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1.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).-
2.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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3.发明公开USE OF AMPK-ACTIVATING IMIDAZOLE DERIVATIVES, PREPARATION PROCESS THEREFOR AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 有权AMPK激活咪唑衍生物，使用过程中其制造和药物组合物含
公开(公告)号：EP2040702A1
公开(公告)日：2009-04-01
申请号：EP07725977.8
申请日：2007-06-12
申请人： Merck Patent GmbH
IPC分类号： A61K31/4164 , C07D233/90 , A61P3/00 , A61P3/10
CPC分类号： C07D233/90
摘要： The invention relates to the use of imidazole derivatives of the formula (I): in which A, R'1, R'2 and R'3 are as defined in the description, as AMPK activators. The invention also relates to processes for the preparation of the said compounds, to their uses for the preparation of medicaments for the treatment of insulin resistance, diabetes and related pathologies, and also obesity, and to the pharmaceutical compositions comprising them. Certain compounds of the formula (I) are novel and, in this respect, also form part of the invention.
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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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5.发明授权7-AZAINDOLE DERIVATIVES AS SELECTIVE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS 有权7-氮杂吲哚衍生物11-β-羟基类固醇脱氢酶1型的选择性抑制剂
公开(公告)号：EP2247589B1
公开(公告)日：2012-11-21
申请号：EP08802728.9
申请日：2008-10-01
申请人： Merck Patent GmbH
IPC分类号： C07D471/04 , A61K31/33 , A61P25/00
CPC分类号： C07D471/04
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6.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).-
7.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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8.发明授权USE OF AMPK-ACTIVATING IMIDAZOLE DERIVATIVES, PREPARATION PROCESS THEREFOR AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 有权AMPK激活咪唑衍生物，使用过程中其制造和药物组合物含
公开(公告)号：EP2040702B1
公开(公告)日：2011-07-27
申请号：EP07725977.8
申请日：2007-06-12
申请人： Merck Patent GmbH
IPC分类号： A61K31/4164 , C07D233/90 , A61P3/00 , A61P3/10
CPC分类号： C07D233/90
摘要： The invention relates to the use of imidazole derivatives of the formula (I): in which A, R'1, R'2 and R'3 are as defined in the description, as AMPK activators. The invention also relates to processes for the preparation of the said compounds, to their uses for the preparation of medicaments for the treatment of insulin resistance, diabetes and related pathologies, and also obesity, and to the pharmaceutical compositions comprising them. Certain compounds of the formula (I) are novel and, in this respect, also form part of the invention.
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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.-
10.发明授权USE OF THIENOPYRIDONE DERIVATIVES AS AMPK ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权THIENOPYRIDONDERIVATEN作为AMPK激活剂和药物组合物使用含
公开(公告)号：EP1915150B1
公开(公告)日：2011-01-26
申请号：EP06762350.4
申请日：2006-07-03
申请人： Merck Patent GmbH
IPC分类号： A61K31/4436 , C07D495/04 , A61P3/10
CPC分类号： C07D495/04 , C07D233/64
摘要： Use of thienopyridone derivatives of formula (I), in which B, R, R6, Y and Z are as defined in the description, and their pharmaceutically acceptable salts, for the preparation of a pharmaceutical composition useful for the treatment of diabetes, metabolic syndrome, related disorders and obesity.
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