公开(公告)号：US20170283424A1

公开(公告)日：2017-10-05

申请号：US15627847

申请日：2017-06-20

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

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

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：US20170087137A1

公开(公告)日：2017-03-30

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

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.

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：US20140038939A1

公开(公告)日：2014-02-06

申请号：US14049458

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: C07D487/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. 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 JAK kinase activity in a patient are disclosed.

公开(公告)号：US20240368186A1

公开(公告)日：2024-11-07

申请号：US18676200

申请日：2024-05-28

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

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

公开(公告)号：US20210277024A1

公开(公告)日：2021-09-09

申请号：US17156384

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Terry Kellar ,  Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Lewis J. Gazzard ,  Timothy Heffron ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D519/00 ,  C07D471/04 ,  A61P37/04

Abstract: Naphthyridine 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 naphthyridine compounds.

公开(公告)号：US20210253580A1

公开(公告)日：2021-08-19

申请号：US17156387

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Joy Alison Drobnick ,  Lewis J. Gazzard ,  Timothy Heffron ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  C07D487/14 ,  C07D498/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D498/04 ,  A61P37/04

Abstract: Isoquinoline 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 isoquinoline compounds.

公开(公告)号：US10407424B2

公开(公告)日：2019-09-10

申请号：US15942321

申请日：2018-03-30

Applicant: Genentech, Inc.

Inventor： Bryan Chan ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Matthew W. Cartwright ,  Emanuela Gancia ,  Graham Jones ,  Blake Daniels ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu ,  Baihua Hu ,  Aijun Lu ,  Joy Drobnick ,  Lewis Gazzard ,  Timothy Heffron ,  Malcolm Huestis ,  Jun Liang ,  Sushant Malhotra ,  Rohan Mendonca

IPC: C07D471/04 ,  A61K31/55 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/551 ,  A61K45/06

Abstract: Naphthyridine compounds and their use as inhibitors of HPK1 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 naphthyridine compounds.

公开(公告)号：US10131675B2

公开(公告)日：2018-11-20

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 ,  C07D491/14 ,  C07D519/00 ,  A61K31/5383 ,  A61K45/06 ,  A61K31/553

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：US20180117044A1

公开(公告)日：2018-05-03

申请号：US15852235

申请日：2017-12-22

Applicant: Genentech, Inc.

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

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

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.