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：US20150368244A1

公开(公告)日：2015-12-24

申请号：US14137972

申请日：2013-12-20

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Charles Goodacre ,  Joseph P. Lyssikatos ,  Calum MacLeod ,  Karen Williams ,  Huifen Chen

IPC: C07D471/14 ,  A61K31/496 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D471/14 ,  A61K31/496 ,  A61K31/519 ,  A61K45/06

Abstract: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) 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: 本发明涉及有用的式（I），（Ia），（Ib），（Ic），（Id），（Ie），（If），（Ig）和（Ih）的1,5-二氮杂咔唑化合物 作为激酶抑制剂，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：US20130261104A1

公开(公告)日：2013-10-03

申请号：US13890949

申请日：2013-05-09

Applicant: Genentech, Inc.

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

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  C07D513/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/541 ,  A61K31/501 ,  A61K31/506 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4375 ,  C07D491/107

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.

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：US09216980B2

公开(公告)日：2015-12-22

申请号：US14255898

申请日：2014-04-17

Applicant: Genentech, Inc.

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

IPC: A61K31/437 ,  A61K31/496 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/553 ,  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：US09206175B2

公开(公告)日：2015-12-08

申请号：US14068774

申请日：2013-10-31

Applicant: Genentech, Inc.

Inventor： Joseph P. Lyssikatos ,  Lewis J. Gazzard ,  Emily Hanan ,  Samuel S. Kintz ,  Hans Edward Purkey

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/47 ,  C07D221/02 ,  C07D471/02 ,  C07D217/00 ,  C07D471/04 ,  C07D217/22 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/04

CPC classification number: C07D471/04 ,  A61K31/47 ,  A61K31/4725 ,  C07D217/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/04

Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O−, and one of X2, X3 and X4 is N or N+—O− and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.

Abstract translation: 本发明提供具有以下通式的新化合物：其中X 1是N或N + O-，X 2，X 3和X 4中的一个是N或N + -O-，X 2，X 3和X 4的其余部分是C。R2，R3 ，R4，R5，R6。 A，B和Y如本文所述。 此外，式I的组合物化合物和使用方法在本文中进一步描述。

公开(公告)号：US11242344B2

公开(公告)日：2022-02-08

申请号：US16858004

申请日：2020-04-24

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Peter Dragovich ,  Lewis J. Gazzard ,  Thomas Pillow ,  Steven T. Staben ,  Binqing Wei ,  Jianfeng Xin

IPC: C07D471/16 ,  C07D493/10 ,  A61P35/00 ,  C07D417/14 ,  C07D413/14 ,  C07D403/04

Abstract: The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.

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.