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：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：US10308614B2

公开(公告)日：2019-06-04

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 ,  F. Anthony Romero ,  Yong Tang ,  Alexander M. Taylor

IPC: C07D237/20 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D498/10 ,  A61K31/50 ,  A61K31/51 ,  C07D401/12 ,  C07D237/22 ,  C07D417/14 ,  C07D413/12 ,  C07D451/02 ,  C07D487/04 ,  A61K45/06 ,  A61K31/337 ,  A61K31/437 ,  A61K31/501

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：US10206931B2

公开(公告)日：2019-02-19

申请号：US15482581

申请日：2017-04-07

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

Inventor： F. Anthony 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: A61K31/551 ,  C07D243/12 ,  C07D403/04 ,  C07D403/14 ,  A61K31/55 ,  C07D223/16 ,  C07D267/14 ,  C07D401/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D243/24 ,  C07D471/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/337 ,  A61K31/5513

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：US20170340604A1

公开(公告)日：2017-11-30

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 ,  Anthony F. Romero ,  Yong Tang ,  Alexander M. Taylor ,  Shumei Wang

IPC: A61K31/40 ,  C07D471/04

CPC classification number: 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：US10202378B2

公开(公告)日：2019-02-12

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 ,  F. Anthony Romero ,  Yong Tang ,  Vickie Hsiao-Wei Tsui ,  Shumei Wang

IPC: A61K31/506 ,  C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  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：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：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：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：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.