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：US20160228432A1

公开(公告)日：2016-08-11

申请号：US14943552

申请日：2015-11-17

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: A61K31/4985 ,  A61K31/495 ,  A61K31/5377 ,  A61K31/496 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: Heteroaryl pyridone and aza-pyridone compounds 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 heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供了杂芳基吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体和其药学上可接受的盐，以及用于治疗免疫疾病如由Btk激酶介导的炎症。 公开了使用杂芳基吡啶酮和氮杂 - 吡啶酮化合物用于体外，原位和体内诊断以及哺乳动物细胞或相关病理条件中的这些疾病的治疗方法。

公开(公告)号：US20140378432A1

公开(公告)日：2014-12-25

申请号：US14479529

申请日：2014-09-08

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: C07D487/04 ,  C07D513/04 ,  C07D471/04 ,  C07D498/04 ,  C07D487/08

CPC classification number: A61K31/4985 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: Heteroaryl pyridone and aza-pyridone compounds 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 heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供了杂芳基吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体和其药学上可接受的盐，以及用于治疗免疫疾病如由Btk激酶介导的炎症。 公开了使用杂芳基吡啶酮和氮杂 - 吡啶酮化合物用于体外，原位和体内诊断以及哺乳动物细胞或相关病理条件中的这些疾病的治疗方法。

公开(公告)号：US08722676B2

公开(公告)日：2014-05-13

申请号：US13667121

申请日：2012-11-02

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  Wendy B. Young

IPC: A61K31/50 ,  A61K31/495 ,  A61K31/501 ,  A61K31/497 ,  A01N43/58 ,  A01N43/60 ,  C07D487/00

CPC classification number: C07D495/04 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5025 ,  A61K45/06 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04

Abstract: Bicyclic piperazine 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.

Abstract translation: 提供了式I的双环哌嗪化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体和其药学上可接受的盐，以及用于治疗免疫疾病如由Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

公开(公告)号：US20140128401A1

公开(公告)日：2014-05-08

申请号：US14154008

申请日：2014-01-13

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Daniel Fred Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: A61K31/506 ,  C07D405/14 ,  C07D401/14 ,  A61K31/502

CPC classification number: A61K31/506 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X1, X2, and X3 are N, 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.

Abstract translation: 提供了其中X 1，X 2和X 3中的一个或两个为N的式I化合物，其包括用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于 治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

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.