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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.
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公开(公告)号:USRE48239E1
公开(公告)日:2020-10-06
申请号:US16175278
申请日:2018-10-30
Applicant: Genentech, Inc.
Inventor: James John Crawford , Daniel Fred Ortwine , BinQing Wei , Wendy B. Young
IPC: C07D487/04 , A61P37/00 , A61P35/00 , A61K9/20 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/4995 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D471/04 , C07D471/14 , C07D487/08 , C07D487/14 , C07D495/04 , C07D495/14 , C07D498/04 , C07D513/04 , C07D519/00
Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and 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.
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公开(公告)号:US20190194203A1
公开(公告)日:2019-06-27
申请号:US16020270
申请日:2018-06-27
Applicant: Genentech, Inc.
Inventor: James John Crawford , Daniel Fred Ortwine , BinQing Wei , Wendy B. Young
IPC: C07D487/04 , A61K9/20
CPC classification number: C07D487/04 , A61K9/20 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/4995 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K45/06 , A61P35/00 , A61P37/00 , C07D471/04 , C07D471/14 , 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.
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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.
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25.
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。
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公开(公告)号:US09238655B2
公开(公告)日:2016-01-19
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: C07D471/00 , C07D487/04 , C07D487/14 , C07D471/04 , C07D471/14 , C07D495/04 , C07D519/00 , A61K31/496 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D495/14 , C07D498/04 , A61K31/4995 , A61K31/501 , C07D487/08 , C07D513/04
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。
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公开(公告)号:US08921353B2
公开(公告)日:2014-12-30
申请号:US14207966
申请日:2014-03-13
Applicant: Genentech, Inc.
Inventor: James John Crawford , Daniel Fred Ortwine , BinQing Wei , Wendy B. Young
IPC: A61K31/00
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 of Formula I are provided, where one or two of X1, X2, and X3 are N, and 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.
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公开(公告)号:US08716274B2
公开(公告)日:2014-05-06
申请号:US13667133
申请日:2012-11-02
Applicant: Genentech, Inc.
Inventor: James John Crawford , Daniel Fred Ortwine , BinQing Wei , Wendy B. Young
IPC: A61K31/00 , C07D471/00
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 of Formula I are provided, where one or two of X1, X2, and X3 are N, and 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: 提供式I的杂芳基吡啶酮和氮杂 - 吡啶酮化合物,其中X1,X2和X3中的一个或两个为N,并且包括可用于抑制Btk激酶和用于治疗免疫疾病的立体异构体,互变异构体及其药学上可接受的盐 例如由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。
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公开(公告)号:US08669251B2
公开(公告)日:2014-03-11
申请号:US13667126
申请日:2012-11-02
Applicant: Genentech, Inc.
Inventor: James John Crawford , Daniel Fred Ortwine , BinQing Wei , Wendy B. Young
IPC: A61K31/5383 , A61K31/5377 , A61K31/502 , C07D498/04 , C07D487/04 , C07D401/14 , C07D413/14
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 II 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 II 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: 提供其中X 1,X 2和X 3中的一个或两个为N的式II的8-氟酞嗪-1(2h) - 酮化合物,包括其可用于抑制Btk激酶的立体异构体,互变异构体及其药学上可接受的盐, 治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式II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条件中的这些病症的治疗的方法。
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公开(公告)号:US20130116262A1
公开(公告)日:2013-05-09
申请号:US13667121
申请日:2012-11-02
Applicant: Genentech, Inc.
Inventor: James John Crawford , Daniel Fred Ortwine , Wendy B. Young
IPC: C07D495/04 , A61K31/4985 , A61K45/06 , C07D487/04 , A61K31/5025 , C07D473/34 , C07D471/04 , A61K31/496
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。
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