公开(公告)号：US20180022707A1

公开(公告)日：2018-01-25

申请号：US15643805

申请日：2017-07-07

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Victor Gehling ,  Vickie Hsiao-Wei Tsui ,  James Richard Jr. Kiefer ,  Jun Liang ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  F. Anthony Romero ,  Alexander M. Taylor

IPC: C07D233/44 ,  C07D487/08 ,  C07D413/12 ,  C07D417/12 ,  C07D403/12 ,  C07D409/12

CPC classification number: C07D233/44 ,  C07D235/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM2b. 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：US20170197915A9

公开(公告)日：2017-07-13

申请号：US14972333

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Steven P. Govek ,  Mehmet Kahraman ,  Johnny Y. Nagasawa ,  Nicholas D. Smith ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC: C07D205/04 ,  A61K31/404 ,  A61K45/06 ,  A61K31/397 ,  C07D207/04 ,  A61K31/40 ,  C07D409/12 ,  A61K31/4025 ,  C07D413/12 ,  A61K31/422 ,  C07D417/12 ,  A61K31/427 ,  C07D401/14 ,  A61K31/4439 ,  C07D411/12 ,  C07D403/12

CPC classification number: C07D205/04 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/416 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5415 ,  A61K45/06 ,  C07D207/04 ,  C07D207/08 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12 ,  C07D403/14 ,  C07D409/02 ,  C07D409/12 ,  C07D411/02 ,  C07D411/12 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  A61K2300/00

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. 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：US20170129855A1

公开(公告)日：2017-05-11

申请号：US15345958

申请日：2016-11-08

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg

IPC: C07D205/04 ,  A61K31/397 ,  C07D401/12 ,  C07D207/06 ,  A61K31/40 ,  A61K45/06 ,  C07D405/12

CPC classification number: C07D205/04 ,  A61K31/397 ,  A61K31/40 ,  A61K45/06 ,  C07D207/06 ,  C07D401/12 ,  C07D405/12

Abstract: Described herein are tetrahydronaphthalene 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：US09505767B2

公开(公告)日：2016-11-29

申请号：US14477566

申请日：2014-09-04

Applicant: Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Yves LeBlanc ,  Jun Liang ,  Steven R. Magnuson ,  Vickie Hsiao-Wei Tsui ,  Birong Zhang

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

Abstract: The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20160175289A1

公开(公告)日：2016-06-23

申请号：US14972326

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Ray ,  Nicholas Charles Ray

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

CPC classification number: A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04

Abstract: 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.

Abstract translation: 本文描述了具有式I结构的雌激素受体调节活性或功能的四氢 - 吡啶并[3,4-b]吲哚-1-基化合物：及其立体异构体，互变异构体或其药学上可接受的盐，以及取代基和结构特征 在此描述。 还描述了包括式I化合物的药物组合物和药物，以及使用这样的雌激素受体调节剂单独和与其它治疗剂组合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。

公开(公告)号：US20160143910A1

公开(公告)日：2016-05-26

申请号：US14776586

申请日：2014-03-14

Applicant: Shilpi ARORA ,  Michael Robert COSTA ,  Ted LAU ,  Patrick TROJER ,  GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Shilpi Arora ,  Michael Robert Costa ,  Ted Lau ,  Patrick Trojer ,  Brian K. Albrecht ,  Shane Buker ,  Marie Classon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Erica L. Jackson ,  Jun Liang ,  Heidi Phillips ,  Peter Sandy ,  Jeffrey Settleman ,  Jean-Philippe Stephan

IPC: A61K31/519 ,  A61K31/437 ,  A61K31/517 ,  A61K45/06 ,  A61K31/337

CPC classification number: A61K31/519 ,  A61K31/337 ,  A61K31/437 ,  A61K31/517 ,  A61K31/555 ,  A61K31/713 ,  A61K33/24 ,  A61K45/06 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/531 ,  A61K2300/00

Abstract: Provided herein are methods of treating and/or preventing cancer drug resistance using antagonists of KDM5.

Abstract translation: 本文提供使用KDM5拮抗剂治疗和/或预防癌症耐药性的方法。

公开(公告)号：US20160060267A1

公开(公告)日：2016-03-03

申请号：US14775405

申请日：2014-03-13

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： 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: C07D487/04 ,  A61K45/06 ,  C12N9/99 ,  A61K31/337 ,  A61K31/517 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377

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

Abstract: 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.

Abstract translation: 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：US20150065522A1

公开(公告)日：2015-03-05

申请号：US14477566

申请日：2014-09-04

Applicant: Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Yves LeBlanc ,  Jun Liang ,  Steven Magnuson ,  Vicki Tsui ,  Birong Zhang

IPC: C07D487/04 ,  A61K45/06 ,  A61N5/10 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

Abstract: The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.

Abstract translation: 本发明涉及式（I）化合物及其盐，其中R 1 -R 4和A具有说明书中定义的任何值及其组成和用途。 该化合物可用作组蛋白脱甲基酶的抑制剂，例如KDM5。 还包括包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。

公开(公告)号：US20140038939A1

公开(公告)日：2014-02-06

申请号：US14049458

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: C07D487/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.