公开(公告)号：US09550777B2

公开(公告)日：2017-01-24

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 ,  A61K31/4439 ,  C07D405/04 ,  A61P25/28 ,  C07D401/14 ,  A61P25/16 ,  C07D401/04

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: 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。

公开(公告)号：US20150051201A1

公开(公告)日：2015-02-19

申请号：US14531349

申请日：2014-11-03

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Bryan K. Chan ,  Jennafer Dotson ,  Anthony Estrada ,  Timothy Heffron ,  Joseph Lyssikatos ,  Zachary Sweeney

IPC: C07D487/04 ,  C07D498/04 ,  C07D498/20 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/506 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D498/04 ,  C07D498/20

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中X，R 1，R 2，R 3和A如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US20140328805A1

公开(公告)日：2014-11-06

申请号：US14267011

申请日：2014-05-01

Applicant: GENENTECH, INC.

Inventor： Anthony Estrada ,  Alan G. Olivero ,  Snahel Patel ,  Michael Siu

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

CPC classification number: A61K31/506 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/553 ,  A61K35/30 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D471/18 ,  C07D487/08 ,  C07D487/14 ,  C07D487/18 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  A61K2300/00

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.

Abstract translation: 本发明提供式I化合物及其实施方案及其盐用于治疗疾病（如神经变性疾病）。 式中的R 1，R 2，R 3，X 1，X 2，A和Cy变量均具有如本文所定义的含义。

公开(公告)号：US20140288043A1

公开(公告)日：2014-09-25

申请号：US13847409

申请日：2013-03-19

Applicant: Genentech, Inc.

Inventor： Bryan Chan ,  Anthony Estrada ,  Daniel Shore ,  Zachary Sweeney

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: A first aspect of the invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, Wherein R1 is a group selected from alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl and cycloalkyl, each of which is optionally substituted, and wherein X1, X2, X3 and X4 are as defined herein. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (1A) and (1B).

Abstract translation: 本发明的第一方面涉及式（1A）或（1B）化合物或其药学上可接受的盐，其中R1是选自烷基，单环杂环烷基，双环杂环烷基和环烷基的基团，其各自任选被取代 ，并且其中X1，X2，X3和X4如本文所定义。 其它方面涉及药物组合物，治疗用途和制备式（1A）和（1B）化合物的方法。

公开(公告)号：US20130158057A1

公开(公告)日：2013-06-20

申请号：US13687421

申请日：2012-11-28

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Mark Chambers ,  Bryan K. Chan ,  Anthony Estrada ,  Zachary Kevin Sweeney

IPC: C07D417/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/12 ,  C07D413/12

CPC classification number: A61K31/505 ,  C07D239/47 ,  C07D239/48 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

公开(公告)号：US20130096102A1

公开(公告)日：2013-04-18

申请号：US13712015

申请日：2012-12-12

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Daniel Jon Burdick ,  Mark Chambers ,  Bryan K. Chan ,  Huifen Chen ,  Anthony Estrada ,  Janet Gunzner-Toste ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Shumei Wang ,  Guiling Zhao

IPC: C07D413/14 ,  C07D498/08 ,  C07D413/12

CPC classification number: C07D413/14 ,  C07D403/14 ,  C07D413/12 ,  C07D473/16 ,  C07D498/06 ,  C07D498/08

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，n。 X，R 1，R 2，R 3，R 5，R 6和R 7如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US11129832B2

公开(公告)日：2021-09-28

申请号：US16666273

申请日：2019-10-28

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Liting Dong ,  Kevin X. Chen ,  Paul Gibbons ,  Malcolm Huestis ,  Terry Kellar ,  Wen Liu ,  Changyou Ma ,  Joseph P. Lyssikatos ,  Alan G. Olivero ,  Snahel Patel ,  Daniel Shore ,  Michael Siu

IPC: C07D471/08 ,  A61K31/506 ,  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-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 I-I all have the meaning as defined herein.

公开(公告)号：USRE47848E1

公开(公告)日：2020-02-11

申请号：US15902746

申请日：2018-02-22

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Alan G. Olivero ,  Snahel Patel ,  Michael Siu ,  Joseph Lyssikatos ,  Malcolm Huestis ,  Terry Kellar

IPC: A61K31/55 ,  C07D403/14 ,  A61K35/30 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  C07D471/08 ,  A61K45/06 ,  A61K31/5386 ,  C07D487/08 ,  C07D413/14 ,  C07D471/18 ,  C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/553 ,  A61K31/155

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：US10179782B2

公开(公告)日：2019-01-15

申请号：US15042310

申请日：2016-02-12

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Elisia Villemure ,  Vishal Verma ,  Daniel Shore ,  Matthew Volgraf ,  Baihua Hu ,  Aijun Lu

IPC: C07D417/14 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D403/14 ,  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.

公开(公告)号：US10028942B2

公开(公告)日：2018-07-24

申请号：US15374047

申请日：2016-12-09

Applicant: Genentech, Inc.

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

IPC: A61K31/4439 ,  A61K31/437 ,  A61K31/4545

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.