischemic cerebral stroke.

WO2015128344 EP3129390

SIALIC ACID DERIVATIVES

SIALIC ACID DERIVATIVES

  • No. 20 を例示
  • BROSSMER REINHARD [DE] PRESCHER HORST [CH]

シアル酸誘導体。アレルギー、自己免疫疾患、慢性炎症、MS、ガン、ウイルス/細菌感染、等処置/予防 Sialic acid derivatives of the formula (I) in which the symbols have the meanings given in the description, are suitable as medicaments, in particular for diseases the progression of which is influenced by Siclec ligands, for the treatment or prevention of allergies, autoimmune diseases, chronic inflammations, paraplegia, multiple sclerosis, cancer, viral diseases, bacterial diseases, parasitic diseases, diseases in which the immune response is impaired under the B-cell activation..

WO2015144799 EP3129376

SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-A]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-A][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS

SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-A]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-A][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS

  • Claim 11
  • JANSSEN PHARMACEUTICA NV [BE]

ROS1阻害剤。ガン等処置/予防 The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS 1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament, for use in the treatment or prevention of a disease or condition selected from non-small cell lung cancer (specifical ly adenocarcinoma ), cholangiocarcinoma, gl ioblastoma, colorectal cancer, gastric adenocarcinoma, ovarian cancer, angiosarcoma, epithelioid hemangioendothelioma, inflammatory myo fibroblastic tumors, breast cancer and chronic myelogenous leukemia..

WO2015148597 EP3129372

AZAQUINAZOLINE INHIBITORS OF ATYPICAL PROTEIN KINASE C

AZAQUINAZOLINE INHIBITORS OF ATYPICAL PROTEIN KINASE C

  • Claim 29 Ex. 1 を例示
  • CANCER RES TECH LTD [GB]

aPKC阻害剤。増殖性疾患、処置 The present application provides a compound of formula (I) and/or a salt thereof. A compound of formula (I) and/or its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders. Compositions comprising a compound of Formula (I) and/or a salt thereof are also provided.

WO2015148839 EP3128842

TREATMENT OF BRCA1-DEFECTIVE CANCER OR RESISTANT CANCERS

TREATMENT OF BRCA1-DEFECTIVE CANCER OR RESISTANT CANCERS

  • Claim 2 ((N-(4- (3,4-dihydroxyphenyl)-5-phenylthiazol-2-yl)-3,4-dihydroxybenzamide)).
  • HOPE CITY [US]

BRCA1欠損、PARP1阻害剤耐性、DNA損傷抗がん剤耐性ガン患者、処置 Provided herein are methods of treating cancer in a subject, by administering COH29 ((N-(4- (3,4-dihydroxyphenyl)-5-phenylthiazol-2-yl)-3,4-dihydroxybenzamide)). The methods of treating include treating a BRCA1 -defective subject, a PARP1 inhibitor-resistant subject or a DNA-damaging anti-cancer agent resistant subject. The methods include treating cancer by administering COH29 and a DNA-damaging anti-cancer agent in a combined synergistic amount.

WO2015148954 EP3129023

POTENT SOLUBLE EPOXIDE HYDROLASE INHIBITORS

POTENT SOLUBLE EPOXIDE HYDROLASE INHIBITORS

  • Claim 4. l-(3-fluoro-4- (trifluoromethoxy)phenyl)-3-(l -isobutyrylpiperidin-4-yl)urea (Cpd. 19).
  • EICOSIS LLC [US]

she阻害剤。慢性糖尿病性神経因性疼痛等処置 The invention discloses a new series of inhibitors of soluble epoxide hydrolase (sEH) with improved physical properties that enhance their druglikeness to treat sEH associated diseases such as chronic diabetic neuropathic pain.

WO2015154022 EP3129371

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

  • Claim 3、8 を例示
  • SYROS PHARMACEUTICALS INC [US]

CDK7阻害剤。ガン、血管新生、炎症疾患、自己免疫疾患、等 The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

WO2015154883 EP3129385

NEOSORAPHENS

NEOSORAPHENS

  • Claim 8 下図を例示
  • HELMHOLTZ-ZENTRUM FÜR INFEKTIONSFORSCHUNG GMBH [DE]; TWINCORE ZENTRUM FÜR EXPERIMENTELLE UND KLINISCHE INFEKTIONSFORSCHUNG GMBH [DE]

ウイルス感染処置、Thl7関連炎症/自己免疫疾患、処置/予防 The present invention relates to compounds according to general formula (I); to compositions, including a pharmaceutical formulation and a combination preparation comprising one or more of the compound (s); to a process for their preparation; to uses thereof, including the use in the treatment or prevention of a viral infection or a Thl7-associated inflammatory and/or autoimmune disease.

WO2015155042 EP3129374

(5,6-DIHYDRO)PYRIMIDO[4,5-E]INDOLIZINES

 (5,6-DIHYDRO)PYRIMIDO[4,5-E]INDOLIZINES

  • Ex. 148 N-[1-[2-(2-ethoxyethoxy)ethyl-3.5-dimethylpyrazol-4-yl]-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilinol-5,6-dihydropyrimido[4,5-e]indolizine-7-carboxamide を例示
  • NETHERLANDS TRANSLATIONAL RES CENTER B V [NL]

TTK阻害剤。ガン処置 The invention relates to a compound of Formula (I). The compounds can be used in pharmaceutical compositions, in particular in the treatment of cancer. The present invention relates to chemical compounds, which modulate the activity of protein kinases, in particular inhibit the activity of the protein kinase TTK

WO2015155197 EP3129387

NOVEL MACROCYCLIC COMPOUNDS

NOVEL MACROCYCLIC COMPOUNDS

  • Claim 11. Ex. 1 を例示
  • BAYER PHARMA AG [DE]

増殖性疾患、ウイルス感染由来疾患、心血管疾患、処置/予防 The present invention relates to novel macrocyclic compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).

