公开(公告)号：US12281101B2

公开(公告)日：2025-04-22

申请号：US17198238

申请日：2021-03-10

Applicant: Genentech, Inc.

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

IPC: C07D403/12 ,  A61K31/55 ,  A61K31/553 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/06 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D491/10 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D498/16 ,  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：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：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.