公开(公告)号：US12297210B2

公开(公告)日：2025-05-13

申请号：US17156384

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Terry Kellar ,  Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Lewis J. Gazzard ,  Timothy Heffron ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D519/00 ,  A61P37/04 ,  C07D471/04

Abstract: Naphthyridine compounds of formula (I): variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

公开(公告)号：US20250114338A1

公开(公告)日：2025-04-10

申请号：US18985513

申请日：2024-12-18

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

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  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：US20210332064A1

公开(公告)日：2021-10-28

申请号：US17220307

申请日：2021-04-01

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Rohan V. Mendonca ,  Michael Siu ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Bryan Chan ,  Edna F. Choo ,  Joy Drobnick ,  Lewis J. Gazzard ,  Timothy Heffron

IPC: C07D498/04 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00

Abstract: 3-Carbonylaminoisoquinoline compounds of formula (I): variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the 3-carbonylaminoisoquinoline compounds.

公开(公告)号：US11034692B1

公开(公告)日：2021-06-15

申请号：US16542129

申请日：2019-08-15

Applicant: Genentech, Inc.

Inventor： Bryan Chan ,  Blake Daniels ,  Joy Drobnick ,  Lewis Gazzard ,  Timothy Heffron ,  Malcolm Huestis ,  Jun Liang ,  Sushant Malhotra ,  Rohan Mendonca ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Matthew W. Cartwright ,  Emanuela Gancia ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu ,  Baihua Hu ,  Aijun Lu

IPC: C07D471/04 ,  A61K45/06 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/551 ,  A61K31/55

Abstract: Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

公开(公告)号：US10988478B1

公开(公告)日：2021-04-27

申请号：US16775650

申请日：2020-01-29

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Alberto Gobbi ,  James Richard Kiefer, Jr. ,  Aleksandr Kolesnikov ,  Alan G. Olivero ,  Joy Drobnick ,  Jun Liang ,  Naomi Rajapaksa ,  Chudi Ndubaku ,  Jianwen Feng

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61P37/02 ,  A61P29/00

Abstract: Compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

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.

公开(公告)号：US10202354B2

公开(公告)日：2019-02-12

申请号：US15643805

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 ,  F. Anthony Romero ,  Alexander M. Taylor

IPC: C07D233/44 ,  C07D235/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

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：US10035801B2

公开(公告)日：2018-07-31

申请号：US14775405

申请日：2014-03-13

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

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Kwong Wah Lai ,  Jun Liang ,  Peter Dragovich ,  Daniel F. Ortwine ,  Sharada Labadie ,  Birong Zhang ,  James Richard Kiefer

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/337 ,  A61K31/517 ,  A61K31/437 ,  C12N9/99 ,  C07D498/04 ,  C07D487/14

CPC classification number: C07D487/04 ,  A61K31/337 ,  A61K31/437 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D487/14 ,  C07D498/04 ,  C12N9/99

Abstract: Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.

公开(公告)号：US09980947B2

公开(公告)日：2018-05-29

申请号：US14972326

申请日：2015-12-17

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

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

CPC classification number: 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：US09969732B2

公开(公告)日：2018-05-15

申请号：US15481757

申请日：2017-04-07

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Maia Vinogradova ,  Xiaojing Wang ,  Jason Zbieg ,  Birong Zhang ,  Tao Wang

IPC: C07D401/04 ,  C07D217/00 ,  A61K31/4725 ,  C07D471/04 ,  C07D401/12 ,  A61K31/4745 ,  C07D403/12 ,  A61K31/55 ,  C07D401/14 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituent 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.