WO2015155231 EP3129016

NOVEL CELL-PERMEABLE SUCCINATE COMPOUNDS

NOVEL CELL-PERMEABLE SUCCINATE COMPOUNDS

  • Claim 13 下図化合物等
  • NEUROVIVE PHARMACEUTICAL AB [SE]

ミトコンドリアでのATP産生増強のための、細胞浸透性コハク酸化合物 The present invention provides novel cell-permeable succinates and cell permeable precursors of succinate aimed at increasing ATP-production in mitochondria. The main part of ATP produced and utilized in the eukaryotic cell originates from mitochondrial oxidative phosphorylation, a process to which high-energy electrons are provided by the Kreb's cycle. Not all Kreb's cycle intermediates are readily permeable to the cellular membrane, one of them being succinate. The provision of the novel cell permeable succinates is envisaged to allow passage over the cellular membrane and thus the cell permeable succinates can be used to enhance mitochondrial ATP-output.

WO2015155262 EP3129368

CYTOTOXIC COMPOUNDS WHICH ARE INHIBITORS OF THE POLYMERISATION OF TUBULIN

CYTOTOXIC COMPOUNDS WHICH ARE INHIBITORS OF THE POLYMERISATION OF TUBULIN

  • Claim 9 下図化合物等
  • CENTRE NAT DE LA RECH SCIENT (C N R S ) [FR] UNIV PARIS-SUD [FR]

チューブリン重合阻害剤。増殖性疾患、処置 The present invention relates to compounds which inhibit tubulin polymerization, processes for their preparation and their uses, for use as medicament for treating or preventing proliferative diseases, such as cancer, psoriasis or fibrosis .

WO2015155332 EP3129380

SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE DERIVATIVES AND THEIR USE AS MDM2-P53 INHIBITORS

SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE DERIVATIVES AND THEIR USE AS MDM2-P53 INHIBITORS

  • # I-33 を例示
  • BOEHRINGER INGELHEIM INT [DE]

MDM2-p53相互作用阻害剤。ガン等処置/予防 The present invention encompasses compounds of formula (I), their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.

WO2015155453 EP3129014

NOVEL ORGANOSELENIUM COMPOUNDS, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL USES THEREOF AS ANTITUMOUR AGENTS

NOVEL ORGANOSELENIUM COMPOUNDS, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL USES THEREOF AS ANTITUMOUR AGENTS

  • Cpd. 38 Ex. E2 を例示
  • TETRAHEDRON [FR]

有機ヒ素化合物。抗腫瘍剤 A selenium compound. This selenium compound has the formula:. This compound is useful as a pharmaceutical substance including antitumor.

WO2015155549 EP3129386

ANTIBACTERIAL COMPOUNDS

ANTIBACTERIAL COMPOUNDS

  • Ex. 109 を例示
  • REDX PHARMA PLC [GB]

抗細菌剤 This invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and to methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds which are capable of treating bacterial infections which are currently hard to treat with existing drug compounds, e.g. those caused by resistant bacterial or mycobacterial strains.

WO2015155626 EP3129388

2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES

2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES

  • Ex. 45 を例示
  • PFIZER [US]

BACE1阻害剤。AD、2型糖尿病、処置 The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed, useful for inhibiting production of amyloid-β protein, inhibiting beta-site amyloid precursor protein cleaving enzyme 1 (BACE1 ), treating Alzheimer's disease or treating Type 2 diabetes

WO2015156417 EP3129369

CYCLOPROPANAMINE COMPOUND AND USE THEREOF

CYCLOPROPANAMINE COMPOUND AND USE THEREOF

  • Claim 11 Ex. 71 を例示
  • TAKEDA PHARMACEUTICALS CO [JP]

LSDl 阻害剤。統合失調症、自閉症、AD、PD、等の神経変性疾患、等予防/治療 The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like.

WO2015156421 EP3129370

DIHYDROTHIAZINE AND DIHYDROOXAZINE DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY

DIHYDROTHIAZINE AND DIHYDROOXAZINE DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY

  • No. I-49 を例示
  • SHIONOGI & CO [JP]

BACE1阻害剤。AD、等治療/予防 The present invention provides a compound which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or phylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins. A compound of the formula (I), or a pharmaceutically acceptable salt thereof, for use in treating or preventing Alzheimer dementia, mild cognitive impairment or prodromal Alzheimer's disease, for use in preventing the progression of Alzheimer dementia, mild cognitive impairment or prodromal Alzheimer's disease, or for use in preventing the progression in a patient asymptomatic at risk for Alzheimer dementia. .

WO2015156601 EP3129378

BROMODOMAIN-INHIBITING COMPOUNDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR PREVENTING OR TREATING A CANCER

BROMODOMAIN-INHIBITING COMPOUNDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR PREVENTING OR TREATING A CANCER

  • Claim 5. (R)-(6-(4-chlorophenyl)-8-methoxy-l-methyl-4H- benzo[f]-[l,2,4]triazolo[4,3-a] [l,4]diazepin-4-yI)methyl methanesulfonate (Compound 1)
  • KAINOS MEDICINE INC [KR]

ブロモドメイン阻害剤。ガン等予防/処置 Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer.

WO2015157057 EP3129350

MACROCYCLES

MACROCYCLES

  • Ex. 1 を例示
  • LUMIPHORE INC [US]

ガン等への診断、処置に使用 The invention relates to chemical compounds and complexes that can be used in therapeutic and diagnostic applications. The compounds disclosed herein are particularly well suited for the preparation of stable, pre-labeled antibodies for use in the diagnosis and treatment of cancer and other diseases.

WO2015157093 EP3129367

2,3-DISUBSTITUTED PYRIDINE COMPOUNDS AS TGF-BETA INHIBITORS AND METHODS OF USE

2,3-DISUBSTITUTED PYRIDINE COMPOUNDS AS TGF-BETA INHIBITORS AND METHODS OF USE

  • Claim 4
  • RIGEL PHARMACEUTICALS INC [US]

TGF-β阻害剤。ガン処置 The invention described herein comprises compounds of formula (IV) and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer. The compounds (IV) inhibit signaling by a member of the TGF-β superfamily such as Nodal or Activin.

