公开(公告)号：US20230121700A1

公开(公告)日：2023-04-20

申请号：US17816855

申请日：2022-08-02

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 ,  A61P29/00 ,  C07D513/04 ,  C07D487/04 ,  A61P25/00 ,  C07D498/04 ,  A61K31/427 ,  A61P23/00 ,  A61P11/00

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：US20240300974A1

公开(公告)日：2024-09-12

申请号：US18516014

申请日：2023-11-21

Applicant: Genentech, Inc.

Inventor： Snahel PATEL ,  Gregory HAMILTON ,  Guiling ZHAO ,  Huifen CHEN ,  Blake DANIELS ,  Craig STIVALA

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

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：US20190100530A1

公开(公告)日：2019-04-04

申请号：US16034207

申请日：2018-07-12

Applicant: Genentech, Inc.

Inventor： Snahel PATEL ,  Gregory HAMILTON ,  Guiling ZHAO ,  Huifen CHEN ,  Blake DANIELS ,  Craig STIVALA

IPC: C07D498/04 ,  C07D487/04 ,  C07D471/04 ,  C07D235/12

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：US20170001997A1

公开(公告)日：2017-01-05

申请号：US15266243

申请日：2016-09-15

Applicant: Genentech, Inc.

Inventor： Jason BURCH ,  Huifen CHEN ,  Xiaojing WANG

IPC: C07D417/14 ,  A61K31/427 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/4709 ,  C07D487/04 ,  A61K45/06

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/4985 ,  A61K45/06 ,  C07D487/04

Abstract: Oxepan-2-yl pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I 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: 包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中X是噻唑基，吡嗪基，吡啶基或嘧啶基的式I的氧杂环庚烷-2-基吡唑-4-基 - 杂环基 - 甲酰胺化合物可用于抑制Pim 激酶，并用于治疗由Pim激酶介导的疾病如癌症。 公开了使用式I化合物在体外，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：US20210340151A1

公开(公告)日：2021-11-04

申请号：US17371001

申请日：2021-07-08

Applicant: Genentech, Inc.

Inventor： Snahel PATEL ,  Gregory HAMILTON ,  Guiling ZHAO ,  Huifen CHEN ,  Blake DANIELS ,  Craig STIVALA

IPC: C07D487/04

Abstract: Some embodiments of the invention provide compounds having the general formula I: wherein R1, R2, R3a and R3b are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

公开(公告)号：US20210139504A1

公开(公告)日：2021-05-13

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 ,  C07D235/12 ,  C07D471/04

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：US20200048197A1

公开(公告)日：2020-02-13

申请号：US16657102

申请日：2019-10-18

Applicant: Genentech, Inc.

Inventor： Huifen CHEN ,  Yanyan CHU ,  Steven DO ,  Anthony ESTRADA ,  Baihua HU ,  Aleksandr KOLESNIKOV ,  Xingyu LIN ,  Joseph P. LYSSIKATOS ,  Daniel SHORE ,  Vishal VERMA ,  Lan WANG ,  Guosheng WU ,  Po-wai YUEN

IPC: C07D207/48 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14 ,  C07D417/12 ,  C07D451/02 ,  C07D491/048 ,  C07D405/14

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II 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：US20230159555A1

公开(公告)日：2023-05-25

申请号：US17814115

申请日：2022-07-21

Applicant: Genentech, Inc.

Inventor： Paul GIBBONS ,  Kwong Wah LAI ,  Christian NILEWSKI ,  Richard M. PASTOR ,  Steven Thomas STABEN ,  Craig STIVALA ,  Bing-Yan ZHU ,  Huifen CHEN

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: Described herein are compounds of Formula (I), Formula (I-A), and Formula (I-B),




solvates thereof, tautomers thereof, and pharmaceutically acceptable salts of the foregoing, Further described herein are methods of inhibiting NLRP3 using said compounds, and methods of and compositions useful in treating NLRP3-dependent disorders.

公开(公告)号：US20200283446A1

公开(公告)日：2020-09-10

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

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：US20200002340A1

公开(公告)日：2020-01-02

申请号：US16558718

申请日：2019-09-03

Applicant: Genentech, Inc.

Inventor： Huifen CHEN ,  Brian SAFINA ,  Daniel SHORE ,  Jack TERRETT ,  Elisia VILLEMURE ,  Matthew VOLGRAF ,  Stuart WARD ,  Aijun LU ,  Robin LAROUCHE-GAUTHIER ,  Francis BEAUMIER ,  Martin DERY ,  Lea CONSTANTINEAU-FORGET ,  Chantal GRAND-MAITRE ,  Luce LEPISSIER

IPC: C07D473/30 ,  C07D471/04 ,  C07D487/04 ,  C07D473/08

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 pain.