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公开(公告)号：EP2822930B1
公开(公告)日：2016-01-20
申请号：EP13710937.7
申请日：2013-03-04
发明人： BUKHTIYAROV, Yuri , CACATIAN, Salvacion , DILLARD, Lawrence, Wayne , DORNER-CIOSSEK, Cornelia , FUCHS, Klaus , JIA, Lanqi , LALA, Deepak, S. , MORALES-RAMOS, Angel , RAST, Georg , REEVES, Jonathan , SINGH, Suresh, B. , VENKATRAMAN, Shankar , XU, Zhenrong , YUAN, Jing , ZHAO, Yi , ZHENG, Yajun
IPC分类号： C07D235/02 , C07D403/06 , C07D407/06 , C07C49/323 , A61K31/4184 , A61P25/28 , A61K31/506 , C07C255/47 , C07C313/06 , C07D405/06 , C07C229/50 , C07C331/14
CPC分类号： A61K31/506 , A61K31/4184 , C07C49/697 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/47 , C07C313/06 , C07C331/14 , C07D235/02 , C07D403/06 , C07D405/06 , C07D407/06
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公开(公告)号：EP2291371A1
公开(公告)日：2011-03-09
申请号：EP09739195.7
申请日：2009-04-30
发明人： CLAREMON, David, A. , ZHUANG, Linghang , LEFTHERIS, Katerina , TICE, Colin, M. , XU, Zhenrong , YE, Yuanjie , SINGH, Suresh, B. , CACATIAN, Salvacion , ZHAO, Wei , HIMMELSBACH, Frank , ECKHARDT, Matthias
IPC分类号： C07D413/10 , C07D413/14 , A61K31/5355 , A61P19/10 , C07D417/10 , C07D417/14
CPC分类号： C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： This invention relates to novel compounds of the Formula I, Ik, Iq
1-21 , Ir
1-21 , Is
1-21 , It
1-7 , pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.摘要翻译： 本发明涉及新的式I化合物，Ik，Iq 1-21，Ir 1-21，Is 1-21，It 1-7，其药学上可接受的盐及其药物组合物，其可用于治疗性治疗 与哺乳动物中调节或抑制11β-HSD1有关的疾病。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇产生或抑制细胞中可的松向皮质醇转化的方法。
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公开(公告)号：EP2291371B1
公开(公告)日：2015-06-10
申请号：EP09739195.7
申请日：2009-04-30
发明人： CLAREMON, David, A. , ZHUANG, Linghang , LEFTHERIS, Katerina , TICE, Colin, M. , XU, Zhenrong , YE, Yuanjie , SINGH, Suresh, B. , CACATIAN, Salvacion , ZHAO, Wei , HIMMELSBACH, Frank , ECKHARDT, Matthias
IPC分类号： C07D413/10 , C07D413/14 , A61K31/5355 , A61P19/10 , C07D417/10 , C07D417/14
CPC分类号： C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
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公开(公告)号：EP2406240B1
公开(公告)日：2015-12-23
申请号：EP10708684.5
申请日：2010-03-12
发明人： CACATIAN, Salvacion , CLAREMON, David, A. , DILLARD, Lawrence, W. , FUCHS, Klaus , HEINE, Niklas , JIA, Lanqi , LEFTHERIS, Katerina , MCKEEVER, Brian , MORALES-RAMOS, Angel , SINGH, Suresh , VENKATRAMAN, Shankar , WU, Guosheng , WU, Zhongren , XU, Zhenrong , YUAN, Jing , ZHENG, Yajun
IPC分类号： C07D233/46 , C07D235/02
CPC分类号： C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
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公开(公告)号：EP2888236A1
公开(公告)日：2015-07-01
申请号：EP13760166.2
申请日：2013-08-26
发明人： BUKHTIYAROV, Yuri , CACATIAN, Salvacion , DILLARD, Lawrence, Wayne , DORNER-CIOSSEK, Cornelia , FUCHS, Klaus , GROSS, Ulrike , HEINE, Niklas , JIA, Lanqi , LALA, Deepak, S. , MORALES-RAMOS, Angel , SINGH, Suresh, B. , SAUER, Achim , VENKATRAMAN, Shankar , XU, Zhenrong , YUAN, Jing , ZHAO, Yi , ZHENG, Yajun
IPC分类号： C07D235/02 , C07D401/06 , C07D403/04 , A61K31/4184 , A61P25/28
CPC分类号： C07D235/02 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/59 , C07C313/06 , C07C331/26 , C07C2603/94 , C07C2603/97 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06
摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β- secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
摘要翻译： 本发明涉及螺环酰基胍和它们作为β-分泌酶（BACE1）活性抑制剂的用途，含有该化合物的药物组合物，以及使用它们作为治疗剂治疗神经变性疾病，以认知衰退为特征的疾病的方法 ，认知障碍，痴呆和特征在于产生β-淀粉样蛋白聚集体的疾病。
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公开(公告)号：EP2300461B1
公开(公告)日：2013-04-17
申请号：EP09739203.9
申请日：2009-04-30
发明人： CLAREMON, David, A. , ZHUANG, Linghang , LEFTHERIS, Katerina , TICE, Colin, M. , XU, Zhenrong , YE, Yuanjie , SINGH, Suresh, B. , CACATIAN, Salvacion , ZHAO, Wei , HIMMELSBACH, Frank
IPC分类号： C07D413/10 , C07D413/14 , A61K31/5355 , A61P19/10
CPC分类号： C07D413/10 , C07D413/14
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公开(公告)号：EP2822930A1
公开(公告)日：2015-01-14
申请号：EP13710937.7
申请日：2013-03-04
发明人： BUKHTIYAROV, Yuri , CACATIAN, Salvacion , DILLARD, Lawrence, Wayne , DORNER-CIOSSEK, Cornelia , FUCHS, Klaus , JIA, Lanqi , LALA, Deepak, S. , MORALES-RAMOS, Angel , RAST, Georg , REEVES, Jonathan , SINGH, Suresh, B. , VENKATRAMAN, Shankar , XU, Zhenrong , YUAN, Jing , ZHAO, Yi , ZHENG, Yajun
IPC分类号： C07D235/02 , C07D403/06 , C07D407/06 , C07C49/323 , A61K31/4184 , A61P25/28
CPC分类号： A61K31/506 , A61K31/4184 , C07C49/697 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/47 , C07C313/06 , C07C331/14 , C07D235/02 , C07D403/06 , C07D405/06 , C07D407/06
摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
摘要翻译： 本发明涉及螺环酰基胍及其作为β-分泌酶（BACE1）活性抑制剂的用途，含有该化合物的药物组合物，以及使用该化合物作为治疗剂治疗神经变性疾病，以认知衰退为特征的疾病的方法 ，认知障碍，痴呆和特征在于产生β-淀粉样蛋白聚集体的疾病。
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公开(公告)号：EP2406240A2
公开(公告)日：2012-01-18
申请号：EP10708684.5
申请日：2010-03-12
发明人： CACATIAN, Salvacion , CLAREMON, David, A. , DILLARD, Lawrence, W. , FUCHS, Klaus , HEINE, Niklas , JIA, Lanqi , LEFTHERIS, Katerina , MCKEEVER, Brian , MORALES-RAMOS, Angel , SINGH, Suresh , VENKATRAMAN, Shankar , WU, Guosheng , WU, Zhongren , XU, Zhenrong , YUAN, Jing , ZHENG, Yajun
IPC分类号： C07D277/60 , C07D271/12 , C07D235/02 , C07D239/70 , C07D491/10 , C07D487/10 , C07D403/06 , C07D405/12 , C07D498/10 , A61K31/4245 , A61K31/4184 , A61K31/4188 , A61K31/517 , A61K31/519 , A61K31/428
CPC分类号： C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
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公开(公告)号：EP2300461A1
公开(公告)日：2011-03-30
申请号：EP09739203.9
申请日：2009-04-30
发明人： CLAREMON, David, A. , ZHUANG, Linghang , LEFTHERIS, Katerina , TICE, Colin, M. , XU, Zhenrong , YE, Yuanjie , SINGH, Suresh, B. , CACATIAN, Salvacion , ZHAO, Wei , HIMMELSBACH, Frank
IPC分类号： C07D413/10 , C07D413/14 , A61K31/5355 , A61P19/10
CPC分类号： C07D413/10 , C07D413/14
摘要： This invention relates to novel compounds of the Formula Ik, Im
1 , Im
2 , Im
5 , In
1 , In
2 , In
5 , lo
1 , lo
2 , lo
5 , Ip
1 , Ip
3 , pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.-
10.发明授权CYCLIC CARBAZATE AND SEMICARBAZIDE INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权循环Carbazates和氨基脲AS11β-羟类固醇脱氢酶1抑制剂
公开(公告)号：EP2252601B1
公开(公告)日：2012-12-19
申请号：EP09703823.6
申请日：2009-01-21
发明人： CLAREMON, David, A. , ZHUANG, Linghang , YE, Yuanjie , SINGH, Suresh, B. , TICE, Colin, M. , CACATIAN, Salvacion
IPC分类号： C07D265/10 , A61K31/417 , A61P37/00
CPC分类号： C07D265/10
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