WO2015157115 EP3129377

MERTK-SPECIFIC PYRIMIDINE COMPOUNDS

MERTK-SPECIFIC PYRIMIDINE COMPOUNDS

  • Claim 15 下図を例示
  • UNIV NORTH CAROLINA CHAPEL HILL [US]

抗MerTK活性/抗Tyro3チロシンキナーゼ活性。抗ガン剤、免疫刺激/免疫モジュレーター剤、抗血小板剤、抗感染症剤、等として Uses of pyrimidines with anti-Mer tyrosine The present invention includes pyrimidine compounds that selectively inhibit Mer tyrosine kinase (MerTK) activity and/or Tyro3 tyrosine kinase activity, and use of these pyrimidine compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.

WO2015157145 EP3129102

IODONIUM ANALOGS AS INHIBITORS OF NADPH OXIDASES AND OTHER FLAVIN DEHYDROGENASES; FORMULATIONS THEREOF; AND USES THEREOF

IODONIUM ANALOGS AS INHIBITORS OF NADPH OXIDASES AND OTHER FLAVIN DEHYDROGENASES; FORMULATIONS THEREOF; AND USES THEREOF

  • Cpd. 15, 16 を例示
  • THE U S A AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES [US] STARKS ASS INC [US]

抗ガン作用、抗炎症作用剤 Disclosed herein are novel iodonium analogs having anticancer and anti-inflammatory activity. A method of treating or preventing a cancer, inhibiting or preventing tumor growth, or treating or preventing an inflammatory condition.

WO2015157182 EP3129366

CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS

CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS

  • Claim 7 l-(3-(3,6-difluoro-9H-carbazol-9-yl)-2-hydroxypropyl)-3-fluoropyrrolidin-2-one Cpd. 9 を例示
  • RESET THERAPEUTICS INC [US]

クリプトクロム介在疾患(糖尿病、クッシング病、NASH、喘息、COPD等)処置 The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.

WO2015157187 EP3129345

METABOTROPIC GLUTAMATE RECEPTOR POSITIVE ALLOSTERIC MODULATORS (PAMS) AND USES THEREOF

METABOTROPIC GLUTAMATE RECEPTOR POSITIVE ALLOSTERIC MODULATORS (PAMS) AND USES THEREOF

  • Claim 16 下図を例示
  • SANFORD-BURNHAM MEDICAL RES INST [US]

Group II mGlus受容体PAMS。CNS疾患(依存症、統合失調症、AD、PD、ALS、等)処置 Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. A method of treating a central nervous disorder (CNS) disorder, wherein the disorder is an addictive disorder, wherein the CNS disorder is schizophrenia and, wherein the CNS disorder is a neurodegenerative disease such as Alzheimer's disease, Parkinson's disease, Huntington's disease, or Lou Gehrig's disease (Amyotrophic Lateral Sclerosis or ALS).

WO2015157313 EP3129354

INHIBITORS OF FATTY ACID AMIDE HYDROLASE (FAAH) ENZYME WITH IMPROVED ORAL BIOAVAILABILITY AND THEIR USE AS MEDICAMENTS

INHIBITORS OF FATTY ACID AMIDE HYDROLASE (FAAH) ENZYME WITH IMPROVED ORAL BIOAVAILABILITY AND THEIR USE AS MEDICAMENTS

  • Claim 67
  • UNIV CALIFORNIA [US] FOND ST ITALIANO DI TECNOLOGIA [IT]

FAAH阻害剤。食欲回復。依存症、不安、PTSD、統合失調症、疼痛、炎症、緑内障、等処置/予防 Described herein, inter alia, are compositions and methods useful for inhibiting fatty acid amide hydrolase, for use in treating or preventing reduced appetite, gastric damage, enteric damage, a nicotine use disorder, tobacco smoking, substance abuse, a cannabis use disorder, a cocaine use disorder, an opioid use disorder, an amphetamine use disorder, a methamphetamine use disorder, an alcohol use disorder, an eating disorder, anxiety, post-traumatic stress disorder, schizophrenia, a mood disorder, pain, inflammation, or ocular glaucoma.

WO2015157376 EP3129375

ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS FOR MANAGING CANCER AND COMPOSITIONS RELATED THERETO

ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS FOR MANAGING CANCER AND COMPOSITIONS RELATED THERETO

  • Claim 6. l-ethyl-8-mercapto-3,7-dimethyl-3,7-dihydro-lH-purine-2,6-dione
  • UNIV EMORY [US]

AEP阻害剤。ガン、転移、処置/予防 This disclosure relates to asparagine endopeptidase inhibitors for managing cancer and compositions related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are substituted 3,7-dihydropurine-2,6-dione derivatives useful for treating or preventing metastasis, tumor growth, and/or cancer. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating a cancer comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.

WO2015157382 EP3129361

TREATMENT OF NEURODEGENERATIVE DISEASES WITH ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS AND COMPOSITIONS RELATED THERETO

TREATMENT OF NEURODEGENERATIVE DISEASES WITH ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS AND COMPOSITIONS RELATED THERETO

  • Cpd. BB1 Cpd. 22を例示
  • UNIV EMORY [US]

AEP阻害剤。AD、等神経変性疾患、処置/予防 This disclosure relates to asparagine endopeptidase inhibitors and compositions and uses related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are useful for treating or preventing neurodegenerative diseases and cognitive disorders such as Alzheimer's Disease. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating or preventing a neurodegenerative disease comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.

WO2015157483 EP3129392

TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY, SUBSTITUTED IN POSITION 3 BY A NON-AROMATIC RING CARRYING A HALOALKYL SUBSTITUENT

TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY, SUBSTITUTED IN POSITION 3 BY A NON-AROMATIC RING CARRYING A HALOALKYL SUBSTITUENT

  • Claim 12 下図を例示
  • VIIV HEALTHCARE UK(NO 4) LTD [GB]

HIV成熟阻害活性。HIV/AIDS処置 Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I. These compounds are useful for the treatment of HIV and AIDS.

WO2015157504 EP3129373

HISTONE DEACETYLASE INHIBITORS

HISTONE DEACETYLASE INHIBITORS

  • Claim 21 Cpd. 1 を例示
  • TAIPEI MEDICAL UNIV [TW] NAT HEALTH RESEARCH INSTITUTES [TW] (+1)

HDAC阻害剤。ガン処置 Fused bicycle indol, indoline, azoindole, or azoindoline compounds of Formula (I) set forth herein. Also disclosed are pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing the same. Further disclosed is a method for treating cancer, e.g., glioma, prostate cancer, and colorectal cancer, with these compounds.

