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1. 发明申请

WO2009135581A3 COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS 审中-公开
标题翻译：用于抑制NHE介导的抗体治疗与流体保持或盐过载和胃肠疾病相关的疾病的化合物和方法
公开(公告)号：WO2009135581A3
公开(公告)日：2010-08-19
申请号：PCT/EP2009002607
申请日：2009-04-08
申请人： MERCK PATENT GMBH , LERICHE CAROLINE , CARNIATO DENIS , ROCHE DIDIER , CHARON CHRISTINE , DOARE LILIANE
发明人： LERICHE CAROLINE , CARNIATO DENIS , ROCHE DIDIER , CHARON CHRISTINE , DOARE LILIANE
IPC分类号： A61P3/06 , A61P1/18 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/46 , A61P9/10 , A61P9/12 , A61P13/00 , A61P17/06 , A61P19/10 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/06
CPC分类号： A61K31/4545 , C07D417/04 , C07D417/14
摘要： The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-ß-HSD-1) 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：本发明涉及式（I）的NIP噻唑衍生物作为1型（11-β-HSD-1）酶11-β-羟基类固醇脱氢酶的选择性抑制剂，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，脂质障碍，青光眼，骨质疏松症，认知障碍，焦虑症，抑郁症，免疫疾病，高血压等疾病和病症。

2. 发明申请

WO1998027078A1 NEW 4-(1-PIPERAZINYL)BENZOIC ACID DERIVATIVES, PROCESS FOR PREPARING THEM AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：新的4-（1-哌嗪基）苯甲酸衍生物，其制备方法及其治疗应用
公开(公告)号：WO1998027078A1
公开(公告)日：1998-06-25
申请号：PCT/EP1997007046
申请日：1997-12-15
申请人： MERCK PATENT GMBH , MOINET, Gérard , BOTTON, Gérard , DOARE, Liliane , KERGOAT, Micheline , MESSANGEAU, Didier
发明人： MERCK PATENT GMBH
IPC分类号： C07D295/15
CPC分类号： C07D295/15 , C07D215/08 , C07D307/52
摘要： The present invention relates to the compounds of formula (I) in which Ar, R1, R2, R3, R4, R5 and R6 have the meanings given in Claim 1. These compounds are useful in the treatment of diabetes.
摘要翻译：本发明涉及其中Ar，R1，R2，R3，R4，R5和R6具有权利要求1中给出的含义的式（I）化合物。这些化合物可用于治疗糖尿病。

3. 发明申请

WO2009135581A2 NOVEL NIP THIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 审中-公开
标题翻译：作为11-β-羟基脱氢酶脱氢酶抑制剂的新型NIP噻唑衍生物
公开(公告)号：WO2009135581A2
公开(公告)日：2009-11-12
申请号：PCT/EP2009002607
申请日：2009-04-08
申请人： MERCK PATENT GMBH , LERICHE CAROLINE , CARNIATO DENIS , ROCHE DIDIER , CHARON CHRISTINE , DOARE LILIANE
发明人： LERICHE CAROLINE , CARNIATO DENIS , ROCHE DIDIER , CHARON CHRISTINE , DOARE LILIANE
IPC分类号： A61P3/06 , A61P1/18 , A61P3/04 , A61P3/08 , A61P3/10 , A61P9/12
CPC分类号： A61K31/4545 , C07D417/04 , C07D417/14
摘要： The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-ß-HSD-1) 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：本发明涉及式（I）的NIP噻唑衍生物作为1型（11-β-HSD-1）酶11-β-羟基类固醇脱氢酶的选择性抑制剂，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，脂质障碍，青光眼，骨质疏松症，认知障碍，焦虑症，抑郁症，免疫疾病，高血压等疾病和病症。

