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1.发明授权THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS 有权THIENOPYRIDON衍生物作为AMP活化蛋白激酶（AMPK）活化剂
公开(公告)号：EP2262500B1
公开(公告)日：2016-04-27
申请号：EP09731265.6
申请日：2009-03-17
申请人： Merck Patent GmbH
IPC分类号： A61K31/4365 , C07D495/04 , A61P3/00 , A61P9/00 , A61P35/00 , A61P29/00
CPC分类号： C07D495/04
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公开(公告)号：EP2285786A1
公开(公告)日：2011-02-23
申请号：EP09765489.1
申请日：2009-05-19
申请人： Merck Patent GmbH
IPC分类号： C07D241/44 , C07D471/04 , A61K31/495 , A61P3/04 , A61P3/10
CPC分类号： C07D241/44 , C07D471/04
摘要： The present invention relates to compounds of formula (I) wherein X, Y, Z, R
1 , R
2 , R
3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.-
公开(公告)号：EP2285786B1
公开(公告)日：2013-10-09
申请号：EP09765489.1
申请日：2009-05-19
申请人： Merck Patent GmbH
IPC分类号： C07D241/44 , C07D471/04 , A61K31/495 , A61P3/04 , A61P3/10
CPC分类号： C07D241/44 , C07D471/04
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4.发明授权THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS 有权THIENOPYRIDON衍生物作为AMP活化蛋白激酶（AMPK）活化剂
公开(公告)号：EP2280952B1
公开(公告)日：2012-06-27
申请号：EP09741799.2
申请日：2009-04-08
申请人： Merck Patent GmbH
IPC分类号： C07D333/38 , C07D495/04 , A61P3/04 , A61P3/10 , A61P29/00 , A61P35/00
CPC分类号： C07D495/04 , C07D333/38
摘要： The present invention relates to compounds of formula (I) wherein R
1 , R
2 and B
1 , B
2 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).-
5.发明授权FUSED PYRROLIDINO-CYCLOPROPANE DERIVATIVES AS SELECTIVE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS 有权共11-β-羟基类固醇脱氢酶1融合PYRROLIDINOCYCLOPROPAN衍生物作为选择性抑制剂，
公开(公告)号：EP2321317B1
公开(公告)日：2014-12-24
申请号：EP09777657.9
申请日：2009-08-05
申请人： Merck Patent GmbH
发明人： VALEUR, Eric , LEPIFRE, Franck , ROCHE, Didier , CARNIATO, Denis , CHRISTMANN-FRANCK, Serge , SCHMIDLIN, Fabien
IPC分类号： C07D471/04 , A61K31/407 , A61P3/10
CPC分类号： C07D471/04
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6.发明公开THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS 有权THIENOPYRIDON衍生物作为AMP活化蛋白激酶（AMPK）活化剂
公开(公告)号：EP2280952A1
公开(公告)日：2011-02-09
申请号：EP09741799.2
申请日：2009-04-08
申请人： Merck Patent GmbH
IPC分类号： C07D333/38 , C07D495/04 , A61P3/04 , A61P3/10 , A61P29/00 , A61P35/00
CPC分类号： C07D495/04 , C07D333/38
摘要： The present invention relates to compounds of formula (I) wherein R
1 , R
2 and B
1 , B
2 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).-
7.发明公开THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS 有权THIENOPYRIDON衍生物作为AMP活化蛋白激酶（AMPK）活化剂
公开(公告)号：EP2262500A1
公开(公告)日：2010-12-22
申请号：EP09731265.6
申请日：2009-03-17
申请人： Merck Patent GmbH
IPC分类号： A61K31/4365 , C07D495/04 , A61P3/00 , A61P9/00 , A61P35/00 , A61P29/00
CPC分类号： C07D495/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).
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8.发明公开FUSED PYRROLIDINO-CYCLOPROPANE DERIVATIVES AS SELECTIVE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS 有权共11-β-羟基类固醇脱氢酶1融合PYRROLIDINOCYCLOPROPAN衍生物作为选择性抑制剂，
公开(公告)号：EP2321317A1
公开(公告)日：2011-05-18
申请号：EP09777657.9
申请日：2009-08-05
申请人： Merck Patent GmbH
发明人： VALEUR, Eric , LEPIFRE, Franck , ROCHE, Didier , CARNIATO, Denis , CHRISTMANN-FRANCK, Serge , SCHMIDLIN, Fabien
IPC分类号： C07D471/04 , A61K31/407 , A61P3/10
CPC分类号： C07D471/04
摘要： The present invention relates to fused pyrrolidino-cyclopropane derivatives according to Formulae (I) to (II), as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-β-HSD-1 ) and the use of such compounds for the treatment and/or prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis/ cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
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