WO2015157559 EP3129381

10',11'-MODIFIED SAXITOXINS USEFUL FOR THE TREATMENT OF PAIN

10',11'-MODIFIED SAXITOXINS USEFUL FOR THE TREATMENT OF PAIN

  • Claim 16 下図化合物等
  • SITEONE THERAPEUTICS INC [US] THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV [US]

サキシトキシン誘導体。電位依存性ナトリウムチャネル機能関連疾患(疼痛等)処置 Provided herein are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function, for example conditions associated with pain. The compounds are 10',11'-modified saxitoxins. The compounds are optionally additionally modified at carbon 13. In certain embodiments, the 10',11'-modified saxitoxins are of Formula I: where R1, R2 and R3 are as described herein. Also provided herein are methods of treating pain in a mammal comprising administering an effective treatment amount of a 10',11' modified saxitoxin or composition to a mammal. In an embodiment, the mammal is a human.

WO2015157594 EP3129362

TUBULYSIN DERIVATIVES

TUBULYSIN DERIVATIVES

  • Claim 6
  • MEDIMMUNE LLC [US]

ツブリシン誘導体。単独/コンジュゲートとしてガン等処置 Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone, as drug conjugates or in combination with other chemotherapies are provided.

WO2016020732 EP3129027

MODULATORS OF CASPASE-6

MODULATORS OF CASPASE-6

  • Claim 11, 12 (Fig. 3a, Fig. 3b)
  • UNIV BRITISH COLUMBIA [CA] UNIVERSITÄT HAMBURG [DE]

カスパーゼ6モジュレーター。神経疾患処置 The current application relates to a pharmaceutical composition for the treatment or amelioration of a neurological disease, wherein the composition comprises a therapeutically effective amount of a caspase-6 inhibitor which is an arylpropynamide derivative. The composition can be formulated for oral or topical administration, subcutaneous, intravenous, or intramuscular injection, infusion, inhalation, or intrthecal injection.

JP

2017-036213

がん幹細胞標的薬組成物 2017-036216 同様特許

がん幹細胞標的薬組成物

2017-036216  同様特許

  • 例示からエリブリン
  • 国立研究開発法人国立がん研究センター

がん幹細胞を標的として、再発や転移を防止し、がんの根治治療を目指すことができる医薬を提供することを課題とする。 VX-222、エリブリン、ビンデシン、β-ルブロマイシン、BIBR1532、及びこれらの誘導体、並びにこれらの薬理学的に許容される塩及び溶媒和物からなる群より選択される化合物を含む、がん幹細胞標的薬組成物を提供する。

2017-036219

化合物、前立腺癌治療薬、アンドロゲン受容体結合阻害剤、及び化合物の製造方法

化合物、前立腺癌治療薬、アンドロゲン受容体結合阻害剤、及び化合物の製造方法

  • 請求項1
  • 学校法人慶應義塾 他

前立腺癌の治療に有効な、アンドロゲン受容体(AR)アンタゴニストとしての活性を有する化合物 式(I)で表される化合物、及び該化合物を含有する医薬組成物、及びストレプトマイセス・エスピーBB47株による該化合物の製造方法

2017-036242

アルツハイマー治療薬

アルツハイマー治療薬

  • チペピジン、クロペラスチン
  • 国立大学法人 熊本大学 他

アルツハイマー病の主原因と考えられているアミロイドβ蛋白質により誘発される新たな認知症、特には、アルツハイマー病の予防および/または治療薬を提供することを目的とする。 GIRKチャンネル活性化電流抑制作用を有する化合物を有効成分として含有するアミロイドβ蛋白質により誘発される認知症、特にはアルツハイマー病の予防および/または治療薬が提供される。該化合物としては、例えば、チペピジン、クロペラスチン、またはそれらの薬理学的に許容される塩が例示される。

2017-036243

ジペプチジルペプチダーゼ-4阻害剤

ジペプチジルペプチダーゼ-4阻害剤

  • ルゴシンB
  • キューサイ株式会社

天然物に由来するDPP-4阻害剤を提供することにある。 DPP-4阻害剤は、ルゴシンBを有効成分とすることを特徴とする。

2017-036260

APJ受容体のトリアゾールアゴニスト

APJ受容体のトリアゾールアゴニスト

  • 例示から
  • アムジエン・インコーポレーテツド

様々な心血管状態および他の状態を処置するために使用できる、APJ(アンギオテンシン受容体様-1)受容体のアゴニスト こうした化合では、心血管状態の処置における特別な利益が見出せる。例えば、そのような化合物は、状態、例えば慢性収縮期心不全および慢性拡張期心不全等の状態の処置において有益になり得る。

2017-036265

メラニン産生抑制作用、コラーゲン産生促進作用及び創傷治癒促進作用を有する化合物

メラニン産生抑制作用、コラーゲン産生促進作用及び創傷治癒促進作用を有する化合物

  • 請求項1
  • 大江生醫股▲ふん▼有限公司

下記化学式Iで示される化合物は特にヒト皮膚線維芽細胞におけるMMP-9の遺伝子発現量及びMITFの遺伝子発現量を抑制する高い抑制活性を有していることが実証された。また、該化合物によれば、MMP-9の遺伝子発現量及びMITFの遺伝子発現量が著しく抑制されると共に、ヒト線維芽細胞におけるコラーゲンの産生量も向上し、且つヒト線維芽細胞におけるメラニンも抑制される

2017-036268

FAK阻害剤としてのピリミジン誘導体

FAK阻害剤としてのピリミジン誘導体

  • 請求項9  A34 を例示
  • メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング

チロシンキナーゼ誘発疾患の処置のための化合物及びその使用。 チロシンキナーゼシグナル伝達を、阻害、制御及び/又は調節し、癌、腫瘍成長、動脈硬化症、加齢黄斑変性症、糖尿病性網膜症、炎症性疾患などの処置に使用される。

