公开(公告)号：US12187709B2

公开(公告)日：2025-01-07

申请号：US18052851

申请日：2022-11-04

Applicant: Genentech, Inc.

Inventor： Malcolm Huestis ,  Michael John Lambrecht ,  Jun Liang ,  Man Un Ung ,  Xiaojing Wang ,  Jason Robert Zbieg ,  Bing-Yan Zhu ,  Lisa Marie Barton ,  Fabio Broccatelli ,  Georgette Marie Castanedo ,  Araz Jakalian ,  Robin Larouche-Gauthier ,  Arun Yadav

IPC: C07D403/12 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D493/08

Abstract: A compound, of formula (I): suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.

公开(公告)号：US20240300927A1

公开(公告)日：2024-09-12

申请号：US18275655

申请日：2022-02-03

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Araz Jakalian ,  Michael John Lambrecht ,  Robin Larouche-Gauthier ,  Malcolm Huestis ,  Man Un Ung ,  Xiaojing Wang ,  Arun Yadav ,  Jason Robert Zbieg ,  Fabio Broccatelli

IPC: C07D405/14 ,  A61K31/4439

CPC classification number: C07D405/14 ,  A61K31/4439

Abstract: Various amide compounds that bind Cbl-B, including those that are selective for C-Cbl, and methods of making and using the same. Representative amide compounds include molecules falling within the following formulae:

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：US11566003B2

公开(公告)日：2023-01-31

申请号：US16921297

申请日：2020-07-06

Applicant: Genentech, Inc.

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

IPC: C07D217/22 ,  A61K31/549 ,  A61P35/00 ,  A61K45/06 ,  C07D401/04 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/501 ,  C07D471/04 ,  C07D413/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D417/04 ,  A61K31/4985 ,  C07D401/14 ,  C07D487/04 ,  A61K31/551 ,  C07D498/04 ,  A61K31/5383 ,  C07D405/14 ,  C07D519/00 ,  C07D498/14 ,  C07D513/04 ,  A61K31/554 ,  A61K31/55 ,  A61K31/472 ,  C07D409/14 ,  C07D491/04 ,  C07D487/14

Abstract: Isoquinoline compounds 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 isoquinoline compounds.

公开(公告)号：US10399939B2

公开(公告)日：2019-09-03

申请号：US15345958

申请日：2016-11-08

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg

IPC: C07D205/04 ,  A61K31/397 ,  A61K31/40 ,  A61K45/06 ,  C07D207/06 ,  C07D401/12 ,  C07D405/12

Abstract: Described herein are tetrahydronaphthalene 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：US09845291B2

公开(公告)日：2017-12-19

申请号：US14972333

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Steven P. Govek ,  Mehmet Kahraman ,  Johnny Y. Nagasawa ,  Nicholas D. Smith ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC: A61K31/397 ,  C07D205/04 ,  C07D403/12 ,  A61K31/404 ,  A61K45/06 ,  C07D207/04 ,  A61K31/40 ,  C07D409/12 ,  A61K31/4025 ,  C07D413/12 ,  A61K31/422 ,  C07D417/12 ,  A61K31/427 ,  C07D401/14 ,  A61K31/4439 ,  C07D411/12

CPC classification number: C07D205/04 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/416 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5415 ,  A61K45/06 ,  C07D207/04 ,  C07D207/08 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12 ,  C07D403/14 ,  C07D409/02 ,  C07D409/12 ,  C07D411/02 ,  C07D411/12 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  A61K2300/00

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20170320871A1

公开(公告)日：2017-11-09

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

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.

公开(公告)号：US20170312252A1

公开(公告)日：2017-11-02

申请号：US15482584

申请日：2017-04-07

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

Inventor： Kwong Wah Lai ,  Jun Liang ,  Birong Zhang ,  Sharada Labadie ,  Daniel Ortwine ,  Peter Dragovich ,  James Kiefer ,  Victor S. Gehling ,  Jean-Christophe Harmange

IPC: A61K31/41 ,  A61K31/4025 ,  C07D207/04 ,  C07D237/04

CPC classification number: A61K31/41 ,  A61K31/4025 ,  C07D207/04 ,  C07D237/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM5. 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：US20160333011A1

公开(公告)日：2016-11-17

申请号：US15220087

申请日：2016-07-26

Applicant: Genentech, Inc.

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diastereomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

公开(公告)号：US20160175284A1

公开(公告)日：2016-06-23

申请号：US14972336

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Li ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Jason Zbieg ,  Steven P. Govek ,  Mehmet Kahraman ,  Johnny Y. Nagasawa ,  Nicholas D. Smith

IPC: A61K31/4025 ,  C07D401/12 ,  A61K31/4184 ,  C07D401/14 ,  A61K31/404 ,  A61K45/06 ,  A61K31/397

CPC classification number: A61K31/4025 ,  A61K31/397 ,  A61K31/404 ,  A61K31/4184 ,  A61K45/06 ,  C07D311/14 ,  C07D401/12 ,  C07D401/14

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula I: 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 compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract translation: 本文描述的是作为式I的雌激素受体调节剂的化合物：及其立体异构体，互变异构体或其药学上可接受的盐，以及本文所述的取代基和结构特征。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这种雌激素受体调节剂单独使用并与其它化合物联合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。