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：US20220073520A1

公开(公告)日：2022-03-10

申请号：US17213362

申请日：2021-03-26

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 ,  C07D403/04 ,  C07D401/04 ,  C07D405/14 ,  C07D237/28 ,  C07D401/14 ,  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：US20160257682A1

公开(公告)日：2016-09-08

申请号：US15152947

申请日：2016-05-12

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Francois Diederich ,  Jennafer Dotson ,  Emily Hanan ,  Timothy Heffron ,  Michael Lainchbury

IPC: C07D471/04 ,  A61K31/517 ,  A61K31/5386 ,  C07D519/00 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

Abstract translation: 本发明涉及作为含有EGFR突变体的T790M抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中用于预防或治疗癌症的新化合物。

公开(公告)号：US12297210B2

公开(公告)日：2025-05-13

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 ,  A61P37/04 ,  C07D471/04

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：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：US20220370420A1

公开(公告)日：2022-11-24

申请号：US17204089

申请日：2021-03-17

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Craig Stivala ,  BinQing Wei ,  Bryan K. Chan ,  Timothy Heffron ,  Michael Lainchbury ,  Andrew Madin ,  Terry Aaron Panchal ,  Eileen Mary Seward ,  Toby Blench ,  Matthew W. Cartwright ,  Elsa Amandine Dechaux ,  Richard Elliott ,  Emanuela Gancia

IPC: A61K31/437 ,  A61K45/06 ,  C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  C07D487/20 ,  C07D471/20 ,  A61K31/5377 ,  A61K31/444 ,  A61K31/496 ,  A61K31/513 ,  A61K31/4985

Abstract: Spirocyclic 2,3-dihydro-7-azaindole 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 spirocyclic 2,3-dihydro-7-azaindole compounds.

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.