2017-036274

抗体-薬物コンジュゲート 2017-036285 同様特許

抗体-薬物コンジュゲート 

2017-036285   同様特許

  • 式(1)
  • 第一三共株式会社

抗腫瘍効果と安全性面に優れる抗腫瘍薬 式(1)で示される抗腫瘍性化合物と抗体とを、次式:-L1-L2-LP-NH-(CH2)n1-La-Lb-Lc-で示される構造のリンカーを介して結合させた抗体-薬物コンジュゲート(抗体はL1の末端において結合し、抗腫瘍性化合物は、1位のアミノ基の窒素原子を結合部位として、Lcの末端において結合する)。

2017-036276

D-プシコースを有効成分とする皮膚機能改善組成物

D-プシコースを有効成分とする皮膚機能改善組成物

  • D-プシコース
  • 株式会社セレーネ 他

安全性の高い皮膚機能改善組成物およびこれを使用した剤を提供する。 D-プシコースおよび/またはその誘導体を有効成分とする安全性の高い皮膚機能改善組成物および、これを使用した皮膚保湿剤、皮膚抗酸化剤および皮膚抗老化剤から選ばれる剤。

2017-036288

HSP90併用療法

HSP90併用療法

  • 請求項66 固体支持体に固定化されたPU-H71
  • スローン - ケタリング・インスティテュート・フォー・キャンサー・リサーチ

Hsp90と関連する重要な腫瘍性タンパク質を同定することのできるプロテオミクスアプローチによる新しい癌治療法 Hsp90の阻害剤および癌関係の経路の成分の阻害剤を同時投与することを含む、癌を患っている対象を治療する方法であって、任意に、前記Hsp90の阻害剤は、それと癌関係の経路の成分との複合体中の、すなわち、該成分と結合している発癌性Hsp90に優先的に結合する、方法。

2017-036295

S1P調節剤を含む医薬組成物

S1P調節剤を含む医薬組成物

  • 2-アミノ-2-[2-(4-オクチルフェニル)エチル]プロパン-1,3-ジオール=FTY720F
  • ノバルティス アーゲー

スフィンゴシン-1ホスフェート(S1P)受容体調節剤、とりわけスフィンゴシン-1ホスフェート受容体アゴニストを含む医薬組成物の提供。 免疫抑制を必要とする対象を処置する S1P受容体アゴニストが2-アミノ-2-[2-(4-オクチルフェニル)エチル]プロパン-1,3-ジオールまたは2-アミノ-2-{2-[4-(1-オキソ-5-フェニルペンチル)-フェニル]エチル}プロパン-1,3-ジオール 臓器または組織移植拒絶の予防または処置用、あるいは炎症性または自己免疫性疾患の 予防または処置用

2017-036297

CD38を特異的に認識する抗体とシクロホスファミドとを含有する抗腫瘍組合せ

CD38を特異的に認識する抗体とシクロホスファミドとを含有する抗腫瘍組合せ

  • シクロホスファミド
  • サノフイ

腫瘍疾患の治療薬 CD38を特異的に認識する抗体と少なくともシクロホスファミドとを含む医薬組合せであって、アポトーシス、抗体依存性細胞性細胞傷害(ADCC)および補体依存性細胞傷害(CDC)により前記抗体がCD38+細胞を殺すことが可能である、医薬組合せ

2017-036298

ドライアイの治療用医薬組成物

ドライアイの治療用医薬組成物

  • TRPM8アゴニスト エチル3-(p-メンタン-3-カルボキサミド) を例示
  • ウニヴェルスィダッド ミゲル エルナンデス デ エルチェ 他

眼球乾燥症、膣乾燥及び口腔灼熱症候群から選択される疾患の治療用又は予防用医薬品の提供。 例えばエチル3-(p-メンタン-3-カルボキサミド)、(-)-イソプレゴール、(+)-シス及び(-)-トランスp-メンタン-3,8-ジオール、(-)-クベボール、イシリン、5-メチル-4-(1-ピロリジニル)-3-[2H]-フラノン、4,5-ジメチル-3-(1-ピロリジニル)-2[5H]-フラノン、4-メチル-3-(1-ピロリジニル)-2[5H]-フラノン、N-エチル-p-メンタン-3-カルボキサミド、2-イソプロピル-5-メチル-シクロヘキサンカルボン酸(2-ヒドロキシ-1,1-ジメチル-エチル酸)-アミド、2-イソプロピル-5-メチル-シクロヘキサンカルボン酸(4-メトキシフェニル)アミド等から選択されるTRPM8アゴニストにより上記疾患の治療を行う。

2017-036309

フェニル誘導体

フェニル誘導体

  • 請求項9  4-(2-エチルブチル)-N-{3-[4-(エチルカルバモイル)フェノキシ]-5-(4-フルオロフェノキシ)フェニル}-4-ヒドロキシ-1-ピペリジンカルボキサミド 実施例15 を例示
  • 小野薬品工業株式会社

S1P2介在性疾患、例えば、血管の収縮に起因する疾患、線維症、呼吸器系疾患等の治療剤

2017-036311

新規糖脂質グリコシド化合物およびその製造方法

新規糖脂質グリコシド化合物およびその製造方法

  • 図2から例示
  • 学校法人近畿大学

抗腫瘍作用を有する新規糖脂質グリコシド化合物及びその製造方法

2017-036312

アルツハイマー型認知症を治療するための方法及び組成物

アルツハイマー型認知症を治療するための方法及び組成物

  • AChEI タクリンを例示 制吐剤NK1受容体アンタゴニスト アプレピタントを例示
  • チェイス・ファーマスーティカルズ・コーポレーション

アセチルコリンエステラーゼ阻害剤(AChEI)の用量を、推奨される最大用量レベルより高く増加させ、そして同時に神経行動機能及び生活の質を改善することを可能にすること。 AChEIを非抗コリン性制吐剤と組み合わせて投与することにより、前記患者の中枢神経系において増進されたアセチルコリンエステラーゼ阻害が達成され、そしてそれによって、前記患者におけるアルツハイマー型認知症の症状がより高い度合いまで改善される、前記方法。AChEIと組み合わせたアルツハイマー型認知症の治療用の医薬組成物の調製のための非抗コリン性制吐剤の使用並びに(a)制吐剤として、5HT3受容体アンタゴニスト、ドーパミン・アンタゴニスト、H1受容体アンタゴニスト、カンナビノイド・アゴニスト、アプレピタント又はカソピタント、及び(b)アセチルコリンエステラーゼ阻害剤を含んでなる医薬組成物の提供。

