Prostane derivatives, processes for their preparation and their pharmaceutical compositions
申请人:IMPERIAL CHEMICAL INDUSTRIES PLC
公开号:EP0010360A1
公开(公告)日:1980-04-30
The disclosure relates to 9β-aryloxy prostane derivatives, for example 16-(3-chlorophenoxy) -11α, 15a-dihydroxy-16 -methyl-9β-phenoxy -18, 19, 20-trinor-5-cis, 13-trans-prostadienoic acid, which possess high activity as abortifacients, cervical softeners, inducers of parturition or inhibitors of gastric acid production in mammals. These properties are typical of prostaglandin analogues of the E series, but chemically the new 9β-aryloxy prostane derivatives are prostaglandin F series analogues and are therefore more stable than the E series analogues previously used for the above purposes. The new derivatives are manufactured by known analogy processes, and are formulated in conventional manner.
本公开涉及 9β-芳氧基前列腺烷衍生物,例如 16-(3-氯苯氧基) -11α,15a-二羟基-16-甲基-9β-苯氧基-18,19,20-三去甲-5-顺式,13-反式-脯氨二烯酸,这些衍生物作为堕胎药、子宫颈软化剂、分娩诱导剂或哺乳动物胃酸分泌抑制剂具有很高的活性。这些特性是 E 系列前列腺素类似物的典型特征,但从化学角度看,新的 9β-aryloxy 前列腺素衍生物是前列腺素 F 系列类似物,因此比以前用于上述目的的 E 系列类似物更稳定。新的衍生物采用已知的类比工艺制造,并以常规方式配制。