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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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公开(公告)号：EP2882718A1
公开(公告)日：2015-06-17
申请号：EP13827574.8
申请日：2013-08-09
发明人： BROOKFIELD, Frederick , BURCH, Jason , GOLDSMITH, Richard A. , HU, Baihua , LAU, Kevin Hon Luen , MACKINNON, Colin H. , ORTWINE, Daniel Fred , PEI, Zhonghua , WU, Guosheng , YUEN, Po-wai , ZHANG, Yamin
IPC分类号： C07D231/56 , A61K31/416 , A61P37/00
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/10 , C07D491/044 , C07D491/10 , C07D491/107 , C07D495/10 , Y02P20/582
摘要： Provided herein are compounds of formula (AA): N N H HN O N N R R 6 A (R a ) p, (AA) stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, R a, p, R and R 6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.
摘要翻译： 本文提供了式（AA）的化合物：其中A，R a，p，R和R 6如本文定义的组合物，其包含 该化合物以及制造和使用该化合物治疗疾病的方法。
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3.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.-
4.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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