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1. 发明申请

WO2004063148A1 INDENONCARBOXYLIC ACIDS DERIVATIVES AND THEIR USE FOR THE TREATMENT OF AND PREVENTING DIABETES AND DYSLIPIDAEMIA 审中-公开
标题翻译：吲哚羧酸衍生物及其用于治疗和预防糖尿病和糖尿病的用途
公开(公告)号：WO2004063148A1
公开(公告)日：2004-07-29
申请号：PCT/EP2003/014296
申请日：2003-12-16
申请人： MERCK PATENT GMBH , ADJE, Nathalie , BRUNET, Michel , ROCHE, Didier , ZEILLER, Jean-Jacques , YVON, Stéphane , GUYARD-DANGREMONT, Valérie , CONTARD, Francis , GUERRIER, Daniel , FERRAND, Gérard , BONHOMME, Yves
发明人： ADJE, Nathalie , BRUNET, Michel , ROCHE, Didier , ZEILLER, Jean-Jacques , YVON, Stéphane , GUYARD-DANGREMONT, Valérie , CONTARD, Francis , GUERRIER, Daniel , FERRAND, Gérard , BONHOMME, Yves
IPC分类号： C07C309/65
CPC分类号： C07C323/56 , C07C45/46 , C07C45/673 , C07C45/68 , C07C49/747 , C07C49/755 , C07C59/72 , C07C59/90 , C07C65/40 , C07C67/30 , C07C67/31 , C07C69/712 , C07C69/736 , C07C69/76 , C07C205/45 , C07C211/60 , C07C229/18 , C07C233/33 , C07C251/44 , C07C255/40 , C07C309/65 , C07C317/44 , C07C323/22 , C07C323/52 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C47/575
摘要： The present invention relates to a compound of the formula ((I): in which: n is an integer chosen from 1, 2 and 3; Y represents O; N-OR 9 , in which R 9 represents H or a saturated hydrocarbon-based aliphatic group; CR 10 R 11 , in which R 10 and R 11 , which may be identical or different, represent H or a saturated hydrocarbon-based aliphatic group; R 1 and R 2 , which may be identical or different, represent H or a saturated aliphatic hydrocarbon-based chain; or alternatively R 1 and R 2 together form an optionally substituted saturated aliphatic hydrocarbon-based chain; the radicals R 3 and R 4 , which may be identical or different, take any of the is meanings given above for R 1 and R 2 , or alternatively R 1 and the group R 4 borne by the carbon alpha to CR 1 R 2 represent nothing and a double bond links the CR 1 R 2 carbon to the alpha CR 3 R 4 carbon; or alternatively one of the radicals R 1 and R 2 forms with one of the radicals R 3 and R 4 an optionally substituted saturated or unsaturated aliphatic hydrocarbon-based chain; one of the radicals R 5 and R 6 represents W, and the other represents Z which is chosen from a saturated or unsaturated aliphatic hydrocarbon-based radical; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic or heterocyclic radical; a radical -alk-Cy, in which alk represents an alkylene chain and Cy represents an optionally substituted saturated, unsaturated and/or aromatic heterocyclic or carbocyclic radical; W represents -XL-CO 2 R 7 ; -X-L-Tet, in which X and L are as defined below and Tet represents optionally substituted tetrazole; in which L represents a saturated or unsaturated aliphatic hydrocarbon-based chain, which is optionally substituted and/or optionally interrupted by optionally substituted arylene; X represents O; NR 8 , in which R 8 represents H; a saturated aliphatic hydrocarbon-based group; a group -CO-R' or -SO 2 -R', in which R' takes any of the meanings given below for R 7 with the exception of H; or R 8 represents an optionally substituted aromatic carbocyclic group; or X represent S(O) m , in which m is chosen from 0, 1 and 2; R 7 represents H; a saturated or unsaturated aliphatic hydrocarbon-based group; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic group; an optionally substituted, saturated, unsaturated and/or aromatic heterocyclic group; and the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, and also mixtures thereof in all proportions, which can be used in the treatment of dyslipidaemia, atherosclerosis and diabetes.
摘要翻译：本发明涉及式（（I）的化合物：其中：n是选自1,2和3的整数; Y代表O; N-OR 9，其中R 9代表H或饱和烃基脂族基团; CR 10 R 11，其中R 10和R 11可以相同或不同，表示H或饱和烃基脂族基团; R 1 和R 2可以相同或不同，表示H或饱和脂族烃基链;或者R 1和R 2一起形成任选取代的饱和脂族烃基链;基团 R 3和R 4可以相同或不同，取代上述R 1和R 2，或者R 1和R 4基团的任何含义由CR 1 R 2的碳原子没有表示，并且CR 1与碳原子数3〜4的碳键连接成双键，或者另一个基团R 其中一个基团R 3和R 4与任选的取代基形成1和R 2 饱和或不饱和脂族烃基链; 基团R 5和R 6中的一个表示W，另一个表示选自饱和或不饱和脂族烃基的基团的Z; 任选取代的饱和，不饱和和/或芳族碳环或杂环基; 一个自由基-alk-Cy，其中alk代表亚烷基链，Cy代表任选取代的饱和，不饱和和/或芳族杂环或碳环基团; W表示-XL-CO 2 R 7; X-L-Tet，其中X和L如下所定义，Tet表示任选取代的四唑; 其中L表示饱和或不饱和的脂族烃基链，其任选被任选取代的和/或任选地被任选取代的亚芳基中断; X表示O; NR 8，其中R 8表示H; 饱和脂族烃基; 基团-CO-R'或-SO 2 -R'，其中R'取代以下对R 7取代的任何含义，除了H; 或R 8表示任选取代的芳族碳环基团; 或X表示S（O）m，其中m选自0,1和2; R 7表示H; 饱和或不饱和脂族烃基; 任选取代的，饱和的，不饱和的和/或芳族的碳环基团; 任选取代的饱和，不饱和和/或芳族杂环基; 和其药学上可接受的衍生物，盐，溶剂合物和立体异构体，以及其各种比例的混合物，其可用于治疗血脂异常，动脉粥样硬化和糖尿病。

