申请人:AMERICAN CYANAMID COMPANY
公开号:EP0072872A1
公开(公告)日:1983-03-02
There is provided novel 1-hydroxy-1-hydroxymethy) prostaglandins and method of use for vasodepression, smooth muscle stimulation and as antilipolytic agents. The novel compounds have the structure:
wherein n is the interger 3-5 inclusive; X is CH2CH2 or CH CH (cis); R1 is hydrogen or hydroxy, R' and R are the same or different and are hydrogen, C, to C. alkyl, C, to C6 alkanoyl or optionally substituted benzoyl, wherein said substituents on said benzoyl moiety are selected from the group C, to C4 alkoxy, halo and trifluoromethyl; and R2 is selected from the group consisting of
wherein R4 is hydrogen or methyl; R5 is selected from the group consisting of C4-C7 alkyl; Rs is selected from the group consisting of C3-C6: R11 is selected from the group consisting of C3-C7 alkyl; the racemic mixtures thereof and the individual optically active enantiomers thereof; and the phar- maceutially acceptable non-toxic salts thereof.
提供了新型 1-羟基-1-羟甲基)前列腺素及其用于血管扩张、刺激平滑肌和作为抗脂肪分解剂的方法。这些新型化合物具有如下结构
其中 n 为 3-5 之间(含);X 为 CH2CH2 或 CH CH(顺式);R1 为氢或羟基,R'和 R 相同或不同,且为氢、C, to C. 烷基、C, to C6 烷酰基或任选取代的苯甲酰基,其中所述苯甲酰基上的所述取代基选自 C, to C4 烷氧基、卤代和三氟甲基组;以及 R2 选自以下组成的组
其中 R4 为氢或甲基;R5 选自 C4-C7 烷基组成的组;Rs 选自 C3-C6 组成的组;R11 选自 C3-C7 烷基组成的组;其外消旋混合物及其单个光学活性对映体;以及其酞酸酯可接受的无毒盐。