公开(公告)号：US10183009B2

公开(公告)日：2019-01-22

申请号：US15592013

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

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：US10155764B2

公开(公告)日：2018-12-18

申请号：US15449692

申请日：2017-03-03

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

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Martin Duplessis ,  Andrew Charles Good ,  Yves LeBlanc ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Richard Pastor ,  Anthony F. Romero ,  Alexander M. Taylor

IPC: C07D487/04 ,  C07D403/12 ,  C07D401/12 ,  C07D237/32 ,  C07D471/04 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/55 ,  C07D237/34 ,  C07D405/12

Abstract: The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein ring A, R1, R3, R4, R5, and each Re have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20180009805A1

公开(公告)日：2018-01-11

申请号：US15658213

申请日：2017-07-24

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

Inventor： Marc Adler ,  Daniel J. Burdick ,  Terry Crawford ,  Martin Duplessis ,  Steven R. Magnuson ,  Christopher G. Nasveschuk ,  Anthony F. Romero ,  Yong Tang ,  Vickie Hsiao-Wei Tsui ,  Shumei Wang

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/506 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/444 ,  C07D519/00 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1-R6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. 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 TAF1-mediated disorders.

公开(公告)号：US20170342067A1

公开(公告)日：2017-11-30

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 ,  A61K45/06 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K45/06 ,  C07D519/00

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：US20170340605A1

公开(公告)日：2017-11-30

申请号：US15592013

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: A61K31/40 ,  C07D471/04

CPC classification number: A61K31/40 ,  C07D471/04

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：US20170334883A1

公开(公告)日：2017-11-23

申请号：US15449706

申请日：2017-03-03

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

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Martin Duplessis ,  Andrew Charles Good ,  Yves LeBlanc ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Richard Pastor ,  Anthony F. Romero ,  Alexander M. Taylor

IPC: C07D403/12 ,  C07D401/12 ,  C07D401/04 ,  C07D253/075 ,  A61K45/06 ,  C07D403/04 ,  A61K31/53

CPC classification number: C07D403/12 ,  A61K31/53 ,  A61K45/06 ,  A61P35/00 ,  C07D249/12 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

Abstract: The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R3-R6, X, and each Re have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09469646B2

公开(公告)日：2016-10-18

申请号：US14839273

申请日：2015-08-28

Applicant: Constellation Pharmaceuticals, Inc.

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

IPC: C07D401/12 ,  C07D401/14 ,  C07D487/04 ,  C07D417/04 ,  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：US20150376190A1

公开(公告)日：2015-12-31

申请号：US14766632

申请日：2014-02-11

Applicant: CONSTELLATION PHARMACEUTICALS, INC.

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

IPC: C07D487/04 ,  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 having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein.

Abstract translation: 具有用于调节组蛋白甲基修饰酶的结构式（II）的试剂，其组合物和用途，例如作为抗癌剂。

公开(公告)号：US10316023B2

公开(公告)日：2019-06-11

申请号：US15449706

申请日：2017-03-03

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

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Martin Duplessis ,  Andrew Charles Good ,  Yves LeBlanc ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor

IPC: C07D249/12 ,  C07D403/04 ,  C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  A61K31/53 ,  A61K31/4196 ,  A61P35/00 ,  C07D253/075 ,  A61K45/06

Abstract: The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R3-R6, X, and each Re have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US10239861B2

公开(公告)日：2019-03-26

申请号：US15643801

申请日：2017-07-07

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

Inventor： Brian K. Albrecht ,  Daniel J. Burdick ,  Alexandre Cote ,  Martin Duplessis ,  Christopher G. Nasveschuk ,  Alexander M. Taylor

IPC: C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D405/12 ,  A61K31/501 ,  A61K31/55 ,  A61K45/06 ,  C07D451/04

Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein R1-R3 have any of the values defined in the specification. The compounds and salts are useful for treating PCAF mediated disorders and/or GCN5 mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as and methods of using said compounds, salts, or compositions in the treatment of various disorders.