2. 发明申请

WO2005014521A1 BUTENOIC ACID DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM, AND USE FOR THE TREATMENT OF DYSLIPIDAEMIA, ATHEROSCLEROSIS AND DIABETES 审中-公开
标题翻译：氨基酸衍生物，其制备方法，包含它们的药物组合物和用于治疗糖尿病，糖皮质激素和糖尿病的用途
公开(公告)号：WO2005014521A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/007776
申请日：2004-07-14
申请人： MERK PATENT GMBH , ZEILLER, Jean-Jacques , DUMAS, Hervé , GUYARD-DANGREMONT, Valérie , BERARD, Isabelle , CONTARD, Francis , GUERRIER, Daniel , FERRAND, Gérard , BONHOMME, Yves
发明人： ZEILLER, Jean-Jacques , DUMAS, Hervé , GUYARD-DANGREMONT, Valérie , BERARD, Isabelle , CONTARD, Francis , GUERRIER, Daniel , FERRAND, Gérard , BONHOMME, Yves
IPC分类号： C07C69/734
CPC分类号： C07C59/68 , C07C59/64 , C07C69/732 , C07C69/734 , C07C69/736
摘要： The present invention relates to butenoic acid derivatives of the formula (I) in which R, R 1 , R 2 and R 3 are as defined in the description, and also to processes for the preparation thereof, to pharmaceutical compositions comprising them and to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes.
摘要翻译：本发明涉及式（I）的丁烯酸衍生物，其中R 1，R 2，R 2和R 3如说明书中所定义，以及其制备方法，包含它们的组合物及其用于治疗血脂异常，动脉粥样硬化和糖尿病的用途。