2017-036314

5-[[4-[[モルホリン-2-イル]メチルアミノ]-5-(トリフルオロメチル)-2-ピリジル]アミノ]ピラジン-2-カルボニトリルおよびその治療上の使用

5-[[4-[[モルホリン-2-イル]メチルアミノ]-5-(トリフルオロメチル)-2-ピリジル]アミノ]ピラジン-2-カルボニトリルおよびその治療上の使用

  • 請求項1
  • キャンサー・リサーチ・テクノロジー・リミテッド

癌などの増殖性状態を含むチェックポイントキナーゼ1(CHK1)によって媒介される疾患及び状態の治療方法 CHK1キナーゼ阻害作用を有する、5-[[4-[[モルホリン-2-イル]メチルアミノ]-5-(トリフルオロメチル)-2-ピリジル]アミノ]ピラジン-2-カルボニトリル化合物 別の薬剤(例えば、(a)DNAトポイソメラーゼIまたはII阻害薬;(b)DNA損傷薬;(c)代謝拮抗薬またはチミジル酸シンターゼ(TS)阻害薬;(d)微小管標的薬;(e)電離放射線;(f)有糸分裂調節薬または有糸分裂チェックポイント調節薬の阻害薬;(g)DNA損傷シグナル伝達物質の阻害薬;又は(h)DNA損傷修復酵素の阻害薬から選択される一種以上)との組み合わせによる医薬組成物。

2017-036317

インダゾール-3-カルボキサミドおよびWNT/β-カテニンシグナル伝達経路阻害剤としてのそれらの使用

インダゾール-3-カルボキサミドおよびWNT/β-カテニンシグナル伝達経路阻害剤としてのそれらの使用

  • 例示から
  • サミュメッド リミテッド ライアビリティ カンパニー

Wnt経路におけるタンパク質、特にキナーゼ活性を阻害し、癌、糖尿病性網膜症、関節リウマチ、真菌又はウイルス感染症、骨又は軟骨疾患、アルツハイマー病、前頭側頭型認知症、レビー小体型認知症、プリオン病、パーキンソン病、ハンチントン病、進行性核上性麻痺、大脳皮質基底核変性症、多系統萎縮症、筋萎縮性側索硬化症等の神経疾患、肺疾患、各種線維性障害等の治療に有用な新規化合物、及び該化合物を含有する薬学的組成物の提供。

2017-036336

抗ウイルス剤としてのピラゾロ[1,5-A]ピリミジン

抗ウイルス剤としてのピラゾロ[1,5-A]ピリミジン

  • 化合物式1を例示
  • ギリアード サイエンシーズ, インコーポレイテッド

ウイルス感染を処置するための、化合物およびその薬学的に受容可能な塩およびエステル、ならびに組成物を提供する。 これらの化合物および組成物は、ヒトRSウイルス感染が挙げられる、ニューモウイルス亜科ウイルス感染を処置するために有用である。別の実施形態は、ニューモウイルス亜科感染の処置を必要とする哺乳動物において、ニューモウイルス亜科感染を処置する方法を提供し、この方法は、治療有効量の式Iの化合物またはその薬学的に受容可能な塩もしくはエステルを投与する工程を包含する。

2017-505282

プラジエノライドピリジン化合物及び使用の方法

プラジエノライドピリジン化合物及び使用の方法

  • 請求項1
  • エーザイ・アール・アンド・ディー・マネジメント株式会社

新規のプラジエノライドピリジン化合物、このような化合物を含有する医薬組成物、及び治療剤としてその化合物を使用する方法を提供する。これらの化合物は、がん、特にそこにあるスプライソソーム及び突然変異を標的とする薬剤が有用であることが知られているがんの治療に有用であることがある

2017-505288

TNF活性のモジュレーターとしての縮合二環式ヘテロ芳香族誘導体

TNF活性のモジュレーターとしての縮合二環式ヘテロ芳香族誘導体

  • 例12  3-メチル-6-[4-(メチルスルホニル)フェニル]-4-(1-フェニルエチル) イソキノリン を例示
  • ユーシービー バイオファルマ エスピーアールエル

ヒトTNFα活性の強力なモジュレーターであり、したがって、自己免疫性及び炎症性障害、神経及び神経変性障害、疼痛及び侵害受容性障害、心血管障害、代謝障害、眼障害並びに腫瘍学的障害を含む、ヒトの様々な病気の治療及び/又は予防に有益である。

2017-505291

脂質合成の複素環式モジュレータ及びその組み合わせ

脂質合成の複素環式モジュレータ及びその組み合わせ

  • 化合物 161 を例示
  • 3-ブイ・バイオサイエンシーズ・インコーポレイテッド

脂肪酸シンターゼ経路の調節不全を特徴とする状態を治療する方法 改善された抗ウイルス性及び抗癌活性を有する脂質合成の複素環式モジュレータ

2017-505293

LTA4H阻害剤としてのヘテロアリールブタン酸誘導体

LTA4H阻害剤としてのヘテロアリールブタン酸誘導体

  • 請求項11  (R)-3-アミノ-4-(5-(4-(ベンゾ[d]チアゾール-2-イルオキシ)フェニル)-2H-テトラゾール-2-イル)ブタン酸 実施例1 を例示
  • ノバルティス アーゲー

特にロイコトリエンA4ヒドロラーゼ(LTA4H)に関して良好な薬物候補である

2017-505299

新しいカリクレイン7阻害剤

新しいカリクレイン7阻害剤

  • 請求項8  [1-メチル-2-[(5-メチルイソキサゾール-3-イル)アミノ]-2-オキソ-エチル]2-(4-クロロフェニル)酢酸エステル 実施例1 を例示
  • シクセラ ファーマ エービー

