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：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：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：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：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：US10358437B2

公开(公告)日：2019-07-23

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 ,  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：US10280149B2

公开(公告)日：2019-05-07

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 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D241/04 ,  C07D211/30

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.