公开(公告)号：US10258603B2

公开(公告)日：2019-04-16

申请号：US15592012

申请日：2017-05-10

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

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Daniel J. Burdick ,  Alexandre Cote ,  Terry Crawford ,  Les A. Dakin ,  Vickie Hsiao-Wei Tsui ,  Michael Charles Hewitt ,  Yves LeBlanc ,  Steven R. Magnuson ,  Christopher G. Nasveschuk ,  F. Anthony Romero ,  Yong Tang ,  Alexander M. Taylor ,  Shumei Wang

IPC: A61K31/40 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, Rc, and Rd have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

公开(公告)号：US10202354B2

公开(公告)日：2019-02-12

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 ,  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：US10150767B2

公开(公告)日：2018-12-11

申请号：US15592017

申请日：2017-05-10

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

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Daniel J. Burdick ,  Alexandre Cote ,  Terry Crawford ,  Les A. Dakin ,  Vickie Hsiao-Wei Tsui ,  Michael Charles Hewitt ,  Yves LeBlanc ,  Steven R. Magnuson ,  Christopher G. Nasveschuk ,  Anthony F. Romero ,  Yong Tang ,  Alexander M. Taylor ,  Shumei Wang

IPC: C07D471/04 ,  A61K31/437 ,  C07D519/00 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4545 ,  A61K45/06

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

公开(公告)号：US20180327386A1

公开(公告)日：2018-11-15

申请号：US15755854

申请日：2016-08-25

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Alisha Arrigo ,  Donald Corson ,  Victor S. Gehling ,  Bruno Patrice Haché ,  Jean-Christophe Harmange ,  Jonathan Lane

IPC: C07D401/14

CPC classification number: C07D401/14 ,  C07B2200/13

Abstract: The present disclosure relates to a crystalline Forms A, B, and C of (R)—N-((4-methoxy-6-methyl-2-oxo-1,2-di-hydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide, each of which are useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline forms 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

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

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

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.

公开(公告)号：US10016405B2

公开(公告)日：2018-07-10

申请号：US15257275

申请日：2016-09-06

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

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.

公开(公告)号：US09969716B2

公开(公告)日：2018-05-15

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 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14

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

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

公开(公告)号：US20180037568A1

公开(公告)日：2018-02-08

申请号：US15549265

申请日：2016-02-04

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Rishi G. Vaswani

IPC: C07D401/14 ,  C07D405/14

CPC classification number: C07D401/14 ,  C07D405/14

Abstract: Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.

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：US09745305B2

公开(公告)日：2017-08-29

申请号：US14769471

申请日：2014-03-12

Applicant: Constellation Pharmaceuticals, Inc.

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

IPC: C07D487/04

CPC classification number: C07D487/04

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