Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use in medicaments
申请人:Aventis Pharma Deutschland GmbH
公开号:US06596742B1
公开(公告)日:2003-07-22
Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1
in any optically isomeric form, and their physiologically acceptable salts, where R1 is C1-C6-alkyl, C3-C9-cycloalkyl, both of which may be unsubstituted or substituted, and R2 and R3 independently of one another are hydrogen, C6-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloxymethyl, O-benzyl, O—C6-C10-aryl, O—C3-C8-cycloalkyl, O—C1-C6-alkyl, SO2—NH—C1-C6-alkyl, SO2—NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2—NH—C3-C8-cycloalkyl, SO2—N(C1-C6-alkyl)2 or COX, where X is O—C1-C6-alkyl, NH—C1-C6-alkyl, NH—C3-C8-cycloalkyl or N(C1-C6-alkyl)2, with the proviso that the substitutents R2 and R3 may in some instances be unsubstituted or substituted and are not both simultaneously hydrogen. A process for their preparation, and their inhibitory effect on the hormone-sensitive lipase, HSL.
式为1的3-苯基-5-烷氧基-1,3,4-噁二唑-2-酮及其生理上可接受的盐,其中R1为C1-C6-烷基、C3-C9环烷基,两者可能未被取代或被取代,而R2和R3彼此独立地为氢、C6-C10芳基、C3-C8环烷基、C6-C10芳氧甲基、O-苄基、O—C6-C10芳基、O—C3-C8环烷基、O—C1-C6烷基、SO2—NH—C1-C6烷基、SO2—NH-(2,2,6,6-四甲基哌啶-4-基)、SO2—NH—C3-C8环烷基、SO2—N(C1-C6烷基)2或COX,其中X为O—C1-C6烷基、NH—C1-C6烷基、NH—C3-C8环烷基或N(C1-C6烷基)2,但R2和R3的取代基在某些情况下可能未被取代或被取代,并且二者不会同时为氢。它们的制备方法及其对激素敏感性脂解酶HSL的抑制作用。