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    • 9. 发明申请
    • CONDENSED PYRAZOLE DERIVATIVES AS PPAR AGONISTS II
    • 浓缩的吡唑衍生物作为PPAR激动剂II
    • WO2007036727A1
    • 2007-04-05
    • PCT/GB2006/003608
    • 2006-09-28
    • INPHARMATICA LIMITEDAYSCOUGH, AndrewTHOMPSON, StephenTAYLOR, SusanneKHAN, Nawaz, Mohammed
    • AYSCOUGH, AndrewTHOMPSON, StephenTAYLOR, SusanneKHAN, Nawaz, Mohammed
    • C07D231/56C07D471/04A61K31/416A61K31/437A61P3/00
    • C07D471/04C07D231/56
    • The invention discloses compounds of formula (I) wherein: R is a carboxylic acid or a derivative thereof; R 1 and R 2 are independently H or alkyl, or together R 1 and R 2 form an alkylene group; L 1 is a single bond, NH, NCH 3 , O, S, CH 2 or CH, wherein when L 1 is CH the dashed line indicates a double bond and R 2 is absent, otherwise the dashed line is a single bond; R 8 and R 9 are independently H, halo, alkyl or alkoxy; L 2 is O or S; L 3 is CH 2 or CH 2 CH 2 ; R 10 and R 11 are independently H, halo, CF 3 , OCF 3 , alkyl or alkoxy; Y 1 is CH or N; Y 2 is CH or N; and R 12 and R 13 are independently H, halo, CF 3 , OCF 3 , alkyl or alkoxy; or a pharmaceutically acceptable derivative thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype δ (PPARδ). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.
    • 本发明公开了式(I)的化合物,其中:R是羧酸或其衍生物; R 1和R 2独立地是H或烷基,或者一起R 1和R 2形成亚烷基 ; L 1是单键,NH,NCH 3,O,S,CH 2或CH,其中当L 1, / SUP>是CH,虚线表示双键并且R 2不存在,否则虚线是单键; R 8和R 9独立地是H,卤素,烷基或烷氧基; L 2是O或S; CH 3是CH 2或CH 2 CH 2; R 10和R 11独立地为H,卤素,CF 3,OCF 3,烷基或烷氧基; Y 1是CH或N; Y 2是CH或N; R 12和R 12独立地为H,卤素,CF 3,OCF 3,烷基或烷氧基; 或其药学上可接受的衍生物,其可用于治疗由过氧化物酶体增殖物激活受体(PPAR)亚型d(PPARd)介导的病症。 因此,本发明的化合物可用于治疗代谢综合征,肥胖症,II型糖尿病,血脂异常,伤口愈合,炎症,神经变性疾病和多发性硬化。