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：US20190144430A1

公开(公告)日：2019-05-16

申请号：US16247995

申请日：2019-01-15

Applicant: Genentech, Inc.

Inventor： Baihua HU ,  Vishal VERMA ,  Matthew VOLGRAF ,  Anthony ESTRADA ,  Joseph LYSSIKATOS

IPC: C07D403/04 ,  C07D231/12 ,  C07D401/04 ,  C07D231/20 ,  C07D239/26 ,  C07D231/16 ,  C07D213/61

Abstract: The invention is concerned with the 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.

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：US20200171029A1

公开(公告)日：2020-06-04

申请号：US16568130

申请日：2019-09-11

Applicant: Genentech, Inc.

Inventor： Anthony ESTRADA ,  Alan G. OLIVERO ,  Snahel PATEL ,  Michael SIU ,  Joseph LYSSIKATOS

IPC: A61K31/506 ,  C07D471/08 ,  A61K45/06 ,  A61K31/5386 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/55 ,  A61K35/30 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/18 ,  C07D487/08 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  A61K31/553 ,  C07D417/14 ,  C07D487/14 ,  C07D487/18 ,  A61K31/444

Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.

公开(公告)号：US20160264567A1

公开(公告)日：2016-09-15

申请号：US15042310

申请日：2016-02-12

Applicant: Genentech, Inc.

Inventor： Po-wai YUEN ,  Anthony ESTRADA ,  Huifen CHEN ,  Aleksandr KOLESNIKOV ,  Elisia VILLEMURE ,  Vishal VERMA ,  Lan WANG ,  Daniel SHORE ,  Steven DO ,  Matthew VOLGRAF ,  Baihua HU ,  Guosheng WU ,  Xingyu LIN ,  Aijun LU

IPC: C07D417/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07F9/6512 ,  C07D417/12 ,  C07D405/14 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07F9/6512

Abstract: The invention is concerned with the compounds of formula I: and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.

Abstract translation: 和其盐和本文公开的其它式II-IX化合物。 此外，本发明涉及制造方法和使用式I-IX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由TRPA1介导的疾病和病症，例如疼痛或哮喘。

公开(公告)号：US20160002228A1

公开(公告)日：2016-01-07

申请号：US14800829

申请日：2015-07-16

Applicant: Genentech, Inc.

Inventor： Anthony ESTRADA ,  Wen Liu ,  Snahel Patel ,  Michael Siu

IPC: C07D471/04 ,  C07D405/14 ,  C07D401/14

CPC classification number: A61K31/4439 ,  A61K31/437 ,  A61K31/4545 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Abstract translation: 本发明提供式（I）化合物及其各种实施方案，以及包含式（I）化合物及其各种实施方案的组合物。 在式I化合物中，基团R 1，R 2，R 3，R 4，R 5，R 6和R 7具有如本文所述的含义。 本发明还提供了使用式I化合物和包含式（I）化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症的方法。