公开(公告)号：US20160024504A1

公开(公告)日：2016-01-28

申请号：US14776051

申请日：2014-03-14

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

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Benjamin Fauber ,  Hon-Ren Huang ,  Jose M. Lora ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Andres Salmeron ,  Robert J. Sims, III ,  Alexander M. Taylor

IPC: C12N15/113 ,  G01N33/50 ,  A61K31/444 ,  A61K31/437 ,  A61K31/496

CPC classification number: C12N15/113 ,  A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/713 ,  C07K14/4702 ,  C12N2310/14 ,  C12N2320/30 ,  G01N33/505 ,  G01N2333/52 ,  G01N2500/04 ,  G01N2500/10 ,  Y02A50/422

Abstract: The invention provides methods for treating Th2 cytokine-mediated diseases by inhibiting bromodomain function.

Abstract translation: 本发明提供了通过抑制溴结构域功能来治疗Th2细胞因子介导的疾病的方法。

公开(公告)号：US20160009718A1

公开(公告)日：2016-01-14

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.

公开(公告)号：US20150259351A1

公开(公告)日：2015-09-17

申请号：US14661797

申请日：2015-03-18

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 ,  C07D409/06 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  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：US09085583B2

公开(公告)日：2015-07-21

申请号：US14377214

申请日：2013-02-11

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: A61K31/535 ,  C07D401/00 ,  C07D487/04 ,  C07D401/14 ,  C07D401/12 ,  C07D417/04 ,  C07D417/14

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：US20150011546A1

公开(公告)日：2015-01-08

申请号：US14377214

申请日：2013-02-11

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 ,  C07D401/14 ,  C07D417/14 ,  C07D401/12

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：US10577350B2

公开(公告)日：2020-03-03

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

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：US10301253B2

公开(公告)日：2019-05-28

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: C07C211/39 ,  C07C211/38 ,  C07C211/17 ,  C07C211/19 ,  A61K31/137 ,  A61K31/136 ,  A61K31/135 ,  A61K31/4465 ,  C07C211/42 ,  C07D231/12 ,  C07D401/12 ,  C07D405/12 ,  C07D211/78 ,  C07D213/38 ,  C07C255/58 ,  C07C217/74 ,  C07C229/50 ,  C07C237/48 ,  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 ,  C07C317/36 ,  C07D205/04 ,  C07D205/12 ,  C07D207/06 ,  C07D211/26 ,  C07D211/46 ,  C07D215/08 ,  C07D295/185 ,  C07D305/08 ,  C07D309/04

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：US09925197B2

公开(公告)日：2018-03-27

申请号：US15277854

申请日：2016-09-27

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Brian K. Albrecht ,  Michael Charles Hewitt ,  Victor S. Gehling ,  Rishi G. Vaswani

IPC: A61K31/55 ,  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.

公开(公告)号：US09763922B2

公开(公告)日：2017-09-19

申请号：US14952821

申请日：2015-11-25

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

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：US20170056388A1

公开(公告)日：2017-03-02

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

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.

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