公开(公告)号：US11247989B2

公开(公告)日：2022-02-15

申请号：US16198581

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 ,  Jeremy M. Murray ,  John Wai ,  Kwong Wah Lai ,  Fei Wang ,  Kevin X. Chen

IPC: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2 X, and Y 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) 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：US11168070B2

公开(公告)日：2021-11-09

申请号：US16886541

申请日：2020-05-28

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: C07D401/04 ,  A61K31/47 ,  A61P25/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D243/14 ,  C07D413/04 ,  C07D267/14 ,  C07D413/10 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  C07D487/22

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：US10696655B2

公开(公告)日：2020-06-30

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: C07D223/16 ,  C07D243/12 ,  C07D243/14 ,  C07D267/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D413/10 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  C07D487/22

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：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：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。

公开(公告)号：US20220127265A1

公开(公告)日：2022-04-28

申请号：US17570139

申请日：2022-01-06

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

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

IPC: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2 X, and Y 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) 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：US11034698B2

公开(公告)日：2021-06-15

申请号：US16715933

申请日：2019-12-16

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Steven Do ,  Joy Drobnick ,  Alberto Gobbi ,  Tamiko Katsumoto ,  James Richard Kiefer, Jr. ,  Jun Liang ,  Naomi S. Rajapaksa ,  Yongsheng Chen ,  Liqiang Fu ,  Kwong Wah Lai ,  Zhiguo Liu ,  John Wai ,  Fei Wang

IPC: C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, Formula VIII, and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

公开(公告)号：US20190241558A1

公开(公告)日：2019-08-08

申请号：US16198581

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 ,  Jeremy M. Murray ,  John Wai ,  Kwong Wah Lai ,  Fei Wang ,  Kevin X. Chen

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2 X, and Y 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) 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：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：US10968203B2

公开(公告)日：2021-04-06

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

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.