公开(公告)号：US20140288123A1

公开(公告)日：2014-09-25

申请号：US14358558

申请日：2012-11-19

Applicant: Constellation Pharmaceuticals, Inc.

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

IPC: C07D213/64

CPC classification number: C07D213/64 ,  C07D221/18 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

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

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：US20180022727A1

公开(公告)日：2018-01-25

申请号：US15643808

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 ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Birong Zhang

IPC: C07D401/06 ,  C07D241/04 ,  C07D211/30 ,  C07D413/06

CPC classification number: C07D401/06 ,  C07D211/30 ,  C07D241/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06

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：US20180009735A1

公开(公告)日：2018-01-11

申请号：US15658219

申请日：2017-07-24

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

Inventor： Brian K. Albrecht ,  James Edmund Audia ,  Alexandre Cote ,  Martin Duplessis ,  Victor S. Gehling ,  Andrew Charles Good ,  Jean-Christophe Harmange ,  Yves LeBlanc ,  Christopher G. Nasveschuk ,  Alexander M. Taylor ,  Rishi G. Vaswani

IPC: C07C211/42 ,  C07D401/12 ,  A61K31/135 ,  A61K31/166 ,  C07D309/04 ,  C07D305/08 ,  C07D295/185 ,  C07D231/12 ,  C07D215/08 ,  C07D213/38 ,  C07D211/46 ,  C07D211/26 ,  C07D207/06 ,  C07D205/12 ,  C07D205/04 ,  C07C317/36 ,  C07C255/58 ,  C07C237/48 ,  C07C229/50 ,  C07C217/74 ,  A61K45/06 ,  A61K31/517 ,  A61K31/495 ,  A61K31/4747 ,  A61K31/4545 ,  A61K31/445 ,  A61K31/4406 ,  A61K31/437 ,  A61K31/4155 ,  A61K31/415 ,  A61K31/40 ,  A61K31/397 ,  A61K31/351 ,  A61K31/337 ,  A61K31/277 ,  A61K31/196 ,  C07D405/12

CPC classification number: C07C211/42 ,  A61K31/135 ,  A61K31/166 ,  A61K31/196 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/4747 ,  A61K31/495 ,  A61K31/517 ,  A61K45/06 ,  C07C217/74 ,  C07C229/50 ,  C07C237/48 ,  C07C255/58 ,  C07C317/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/94 ,  C07D205/04 ,  C07D205/12 ,  C07D207/06 ,  C07D211/26 ,  C07D211/46 ,  C07D211/78 ,  C07D213/38 ,  C07D215/08 ,  C07D231/12 ,  C07D295/185 ,  C07D305/08 ,  C07D309/04 ,  C07D401/12 ,  C07D405/12

Abstract: Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. 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 LSD1-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：US20170333406A1

公开(公告)日：2017-11-23

申请号：US15667227

申请日：2017-08-02

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

Inventor： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC: A61K31/437 ,  C07D471/04 ,  A61K45/06 ,  A61K31/55 ,  A61K31/5415 ,  A61K31/5377 ,  A61K31/4375 ,  A61K31/506 ,  A61K31/498 ,  A61K31/496 ,  A61K31/4725 ,  A61K31/4709 ,  C07D519/00 ,  A61K31/538

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, 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) of formula (II) 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：US20170312262A9

公开(公告)日：2017-11-02

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

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：US09409865B2

公开(公告)日：2016-08-09

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: C07D213/62 ,  C07D213/64 ,  C07D213/81 ,  C07D405/12 ,  C07D401/12

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：US20160158207A1

公开(公告)日：2016-06-09

申请号：US14952821

申请日：2015-11-25

Applicant: Constellation Pharmaceuticals, Inc. ,  Genentech, Inc.

Inventor： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC: A61K31/437 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/4709 ,  A61K31/498 ,  A61K45/06 ,  A61K31/55 ,  C07D519/00 ,  A61K31/4375 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  C07D471/04 ,  A61K31/506

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, 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) of formula (II) 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.

Abstract translation: 本发明涉及式（I）或式（II）化合物及其盐，其中式（I）的R 1 -R 4和式（II）的R 1 -R 3具有本文定义的任何值，组合物 及其用途。 该化合物可用作CBP和/或EP300的抑制剂。 还包括包含式（II）的式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种CBP和/或EP300介导的病症中使用这些化合物和盐的方法。