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1.发明授权HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY 有权HETEROARYLPYRIDON-和AZA吡啶酮AS BTK活性抑制
公开(公告)号：EP2773638B1
公开(公告)日：2015-10-07
申请号：EP12783837.3
申请日：2012-11-02
IPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04 , C07D519/00 , A61K31/4985 , C07D487/14 , A61K31/381 , A61K31/4353 , A61P35/00 , A61P37/00
CPC分类号： 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
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2.发明公开HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY 有权HETEROARYLPYRIDON-和AZA吡啶酮AS BTK活性抑制
公开(公告)号：EP2773638A1
公开(公告)日：2014-09-10
申请号：EP12783837.3
申请日：2012-11-02
IPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04 , C07D519/00 , A61K31/4985 , C07D487/14 , A61K31/381 , A61K31/4353 , A61P35/00 , A61P37/00
CPC分类号： 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
摘要： Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X
1 , X
2 , and X
3 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.-
3.发明公开HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS WITH ELECTROPHILIC FUNCTIONALITY 有权杂芳基吡啶酮和具有电子亲和功能的氮杂 - 吡啶酮化合物
公开(公告)号：EP3077384A1
公开(公告)日：2016-10-12
申请号：EP14808596.2
申请日：2014-12-04
发明人： CRAWFORD, James , WEI, BinQing , YOUNG, Wendy B.
IPC分类号： C07D401/14 , C07D495/04 , A61K31/5025 , A61P35/00 , A61P37/00
CPC分类号： C07D401/14 , A61K31/496 , A61K31/4985 , A61K31/502 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K39/3955 , C07D487/04 , C07D495/04
摘要： Heteroaryl pyridone and aza-pyridone amide compounds with electrophilic functionality of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. 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.
摘要翻译： 提供了具有式I的亲电子官能团的杂芳基吡啶酮和氮杂 - 吡啶酮酰胺化合物，包括其立体异构体，互变异构体和药学上可接受的盐，其可用于抑制Btk并用于治疗癌症和免疫病症，如由Btk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治疗哺乳动物细胞中的这些病症或相关病理学病症的方法。
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4.发明公开ALKYLATED PIPERAZINE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY 有权ALKYLIERTE PIPERAZIN-VERBINDUNGEN ALS INHIBITOREN VON BTKAKTIVITÄT
公开(公告)号：EP2773639A1
公开(公告)日：2014-09-10
申请号：EP12783838.1
申请日：2012-11-02
IPC分类号： C07D471/04 , C07D495/04 , C07D519/00 , A61K31/4985 , A61K31/381 , A61P35/00 , A61P37/00
CPC分类号： C07D513/04 , A61K31/496 , A61K31/4985 , A61K31/5025 , A61K31/5386 , A61K45/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/08 , C07D519/00
摘要： Alkylated 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.摘要翻译： 提供式I的烷基化哌嗪化合物，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条件中的这些疾病的治疗的方法。
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5.发明公开8-FLUOROPHTHALAZIN-1 (2H) - ONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY 有权8-FLUOROPHTHALAZIN-1（2H）-ON-VERBINDUNGEN ALS INHIBITOREN VON BTKAKTIVITÄT
公开(公告)号：EP2773632A1
公开(公告)日：2014-09-10
申请号：EP12783834.0
申请日：2012-11-02
IPC分类号： C07D401/10 , C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/502 , A61P35/00 , A61P37/00
CPC分类号： A61K31/506 , A61K31/502 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D401/10 , C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D498/04 , C07D513/04
摘要： 8-Fluorophthalazin-1(2h)-one compounds of Formula (II) where one or two of X
1 , X
2 , and X
3 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.摘要翻译： 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-氟吲嗪-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Btk激酶介导的免疫疾病如炎症。 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疾病的治疗的方法。
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