公开(公告)号：US11655245B2

公开(公告)日：2023-05-23

申请号：US16903020

申请日：2020-06-16

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: A61K31/427 ,  A61P11/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D513/04 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D471/04 ,  C07D413/14

CPC classification number: C07D413/14 ,  A61K31/427 ,  A61P11/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The invention relates to methods of using compounds formula I:




and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. 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 pain.

公开(公告)号：US10710994B2

公开(公告)日：2020-07-14

申请号：US16355352

申请日：2019-03-15

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: A61P23/00 ,  A61P11/00 ,  A61P29/00 ,  A61P25/00 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D413/14 ,  C07D498/04 ,  C07D513/04 ,  A61K31/427

Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. 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 pain.

公开(公告)号：US20190284179A1

公开(公告)日：2019-09-19

申请号：US16355352

申请日：2019-03-15

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: C07D413/14 ,  C07D473/30 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D487/04 ,  A61P25/00 ,  A61P29/00

Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. 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 pain.

公开(公告)号：US10154995B2

公开(公告)日：2018-12-18

申请号：US15684733

申请日：2017-08-23

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: A61K31/506 ,  C07D417/14 ,  C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  C07D471/04 ,  C07D403/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06

Abstract: Compounds of Formula I or a stereoisomer, tautomer 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 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.

公开(公告)号：US09763942B2

公开(公告)日：2017-09-19

申请号：US15197479

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: C07D403/14 ,  C07D471/04 ,  C07D417/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/14

CPC classification number: A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of Formula I or a stereoisomer, tautomer 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 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.

公开(公告)号：US09592235B2

公开(公告)日：2017-03-14

申请号：US15184310

申请日：2016-06-16

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Terry Crawford ,  Seth F. Harris ,  Steven R. Magnuson ,  Chudi Ndubaku ,  Lan Wang

IPC: A61K31/551 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04 ,  C07D403/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D239/95 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/553

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: The invention provides a method of treating cancer in a patient by administering a compound of formula (I): wherein R1 R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

Abstract translation: 本发明提供具有以下通式的新化合物：其中A，R 1，R 2和R 3如本文所定义，包括该化合物的组合物和使用该化合物的方法。

公开(公告)号：US09586956B2

公开(公告)日：2017-03-07

申请号：US14448941

申请日：2014-07-31

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Terry Crawford ,  Steven R. Magnuson ,  Chudi Ndubaku ,  Lan Wang

IPC: C07D471/04 ,  C07D401/12 ,  C07D413/12 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D413/04

CPC classification number: C07D471/04 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12

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

Abstract translation: 本发明提供具有以下通式的新化合物：其中A，R 1和R 2如本文所述，包括该化合物的组合物和使用该化合物的方法。

公开(公告)号：US09212173B2

公开(公告)日：2015-12-15

申请号：US14531271

申请日：2014-11-03

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Daniel Jon Burdick ,  Bryan K. Chan ,  Mark Chambers ,  Huifen Chen ,  Anthony Estrada ,  Zachary Kevin Sweeney

IPC: A61K31/506 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D407/14 ,  C07D405/14

CPC classification number: C07D403/12 ,  A61K31/506 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14

Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 作为LRRK2的调节剂的吡唑化合物，制备化合物的方法，以及使用该化合物治疗与LRRK2受体相关的疾病如帕金森病的方法。

公开(公告)号：US20150328195A1

公开(公告)日：2015-11-19

申请号：US14743835

申请日：2015-06-18

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

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：US20150218176A1

公开(公告)日：2015-08-06

申请号：US14688724

申请日：2015-04-16

Applicant: Genentech, Inc.

Inventor： Daniel Burdick ,  Huifen Chen ,  Shumei Wang ,  Weiru Wang

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/4985

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K45/06

Abstract: Compounds having the formula I wherein R1 and R2 are as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中R 1和R 2如本文所定义，是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。