公开(公告)号：US09670208B2

公开(公告)日：2017-06-06

申请号：US15197445

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  John Gaudino ,  Indrani W. Gunawardana ,  Erik James Hicken ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Lewis Gazzard ,  Jane Schmidt ,  Steve Do

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/444 ,  C07D487/04 ,  C07D519/00 ,  A61K31/55

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.

公开(公告)号：US20140249127A1

公开(公告)日：2014-09-04

申请号：US14181418

申请日：2014-02-14

Applicant: Genentech, Inc. ,  Array BioPharma Inc.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: C07D417/14 ,  C07D409/14 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/04

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐，其可用于治疗过度增生，疼痛和炎性疾病。 公开了使用式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20140171407A1

公开(公告)日：2014-06-19

申请号：US14182190

申请日：2014-02-17

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Lewis Gazzard ,  Karen Williams ,  Huifen Chen ,  Samuel Kintz ,  Joy Drobnick ,  Joseph P. Lyssikatos ,  Simon Goodacre ,  Calum Macleod ,  Charles Ellwood

IPC: C07D471/14 ,  A61K31/4375 ,  C07D453/02 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/439 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D453/02 ,  C07D519/00

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US08697715B2

公开(公告)日：2014-04-15

申请号：US13782513

申请日：2013-03-01

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: A01N43/54 ,  A61K31/505

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐，其可用于治疗过度增生，疼痛和炎性疾病。 公开了使用式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20240076295A1

公开(公告)日：2024-03-07

申请号：US18108045

申请日：2023-02-10

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Andrew P. Crew ,  Jing Wang ,  Michael Berlin ,  Peter Dragovich ,  Huifen Chen ,  Leanna Staben

IPC: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/54 ,  A61P35/00 ,  C07D413/14

CPC classification number: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/545 ,  A61P35/00 ,  C07D413/14

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US11834461B2

公开(公告)日：2023-12-05

申请号：US17147449

申请日：2021-01-12

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen ,  Blake Daniels ,  Craig Stivala

IPC: C07D498/04 ,  C07D487/04 ,  A61P25/16 ,  A61P25/28 ,  A61P17/06 ,  A61P21/00 ,  A61P19/02 ,  A61P1/00 ,  C07D235/12 ,  C07D471/04

CPC classification number: C07D498/04 ,  A61P25/16 ,  A61P25/28 ,  C07D235/12 ,  C07D471/04 ,  C07D487/04 ,  A61P1/00 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00

Abstract: The invention provides novel compounds having the general formula I:




wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

公开(公告)号：US11673892B2

公开(公告)日：2023-06-13

申请号：US16844952

申请日：2020-04-09

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Gregory Hamilton ,  Snahel Patel ,  Guiling Zhao ,  Blake Daniels ,  Craig Stivala

IPC: C07D487/04 ,  C07D519/00 ,  A61P25/28 ,  A61K31/4196 ,  A61P25/16

CPC classification number: C07D487/04 ,  A61P25/28 ,  C07D519/00 ,  C07B2200/05

Abstract: The invention provides novel compounds having the general formula I:




or pharmaceutically acceptable salts thereof, wherein

RA, RB1, RB2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

公开(公告)号：US20220339129A1

公开(公告)日：2022-10-27

申请号：US17141070

申请日：2021-01-04

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen

IPC: A61K31/16 ,  A61P9/10 ,  C07D519/00 ,  A61P9/00 ,  A61P29/00 ,  A61P43/00 ,  A61K31/396 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/5383 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048

Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

公开(公告)号：US10913742B2

公开(公告)日：2021-02-09

申请号：US16421114

申请日：2019-05-23

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Daniel Shore ,  Elisia Villemure ,  Matthew Volgraf ,  Baihua Hu ,  Aijun Lu ,  Andrew Cridland ,  Stuart Ward ,  Francis Beaumier ,  Martin Dery ,  Robin Larouche-Gauthier

IPC: C07D487/04 ,  C07D473/30 ,  C07D471/04 ,  C07D513/04 ,  A61K31/519 ,  A61P11/06 ,  C07D498/04

Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as respiratory disorders or pain.

公开(公告)号：US20180127393A1

公开(公告)日：2018-05-10

申请号：US15625297

申请日：2017-06-16

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: C07D401/04 ,  C07D471/04 ,  C07D417/14 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.