公开(公告)号：US20250042919A1

公开(公告)日：2025-02-06

申请号：US18882588

申请日：2024-09-11

Applicant: Genentech, Inc.

Inventor： Lewis J. Gazzard ,  Samantha Alyson Green ,  Matthew Leo Landry ,  Sushant Malhotra ,  Michael Siu ,  Steven Do ,  Yun-Xing Cheng ,  Limin Cheng ,  Jianfeng Xin ,  Mingtao He

IPC: C07D498/22 ,  A61K31/553 ,  A61K45/06 ,  A61P35/00 ,  C07D519/00

Abstract: Provided herein are tetracyclic oxazepinyl compounds useful in the treatment on cancers.

公开(公告)号：US20240368170A1

公开(公告)日：2024-11-07

申请号：US18769184

申请日：2024-07-10

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Michael Siu ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Bryan K. Chan ,  Lewis J. Gazzard ,  Timothy Heffron ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D487/04 ,  C07D237/28 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D417/04

Abstract: Cinnoline compounds of formula (I): variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the cinnoline compounds.

公开(公告)号：US20220389020A1

公开(公告)日：2022-12-08

申请号：US17648045

申请日：2022-01-14

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC: C07D487/04 ,  A61P17/06 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I 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 Janus kinase activity in a patient are disclosed.

公开(公告)号：US10028954B2

公开(公告)日：2018-07-24

申请号：US15041375

申请日：2016-02-11

Applicant: Genentech, Inc.

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

IPC: A61K31/506 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/444

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.

公开(公告)号：US20170369510A1

公开(公告)日：2017-12-28

申请号：US15699095

申请日：2017-09-08

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Snahel Patel ,  Terry Kellar ,  Malcolm Huestis ,  Daniel Shore ,  Michael Siu

IPC: C07D498/14 ,  A61K45/06 ,  A61K31/553 ,  C07D519/00 ,  A61K31/5383

CPC classification number: C07D498/14 ,  A61K31/5383 ,  A61K31/553 ,  A61K45/06 ,  C07D491/14 ,  C07D519/00

Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein ring A and R1-R2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.

公开(公告)号：US20170239246A9

公开(公告)日：2017-08-24

申请号：US15041375

申请日：2016-02-11

Applicant: Genentech, Inc.

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

IPC: A61K31/506 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/55

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.

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：US20150080367A1

公开(公告)日：2015-03-19

申请号：US14550528

申请日：2014-11-21

Applicant: Genentech, Inc.

Inventor： Frederick Cohen ,  Malcolm Huestis ,  Cuong Ly ,  Snahel Patel ,  Michael Siu ,  Xianrui Zhao

IPC: C07D401/14 ,  C07D491/107 ,  C07D487/08 ,  C07D405/14

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D487/08 ,  C07D491/107

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, m, n and the C-linked Ring 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，m，n和C连接的环具有如本文所述的含义。 本发明还提供使用式I化合物的方法和包含式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。

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：US20240025919A1

公开(公告)日：2024-01-25

申请号：US18199449

申请日：2023-05-19

Applicant: Genentech, Inc.

Inventor： Matthew Leo Landry ,  Christian Nilewski ,  Michael Siu ,  Elisia Villemure ,  Yong Wang ,  BinQing Wei ,  Melissa Ann Ashley ,  Steven Do ,  Lewis John Gazzard ,  Samantha Alyson Green

IPC: C07D519/00 ,  C07D498/22 ,  A61P35/00

CPC classification number: C07D519/00 ,  A61P35/00 ,  C07D498/22

Abstract: Provided herein are aza-tetracyclic oxazepinyl compounds useful in the treatment of cancers.