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    Thia-and oxazoles and their use as ppars activators
    2.
    发明授权
    Thia-and oxazoles and their use as ppars activators 失效
    Thia和恶唑及其作为ppars激活剂的用途

    公开(公告)号：US07196107B2

    公开(公告)日：2007-03-27

    申请号：US10451307

    申请日：2001-12-18

    申请人： Paul John Beswick ,  Vipulkumar Patel ,  Michael Lawrence Sierra

    发明人： Paul John Beswick ,  Vipulkumar Patel ,  Michael Lawrence Sierra

    IPC分类号： A61K31/426 ,  A61K31/421 ,  C07D277/20 ,  C07D263/30

    CPC分类号： C07D277/24

    摘要： A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5. Use of a compound of formula (I) for the manufacture of a medicament for the prevention or treatment of a hPPAR mediated disease or condition, such as dyslipidemia, syndrome X, heart failure, hypercholesteremia, cardiovascular disease, type II diabetes mellitus, type 1 diabetes, insulin resistance hyperlipidemia, obesity, anorexia bulimia, inflammation and anorexia nervosa

    摘要翻译： 式（I）化合物或其药学上可接受的盐和溶剂化物。 R 1和R 2独立地为H或C 1-3烷基，m为0-3; X 1是NH，NCH 3，O，S; R 3，R 4和R 5独立地为H，CH 3，CF 3， OCH 3，OCH 3，烯丙基或卤素; 其中n为1或2;（3）其中n为1或2; R 10和R 11独立地代表H，氟或C 1-16烷基; R 26和R 27独立地是H，C 1-3烷基或R 26和R 26， 27与它们所键合的碳原子一起形成3-5元环烯基环。 R 6和R 7独立地表示H，氟或C 1-16烷基; R 9是C 1-6烷基或CF 3 N; Y和Z之一是N，另一个是S或O; 每个R 8独立地表示CF 3，OCH 3，CH 3或卤素; y是O，1,2,3,4,5。式（I）化合物在制备用于预防或治疗hPPAR介导的疾病或病症如血脂异常，综合征X，心脏的药物中的用途 失败，高胆固醇血症，心血管疾病，II型糖尿病，1型糖尿病，胰岛素抵抗性高脂血症，肥胖，厌食症，炎症和神经性厌食

    Substituted oxazoles and thiazoles as hPPAR alpha agonists
    6.
    发明授权
    Substituted oxazoles and thiazoles as hPPAR alpha agonists 失效
    取代的恶唑和噻唑作为hPPARα激动剂

    公开(公告)号：US07091225B2

    公开(公告)日：2006-08-15

    申请号：US10451298

    申请日：2001-12-18

    申请人： Michael Lawrence Sierra

    发明人： Michael Lawrence Sierra

    IPC分类号： A61K31/426 ,  A61K31/421 ,  C07D277/20 ,  C07D263/30

    CPC分类号： C07D277/24 ,  C07D277/26

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein X is O or S X1 is O or S; X is S or O; R1 and R2 are independently H, methyl, or halogen; R4 and R5 are independently H or C1-3 alkyl or R4 and R5 may, together with the carbon atom to which they are bonded, form a 3–5 membered cycloalkyl ring; R6 and R7 are independently H, C1-3 alkyl, or allyl; each R3 is independently halogen, C1-6 straight or branched alkyl, or CF3; and y is 0, 1, 2, 3, 4 or 5 act as hPPAR alpha agonists.

    摘要翻译： 式（I）化合物及其药学上可接受的盐，溶剂化物和可水解的酯，其中X为O或S X1为O或S; X是S或O; R1和R2独立地为H，甲基或卤素; R 4和R 5独立地为H或C 1-3烷基或R 4和R 5可以与它们所键合的碳原子一起形成3-5元环烷基环; R6和R7独立地为H，C1-3烷基或烯丙基; 每个R 3独立地为卤素，C 1-6直链或支链烷基或CF 3; y为0,1,2,3,4或5作为hPPARα激动剂。

    Substituted oxazoles and thiazoles derivatives as HPPAr alpha activators
    9.
    发明授权
    Substituted oxazoles and thiazoles derivatives as HPPAr alpha activators 失效
    取代的恶唑和噻唑衍生物作为HPPArα激活剂

    公开(公告)号：US06518290B1

    公开(公告)日：2003-02-11

    申请号：US10148765

    申请日：2002-05-31

    申请人： Michael Lawrence Sierra

    发明人： Michael Lawrence Sierra

    IPC分类号： A61K31421

    CPC分类号： C07D263/34 ,  C07D277/56 ,  C07D401/04

    摘要： A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein; X1 represents O or S; R1 and R2 independently represent H, halogen, —CH3 and —OCH3; n represents 1 or 2; X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R3 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, NO2, NH2, CF3, OCF3, OC1-6 straight or branched alkyl, C1-6 straight or branched alkyl, alkenyl or alkynyl with the provision that when R3 is pyridyl, the N is unsubstituted; R4 represents CF3 or CH3

    摘要翻译： 式（I）化合物及其药学上可接受的盐，溶剂合物和可水解的酯，其中X1表示O或S; R1和R2独立地表示H，卤素，-CH3和-OCH3; n表示1或2; X2表示NH，NCH3 或O; Y和Z之一是N，另一个是O或S; R 3表示苯基或吡啶基（其中N在2或3位），并且任选地被一个或多个卤素，NO 2，NH 2，CF 3 OCF 3，OC 1-6直链或支链烷基，C 1-6直链或支链烷基，烯基或炔基，条件是当R3为吡啶基时，N为未取代的; R4为CF3或CH3