3. 发明申请

WO2003011819A1 BUTYRIC ACID DERIVATIVES 审中-公开
标题翻译：丁酸衍生物
公开(公告)号：WO2003011819A1
公开(公告)日：2003-02-13
申请号：PCT/EP2002/007383
申请日：2002-07-03
申请人： MERCK PATENT GMBH , ROCHE, Didier , ZEILLER, Jean-Jacques , CONTARD, Francis , GUYARD-DANGREMONT, Valérie , GUERRIER, Daniel , DUPONT, Hervé , BERTHELON, Jean-Jacques
发明人： ROCHE, Didier , ZEILLER, Jean-Jacques , CONTARD, Francis , GUYARD-DANGREMONT, Valérie , GUERRIER, Daniel , DUPONT, Hervé , BERTHELON, Jean-Jacques
IPC分类号： C07C323/52
CPC分类号： C07D213/70 , C07C317/46 , C07C323/52 , C07C391/00 , C07D215/36 , C07D249/12 , C07D277/74 , C07D311/30
摘要： The present invention relates to a compound of the formula I: (Formula I) in which: A, B, R 1 , Z, n and R 2 are as defined in Claim 1. These compounds are useful in the treatment of dyslipidaemia, atherosclerosis and diabetes.
摘要翻译：本发明涉及式I化合物：（式I）其中：A，B，R 1，Z，n和R 2如权利要求1中所定义。这些化合物可用于治疗血脂异常，动脉粥样硬化和糖尿病。

4. 发明申请

WO2004031116A1 NOVEL SUBSTITUTED ARYLHEXADIENOIC ACIDS AND ESTERS THEREOF WHICH CAN BE USED FOR THE TREATMENT AND PREVENTION OF DIABETES, DYSLIPIDAEMIA AND ATHEROSCLEROSIS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND PROCESSES FOR THE PREPARATION OF THEM 审中-公开
标题翻译：可用于治疗和预防糖尿病，糖尿病和甲状腺功能亢进症的新方法，其中包括其制备它们的药物组合物及其制备方法
公开(公告)号：WO2004031116A1
公开(公告)日：2004-04-15
申请号：PCT/EP2003/008887
申请日：2003-08-11
申请人： MERCK PATENT GMBH , BRUNET, Michel , ZEILLER, Jean-Jacques , FERRAND, Gérard , BONHOMME, Yves
发明人： BRUNET, Michel , ZEILLER, Jean-Jacques , FERRAND, Gérard , BONHOMME, Yves
IPC分类号： C07C59/90
CPC分类号： C07C69/738 , C07C67/343
摘要： The invention relates to compounds of the formula (I), and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其制备方法以及包含它们的药物组合物，其特别用于治疗和预防血脂障碍，动脉粥样硬化和糖尿病。

5. 发明申请

WO2006074798A1 HYDROXYPHENOL DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM, AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译：羟基苯酚衍生物，其制备方法，包含它们的药物组合物及其治疗用途
公开(公告)号：WO2006074798A1
公开(公告)日：2006-07-20
申请号：PCT/EP2005/013858
申请日：2005-12-22
申请人： MERCK PATENT GMBH , ADJE, Nathalie , VIDAL, Catherine , ZEILLER, Jean-Jacques , YVON, Stéphane
发明人： ADJE, Nathalie , VIDAL, Catherine , ZEILLER, Jean-Jacques , YVON, Stéphane
IPC分类号： C07C59/90 , C07D263/34 , C07D265/36 , C07C323/62
CPC分类号： C07D295/205 , C07C59/90 , C07C323/22 , C07C2602/08 , C07D263/32
摘要： Compounds of the formula (I): in which A, R 1 , R 2 , X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
摘要翻译：式（I）化合物：其中A，R 1，R 2，X，Y和Z在说明书中定义，其制备方法化合物，其用于治疗血脂异常，动脉粥样硬化和糖尿病的用途，以及包含它们的药物组合物。

6. 发明申请

WO2005053676A1 USE OF PENTADIENOIC ACID DERIVATIVES FOR THE TREATMENT OF HYPERURICEMIA 审中-公开
标题翻译：用于治疗高血压的戊二酸衍生物的应用
公开(公告)号：WO2005053676A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012381
申请日：2004-11-02
申请人： MERCK PATENT GMBH , BOIZEL, Robert , FOUQUERAY, Pascale , GUERRIER, Daniel , ZEILLER, Jean-Jacques , BRUTZKUS, Bertrand
发明人： BOIZEL, Robert , FOUQUERAY, Pascale , GUERRIER, Daniel , ZEILLER, Jean-Jacques , BRUTZKUS, Bertrand
IPC分类号： A61K31/35
CPC分类号： C07D311/12 , A61K31/35 , A61K31/353 , A61K31/382 , A61K31/7048 , C07D313/08 , C07D313/10 , C07D335/06 , C07D337/08
摘要： The use of a pentadienoic acid derivative of formula (I) for the preparation of a medicament for the prevention or treatment of hyperuricemia and/or one or several associated disorders or diseases, and/or for reducing the serum uric acid level of a subject. Medical compositions for these prevention and/or treatment, comprising such a pentadienoic acid derivative.
摘要翻译：式（I）的戊二烯酸衍生物在制备用于预防或治疗高尿酸血症和/或一种或多种相关疾病或疾病的药物中的用途和/或用于降低受试者的血清尿酸水平。用于这些预防和/或治疗的医药组合物，包含这种戊二烯酸衍生物。

