公开(公告)号：US20140005168A1

公开(公告)日：2014-01-02

申请号：US13927278

申请日：2013-06-26

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Vickie H. Tsui ,  Xiaojing Wang

IPC: C07D471/04 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/513 ,  C07D491/052 ,  A61K31/55 ,  C07D471/10 ,  C07D487/10 ,  A61K45/06 ,  A61K31/501 ,  A61K31/496 ,  A61K31/444

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式I的5-氮杂吲唑化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，可用于抑制Pim激酶和用于治疗由Pim激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

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：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：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：US09931323B2

公开(公告)日：2018-04-03

申请号：US15085164

申请日：2016-03-30

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Minghua Sun ,  Xiaojing Wang ,  Wesley Blackaby ,  Alastair James Hodges ,  Andrew Sharpe

IPC: A61K31/427 ,  A61K31/4439 ,  A61K31/4375 ,  A61K45/06 ,  C07D417/12 ,  C07D405/14 ,  A61K31/497 ,  A61K31/506 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

CPC classification number: A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

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：US09573943B2

公开(公告)日：2017-02-21

申请号：US14153891

申请日：2014-01-13

Applicant: Genentech, Inc.

Inventor： Xiaojing Wang

IPC: A61K31/4155 ,  C07D401/14 ,  C07D403/14 ,  C07D417/14 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

CPC classification number: C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12

Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式I的吡唑-4-基 - 杂环基 - 甲酰胺化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中X是噻唑基，吡啶基，吡啶基或嘧啶基，可用于抑制Pim激酶， 治疗由Pim激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。