公开(公告)号：US20190152949A1

公开(公告)日：2019-05-23

申请号：US16198597

申请日：2018-11-21

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

Inventor： Patrick Cyr ,  Sarah Bronner ,  F. Anthony Romero ,  Steven Magnuson ,  Vickie Hsiao-Wei Tsui ,  John Wai ,  Kwong Wah Lai ,  Fei Wang

IPC: C07D401/14 ,  A61K45/06 ,  A61K31/5513 ,  A61K31/4375 ,  A61K31/435 ,  A61K31/437 ,  C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/22 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/496 ,  C07D405/14 ,  C07D409/14

Abstract: The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 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：US20180265497A1

公开(公告)日：2018-09-20

申请号：US15989008

申请日：2018-05-24

Applicant: Genentech, Inc. ,  The Regents of the University of California

Inventor： Marie-Gabrielle Braun ,  Paul Gibbons ,  Wendy Lee ,  Cuong Ly ,  Joachim Rudolph ,  Jacob Schwarz ,  Avi Ashkenazi ,  Leo Fu ,  Tommy Lai ,  Fei Wang ,  Ramsay Beveridge ,  Liang Zhao

IPC: C07D401/14 ,  A61K31/506 ,  C07D401/04 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  A61P35/00 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I or I′ structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I or I′ compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.