7. 发明公开

EP1098893A1 CYCLIC COMPOUNDS USEFUL IN THE TREATMENT OF DYSLIPIDEMIA, ATHEROSCLEROSIS AND DIABETES, PHARMACEUTICAL COMPOSITIONS AND PREPARATION PROCESS 有权
标题翻译：骑行连接，适用于的血脂异常，动脉粥样硬化和糖尿病的治疗中，药物组合物含及其制备方法
公开(公告)号：EP1098893A1
公开(公告)日：2001-05-16
申请号：EP99934643.0
申请日：1999-07-09
申请人： MERCK PATENT GmbH
发明人： BERTHELON, Jean-Jacques , GUERRIER, Daniel , RASP , Eric , ZEILLER, Jean-Jacques
IPC分类号： C07D319/06 , C07D319/08 , A61K31/335
CPC分类号： C07D319/08 , C07D319/06 , C07D405/06 , C07D407/04 , C07D409/04
摘要： The present invention relates to cyclic compounds which can be used in the treatment of dyslipidaemia, atherosclerosis and diabetes, to processes for preparing these compounds. The compounds of the invention correspond to formula (I) wherein the radicals X, Y, R, R1, R2, R3, R4, R5, R6, R7 have meanings as given in claim 1.

8. 发明公开

EP1836150A1 HYDROXYPHENOL DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM, AND THERAPEUTIC USES THEREOF 有权
标题翻译：羟基苯酚衍生物，HERSTELLUNGSVERFAHRENDAFÜR，药剂师ZUSAMMENSETZUNGEN DAMIT UNDERAPEUTISCHE VERWENDUNG
公开(公告)号：EP1836150A1
公开(公告)日：2007-09-26
申请号：EP05823908.8
申请日：2005-12-22
申请人： Merck Patent GmbH
发明人： ADJE, Nathalie , VIDAL, Catherine , ZEILLER, Jean-Jacques , YVON, Stéphane
IPC分类号： C07C59/90 , C07D263/34 , C07D265/36 , C07C323/62
CPC分类号： C07D295/205 , C07C59/90 , C07C323/22 , C07C2602/08 , C07D263/32
摘要： Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
摘要翻译：式（I）化合物：其中A，R 1，R 2，X，Y和Z在说明书中定义，制备这些化合物的方法，其用于治疗血脂异常，动脉粥样硬化和糖尿病的用途，以及包含它们的药物组合物。

10. 发明授权

EP1546083B1 NOVEL SUBSTITUTED ARYLHEXADIENOIC ACIDS AND ESTERS THEREOF WHICH CAN BE USED FOR THE TREATMENT AND PREVENTION OF DIABETES, DYSLIPIDAEMIA AND ATHEROSCLEROSIS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND PROCESSES FOR THE PREPARATION OF THEM 有权
标题翻译：新的取代ARYLHEXADIENSÄUREN及其酯类，导致在治疗和糖尿病的预防和动脉粥样硬化血脂异常合适的药物组合物，含有AND METHOD FOR THEIR
公开(公告)号：EP1546083B1
公开(公告)日：2010-08-11
申请号：EP03798876.3
申请日：2003-08-11
申请人： Merck Patent GmbH
发明人： BRUNET, Michel , ZEILLER, Jean-Jacques , FERRAND, Gérard , BONHOMME, Yves
IPC分类号： C07C59/90 , C07C59/64 , A61K31/201 , A61K31/22 , A61P9/10 , A61P3/10 , A61P3/04 , C07C69/738 , C07C51/373
CPC分类号： C07C69/738 , C07C67/343
摘要： The invention relates to compounds of the formula (I), and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.

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