公开(公告)号：US20140171407A1

公开(公告)日：2014-06-19

申请号：US14182190

申请日：2014-02-17

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Lewis Gazzard ,  Karen Williams ,  Huifen Chen ,  Samuel Kintz ,  Joy Drobnick ,  Joseph P. Lyssikatos ,  Simon Goodacre ,  Calum Macleod ,  Charles Ellwood

IPC: C07D471/14 ,  A61K31/4375 ,  C07D453/02 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/439 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D453/02 ,  C07D519/00

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

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：US09440976B2

公开(公告)日：2016-09-13

申请号：US14743835

申请日：2015-06-18

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Lewis Gazzard ,  Karen Williams ,  Huifen Chen ,  Samuel Kintz ,  Joy Drobnick ,  Joseph P. Lyssikatos ,  Simon Goodacre ,  Calum Macleod ,  Charles Ellwood

IPC: C07D471/14 ,  C07D453/02 ,  A61K31/5377 ,  C07D519/00 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D453/02 ,  C07D519/00

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US20130261104A1

公开(公告)日：2013-10-03

申请号：US13890949

申请日：2013-05-09

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  C07D513/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/541 ,  A61K31/501 ,  A61K31/506 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4375 ,  C07D491/107

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

公开(公告)号：US09216980B2

公开(公告)日：2015-12-22

申请号：US14255898

申请日：2014-04-17

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: A61K31/437 ,  A61K31/496 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/553 ,  C07D519/00

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

Abstract translation: 式（I）化合物用于治疗癌症的方法：其中X，Y，X，R 3，R 5和R 6如本文所定义。

公开(公告)号：US20150087630A1

公开(公告)日：2015-03-26

申请号：US14255898

申请日：2014-04-17

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/553 ,  A61K31/55 ,  A61K31/541 ,  A61K31/4375 ,  C07D519/00

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

Abstract translation: 式（I）化合物用于治疗癌症的方法：其中X，Y，X，R 3，R 5和R 6如本文所定义。

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.