申请人:ORTHO PHARMACEUTICAL CORPORATION
公开号:EP0225044A1
公开(公告)日:1987-06-10
A composition adapted to be topically applied to a mammal for treating mammalian peptic ulcer disease containing an effective amount of a prostaglandin analog in a pharmacuetical carrier suitable for administration to the skin of the mammal to be treated, said prostaglandin analog having a structure that corresponds to the formula:
wherein: R has the formula -CH₂- Y - (CH₂)₂-Z;
-Y- is selected from the group consisting of -(CH₂)-₃ , cis -HC=CHCH₂-, and cis,cis -HC=C=CH-;
-Z is selected from the group consisting of -CH₂ OH, and -CO₂X, wherein X is hydrogen, a pharmacologically acceptable cation or C₁-C₆ alkyl;
R¹ is n-butyl or phenoxy;
R² is selected from the group consisting of hydrogen, methyl and hydroxyl;
R³ is selected from the group consisting of hydrogen, methyl and hydroxyl, with the proviso that R² and R³ cannot both be hydrogen or both be hydroxyl; and
R⁴ and R⁵ are the same or different and are selected from the group consisting of hydrogen and hydroxyl, but are not both hydroxyl.
一种可局部应用于哺乳动物以治疗哺乳动物消化性溃疡病的组合物,该组合物含有有效量的前列腺素类似物,该前列腺素类似物包含在适于施用到待治疗的哺乳动物皮肤的药用载体中,所述前列腺素类似物具有符合式的结构:
其中R 的式子为 -CH₂- Y - (CH₂)₂-Z;
-Y-选自由-(CH₂)-₃、顺式-HC=CHCH₂-和顺式,顺式-HC=C=CH-组成的组;
-Z选自由-CH₂ OH和-CO₂X组成的组,其中X是氢、药理学上可接受的阳离子或C₁-C₆烷基;
R¹ 是正丁基或苯氧基;
R² 选自由氢、甲基和羟基组成的组;
R³ 选自氢、甲基和羟基组成的组,但 R² 和 R³ 不能都是氢或都是羟基;以及
R⁴ 和 R⁵ 相同或不同,选自由氢和羟基组成的组,但不能都是羟基。