ヒトのカリクレイン7(KLK7)(セリンプロテアーゼ角質層キモトリプシン酵素(SCCE)としても知られる)の活性を阻害するための方法 疾患の処置および予防のための、より具体的には皮膚病の処置および予防

2017-505304

12-EPI-プロイロムチリン

12-EPI-プロイロムチリン

  • 請求項12   実施例1 を例示
  • ナブリヴァ セラピュティクス アクチエンゲゼルシャフト

特にグラム陰性細菌、特に大腸菌によって媒介される疾患の治療において使用

2017-505305

抗STEAP1抗体及びイムノコンジュゲートを使用する方法

抗STEAP1抗体及びイムノコンジュゲートを使用する方法

  • 請求項5  アンドロゲン受容体阻害剤が4-{3-[4-シアノ-3-(トリフルオロメチル)フェニル]-5,5-ジメチル-4-オキソ-2-スルファニリデンイミダゾリジン-1-イル}-2-フルオロ-N-メチルベンズアミド
  • ジェネンテック, インコーポレイテッド

抗STEAP-1抗体及びイムノコンジュゲートを使用して、特定のアンドロゲン受容体阻害剤ナイーブ前立腺がんにおいて前立腺がんを治療する方法である。

2017-505313

新規CYP-エイコサノイド誘導体

新規CYP-エイコサノイド誘導体

  • 請求項13 下図化合物等
  • マックス-デルブルック-セントラム フール モレクラーレ メディツィン(エムディーシー) 他

ω-3(n-3)多価不飽和脂肪酸(PUFA)からシトクロムP450(CYP)酵素により生産されるエポキシ代謝物の類似体である、一般式(I)による化合物に関する。 更に、これらの化合物を1種類以上含む組成物と、炎症、増殖、高血圧、凝固、免疫機能、病的血管新生、心不全、及び心不整脈に関連する状態及び疾患を治療又は予防するための、これらの化合物又は組成物の使用とに関する。

2017-505315

3-置換カルボニル-ナフト[2,3-b]フラン誘導体又はその薬学的に許容される塩

3-置換カルボニル-ナフト[2,3-b]フラン誘導体又はその薬学的に許容される塩

  • 請求項14 メチル 2-(1,1-ジメトキシエチル)-4,9-ジオキソ-4,9-ジヒドロナフト[2,3-b]フラン-3-カルボキシレート 実施例1を例示
  • ボストン バイオメディカル, インコーポレイテッド

癌細胞の増殖及びスフェア形成能の抑制に優れた効果を示し、抗腫瘍薬又は細胞増殖阻害剤として有用

2017-505316

抗精神病薬物およびVMAT2阻害剤を含む医薬組成物およびその使用

抗精神病薬物およびVMAT2阻害剤を含む医薬組成物およびその使用

  • 請求項13  VMAT2阻害剤が、テトラベナジン
  • ニューロクライン バイオサイエンシーズ,インコーポレイテッド

抗精神病化合物およびVMAT2阻害剤を含む医薬組成物を、それを必要とする対象に投与することによって、統合失調症および統合失調性感情障害を処置する新しい方法 抗精神病薬およびVMAT2阻害剤の組合せが、治療相乗作用を示し、精神神経系障害、例えば統合失調症、統合失調性感情障害、双極性疾患、大うつ病性障害、および一般に抗精神病薬で処置される他の状態の処置における抗精神病薬の治療指数を改善するという発見に関する。本明細書では、抗精神病薬を現在受けている患者の疾患を処置する新しい方法、および統合失調症などの精神神経系障害の処置において有用な医薬組成物が提供される。より具体的には、本明細書に記載の方法は、抗精神病薬およびVMAT2阻害剤を組み合わせて投与することを含む。

2017-505318

RORガンマのジヒドロピロロピリジン阻害剤

RORガンマのジヒドロピロロピリジン阻害剤

  • 化合物番号3 を例示
  • ヴァイティー ファーマシューティカルズ,インコーポレイテッド

RORγによって媒介される疾患及び障害の治療に有用 炎症性、代謝性、自己免疫性、及び他の疾患または障害の治療 疾患または障害が、喘息、アトピー性皮膚炎、座瘡、クローン病、限局性腸炎、潰瘍性大腸炎、シェーグレン症候群、ブドウ膜炎、ベーチェット病、皮膚筋炎、多発性硬化症、強直性脊椎炎、全身性エリテマトーデス(SLE)、強皮症、乾癬、乾癬性関節炎(PsA)、ステロイド耐性喘息、及びリウマチ性関節炎から選択される

2017-505319

EGFR-T790Mキナーゼ阻害剤として置換されたピリミジニウム類化合物

EGFR-T790Mキナーゼ阻害剤として置換されたピリミジニウム類化合物

  • 請求項6 下図を例示
  • チャンスー メドリューション リミテッド

プロテインキナーゼ阻害活性を有するとともに、プロテインキナーゼにより媒介される疾病あるいは症例の治療 EGFR-T790Mキナーゼにより媒介される症例の治療又は予防 非小細胞肺がんの治療

2017-505321

異常な細胞成長を処置するための方法および組成物

異常な細胞成長を処置するための方法および組成物

  • FAK阻害剤 VS-6063とMEK阻害剤 GDC-0623を例示
  • ベラステム・インコーポレーテッド

異常な細胞成長(例えば、がん)を処置するための、FAK阻害剤およびMEK阻害剤の組み合わせ FAK阻害剤(例えば、VS-6063または薬学的に許容されるその塩)をMEK阻害剤(例えば、GDC-0623、コビメチニブ、トラメチニブ、ピマセルチブ、AZD6244)と組み合わせて上記被験体に投与し、これにより上記被験体を処置

2017-505322

化合物の組成物およびその使用

化合物の組成物およびその使用

  • 請求項8  4-{[4-アミノ-3-(4-シクロヘキシルピペラジン-1-イル)-9,10-ジオキソ-9,10-ジヒドロアントラセン-1-イル]アミノ}ベンゼンスルホンアミド 表1(10)を例示
  • ブイエム オンコロジー リミテッド ライアビリティ カンパニー

