首页> 外国专利> PEROXISIME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST TRIAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE

PEROXISIME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST TRIAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE

机译:培罗昔明增效剂活化的受体α激动剂三唑衍生物和包含它们的药物成分及其用途

摘要

The present invention relates to compounds of formula (I) which act as agonists on peroxisome proliferator activated receptors and as such are useful in the treatment and prevention of diabetes mellitus, cardiovascular disease, obesity, inflammatory bowel disease, among others. The invention also relates to pharmaceutical compositions containing the compounds of formula (I). Substituents of formula (I) have a variety of meanings, such as (a) R 1 is hydrogen, optionally substituted, which is optionally alkyl, aryl (C 0-4) alkyl, heteroaryl (C0-4) alkyl, ( C3-6cycloalkyl) arylC0-2alkyl and phenyl; (b) W is O or S; (c) R2 is hydrogen or an optionally substituted group selected from alkyl, allyl, arylC0-4alkyl, heteroarylC0-4alkyl, and C3-6cycloalkyl; (d) X is an optionally substituted C 1 -C 5 alkylene linker, wherein one of the carbon atoms of the linker may be replaced by O, NH or S. (e) Y is C, O, S, NH or a single bond; and (f) is hydrogen, C (R 3) (R 4) A, A, optionally substituted, optionally (CH 2) n COOR 19, alkyl, allyl, aryl (C 0 -C 4) alkyl, thio (1-4); C 1-4 -alkyl, thioaryl, alkoxy-aryl, C 1-4 -alkoxy-C 1-4 -alkyl, amino-aryl and amino-C 1-4 -alkyl, wherein (i) ) n is 0, 1, 2 or 3; (ii) A is a functional group selected from carboxyl, (C 1 -C 3) alkyl, nitrile, carboxamide, substituted or unsubstituted sulfonamide, substituted or unsubstituted acylsulfonamide, and substituted or unsubstituted tetrazolyl; (iii) R 3 is hydrogen, saturated or unsaturated C 1 -C 5 alkyl, C 1 -C 5 alkoxy, and (iv) R 4 is hydrogen, halogen, substituted or unsubstituted alkyl, alkoxy, C 3 -C 6 cycloalkyl, aryl; - (C 0 -C 4 alkyl) and phenyl, or R 3 and R 4 together may form a C 3 -C 4 cycloalkyl group; SHE
机译:本发明涉及式(I)的化合物,其对过氧化物酶体增殖物激活的受体起激动剂的作用,因此可用于治疗和预防糖尿病,心血管疾病,肥胖症,炎性肠病等。本发明还涉及含有式(I)化合物的药物组合物。式(I)的取代基具有多种含义,例如(a)R 1是氢,任选地被取代,其任选地是烷基,芳基(C 0-4)烷基,杂芳基(C0-4)烷基,(C3- 6环烷基)芳基C0-2烷基和苯基; (b)W是O或S; (c)R2为氢或选自烷基,烯丙基,芳基C0-4烷基,杂芳基C0-4烷基和C3-6环烷基的任选取代的基团; (d)X是任选取代的C 1 -C 5亚烷基接头,其中该接头的碳原子之一可以被O,NH或S取代。(e)Y是C,O,S,NH或单个键; (f)是氢,C(R 3)(R 4)A,A,任选取代,任选(CH 2)n COOR 19,烷基,烯丙基,芳基(C 0 -C 4)烷基,硫代(1- 4); C 1-4-烷基,硫代芳基,烷氧基-芳基,C 1-4-烷氧基-C 1-4-烷基,氨基-芳基和氨基-C 1-4-烷基,其中(i))n为0,1 ,2或3; (ii)A是选自羧基,(C 1 -C 3)烷基,腈,羧酰胺,取代或未取代的磺酰胺,取代或未取代的酰基磺酰胺,以及取代或未取代的四唑基的官能团; (iii)R 3是氢,饱和或不饱和的C 1 -C 5烷基,C 1 -C 5烷氧基,和(iv)R 4是氢,卤素,取代或未取代的烷基,烷氧基,C 3 -C 6环烷基,芳基-(C 0 -C 4烷基)和苯基,或R 3和R 4一起可以形成C 3 -C 4环烷基;她

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