公开(公告)号：US09624244B2

公开(公告)日：2017-04-18

申请号：US14405211

申请日：2013-06-06

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Victor S. Gehling ,  Alexander M. Taylor ,  Rishi G. Vaswani

IPC: A61K31/55 ,  C07D498/04 ,  C07D498/10

CPC classification number: C07D498/10 ,  A61K31/55 ,  C07D498/04

Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. 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：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：US09493483B2

公开(公告)日：2016-11-15

申请号：US14405209

申请日：2013-06-06

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Michael Charles Hewitt ,  Victor S. Gehling ,  Rishi G. Vaswani

IPC: A61K31/55 ,  C07D498/04

CPC classification number: A61K31/55 ,  C07D498/04

Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. 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：US20160185757A1

公开(公告)日：2016-06-30

申请号：US14911343

申请日：2014-08-15

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  James Edmund Audia ,  Les A. Dakin ,  Martin Duplessis ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Christopher G. Nasveschuk ,  Rishi G. Vaswani

IPC: C07D401/14 ,  C07D413/14 ,  C07D405/14

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14

Abstract: Agents of formulas (I)/(II)/(III) for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

Abstract translation: 本文提供了用于调节甲基修饰酶的式（I）/（II）/（III）的试剂，其组合物和用途。

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：US20150368229A1

公开(公告)日：2015-12-24

申请号：US14839273

申请日：2015-08-28

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  James Edmund Audia ,  Andrew Cook ,  Les A. Dakin ,  Martin Duplessis ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Christopher G. Nasveschuk ,  Rishi G. Vaswani

IPC: C07D401/14 ,  C07D471/04 ,  C07D405/14

CPC classification number: A61K31/4545 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

Abstract translation: 本文提供了用于调节甲基修饰酶的组合物及其用途。

公开(公告)号：US20150315148A1

公开(公告)日：2015-11-05

申请号：US14707874

申请日：2015-05-08

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  James Edmund Audia ,  Alexandre Gagnon ,  Jean-Christophe Harmange ,  Christopher G. Nasveschuk

IPC: C07D213/64 ,  C07D213/81 ,  C07D401/12 ,  C07D405/12

CPC classification number: C07D213/64 ,  C07D213/81 ,  C07D401/12 ,  C07D405/12

Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

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。