公开(公告)号：US10301253B2

公开(公告)日：2019-05-28

申请号：US15658219

申请日：2017-07-24

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： 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

摘要： 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：US10183009B2

公开(公告)日：2019-01-22

申请号：US15592013

申请日：2017-05-10

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： A61K31/40 ,  C07D471/04

摘要： 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：US10155764B2

公开(公告)日：2018-12-18

申请号：US15449692

申请日：2017-03-03

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： C07D487/04 ,  C07D403/12 ,  C07D401/12 ,  C07D237/32 ,  C07D471/04 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/55 ,  C07D237/34 ,  C07D405/12

摘要： 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：US20170342067A1

公开(公告)日：2017-11-30

申请号：US15592017

申请日：2017-05-10

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： C07D471/04 ,  A61K45/06 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/437

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K45/06 ,  C07D519/00

摘要： 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：US20170340605A1

公开(公告)日：2017-11-30

申请号：US15592013

申请日：2017-05-10

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： A61K31/40 ,  C07D471/04

CPC分类号： A61K31/40 ,  C07D471/04

摘要： 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：US20170334883A1

公开(公告)日：2017-11-23

申请号：US15449706

申请日：2017-03-03

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： C07D403/12 ,  C07D401/12 ,  C07D401/04 ,  C07D253/075 ,  A61K45/06 ,  C07D403/04 ,  A61K31/53

CPC分类号： C07D403/12 ,  A61K31/53 ,  A61K45/06 ,  A61P35/00 ,  C07D249/12 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

摘要： 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：US10358437B2

公开(公告)日：2019-07-23

申请号：US15449706

申请日：2017-03-03

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： C07D249/12 ,  C07D403/04 ,  C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  A61K31/53 ,  A61K31/4196 ,  A61P35/00 ,  C07D253/075 ,  A61K45/06

摘要： 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：US10258603B2

公开(公告)日：2019-04-16

申请号：US15592012

申请日：2017-05-10

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： A61K31/40 ,  C07D471/04 ,  C07D519/00

摘要： 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

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： 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分类号： C07D471/04 ,  A61K31/437 ,  C07D519/00 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4545 ,  A61K45/06

摘要： 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

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： 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分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

摘要： 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.