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公开(公告)号：EP2195312B1
公开(公告)日：2012-11-21
申请号：EP08785525.0
申请日：2008-08-13
申请人： Merck Patent GmbH
IPC分类号： C07D417/12 , C07D213/74 , C07D401/12 , C07D401/14 , C07D417/14 , A61P3/00 , A61K31/4427 , A61K31/444
CPC分类号： C07D417/12 , C07D213/74 , C07D401/12 , C07D401/14 , C07D417/14
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12.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).-
13.发明公开PYRAZINONE DERIVATIVES AS INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES 有权PYRAZINONDERIVATE ALS INSULINAUSSCHEIDUNGSSTIMULATOREN，用于治疗糖尿病的生产工艺和用途
公开(公告)号：EP2250156A1
公开(公告)日：2010-11-17
申请号：EP09718204.2
申请日：2009-01-15
申请人： Merck Patent GmbH
IPC分类号： C07D241/18 , A61K31/4965 , A61P3/10
CPC分类号： C07D241/08 , C07D241/18
摘要： The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
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14.发明公开N- ( PYRAZOLE- 3 -YL) -BENZAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS 有权N-（PYRAZOL-3-YL）BENZAMIDDERIVATE ALS GLUCOKINASEAKTIVATOREN
公开(公告)号：EP2197849A1
公开(公告)日：2010-06-23
申请号：EP08801938.5
申请日：2008-09-09
申请人： Merck Patent GmbH
发明人： BURGDORF, Lars, Thore , CARNIATO, Denis , EMDE, Ulrich , BEIER, Norbert , GLEITZ, Johannes , CHARON, Christine
IPC分类号： C07D231/40 , C07D401/06 , C07D409/12 , C07D409/14 , A61K31/4155 , A61P3/04 , A61P3/10
CPC分类号： C07D401/06 , C07D231/40 , C07D409/12 , C07D409/14
摘要： Novel heterocyclic compounds of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, Alk and D have the meanings indicate in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
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15.发明公开2-ADAMANTYLUREA DERIVATIVES AS SELECTIVE 11BETA-HSD1 INHIBITORS 有权2-ADAMANTYLUREA衍生物作为选择性11BETA-HSD1抑制剂
公开(公告)号：EP1960352A1
公开(公告)日：2008-08-27
申请号：EP06818709.5
申请日：2006-11-22
申请人： Merck Patent GmbH
IPC分类号： C07C275/28
CPC分类号： C07D261/14 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C323/44 , C07C2601/08 , C07C2602/08 , C07C2603/74 , C07D213/40 , C07D213/75 , C07D233/54 , C07D249/14 , C07D295/088 , C07D295/215 , C07D307/52 , C07D319/08 , C07D333/20 , C07D333/36
摘要： The present invention relates to 2-adamantylurea derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
摘要翻译： 本发明涉及作为11-β-羟基类固醇脱氢酶1型（11β-HSD1）的选择性抑制剂的式（I）的2-金刚烷基脲衍生物以及这些化合物用于治疗和预防代谢综合征，糖尿病， 胰岛素抵抗，肥胖症，血脂障碍，青光眼，骨质疏松症，认知障碍，焦虑症，抑郁症，免疫障碍，高血压和其他疾病和病症。
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16.发明授权PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES 有权吡啶并呋喃酮衍生物胰岛素分泌促进剂，获得它们的方法及其用于治疗糖尿病的方法
公开(公告)号：EP2247292B1
公开(公告)日：2017-04-12
申请号：EP09717128.4
申请日：2009-02-27
申请人： Merck Patent GmbH
IPC分类号： A61K31/4985 , C07D471/04
CPC分类号： C07D471/04
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17.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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18.发明授权PYRAZINONE DERIVATIVES AS INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES 有权PYRAZINONDERIVATE ALS INSULINAUSSCHEIDUNGSSTIMULATOREN，用于治疗糖尿病的生产工艺和用途
公开(公告)号：EP2250156B1
公开(公告)日：2015-05-06
申请号：EP09718204.2
申请日：2009-01-15
申请人： Merck Patent GmbH
IPC分类号： C07D241/18 , A61K31/4965 , A61P3/10
CPC分类号： C07D241/08 , C07D241/18
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19.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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20.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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