公开(公告)号：US20230045776A9

公开(公告)日：2023-02-09

申请号：US17185319

申请日：2021-02-25

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li ,  Tommy Lai ,  Jiangpeng Liao ,  Zhiguo Liu ,  John Wai ,  Tao Wang

IPC: A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and 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 compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US10729738B2

公开(公告)日：2020-08-04

申请号：US15293743

申请日：2016-10-14

Applicant: Genentech, Inc.

Inventor： Peter Dragovich ,  Zhonghua Pei ,  Thomas Pillow ,  Jack Sadowsky ,  Jinhua Chen ,  John Wai

IPC: A61K38/05 ,  A61K47/54 ,  A61K47/68 ,  A61K47/64 ,  A61K47/55 ,  A61K31/5365 ,  A61K31/5517

Abstract: The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

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：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：US10966963B2

公开(公告)日：2021-04-06

申请号：US15955539

申请日：2018-04-17

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li ,  Tommy Lai ,  Jiangpeng Liao ,  Zhiguo Liu ,  John Wai ,  Tao Wang

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and 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 compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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：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：US20210236473A1

公开(公告)日：2021-08-05

申请号：US17185319

申请日：2021-02-25

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Simon Charles Goodacre ,  Nicholas Charles Ray ,  Jun Li ,  Tommy Lai ,  Jiangpeng Liao ,  Zhiguo Liu ,  John Wai ,  Tao Wang

IPC: A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and 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 compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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.