公开(公告)号：US20250064945A1

公开(公告)日：2025-02-27

申请号：US18709947

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Huifen Chen ,  Peter Scott Dragovich ,  Leanna Renee Staben ,  Jing Wang

IPC: A61K47/55 ,  A61K31/519 ,  A61K47/54 ,  C07D487/04 ,  C07D519/00

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20250059198A1

公开(公告)日：2025-02-20

申请号：US18710130

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Fabio Broccatelli ,  Huifen Chen ,  Peter Scott Dragovich ,  Jing Wang

IPC: C07D487/08 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/551 ,  C07D413/14 ,  C07D417/14 ,  C07D498/10

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US11607396B2

公开(公告)日：2023-03-21

申请号：US17141070

申请日：2021-01-04

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen

IPC: A61K31/16 ,  A61P9/10 ,  C07D519/00 ,  A61P9/00 ,  A61P29/00 ,  A61P43/00 ,  A61K31/396 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/5383 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048

Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

公开(公告)号：US11098058B2

公开(公告)日：2021-08-24

申请号：US16034207

申请日：2018-07-12

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen ,  Blake Daniels ,  Craig Stivala

IPC: C07D498/04 ,  C07D487/04 ,  A61P25/16 ,  A61P25/28 ,  C07D235/12 ,  C07D471/04 ,  A61P17/06 ,  A61P21/00 ,  A61P19/02 ,  A61P1/00

Abstract: The invention provides novel compounds having the general formula I: wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

公开(公告)号：US11071721B2

公开(公告)日：2021-07-27

申请号：US15828271

申请日：2017-11-30

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen

IPC: C07D471/04 ,  A61K31/16 ,  A61P9/10 ,  C07D519/00 ,  A61P9/00 ,  A61P29/00 ,  A61P43/00 ,  A61K31/396 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/5383 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048

Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

公开(公告)号：US10988459B2

公开(公告)日：2021-04-27

申请号：US15200058

申请日：2016-07-01

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Craig Stivala ,  Huifen Chen ,  Guiling Zhao

IPC: A61K31/551 ,  C07D487/04 ,  C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04 ,  C07D495/04 ,  C07D491/04 ,  C07D491/10 ,  C07D413/14 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D519/00

Abstract: The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

公开(公告)号：US20200038378A1

公开(公告)日：2020-02-06

申请号：US16590329

申请日：2019-10-01

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： ANDREW P. CREW ,  Jing Wang ,  Michael Berlin ,  Peter Dragovich ,  Huifen Chen ,  Leanna Staben

IPC: A61K31/427 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/4245 ,  A61K31/541 ,  A61K31/496 ,  A61K47/54

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20180153831A1

公开(公告)日：2018-06-07

申请号：US15828271

申请日：2017-11-30

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen

IPC: A61K31/16 ,  A61K31/5383 ,  A61K31/44 ,  A61K31/4196 ,  A61K31/416 ,  A61P9/10 ,  A61K31/397 ,  A61K31/396 ,  A61P29/00 ,  A61P43/00 ,  A61K31/4025

CPC classification number: A61K31/16 ,  A61K31/396 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/5383 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D519/00

Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

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：US20240076295A1

公开(公告)日：2024-03-07

申请号：US18108045

申请日：2023-02-10

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Andrew P. Crew ,  Jing Wang ,  Michael Berlin ,  Peter Dragovich ,  Huifen Chen ,  Leanna Staben

IPC: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/54 ,  A61P35/00 ,  C07D413/14

CPC classification number: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/545 ,  A61P35/00 ,  C07D413/14

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.