あるタイプの癌、疼痛、炎症、再狭窄、アテローム性動脈硬化症、乾癬、血栓症、アルツハイマー病;髄鞘発育不全または髄鞘脱落に関する疾患、障害、損傷または機能不全の治療および/または予防

2017-505323

ムスカリンM1受容体アゴニストとしての二環式アザ化合物

ムスカリンM1受容体アゴニストとしての二環式アザ化合物

  • 請求項18 実施例2-87 を例示
  • ヘプタレス セラピューティクス リミテッド

ムスカリンM1受容体及び/またはM4受容体のアゴニストであり、ムスカリンM1/M4受容体媒介性疾患の処置に有用

2017-505327

6-ヘテロアリールオキシ-および6-アリールオキシ-キノリン-2-カルボキシアミドならびにその使用

6-ヘテロアリールオキシ-および6-アリールオキシ-キノリン-2-カルボキシアミドならびにその使用

  • 請求項24  ピペラジン-1-イル(6-{[5-(トリフルオロメチル)ピリジン-2-イル]オキシ}キノリン-2-イル)メタノン 実施例1 を例示
  • アッヴィ・インコーポレイテッド

電位開口型ナトリウムチャネル、例えば、Nav1.7および/またはNav1.8によって予防または寛解される状態または障害を処置するうえで有用 疼痛、神経障害、炎症、自己免疫疾患、線維症、慢性腎臓疾患および癌に関連した状態および障害を処置または予防するのに有用

2017-505328

PDE1阻害剤としてのヘキサヒドロフロピロール

PDE1阻害剤としてのヘキサヒドロフロピロール

  • 請求項3 (3aS,6aS)-4-(7,8-ジメトキシキナゾリン-4-イル)ヘキサヒドロ-2H-フロ[3,2-b]ピロール 実施例1 の(3aS,6aS)体
  • ハー・ルンドベック・アクチエゼルスカベット

PDE1阻害剤としてのヘキサヒドロフロピロール、ならびに医薬、特に、神経変性障害および精神障害を治療 統合失調症に関連する認知障害の治療 注意欠陥多動障害(ADHD)の治療 アルツハイマー病の治療 パーキンソン病の治療 ハンチントン病の治療

2017-505329

炎症性障害の治療のための新規な塩及びその医薬組成物 2017-505330 同様特許

炎症性障害の治療のための新規な塩及びその医薬組成物 

2017-505330 同様特許

  • 請求項1
  • ガラパゴス・ナムローゼ・フェンノートシャップ

炎症性病態、自己免疫疾患、増殖性疾患、アレルギー、移植片拒絶、軟骨恒常性の低下及び/もしくは破壊を伴う疾患、先天性軟骨形成異常、及び/又はIL6もしくはインターフェロンの分泌過多に関連する疾患の予防並びに/又は治療に有用な化合物1の塩

2017-505333

心血管疾患の治療または予防に用いるためのコレステリルエステル転送タンパク質(CETP)阻害剤および当該阻害剤を含む医薬組成物

心血管疾患の治療または予防に用いるためのコレステリルエステル転送タンパク質(CETP)阻害剤および当該阻害剤を含む医薬組成物

  • 請求項1
  • 田辺三菱製薬株式会社

心血管疾患、特に脂質異常症または混合型脂質異常症に罹患したまたはリスクが高い対象の治療に用いるための、コレステリルエステル転送タンパク質(CETP)阻害剤

2017-505337

IRAK4阻害剤としてのインダゾール化合物

IRAK4阻害剤としてのインダゾール化合物

  • 請求項20 実施例1 を例示
  • アウリジーン ディスカバリー テクノロジーズ リミテッド

キナーゼ阻害剤、特にIRAK4阻害剤として治療的に有用 IRAK4酵素によって媒介される疾患又は障害におけるそれらの使用において有用 IRAK4媒介の障害又は疾患又は状態が、がん、炎症性障害、自己免疫疾患、代謝障害、遺伝性障害、ホルモン関連疾患、免疫不全障害、細胞死に関連する状態、破壊性骨障害、トロンビン誘発血小板凝集、肝臓疾患及び心血管障害からなる群から選択される

2017-505343

ホスホイノシチド3-キナーゼ阻害剤としての三環式複素環式化合物

ホスホイノシチド3-キナーゼ阻害剤としての三環式複素環式化合物

  • 請求項13 下図化合物等
  • カルス セラピューティクス リミテッド

クラスIAホスホイノシチド3-キナーゼ酵素、PI3K-p110δの阻害剤として有用であり、したがって、がん、免疫疾患および炎症性疾患の治療において潜在的な実用可能性を有する

2017-505345

がんの処置のためのPI3K阻害剤を含む組合せ医薬

がんの処置のためのPI3K阻害剤を含む組合せ医薬

  • (S)-ピロリジン-1,2-ジカルボン酸2-アミド1-({4-メチル-5-[2-(2,2,2- トリフルオロ-1,1-ジメチル-エチル)-ピリジン-4-イル]-チアゾール-2-イル}-アミド)
  • ノバルティス アーゲー

(a)α-アイソフォーム特異的ホスファチジルイノシトール-3-キナーゼ阻害剤(S)-ピロリジン-1,2-ジカルボン酸2-アミド1-({4-メチル-5-[2-(2,2,2-トリフルオロ-1,1-ジメチル-エチル)-ピリジン-4-イル]-チアゾール-2-イル}-アミド)または任意の薬学的に許容されるその塩、(b)mTOR阻害剤、および(c)エキセメスタンまたは任意の薬学的に許容されるその塩を含む、特に増殖性疾患の処置または予防における使用のための組合せ医薬 mTOR阻害剤が、RAD、ラパマイシン(シロリムス)等

2017-505346

新規な3-(インドール-3-イル)-ピリジン誘導体、医薬組成物、および使用方法

新規な3-(インドール-3-イル)-ピリジン誘導体、医薬組成物、および使用方法

  • 実施例34 を例示
  • アイティーオス セラペウティクス

式Iの化合物のTDO2阻害薬としての使用 がん、パーキンソン病、アルツハイマー病、およびハンチントン病などの神経変性障害、HCVおよびHIVなどの慢性ウイルス感染症、うつ病、および肥満の治療および/または予防