4. 发明申请

WO2008074384A1 2-ADAMANTYL-BUTYRAMIDE DERIVATIVES AS SELECTIVE 11βETA-HSD1 INHIBITORS 审中-公开
标题翻译： 2-ADAMANTYL-BUTYRAMIDE DERIVATIVES AS SELECTIVE11βETA-HSD1 INHIBITORS
公开(公告)号：WO2008074384A1
公开(公告)日：2008-06-26
申请号：PCT/EP2007/010124
申请日：2007-11-22
申请人： MERCK PATENT GMBH , ROCHE, Didier , CARNIATO, Denis , DOARE, Liliane , CHARON, Christine , LERICH, Caroline
发明人： ROCHE, Didier , CARNIATO, Denis , DOARE, Liliane , CHARON, Christine , LERICH, Caroline
IPC分类号： A61K31/41 , A61K31/16 , A61K31/4402 , A61K31/426 , A61K31/4453 , A61K31/4245 , A61K31/194 , A61K31/19 , C07C233/06 , C07C233/08 , C07C233/13 , C07C233/15 , C07C233/23 , C07C233/26 , C07C235/22
CPC分类号： C07D413/04 , C07C233/06 , C07C233/08 , C07C233/13 , C07C233/15 , C07C233/23 , C07C233/26 , C07C235/14 , C07C235/22 , C07D207/27 , C07D213/40 , C07D213/75 , C07D271/06 , C07D277/46 , C07D295/18 , C07D295/185
摘要： The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) 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：本发明涉及式I的2-金刚烷基 - 丁酰胺衍生物作为11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的选择性抑制剂以及这些化合物用于治疗和预防代谢综合征的用途，糖尿病，胰岛素抵抗，肥胖症，脂质障碍，青光眼，骨质疏松症，认知障碍，焦虑症，抑郁症，免疫疾病，高血压等疾病和病症。

5. 发明申请

WO1997047612A1 NOVEL THIAZOLIDONE-2 DERIVATIVES, 4-DIKETONE SUBSTITUTED, METHOD FOR OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新的噻唑烷二酮衍生物，取代的4-取代酮，用于获得它们的方法和含有它们的药物组合物
公开(公告)号：WO1997047612A1
公开(公告)日：1997-12-18
申请号：PCT/EP1997002851
申请日：1997-06-02
申请人： MERCK PATENT GMBH , MOINET, Gérard , BOTTON, Gérard , PRUGNARD, Etienne , DOARE, Liliane , KERGOAT, Micheline , MESANGEAU, Didier
发明人： MERCK PATENT GMBH
IPC分类号： C07D277/34
CPC分类号： C07D277/34
摘要： The invention relates to the field of chemistry and more particularly to that of therapeutic chemistry. The invention more precisely features novel 5-phenoxyalkyl 2,4-thiazolidinediketones of general formula (I): in which A represents one linear or branched alkylene group comprising 2 to 16 carbon atoms D represents one monocyclic, bycyclic or tricyclic, homocarbonaceous or heterocarbonaceous aromatic structure capable of enclosing one or several heteroatoms X represents the aromatic structure substituent and is as defined in claim 1 n is one integer ranging from 1 to 3 with the restriction that if A represents one butyl radical, (a) does not represent the 4-chlorophenyl group. The invention also disclosed tautomer, enantiomer, diastereoisomer and epimer forms of general formula (I) compounds, in free or salified form. The invention also discloses methods for obtaining general formula (I) compounds, their use as antidiabetic agents, and in the insulin resistance metabolic syndrome, as well as in the pharmaceutical compositions that contain general formula (I) compounds.
摘要翻译：本发明涉及化学领域，更具体地涉及治疗化学领域。本发明更精确地具有通式（I）的新型5-苯氧基烷基2,4-噻唑烷二酮：其中A代表一个包含2至16个碳原子的直链或支链亚烷基，D代表一个单环，多环或三环，同碳杂环或杂多碳芳族能够封闭一个或几个杂原子的结构X表示芳族结构取代基，如权利要求1中所定义，n为1至3的整数，限制如果A表示一个丁基，（a）不代表4- 氯苯基。本发明还公开了游离或盐化形式的通式（I）化合物的互变异构体，对映体，非对映异构体和差向异构体形式。本发明还公开了获得通式（I）化合物，其作为抗糖尿病剂的用途，以及在胰岛素抵抗代谢综合征中以及含有通式（I）化合物的药物组合物中的方法。

