公开(公告)号：US12139496B2

公开(公告)日：2024-11-12

申请号：US17153536

申请日：2021-01-20

Applicant: GENENTECH, INC.

Inventor： Steven McKerrall ,  Brian Salvatore Safina ,  Aleksandr Kolesnikov ,  Birong Zhang ,  Wenfeng Liu ,  Kwong Wah Lai

IPC: A61K31/5365 ,  A61K31/4375 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/24 ,  A61P29/00 ,  C07D471/04 ,  C07D498/04

Abstract: The invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; wherein, A, B, ring C, R3, R4, R5, R6, and R7 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

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：US10457654B2

公开(公告)日：2019-10-29

申请号：US15799771

申请日：2017-10-31

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Daniel Sutherlin ,  Steven McKerrall ,  Michael Scott Wilson ,  Kwong Wah Lai ,  Philippe Bergeron ,  Birong Zhang ,  Ramsay Beveridge ,  Jean-Philippe Leclerc ,  Alexandre Lemire ,  Liang Zhao ,  Claudio Sturino

IPC: C07D285/08 ,  C07D277/52 ,  C07D239/69 ,  C07D213/76 ,  C07D261/16 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K31/427 ,  A61P19/02 ,  A61P29/00

Abstract: The invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables X, Y1—Y5, R1, R2, R3, R4, and Het have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US10022354B2

公开(公告)日：2018-07-17

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

Abstract: The present invention relates to 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 said compositions in the treatment of various disorders.

公开(公告)号：US20170362228A1

公开(公告)日：2017-12-21

申请号：US15623884

申请日：2017-06-15

Applicant: Genentech, Inc.

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

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  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：US20160347742A1

公开(公告)日：2016-12-01

申请号：US15164102

申请日：2016-05-25

Applicant: Genentech, Inc.

Inventor： Sharada Labadie ,  Jun Liang ,  Daniel Fred Ortwine ,  Xiaojing Wang ,  Birong Zhang ,  Nicholas D. Smith ,  Steven P. Govek ,  Mehmet Kahraman ,  Andiliy G. Lai ,  Johnny Y. Nagasawa ,  Simon Charles Goodacre ,  Nicholas Charles Ray

IPC: C07D405/14 ,  A61K31/497 ,  A61K31/397 ,  C07D491/052 ,  A61K31/4162 ,  C07D405/12 ,  A61K31/4439 ,  A61K31/416

CPC classification number: C07D405/14 ,  A61K31/397 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/497 ,  C07D405/04 ,  C07D405/12 ,  C07D491/052

Abstract: Described herein are compounds that are estrogen receptor modulators. 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: 本文描述的是雌激素受体调节剂的化合物。 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。

公开(公告)号：US12233052B2

公开(公告)日：2025-02-25

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

IPC: A61K31/437 ,  A61K31/138 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/565 ,  A61K45/06 ,  C07D471/04 ,  A61P5/30 ,  A61P35/00 ,  A61P43/00

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：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：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.