[EN] (3-{3-'(2,4-BIS-TRIFLUORMETHYL-BENZYL)-(5-ETHYL-PYRIMIDIN-2-YL)-AMINO!-PROPOXY}-PHENYL)-ACETIC ACID AND RELATED COMPOUNDS AS MODULATORS OF PPARS AND METHODS OF TREATING METABOLIC DISORDERS<br/>[FR] ACIDE (3-{3- (2,4-BIS-TRIFLUORMETHYL-BENZYL)-(5-ETHYL-PYRIMIDIN-2-YL)-AMINO!-PROPOXY}-PHENYL)-ACETIQUE ET COMPOSES ASSOCIES EN TANT QUE MODULATEURS DE PPAR, ET PROCEDES POUR TRAITER DES TROUBLES DU METABOLISME
申请人:KALYPSYS INC
公开号:WO2004093879A1
公开(公告)日:2004-11-04
Disclosed are compounds of formula I as modulators of peroxisome proliferator activated receptors (PPARs) for the treatment of metabolic diseases such as obesity: wherein Ar1 is selected from the group consisting of a monocyclic heteroarornatic ring structure and a bicyclic heteroaromatic ring structure; Ar2 is selected from the group consisting of a monocyclic, a bicyclic, and a tricyclic carbocyclic aryl ring structure R1 is selected from the group consisting of alkyl, optionally substituted a five-membered or six-membered heteroarylring or a six-membered aryl ring, optionally substituted R2 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituied cyano; nitro; an amino; an amido; perhaloalkyl; and halogen; R3 is selected from the group consisting of hydrogen; alkyl, optionally substituted and B is a five-membered or six-membered heteroaryl ring, or -(CH2)j-C(O)OR4, wherein j is 0 or I 1 when Ar2 is a bicyclic or tricyclic carbocyclic ring structure and j is 1 when Ar2 is a monocyclic carbocyclic ring structure; and R4 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituted. The obtional substituents are as defined in claim 1.
公开了如下式化合物作为过氧化物酶增殖物激活受体(PPARs)的调节剂,用于治疗肥胖等代谢性疾病:其中Ar1选自由单环杂芳环结构和双环杂芳环结构组成的群体;Ar2选自由单环、双环和三环碳环芳基环结构组成的群体;R1选自烷基、可选择地取代的五元环或六元环杂芳基环或六元芳基环,可选择地取代;R2选自氢;烷基,可选择地取代的五元环或六元环杂芳基环或六元芳基环,可选择地取代氰基;硝基;氨基;酰胺基;全氟烷基;和卤素;R3选自氢;烷基,可选择地取代;B是五元环或六元环杂芳基环,或-(CH2)j-C(O)OR4,其中j为0或1,当Ar2为双环或三环碳环环结构时,j为1,当Ar2为单环碳环环结构时;R4选自氢;烷基,可选择地取代的五元环或六元环杂芳基环或六元芳基环,可选择地取代。可选择的取代基的定义如权利要求1所述。