公开(公告)号：US20170312252A1

公开(公告)日：2017-11-02

申请号：US15482584

申请日：2017-04-07

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： Kwong Wah Lai ,  Jun Liang ,  Birong Zhang ,  Sharada Labadie ,  Daniel Ortwine ,  Peter Dragovich ,  James Kiefer ,  Victor S. Gehling ,  Jean-Christophe Harmange

IPC分类号： A61K31/41 ,  A61K31/4025 ,  C07D207/04 ,  C07D237/04

CPC分类号： A61K31/41 ,  A61K31/4025 ,  C07D207/04 ,  C07D237/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

摘要： The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US10022354B2

公开(公告)日：2018-07-17

申请号：US15482584

申请日：2017-04-07

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： Kwong Wah Lai ,  Jun Liang ,  Birong Zhang ,  Sharada Labadie ,  Daniel Ortwine ,  Peter Dragovich ,  James Kiefer ,  Victor S. Gehling ,  Jean-Christophe Harmange

IPC分类号： C07D237/04 ,  A61K31/41 ,  A61K31/4025 ,  C07D207/04

摘要： The present invention relates to compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US10035801B2

公开(公告)日：2018-07-31

申请号：US14775405

申请日：2014-03-13

申请人： CONSTELLATION PHARMACEUTICALS, INC. ,  GENENTECH, INC.

发明人： Brian K. Albrecht ,  Steven F. Bellon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Kwong Wah Lai ,  Jun Liang ,  Peter Dragovich ,  Daniel F. Ortwine ,  Sharada Labadie ,  Birong Zhang ,  James Richard Kiefer

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/337 ,  A61K31/517 ,  A61K31/437 ,  C12N9/99 ,  C07D498/04 ,  C07D487/14

CPC分类号： C07D487/04 ,  A61K31/337 ,  A61K31/437 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D487/14 ,  C07D498/04 ,  C12N9/99

摘要： Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.

公开(公告)号：US20160060267A1

公开(公告)日：2016-03-03

申请号：US14775405

申请日：2014-03-13

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： Brian K. Albrecht ,  Steven F. Bellon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Kwong Wah Lai ,  Jun Liang ,  Peter Dragovich ,  Dan Ortwine ,  Sharada Labadie ,  Birong Zhang ,  Jim Kiefer

IPC分类号： C07D487/04 ,  A61K45/06 ,  C12N9/99 ,  A61K31/337 ,  A61K31/517 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377

CPC分类号： C07D487/04 ,  A61K31/337 ,  A61K31/437 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D487/14 ,  C07D498/04 ,  C12N9/99

摘要： Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.

摘要翻译： 提供了可用作一种或多种组蛋白脱甲基酶抑制剂的化合物，例如KDM5。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用本发明组合物治疗各种疾病的方法。

公开(公告)号：US10053451B2

公开(公告)日：2018-08-21

申请号：US15164102

申请日：2016-05-25

申请人： Genentech, Inc.

发明人： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Birong Zhang ,  Nicholas D. Smith ,  Steven P. Govek ,  Mehmet Kahraman ,  Andiliy G. Lai ,  Johnny Y. Nagasawa ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC分类号： C07D405/14 ,  A61K31/497 ,  A61K31/397 ,  C07D491/052 ,  A61K31/4162 ,  C07D405/12 ,  A61K31/4439 ,  A61K31/416 ,  C07D405/04

CPC分类号： C07D405/14 ,  A61K31/397 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/497 ,  C07D405/04 ,  C07D405/12 ,  C07D491/052

摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US10966963B2

公开(公告)日：2021-04-06

申请号：US15955539

申请日：2018-04-17

申请人： Genentech, Inc.

发明人： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li ,  Tommy Lai ,  Jiangpeng Liao ,  Zhiguo Liu ,  John Wai ,  Tao Wang

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06

摘要： Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US10654867B2

公开(公告)日：2020-05-19

申请号：US16565041

申请日：2019-09-09

申请人： Genentech, Inc.

发明人： Sharada Labadie ,  Jun Li ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Nicholas Charles Ray ,  Simon Goodacre ,  Jiangpeng Liao

IPC分类号： A61K31/4985 ,  A61K31/397 ,  C07D495/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K45/06 ,  A61K31/4365 ,  C07D487/04 ,  C07F7/18 ,  C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/695 ,  A61K31/55

摘要： Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I, II, and III compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20200002353A1

公开(公告)日：2020-01-02

申请号：US16565041

申请日：2019-09-09

申请人： Genentech, Inc.

发明人： Sharada Labadie ,  Jun Li ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Nicholas Charles Ray ,  Simon Goodacre ,  Jiangpeng Liao

IPC分类号： C07D495/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K45/06 ,  A61K31/4365 ,  C07D487/04 ,  A61K31/55 ,  A61K31/4985 ,  C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/695 ,  C07F7/18

摘要： Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I, II, and III compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20180002344A1

公开(公告)日：2018-01-04

申请号：US15623904

申请日：2017-06-15

申请人： Genentech, Inc.

发明人： Sharada Labadie ,  Jun Li ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Nicholas Charles Ray ,  Simon Goodacre ,  Jiangpeng Liao

IPC分类号： C07D495/04 ,  C07D491/048 ,  C07D487/04 ,  C07D471/14 ,  C07D471/04 ,  A61K31/695 ,  A61K31/4355 ,  A61K31/55 ,  A61K31/4985 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/4365 ,  C07F7/18 ,  A61K45/06

CPC分类号： C07D495/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/55 ,  A61K31/695 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/048 ,  C07F7/1804

摘要： Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I, II, and III compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20230045776A9

公开(公告)日：2023-02-09

申请号：US17185319

申请日：2021-02-25

申请人： Genentech, Inc.

发明人： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li ,  Tommy Lai ,  Jiangpeng Liao ,  Zhiguo Liu ,  John Wai ,  Tao Wang

IPC分类号： A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04

摘要： Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.