公开(公告)号：US10053451B2

公开(公告)日：2018-08-21

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 ,  C07D405/04

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.

公开(公告)号：US09963446B2

公开(公告)日：2018-05-08

申请号：US15266243

申请日：2016-09-15

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Huifen Chen ,  Xiaojing Wang

IPC: C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/06 ,  C07D487/04 ,  A61K45/06

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/4985 ,  A61K45/06 ,  C07D487/04

Abstract: Oxepan-2-yl pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein 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：US09505785B2

公开(公告)日：2016-11-29

申请号：US14059626

申请日：2013-10-22

Applicant: GILEAD CONNECTICUT, INC. ,  GENENTECH, INC.

Inventor： Antonio J. M. Barbosa ,  Peter A. Blomgren ,  Kevin S. Currie ,  Ravi Krishnamoorthy ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Scott A. Mitchell ,  Daniel Ortwine ,  Aaron C. Schmitt ,  Xiaojing Wang ,  Jianjun Xu ,  Wendy Young ,  Honglu Zhang ,  Zhongdong Zhao ,  Pavel E. Zhichkin

IPC: C07D519/00 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07D471/14

CPC classification number: C07D519/00 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07C69/65 ,  C07D209/52 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07F5/04

Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US09505746B2

公开(公告)日：2016-11-29

申请号：US14082337

申请日：2013-11-18

Applicant: Genentech, Inc.

Inventor： Alastair James Hodges ,  Mizio Matteucci ,  Andrew Sharpe ,  Minghua Sun ,  Xiaojing Wang ,  Vickie H. Tsui

IPC: A61K31/4965 ,  A61K31/44 ,  A61K31/415 ,  C07D417/14 ,  C07D401/14 ,  C07D403/14 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10 ,  A61K31/427 ,  A61K31/435 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/435 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10

Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein 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：US20160213652A1

公开(公告)日：2016-07-28

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

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.

Abstract translation: 式I的环醚吡唑-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R 2是环状醚，X是噻唑基，吡嗪基，吡啶基或嘧啶基，是有用的 用于抑制Pim激酶，以及用于治疗诸如由Pim激酶介导的癌症的疾病。 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：US20140088117A1

公开(公告)日：2014-03-27

申请号：US14036160

申请日：2013-09-25

Applicant: Genentech, Inc.

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

IPC: C07D417/12 ,  A61K31/427 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/506 ,  C07D405/14 ,  A61K31/497

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.

Abstract translation: 式I的环醚吡唑-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R 2是环状醚，X是噻唑基，吡嗪基，吡啶基或嘧啶基，是有用的 用于抑制Pim激酶，以及用于治疗诸如由Pim激酶介导的癌症的疾病。 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：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：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：US09434725B2

公开(公告)日：2016-09-06

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

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.