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1.发明申请COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 有权用BTK抑制活性生产吡嗪和吡啶化合物的组合物和方法公开(公告)号：US20150259363A1
公开(公告)日：2015-09-17
申请号：US14727050
申请日：2015-06-01
申请人： Merck Patent GmbH
发明人： Brian L. HODOUS , Lesley LIU-BUJALSKI , Reinaldo JONES , Donald BANKSTON , Theresa L. JOHNSON , Igor MOCHALKIN , Ngan NGUYEN , Hui QIU , Andreas GOUTOPOULOS , Nadia BRUGGER
IPC分类号： C07F5/02 , A61K31/506 , C07D401/12 , A61K31/513 , C07D239/48 , A61K31/5377 , C07D403/04 , C07D401/04 , C07D401/14 , C07D451/02 , A61K31/55 , C07D413/12 , C07D403/12 , A61K31/505
CPC分类号： A61K31/69 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/10 , C07D495/04 , C07F5/022
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
摘要翻译： 本发明提供了式（I），式（II），式（III），式（IV）和式（V））的新型嘧啶和吡啶化合物，其用于治疗过度增殖性疾病的制造和用途，包括但不限于 癌症，狼疮，过敏性疾病，干燥病和类风湿性关节炎。 在优选的实施方案中，本发明描述不可逆激酶抑制剂，包括但不限于Bruton酪氨酸激酶的抑制剂。
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公开(公告)号：US20220389004A1
公开(公告)日：2022-12-08
申请号：US17271009
申请日：2019-08-26
申请人： Merck Patent GmbH
发明人： Richard D. CALDWELL , Lesley LIU-BUJALSKI , Justin POTNICK , Constantin NEAGU , Shashank KULKARNI , Reinaldo JONES , Hui QIU
IPC分类号： C07D471/04
摘要： The present invention relates to fused imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
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公开(公告)号：US20180243324A1
公开(公告)日：2018-08-30
申请号：US15969907
申请日：2018-05-03
申请人： Merck Patent GmbH
发明人： Brian L. HODOUS , Lesley LIU-BUJALSKI , Reinaldo JONES , Donald BANKSTON , Theresa L. JOHNSON , Igor MOCHALKIN , Ngan NGUYEN , Hui QIU , Andreas GOUTOPOULOS , Nadia BRUGGER
IPC分类号： A61K31/69 , A61K31/44 , A61K31/5377 , A61K31/55 , A61K31/505 , A61K31/506 , A61K31/4545
CPC分类号： A61K31/69 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/10 , C07D495/04 , C07F5/022
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
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公开(公告)号：US20170217905A1
公开(公告)日：2017-08-03
申请号：US15490370
申请日：2017-04-18
申请人： Merck Patent GmbH
发明人： Ruoxi LAN , Bayard R. HUCK , Xiaoling CHEN , Lizbeth C. DESELM , Hui QIU , Yufang XIAO , Constantin NEAGU , Igor MOCHALKIN , Theresa L. JOHNSON
IPC分类号： C07D239/48 , C07D239/49 , C07D403/04 , C07D403/12 , C07D413/04 , C07D401/12 , C07D401/04 , C07D401/14 , C07D413/14 , C07D405/14 , C07D417/14 , A61K31/506 , C07D413/06
CPC分类号： A61K31/506 , C07D239/48 , C07D239/49 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
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公开(公告)号：US20180318299A1
公开(公告)日：2018-11-08
申请号：US16031193
申请日：2018-07-10
申请人： Merck Patent GmbH
IPC分类号： A61K31/505 , C07D471/04 , C07D409/12 , C07D403/04 , C07D239/48 , C07D413/12 , C07D471/10 , C07D487/04 , C07D403/12 , C07D401/04
CPC分类号： A61K31/505 , C07D239/48 , C07D401/04 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D471/10 , C07D487/04
摘要： The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
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6.发明申请公开(公告)号：US20170136048A1
公开(公告)日：2017-05-18
申请号：US15417953
申请日：2017-01-27
申请人： Merck Patent GmbH