6. 发明申请

WO2009135581A9 NIP THIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 审中-公开
公开(公告)号：WO2009135581A9
公开(公告)日：2009-11-12
申请号：PCT/EP2009/002607
申请日：2009-04-08
申请人： MERCK PATENT GMBH , LERICHE, Caroline , CARNIATO, Denis , ROCHE, Didier , CHARON, Christine , DOARE, Liliane
发明人： LERICHE, Caroline , CARNIATO, Denis , ROCHE, Didier , CHARON, Christine , DOARE, Liliane
IPC分类号： A61P3/06 , A61P3/04 , A61P1/18 , A61P3/10 , A61P9/12 , A61P3/08 , A61P5/46 , A61P9/10 , A61P13/00 , A61P17/06 , A61P19/10 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/06
摘要： The present invention relates to NIP thiazole derivatives of formula (I) 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 prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

7. 发明申请

WO2008052638A1 DIAZEPANE-ACETAMIDE DERIVATIVES AS SELECTIVE 11β-HSD1 INHIBITORS 审中-公开
标题翻译：作为选择性11β-HSD1抑制剂的DIAZEPANE-ACATAMIDE DERIVATIVES
公开(公告)号：WO2008052638A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/008664
申请日：2007-10-05
申请人： MERK PATENT GMBH , CARNIATO, Denis , LERICHE, Caroline , ROCHE, Didier , CHARON, Christine , DOARE, Liliane
发明人： CARNIATO, Denis , LERICHE, Caroline , ROCHE, Didier , CHARON, Christine , DOARE, Liliane
IPC分类号： C07D243/08 , A61K31/551 , A61P3/00
CPC分类号： C07D243/08
摘要： The present invention relates to diazepane-acetamide derivatives of formula I 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 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：本发明涉及式I的二氮杂环庚烷 - 乙酰胺衍生物作为酶1-β-羟基类固醇脱氢酶1型（11β-HSD-1）的选择性抑制剂，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，脂质障碍，青光眼，骨质疏松症，认知障碍，焦虑症，抑郁症，免疫疾病，高血压等疾病和病症。

8. 发明申请

WO0030624A3 USE OF BENZOYLGUANIDINES FOR THE TREATMENT OF NON-INSULIN-DEPENDENT DIABETES MELLITUS 审中-公开
标题翻译：苯甲酰胍对治疗非胰岛素依赖性糖尿病的作用
公开(公告)号：WO0030624A3
公开(公告)日：2000-10-05
申请号：PCT/EP9908795
申请日：1999-11-16
申请人： MERCK PATENT GMBH , GERICKE ROLF , BAUMGARTH MANFRED , MINCK KLAUS , MESANGEAU DIDIER , DOARE LILIANE , KERGOAT MICHELINE
发明人： GERICKE ROLF , BAUMGARTH MANFRED , MINCK KLAUS , MESANGEAU DIDIER , DOARE LILIANE , KERGOAT MICHELINE
IPC分类号： C07D207/327 , A61K31/155 , A61K31/166 , A61K31/40 , A61K31/402 , A61P3/10 , A61P5/48 , C07C279/22
CPC分类号： A61K31/402 , A61K31/155
摘要： (57) Abstract The invention relates to the use of benzoylguanidines of formula (I) wherein R is A; R is Het, CnFmH2n+1-mOp, R , OR , OH, benzyl, CN, Hal, SOq-R , Ph, O-Ph, O-Het, NH-Het, NH2, NHA, NA2 or NH-Ph; R is SO2A'; R is a straight-chain or branched alkyl radical having 1 to 8 C atoms or cycloalkyl having 3 to 8 C atoms which can be unsubstituted or mono-, di- or trisubstituted by A; R is A or Ph; A, A' in each case independently of one another are alkyl having 1 to 6 C atoms, and/or their physiologically acceptable salts and solvates for the production of a medicament for the treatment of non-insulin-dependent diabetes mellitus.
摘要翻译：（57）摘要本发明涉及式（I）的苯甲酰基胍：其中R 1是A; R 2是Het，CnFmH 2n + 1-mOp，R 4，OR 4，OH，苄基，CN，Hal，SOq-R 5，Ph，O-Ph，O-Het，NH- Het，NH 2，NHA，NA 2或NH-Ph; R 3是SO 2 A'; R 4是具有1至8个C原子的直链或支链烷基或具有3至8个C原子的环烷基，其可以是未取代的或者被A单取代，二取代或三取代; R 5是A或Ph; A，A'在每种情况下彼此独立地为具有1至6个C原子的烷基，和/或其生理学上可接受的盐和溶剂合物用于制备用于治疗非胰岛素依赖性糖尿病的药物。

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