公开(公告)号：US20150197509A1

公开(公告)日：2015-07-16

申请号：US14671643

申请日：2015-03-27

Applicant: Hoffmann-La Roche Inc. ,  GENENTECH, INC.

Inventor： Christine E. BROTHERTON-PLEISS ,  Huifen CHEN ,  Shaoqing CHEN ,  Zhi CHEN ,  Shawn David ERICKSON ,  Anthony ESTRADA ,  Kyungjin KIM ,  Hongju LI ,  Allen John LOVEY ,  Joseph P. LYSSIKATOS ,  Yimin QIAN ,  Sung-Sau SO ,  Peter Michael WOVKULICH ,  Lin YI, I

IPC: C07D409/12 ,  C07C311/17 ,  C07D239/26 ,  C07C311/20 ,  C07D403/12 ,  C07D305/06 ,  C07D401/04 ,  C07D401/12 ,  C07D305/08 ,  C07D237/08 ,  C07C311/16 ,  C07D213/40

CPC classification number: C07D409/12 ,  C07C311/16 ,  C07C311/17 ,  C07C311/19 ,  C07C311/20 ,  C07C2601/02 ,  C07D213/26 ,  C07D213/40 ,  C07D231/18 ,  C07D237/08 ,  C07D239/26 ,  C07D239/42 ,  C07D241/12 ,  C07D305/06 ,  C07D305/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/14

Abstract: The invention is concerned with the compounds of formula (I): and salts thereof, wherein X, Y, Z, R1, R2, R3, R3′, R4, R5 and R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and 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.

Abstract translation: 本发明涉及式（I）化合物及其盐，其中X，Y，Z，R 1，R 2，R 3，R 3，R 4，R 5和R 6在详细说明书和权利要求书中定义。 此外，本发明涉及制备和使用式（I）化合物的方法以及含有这些化合物的药物组合物。 该化合物可用于治疗TRPA1介导的疾病和病症，例如疼痛。

公开(公告)号：US20200181154A1

公开(公告)日：2020-06-11

申请号：US16789081

申请日：2020-02-12

Applicant: Genentech, Inc.

Inventor： Roland J. BILLEDEAU ,  James J. CRAWFORD ,  Saul JAIME-FIGUEROA ,  Wendy LEE ,  Francisco Javier LOPEZ-TAPIA ,  Sung-Sau SO

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/14 ,  C07D471/04 ,  A61K31/502 ,  C07D405/14 ,  C07D401/14 ,  A61K31/519 ,  A61K31/5025 ,  A61K31/4985 ,  A61K31/496 ,  A61K45/06

Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20190194209A1

公开(公告)日：2019-06-27

申请号：US16289287

申请日：2019-02-28

Applicant: Genentech, Inc.

Inventor： Roland J. BILLEDEAU ,  James J. CRAWFORD ,  Saul JAIME-FIGUEROA ,  Wendy LEE ,  Francisco Javier LOPEZ-TAPIA ,  Sung-Sau SO

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/5025 ,  A61K31/4985 ,  A61K31/496 ,  A61K45/06 ,  C07D401/14 ,  C07D471/14 ,  C07D471/04 ,  A61K31/502 ,  C07D405/14 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/519 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20180057500A1

公开(公告)日：2018-03-01

申请号：US15690140

申请日：2017-08-29

Applicant: Genentech, Inc.

Inventor： Roland J BILLEDEAU ,  James J. CRAWFORD ,  Saul JAIME-FIGUEROA ,  Wendy LEE ,  Francisco Javier LOPEZ-TAPIA ,  Sung-Sau SO

IPC: C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  C07D401/14 ,  A61K31/502 ,  C07D471/14 ,  A61K31/496

CPC classification number: C07D487/04 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/519 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.