公开(公告)号：US09365583B2

公开(公告)日：2016-06-14

申请号：US14576890

申请日：2014-12-19

Applicant: Genentech, Inc.

Inventor： Michael Siu ,  Anthony Estrada ,  Wen Liu ,  Joseph P. Lyssikatos ,  Snahel Patel ,  Guibai Liang ,  Kevin Chen

IPC: C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/10 ,  C07D401/04

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/10

Abstract: The present invention provides for compounds of formula 0 and various embodiments thereof, and compositions comprising compounds of formula 0 and various embodiments thereof. In compounds of formula 0, the groups R1A, R1B, R1C, R1D, R2, R3, R4, R5 and R6 have the meaning as described herein. The present invention also provides for methods of using compounds of formula 0 and compositions comprising compounds of formula 0 as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Abstract translation: 本发明提供式0化合物及其各种实施方案，以及包含式0化合物及其各种实施方案的组合物。 在式0的化合物中，基团R1A，R1B，R1C，R1D，R2，R3，R4，R5和R6具有如本文所述的含义。 本发明还提供使用式0化合物和包含式0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：US10206931B2

公开(公告)日：2019-02-19

申请号：US15482581

申请日：2017-04-07

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： F. Anthony Romero ,  Steven R. Magnuson ,  Richard Pastor ,  Vickie Hsiao-Wei Tsui ,  Jeremy Murray ,  Terry Crawford ,  Daniel J. Burdick ,  Brian K. Albrecht ,  Alexandre Cote ,  Alexander M. Taylor ,  Christopher G. Nasveschuck ,  Yves LeBlanc ,  Michael Charles Hewitt ,  Kwong Wah Lai ,  Kevin Chen

IPC: A61K31/551 ,  C07D243/12 ,  C07D403/04 ,  C07D403/14 ,  A61K31/55 ,  C07D223/16 ,  C07D267/14 ,  C07D401/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D243/24 ,  C07D471/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/337 ,  A61K31/5513

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

公开(公告)号：US20170312292A1

公开(公告)日：2017-11-02

申请号：US15482581

申请日：2017-04-07

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Anthony F. Romero ,  Steven R. Magnuson ,  Richard Pastor ,  Vickie Hsiao-Wei Tsui ,  Jeremy Murray ,  Terry Crawford ,  Daniel J. Burdick ,  Brian K. Albrecht ,  Alexandre Cote ,  Alexander M. Taylor ,  Christopher G. Nasveschuck ,  Yves LeBlanc ,  Michael Charles Hewitt ,  Kwong Wah Lai ,  Kevin Chen

IPC: A61K31/55 ,  C07D403/04 ,  C07D243/24 ,  A61K31/5513 ,  C07D243/12 ,  C07D223/16 ,  C07D403/14 ,  C07D267/14

CPC classification number: A61K31/55 ,  A61K31/337 ,  A61K31/5513 ,  A61K45/06 ,  C07D223/16 ,  C07D243/12 ,  C07D243/24 ,  C07D267/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

公开(公告)号：US20150175619A1

公开(公告)日：2015-06-25

申请号：US14576890

申请日：2014-12-19

Applicant: Genentech, Inc.

Inventor： Michael Siu ,  Anthony Estrada ,  Wen Liu ,  Joseph P. Lyssikatos ,  Snahel Patel ,  Guibai Liang ,  Kevin Chen

IPC: C07D491/107 ,  C07D401/04 ,  C07D491/08 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D407/14

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/10

Abstract: The present invention provides for compounds of formula 0 and various embodiments thereof, and compositions comprising compounds of formula 0 and various embodiments thereof. In compounds of formula 0, the groups R1A, R1B, R1C, R1D, R2, R3, R4, R5 and R6 have the meaning as described herein. The present invention also provides for methods of using compounds of formula 0 and compositions comprising compounds of formula 0 as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Abstract translation: 本发明提供式0化合物及其各种实施方案，以及包含式0化合物及其各种实施方案的组合物。 在式0的化合物中，基团R1A，R1B，R1C，R1D，R2，R3，R4，R5和R6具有如本文所述的含义。 本发明还提供使用式0化合物和包含式0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。