公开(公告)号：US20220306635A1

公开(公告)日：2022-09-29

申请号：US17068574

申请日：2020-10-12

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Xingyu Lin ,  Po-wai Yuen ,  Rohan Mendonca ,  Brendan Parr ,  Richard Pastor ,  Zhonghua Pei ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Xiaokai Li ,  Roheeth Pavana ,  Hima Potturi ,  Venkata Velvadapu ,  Jesse Waldo ,  Zuhui Zhang ,  Guosheng Wu ,  Benjamin Douglas Sellers

IPC: C07D487/04 ,  A61P35/00 ,  A61K38/16 ,  A61K45/06 ,  C07D519/00

Abstract: Presently provided are inhibitors of cellularly expressed TD02 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

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：US20190016726A1

公开(公告)日：2019-01-17

申请号：US16065397

申请日：2016-12-23

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Xingyu Lin ,  Po-wai Yuen ,  Rohan Mendonca ,  Brendan Parr ,  Richard Pastor ,  Zhonghua Pei ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Xiaokai Li ,  Roheeth Pavana ,  Hima Potturi ,  Venkata Velvadapu ,  Jesse Waldo ,  Zuhui Zhang ,  Guosheng Wu

IPC: C07D487/04 ,  A61P35/00 ,  C07D519/00 ,  A61K38/16

Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

公开(公告)号：US20160304519A1

公开(公告)日：2016-10-20

申请号：US15197445

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  John Gaudino ,  Indrani W. Gunawardana ,  Erik James Hicken ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Lewis Gazzard ,  Jane Schmidt ,  Steve Do

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/444 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，其可用于治疗疾病。 公开了使用式I化合物或其立体异构体，互变异构体或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗这些疾病或相关病理状况的方法。

公开(公告)号：US20150087630A1

公开(公告)日：2015-03-26

申请号：US14255898

申请日：2014-04-17

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/553 ,  A61K31/55 ,  A61K31/541 ,  A61K31/4375 ,  C07D519/00

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

Abstract translation: 式（I）化合物用于治疗癌症的方法：其中X，Y，X，R 3，R 5和R 6如本文所定义。

公开(公告)号：US11566003B2

公开(公告)日：2023-01-31

申请号：US16921297

申请日：2020-07-06

Applicant: Genentech, Inc.

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

IPC: C07D217/22 ,  A61K31/549 ,  A61P35/00 ,  A61K45/06 ,  C07D401/04 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/501 ,  C07D471/04 ,  C07D413/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D417/04 ,  A61K31/4985 ,  C07D401/14 ,  C07D487/04 ,  A61K31/551 ,  C07D498/04 ,  A61K31/5383 ,  C07D405/14 ,  C07D519/00 ,  C07D498/14 ,  C07D513/04 ,  A61K31/554 ,  A61K31/55 ,  A61K31/472 ,  C07D409/14 ,  C07D491/04 ,  C07D487/14

Abstract: Isoquinoline compounds 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：US10800780B2

公开(公告)日：2020-10-13

申请号：US16065397

申请日：2016-12-23

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Xingyu Lin ,  Po-wai Yuen ,  Rohan Mendonca ,  Brendan Parr ,  Richard Pastor ,  Zhonghua Pei ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Xiaokai Li ,  Roheeth Pavana ,  Hima Potturi ,  Venkata Velvadapu ,  Jesse Waldo ,  Zuhui Zhang ,  Guosheng Wu ,  Benjamin Douglas Sellers

IPC: A61K31/4188 ,  A61K31/407 ,  A61K31/4035 ,  C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61K45/06 ,  A61K38/16

Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

公开(公告)号：US20160303126A1

公开(公告)日：2016-10-20

申请号：US15197479

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: A61K31/506 ,  C07D403/14 ,  C07D471/04 ,  A61K31/4439 ,  C07D417/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/444 ,  A61K45/06 ,  C07D405/14

CPC classification number: A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

公开(公告)号：US09388171B2

公开(公告)日：2016-07-12

申请号：US14011501

申请日：2013-08-27

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Jim Blake ,  Huifen Chen ,  Mark Chicarelli ,  John Gaudino ,  Lewis Gazzard ,  Sam Kintz ,  Pete Mohr ,  Kirk Robarge ,  Jacob Schwarz ,  Aihe Zhou

IPC: C07D471/04 ,  C07D217/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  A61K31/4725 ,  A61K31/4375 ,  A61K31/472 ,  A61P35/00

CPC classification number: C07D405/14 ,  C07D217/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D471/04

Abstract: Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中本文定义的R2，X和Z是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。

公开(公告)号：US20240132507A1

公开(公告)日：2024-04-25

申请号：US18496146

申请日：2023-10-27

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Zhonghua Pei ,  Brendan Parr ,  Wendy Liu ,  Richard Pastor ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Hima Potturi ,  Guoshen Wu ,  Xingyu Lin ,  Yanyan Chu ,  Po-wai Yuen

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Presently provided are inhibitors of TD02 and IDO1 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.