首页> 外国专利> New Phenylthiazolyl/phenyloxazolyl derivatives are peroxisome proliferator-activated receptor agonist useful to treat e.g. diabetic, dyslipidemia, cardiovascular disease, hypertension, inflammatory diseases and cerebral ischaemia

New Phenylthiazolyl/phenyloxazolyl derivatives are peroxisome proliferator-activated receptor agonist useful to treat e.g. diabetic, dyslipidemia, cardiovascular disease, hypertension, inflammatory diseases and cerebral ischaemia

机译:新的苯基噻唑基/苯并恶唑基衍生物是过氧化物酶体增殖物激活的受体激动剂,可用于治疗例如环孢霉素。糖尿病,血脂异常,心血管疾病,高血压,炎性疾病和脑缺血

摘要

Phenylthiazolyl/phenyloxazolyl derivatives (I) and their stereoisomeres (diastereoisomers, enantiomers), racemic mixtures, geometrical isomers, tautomers, salts, hydrates, solvates, solid forms or their mixtures are new. Phenylthiazolyl/phenyloxazolyl derivatives of formula (I) and their stereoisomeres (diastereoisomers, enantiomers), racemic mixtures, geometrical isomers, tautomers, salts, hydrates, solvates, solid forms or their mixtures are new. X1halo, R1, -SR1 or -OR1; X2R2; X3halo, R3, -SR3 or -OR3; X4halo, R4, -SR4 or -OR4; X5R5, -SR5 or -OR5; X6R6, -SR6 or -OR6; X7R7, -SR7 or -OR7; X8S or O; R1, R3, R4, R6, R7 = H or alkyl; R2H or alkyl (optionally substituted by (hetero)cycloalkyl or (hetero)aryl); R5alkyl substituted by -COOR12, -CONR12R13, -SO3H or -SO2NR12R13, where substitutents are substituted by optionally substituted by (hetero)cycloalkyl or (hetero)aryl; A : CO, C=N-O-H, C=N-O-R11, -CR9R10 or R11; R9, R10H, alkyl or -OR11; R11H, aryl, heterocycloalkyl, heteroaryl or alkyl (optionally substituted by (hetero)cycloalkyl or (hetero)aryl); B12C alkyl (unsubstituted, saturated) or 2C alkene (unsubstituted); and R12, R13H or alkyl (unsubstituted). An independent claim is included for a pharmaceutical composition comprising (I), in a support, optionally in combination with therapeutic and/or cosmetic active ingredients and a compound. [Image] ACTIVITY : Analgesic; Antianginal; Antidiabetic; Antilipemic; Cardiovascular-Gen; Anorectic; Hypotensive; Antiinflammatory; Cerebroprotective; Vasotropic; Immunosuppressive; Cytostatic; Neuroprotective. MECHANISM OF ACTION : Peroxisome proliferator-activated receptor agonist.
机译:苯基噻唑基/苯基恶唑基衍生物(I)及其立体异构体(非对映异构体,对映异构体),外消旋混合物,几何异构体,互变异构体,盐,水合物,溶剂化物,固体形式或它们的混合物是新的。式(I)的苯基噻唑基/苯基恶唑基衍生物及其立体异构体(非对映异构体,对映异构体),外消旋混合物,几何异构体,互变异构体,盐,水合物,溶剂化物,固体形式或其混合物是新的。 X1halo,R1,-SR1或-OR1; X2R2; X3halo,R3,-SR3或-OR3; X4halo,R4,-SR4或-OR4; X5R5,-SR5或-OR5; X6R6,-SR6或-OR6; X7R7,-SR7或-OR7; X8S或O; R1,R3,R4,R6,R7 = H或烷基; R 2 H或烷基(任选地被(杂)环烷基或(杂)芳基取代);被-COOR12,-CONR12R13,-SO3H或-SO2NR12R13取代的R5烷基,其中取代基被任选地被(杂)环烷基或(杂)芳基取代的取代基; A:CO,C = N-O-H,C = N-O-R11,-CR9R10或R11; R9,R10H,烷基或-OR11; R11H,芳基,杂环烷基,杂芳基或烷基(任选地被(杂)环烷基或(杂)芳基取代); B12C烷基(未取代的,饱和的)或2C烯烃(未取代的); R12,R13H或烷基(未取代)。包括对药物组合物的独立权利要求,所述药物组合物包含在载体中的(I),任选地与治疗和/或美容活性成分和化合物组合。 [图片]活动:止痛药;抗心绞痛抗糖尿病抗血脂;心血管基因厌食的;降压;消炎(药;脑保护变压性免疫抑制细胞抑制具有神经保护作用。作用机理:过氧化物酶体增殖物激活的受体激动剂。

著录项

  • 公开/公告号FR2910893A1

    专利类型

  • 公开/公告日2008-07-04

    原文格式PDF

  • 申请/专利权人 GENFIT SOCIETE ANONYME;

    申请/专利号FR20060056065

  • 发明设计人 DELHOMEL JEAN FRANCOIS;

    申请日2006-12-29

  • 分类号C07D277/24;A61K31/426;A61P3;

  • 国家 FR

  • 入库时间 2022-08-21 19:47:04

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