发明人： Brian L. HODOUS , Lesley LIU-BUJALSKI , Reinaldo JONES , Donald BANKSTON , Theresa L. JOHNSON , Igor MOCHALKIN , Ngan NGUYEN , Hui QIU , Andreas GOUTOPOULOS , Nadia BRUGGER
IPC分类号： A61K31/69 , A61K31/505 , A61K31/44 , A61K31/55 , A61K31/5377 , A61K31/506 , A61K31/4545
CPC分类号： A61K31/69 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/10 , C07D495/04 , C07F5/022
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
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公开(公告)号：US20160264548A1
公开(公告)日：2016-09-15
申请号：US15029420
申请日：2014-10-21
申请人： Hui QIU , Richard D. CALDWELL , Constantin NEAGU , Igor MOCHALKIN , Lesley LIUBUJALSKI , Reinaldo JONES , Devon TATE , Theresa L. JOHNSON , Anna GARDBERG , MERCK PATENT GMBH
发明人： Hui QIU , Richard D. CALDWELL , Constantin NEAGU , Igor MOCHALKIN , Lesley LIU-BUJALSKI , Reinaldo JONES , Devon TATE , Theresa L. JOHNSON , Anna GARDBERG
IPC分类号： C07D401/04 , C07D401/14 , C07D409/04 , C07D405/04 , C07D413/14 , C07D401/12 , C07D403/12 , C07D403/04 , C07D405/14 , C07D495/04 , C07D239/47 , C07F5/02 , C07D487/08 , C07D487/10 , C07D487/04 , C07D239/48 , C07D471/08 , C07D451/02 , C07D213/82
CPC分类号： C07D401/04 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K9/0078 , A61K9/02 , A61K9/06 , A61K9/08 , A61K9/1688 , A61K9/19 , A61K9/2018 , A61K9/2059 , A61K9/2826 , A61K9/286 , A61K47/06 , A61K47/186 , C07D213/81 , C07D213/82 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/06 , C07D413/14 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D487/10 , C07D495/04 , C07F5/022
摘要： The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
摘要翻译： 本发明涉及可用作BTK抑制剂的吡啶，嘧啶，吡嗪和哒嗪化合物及其药学上可接受的组合物。
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公开(公告)号：US20170008857A1
公开(公告)日：2017-01-12
申请号：US15205136
申请日：2016-07-08
申请人： Merck Patent GmbH
IPC分类号： C07D239/48 , C07D403/04 , C07D413/12 , C07D471/10 , C07D403/12 , C07D401/04 , C07D487/04
CPC分类号： A61K31/505 , C07D239/48 , C07D401/04 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D471/10 , C07D487/04
摘要： The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
摘要翻译： 本发明涉及可用作BTK抑制剂的嘧啶化合物及其药学上可接受的组合物。
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公开(公告)号：US20160096834A1
公开(公告)日：2016-04-07
申请号：US14876224
申请日：2015-10-06
申请人： Merck Patent GmbH
发明人： Pascale GAILLARD , Jeyaprakashnarayanan SEENISAMY , Lesley LIU-BUJALSKI , Richard D. CALDWELL , Justin POTNICK , Hui QIU , Constantin NEAGU , Reinaldo JONES , Annie Cho WON , Andreas GOUTOPOULOS , Brian A. SHERER , Theresa L. JOHNSON , Anna GARDBERG
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
摘要翻译： 本发明涉及可用作BTK抑制剂的咪唑并吡啶化合物及其药学上可接受的组合物。
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公开(公告)号：US20170226113A1
公开(公告)日：2017-08-10
申请号：US15499460
申请日：2017-04-27
申请人： Merck Patent GmbH
发明人： Lesley LIU-BUJALSKI , Ngan NGUYEN , Hui QIU , Reinaldo JONES , Igor MOCHALKIN , Richard D. CALDWELL
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , C07D471/04
摘要： The present invention relates to pyridine, pyrimidine, and pyrazene compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
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