公开(公告)号：US20200038378A1

公开(公告)日：2020-02-06

申请号：US16590329

申请日：2019-10-01

申请人： Arvinas Operations, Inc. ,  Genentech, Inc.

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

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

摘要： 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：US20190300521A1

公开(公告)日：2019-10-03

申请号：US16372345

申请日：2019-04-01

申请人： Arvinas Operations, Inc. ,  Genentech, Inc.

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

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

摘要： 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：US20240076295A1

公开(公告)日：2024-03-07

申请号：US18108045

申请日：2023-02-10

申请人： Arvinas Operations, Inc. ,  Genentech, Inc.

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

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

CPC分类号： C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/545 ,  A61P35/00 ,  C07D413/14

摘要： 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：US11655245B2

公开(公告)日：2023-05-23

申请号：US16903020

申请日：2020-06-16

申请人： Genentech, Inc.

发明人： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC分类号： A61K31/427 ,  A61P11/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D513/04 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D471/04 ,  C07D413/14

CPC分类号： C07D413/14 ,  A61K31/427 ,  A61P11/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： The invention relates to methods of using compounds formula I:




and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US10710994B2

公开(公告)日：2020-07-14

申请号：US16355352

申请日：2019-03-15

申请人： Genentech, Inc.

发明人： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC分类号： A61P23/00 ,  A61P11/00 ,  A61P29/00 ,  A61P25/00 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D413/14 ,  C07D498/04 ,  C07D513/04 ,  A61K31/427

摘要： The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20190284179A1

公开(公告)日：2019-09-19

申请号：US16355352

申请日：2019-03-15

申请人： Genentech, Inc.

发明人： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC分类号： C07D413/14 ,  C07D473/30 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D487/04 ,  A61P25/00 ,  A61P29/00

摘要： The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US10154995B2

公开(公告)日：2018-12-18

申请号：US15684733

申请日：2017-08-23

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： 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分类号： A61K31/506 ,  C07D417/14 ,  C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  C07D471/04 ,  C07D403/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06

摘要： 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：US09763942B2

公开(公告)日：2017-09-19

申请号：US15197479

申请日：2016-06-29

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： 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分类号： C07D403/14 ,  C07D471/04 ,  C07D417/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/14

CPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

摘要： 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：US09592235B2

公开(公告)日：2017-03-14

申请号：US15184310

申请日：2016-06-16

申请人： Genentech, Inc.

发明人： Huifen Chen ,  Terry Crawford ,  Seth F. Harris ,  Steven R. Magnuson ,  Chudi Ndubaku ,  Lan Wang

IPC分类号： A61K31/551 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04 ,  C07D403/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D239/95 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/553

CPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

摘要： The invention provides a method of treating cancer in a patient by administering a compound of formula (I): wherein R1 R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

摘要翻译： 本发明提供具有以下通式的新化合物：其中A，R 1，R 2和R 3如本文所定义，包括该化合物的组合物和使用该化合物的方法。

公开(公告)号：US09586956B2

公开(公告)日：2017-03-07

申请号：US14448941

申请日：2014-07-31

申请人： Genentech, Inc.

发明人： Huifen Chen ,  Terry Crawford ,  Steven R. Magnuson ,  Chudi Ndubaku ,  Lan Wang

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D413/12 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D413/04

CPC分类号： C07D471/04 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12

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

摘要翻译： 本发明提供具有以下通式的新化合物：其中A，R 1和R 2如本文所述，包括该化合物的组合物和使用该化合物的方法。