公开(公告)号：US20160159797A1

公开(公告)日：2016-06-09

申请号：US15044231

申请日：2016-02-16

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Wendy Lee ,  Vickie Hsiao-Wei Tsui ,  Xiaojing Wang ,  Zhaoyang Wen

IPC: C07D471/04 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  A61K31/55 ,  A61K31/551 ,  C07D519/00 ,  A61K31/4995 ,  A61K31/437 ,  A61K31/496

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D231/00 ,  C07D519/00

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, 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：US20130203732A1

公开(公告)日：2013-08-08

申请号：US13834316

申请日：2013-03-15

Applicant: GENENTECH, INC.

Inventor： Xiaojing Wang

IPC: C07D417/14 ,  C07D401/14 ,  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。

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：US10654867B2

公开(公告)日：2020-05-19

申请号：US16565041

申请日：2019-09-09

Applicant: Genentech, Inc.

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

IPC: A61K31/4985 ,  A61K31/397 ,  C07D495/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K45/06 ,  A61K31/4365 ,  C07D487/04 ,  C07F7/18 ,  C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/695 ,  A61K31/55

Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 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, II, and III 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：US20200002353A1

公开(公告)日：2020-01-02

申请号：US16565041

申请日：2019-09-09

Applicant: Genentech, Inc.

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

IPC: C07D495/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K45/06 ,  A61K31/4365 ,  C07D487/04 ,  A61K31/55 ,  A61K31/4985 ,  C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/695 ,  C07F7/18

Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 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, II, and III 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：US20190152970A1

公开(公告)日：2019-05-23

申请号：US16250879

申请日：2019-01-17

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 ,  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：US20180002344A1

公开(公告)日：2018-01-04

申请号：US15623904

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 ,  Jiangpeng Liao

IPC: C07D495/04 ,  C07D491/048 ,  C07D487/04 ,  C07D471/14 ,  C07D471/04 ,  A61K31/695 ,  A61K31/4355 ,  A61K31/55 ,  A61K31/4985 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/4365 ,  C07F7/18 ,  A61K45/06

CPC classification number: C07D495/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/55 ,  A61K31/695 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/048 ,  C07F7/1804

Abstract: Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 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, II, and III 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：US09850239B2

公开(公告)日：2017-12-26

申请号：US15044231

申请日：2016-02-16

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Wendy Lee ,  Vickie Hsiao-Wei Tsui ,  Xiaojing Wang ,  Zhaoyang Wen

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D519/00 ,  C07D231/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D231/00 ,  C07D519/00

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, 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：US20160304450A1

公开(公告)日：2016-10-20

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

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：US08669361B2

公开(公告)日：2014-03-11

申请号：US13834316

申请日：2013-03-15

Applicant: Genentech, Inc.

Inventor： Xiaojing Wang

IPC: C07D239/00

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。