公开(公告)号：US20160244456A1

公开(公告)日：2016-08-25

申请号：US15144422

申请日：2016-05-02

Applicant: Genentech, Inc.

Inventor： Jeffrey BLANEY ,  Paul A. GIBBONS ,  Emily HANAN ,  Joseph P. LYSSIKATOS ,  Steven R. MAGNUSON ,  Richard PASTOR ,  Thomas E. RAWSON ,  Aihe ZHOU ,  Bing-Yan ZHU

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.

Abstract translation: 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：US20230218782A1

公开(公告)日：2023-07-13

申请号：US18056856

申请日：2022-11-18

Applicant: Genentech, Inc.

Inventor： Jan MARIK ,  Joseph P. LYSSIKATOS ,  Simon Peter WILLIAMS

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04

CPC classification number: A61K51/0459 ,  C07B59/002 ,  C07D487/04 ,  C07B2200/05

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V):










and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

公开(公告)号：US20180282272A1

公开(公告)日：2018-10-04

申请号：US16001770

申请日：2018-06-06

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 ,  C07D451/02 ,  C07D491/048 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D403/12 ,  C07D417/12 ,  C07D401/12

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：US20160221945A1

公开(公告)日：2016-08-04

申请号：US15095467

申请日：2016-04-11

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 ,  C07D403/14 ,  C07D417/12 ,  C07D405/14 ,  C07D491/048 ,  C07D451/02 ,  C07D401/14 ,  C07D401/12

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.

Abstract translation: 本发明涉及式I或II化合物及其盐。 此外，本发明涉及制备方法和使用式I或II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：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：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.