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.

公开(公告)号：US20180290976A1

公开(公告)日：2018-10-11

申请号：US15567978

申请日：2016-04-22

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  James Edmund Audia ,  Alexandre Côté ,  Martin Duplessis ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Rishi G. Vaswani

IPC: C07D211/26 ,  C07D211/58 ,  C07C211/40 ,  C07D213/38 ,  C07C229/10 ,  C07D213/73 ,  C07C255/58 ,  C07D211/76 ,  C07D401/06 ,  C07C215/42 ,  C07C233/41 ,  C07C217/08 ,  C07C237/06 ,  C07D295/195 ,  C07C229/38 ,  C07C255/30 ,  C07D213/69 ,  C07D305/06

CPC classification number: C07D211/26 ,  A61P35/00 ,  C07B2200/07 ,  C07C211/09 ,  C07C211/36 ,  C07C211/40 ,  C07C215/14 ,  C07C215/42 ,  C07C215/44 ,  C07C217/08 ,  C07C229/10 ,  C07C229/38 ,  C07C229/46 ,  C07C233/41 ,  C07C237/06 ,  C07C255/24 ,  C07C255/30 ,  C07C255/58 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/44 ,  C07D205/12 ,  C07D207/32 ,  C07D211/22 ,  C07D211/36 ,  C07D211/58 ,  C07D211/76 ,  C07D213/38 ,  C07D213/64 ,  C07D213/69 ,  C07D213/73 ,  C07D215/44 ,  C07D239/30 ,  C07D263/32 ,  C07D295/195 ,  C07D305/06 ,  C07D309/20 ,  C07D317/28 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D405/04 ,  C07D417/06

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 LSD1. 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 LSD1.

公开(公告)号：US09980952B2

公开(公告)日：2018-05-29

申请号：US15155749

申请日：2016-05-16

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

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：US20180086720A1

公开(公告)日：2018-03-29

申请号：US15686028

申请日：2017-08-24

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

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

IPC: C07D237/20 ,  C07D401/12 ,  C07D401/04 ,  C07D487/04 ,  C07D403/04 ,  C07D487/08 ,  C07D498/10 ,  C07D471/10 ,  C07D403/14 ,  C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  C07D405/14 ,  C07D417/14 ,  C07D237/22 ,  C07D451/02 ,  C07D413/04

CPC classification number: C07D237/20 ,  A61K31/337 ,  A61K31/437 ,  A61K31/501 ,  A61K45/06 ,  C07D237/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D498/10 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I): and salts thereof, wherein: R1-R4 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. 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 BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.

公开(公告)号：US20180037566A1

公开(公告)日：2018-02-08

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

CPC classification number: C07D401/12 ,  A61K31/501 ,  A61K31/55 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  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.

公开(公告)号：US20170312292A1

公开(公告)日：2017-11-02

申请号：US15482581

申请日：2017-04-07

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

Inventor： Anthony F. Romero ,  Steven R. Magnuson ,  Richard Pastor ,  Vickie Hsiao-Wei Tsui ,  Jeremy Murray ,  Terry Crawford ,  Daniel J. Burdick ,  Brian K. Albrecht ,  Alexandre Cote ,  Alexander M. Taylor ,  Christopher G. Nasveschuck ,  Yves LeBlanc ,  Michael Charles Hewitt ,  Kwong Wah Lai ,  Kevin Chen

IPC: A61K31/55 ,  C07D403/04 ,  C07D243/24 ,  A61K31/5513 ,  C07D243/12 ,  C07D223/16 ,  C07D403/14 ,  C07D267/14

CPC classification number: A61K31/55 ,  A61K31/337 ,  A61K31/5513 ,  A61K45/06 ,  C07D223/16 ,  C07D243/12 ,  C07D243/24 ,  C07D267/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. 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 CBP and/or EP300-mediated disorders.

公开(公告)号：US20170275289A1

公开(公告)日：2017-09-28

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

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

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：US20150148337A1

公开(公告)日：2015-05-28

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: 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.

Abstract translation: 本发明涉及可用作含溴结构域蛋白质的抑制剂的化合物。 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所述组合物治疗各种疾病的方法。

公开(公告)号：US20140315949A1

公开(公告)日：2014-10-23

申请号：US14358455

申请日：2012-11-19

Applicant: Constellation Pharmaceuticals, Inc.

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

IPC: C07D213/64 ,  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.

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