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    INDENONCARBOXYLIC ACIDS DERIVATIVES AND THEIR USE FOR THE TREATMENT OF AND PREVENTING DIABETES AND DYSLIPIDAEMIA
    2.
    发明申请
    INDENONCARBOXYLIC ACIDS DERIVATIVES AND THEIR USE FOR THE TREATMENT OF AND PREVENTING DIABETES AND DYSLIPIDAEMIA 审中-公开
    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

    Applicant: 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

    Inventor： ADJE, Nathalie ,  BRUNET, Michel ,  ROCHE, Didier ,  ZEILLER, Jean-Jacques ,  YVON, Stéphane ,  GUYARD-DANGREMONT, Valérie ,  CONTARD, Francis ,  GUERRIER, Daniel ,  FERRAND, Gérard ,  BONHOMME, Yves

    IPC: C07C309/65

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 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。

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