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公开(公告)号：US20160016936A1
公开(公告)日：2016-01-21
申请号：US14775205
申请日：2014-03-10
申请人： Ruoxi LAN , Xiaoling CHEN , Yufang XIAO , Bayard R. HUCK , Andreas GOUTOPOULOS , MERCK PATENT GMBH
发明人： Ruoxi LAN , Xiaoling CHEN , Yufang XIAO , Bayard R. HUCK , Andreas GOUTOPOULOS
IPC分类号： C07D401/14 , C07D487/04 , A61K31/519 , A61K31/506
CPC分类号： A61K31/519 , A61K31/506 , C07D401/14 , C07D487/04
摘要： The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型杂环胺，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US20230019491A1
公开(公告)日：2023-01-19
申请号：US16756769
申请日：2018-10-17
发明人： Srinivasa R. Karra , Yufang XIAO , Brian Sherer
IPC分类号： C07D405/14 , C07D417/14 , C07D498/08 , C07D493/08 , C07D491/048 , C07D453/02 , C07D401/14 , C07D413/14
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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![TETRAHYDROPYRIDO[3,4-d]PYRIMIDINES AS HPK1 INHIBITORS](/abs-image/US/2024/01/25/US20240025922A1/abs.jpg.150x150.jpg)
公开(公告)号：US20240025922A1
公开(公告)日：2024-01-25
申请号：US18313652
申请日：2023-05-08
申请人： Merck Patent GmbH
发明人： Momar TOURE , Bin LI , Constantin NEAGU , Yanping WANG , Theresa JOHNSON , Andrea UNZUE LOPEZ , Yufang XIAO , Emily FRIIS , Maria DIPOTO , Satenig GULER
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： Tetrahydropyrido[3,4-d]pyrimidines compounds are provided that are potent HPK1 inhibitors. The compounds are useful to treat or prevent cancer and/or inflammatory and/or autoimmune diseases or symptoms thereof in mammals, particularly humans. The compounds have a chemical structure of the general Formula (I), (II), (III), (IV) or (V) or enantiomers or diastereomers or mixtures thereof or pharmaceutically acceptable salts thereof.
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公开(公告)号：US20160376283A1
公开(公告)日：2016-12-29
申请号：US15194780
申请日：2016-06-28
申请人： Merck Patent GmbH
发明人： Brian A. SHERER , Srinivasa KARRA , Yufang XIAO
IPC分类号： C07D491/048 , C07D519/00
CPC分类号： C07D491/048 , C07D405/04 , C07D519/00
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
摘要翻译： 本发明涉及可用作TBK /IKKε抑制剂的式I化合物及其药学上可接受的组合物。
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公开(公告)号：US20160339028A1
公开(公告)日：2016-11-24
申请号：US15227017
申请日：2016-08-03
申请人： Merck Patent GmbH
发明人： Bayard R. HUCK , Xiaoling CHEN , Yufang XIAO , Ruoxi LAN , Lizbeth Celeste DE SELM , Constantin NEAGU , Justin POTNICK , Srinivasa R. KARRA , Theresa L. JOHNSON
IPC分类号： A61K31/517 , C07D401/12 , C07D239/74 , C07D403/04 , A61K31/496 , C07D215/48 , A61K31/47 , C07D401/14 , A61K31/4709 , C07D403/12 , C07D401/04
CPC分类号： A61K31/517 , A61K31/47 , A61K31/4709 , A61K31/496 , C07D215/48 , C07D239/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12
摘要： The invention provides novel heterocyclic carboxamide compounds compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供了根据式（I）的新型杂环羧酰胺化合物其用于治疗过度增殖性疾病如癌症的制造和用途。
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公开(公告)号：US20210214339A1
公开(公告)日：2021-07-15
申请号：US16756954
申请日：2018-10-17
发明人： Srinivasa R. KARRA , Yufang XIAO , Brian SHERER , Eugene CHECKLER
IPC分类号： C07D401/14 , C07D405/14 , C07D419/14 , C07D498/18
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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公开(公告)号：US20180244682A1
公开(公告)日：2018-08-30
申请号：US15963273
申请日：2018-04-26
申请人： Merck Patent GmbH
发明人： Brian A. SHERER , Srinivasa KARRA , Yufang XIAO
IPC分类号： C07D491/048 , C07D519/00 , C07D405/04
CPC分类号： C07D491/048 , C07D405/04 , C07D519/00
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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8.发明申请公开(公告)号：US20150353497A1
公开(公告)日：2015-12-10
申请号：US14730351
申请日：2015-06-04
申请人： Merck Patent GmbH
IPC分类号： C07D215/48 , C07D401/14 , C07D405/04 , C07D401/04
CPC分类号： A61K31/47 , A61K31/4709 , C07D215/48 , C07D401/04 , C07D401/14 , C07D405/04
摘要： The present invention relates to quinoline compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
摘要翻译： 本发明涉及可用作P2X7的拮抗剂和用于治疗P2X7相关疾病的喹啉化合物及其药学上可接受的组合物。
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公开(公告)号：US20180072757A1
公开(公告)日：2018-03-15
申请号：US15818035
申请日：2017-11-20
申请人： Merck Patent GmbH
发明人： Ruoxi LAN , Bayard R. HUCK , Xiaoling CHEN , Yufang XIAO
IPC分类号： C07D498/04 , A61K45/06 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5383 , C07D475/06 , A61N5/10 , C07D239/70 , C07D471/04 , C07D487/04
CPC分类号： C07D498/04 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D239/70 , C07D471/04 , C07D475/06 , C07D487/04
摘要： The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in 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：US20160184308A1
公开(公告)日：2016-06-30
申请号：US15060050
申请日：2016-03-03
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： A61K31/506
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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