公开(公告)号：US20200216456A1

公开(公告)日：2020-07-09

申请号：US16626191

申请日：2018-06-28

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 ,  Powai Yuen

IPC: C07D487/04

Abstract: Presently provided are inhibitors of TD02 and IDOl 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.

公开(公告)号：US09440976B2

公开(公告)日：2016-09-13

申请号：US14743835

申请日：2015-06-18

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Lewis Gazzard ,  Karen Williams ,  Huifen Chen ,  Samuel Kintz ,  Joy Drobnick ,  Joseph P. Lyssikatos ,  Simon Goodacre ,  Calum Macleod ,  Charles Ellwood

IPC: C07D471/14 ,  C07D453/02 ,  A61K31/5377 ,  C07D519/00 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D453/02 ,  C07D519/00

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US11944606B2

公开(公告)日：2024-04-02

申请号：US17178021

申请日：2021-02-17

Applicant: Genentech, Inc.

Inventor： Timothy Heffron ,  Sushant Malhotra ,  BinQing Wei ,  Bryan Chan ,  Lewis Gazzard ,  Emanuela Gancia ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  Yonghan Hu

IPC: A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  C07D471/04

CPC classification number: A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  C07D471/04

Abstract: Azaindole 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 azaindole compounds.

公开(公告)号：US11603373B2

公开(公告)日：2023-03-14

申请号：US16626219

申请日：2018-06-20

Applicant: Genentech, Inc.

Inventor： Zhonghua Pei ,  Richard Pastor ,  Lewis Gazzard ,  Brendan Parr ,  Wendy Liu ,  Rohan Mendonca ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D221/00 ,  C07D335/00 ,  C07D487/04 ,  C07D471/08 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00

Abstract: Presently provided are inhibitors of cellularly expressed 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.

公开(公告)号：US11034692B1

公开(公告)日：2021-06-15

申请号：US16542129

申请日：2019-08-15

Applicant: Genentech, Inc.

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

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

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：US10952995B2

公开(公告)日：2021-03-23

申请号：US16568459

申请日：2019-09-12

Applicant: Genentech, Inc.

Inventor： Timothy Heffron ,  Sushant Malhotra ,  BinQing Wei ,  Bryan Chan ,  Lewis Gazzard ,  Emanuela Gancia ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  Yonghan Hu

IPC: A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  C07D471/04

Abstract: Azaindole 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 azaindole compounds.

公开(公告)号：US20170348310A1

公开(公告)日：2017-12-07

申请号：US15684733

申请日：2017-08-23

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

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：US09670208B2

公开(公告)日：2017-06-06

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

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.

公开(公告)号：US20140171407A1

公开(公告)日：2014-06-19

申请号：US14182190

申请日：2014-02-17

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Lewis Gazzard ,  Karen Williams ,  Huifen Chen ,  Samuel Kintz ,  Joy Drobnick ,  Joseph P. Lyssikatos ,  Simon Goodacre ,  Calum Macleod ,  Charles Ellwood

IPC: C07D471/14 ,  A61K31/4375 ,  C07D453/02 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/439 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D453/02 ,  C07D519/00

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US11827639B2

公开(公告)日：2023-11-28

申请号：US16626191

申请日：2018-06-28

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 ,  Powai Yuen

IPC: C07D487/04 ,  A61K31/4188 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/437 ,  A61K31/4725 ,  A61K31/5377 ,  A61K45/06

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.