申请人:Eli Lilly and Company
公开号:US05605924A1
公开(公告)日:1997-02-25
The present invention relates to compounds of the formula ##STR1## where X is a bond or --CH2--; R.sup.2 is pyrrolidino; R is OH, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR2## R.sup.1 is hydrogen, OH, fluoro, chloro, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR3## each R.sup.3 is independently C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl where the substituent is fluoro, chloro, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; each n is independently 3, 4 or 5; and pharmaceutically acceptable salts and solvates thereof; provided that at least one of R and R.sup.1 is ##STR4## The invention also relates to methods of use of the compounds of formula I and pharmaceutical compositions which comprise compounds of formula I.
本发明涉及式为##STR1##的化合物,其中X为键或--CH2--; R.sup.2为吡咯烷基; R为OH,--OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3或##STR2## R.sup.1为氢,OH,氟,氯,--OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3或##STR3##每个R.sup.3独立地为C.sub.1 -C.sub.6烷基,C.sub.3 -C.sub.6环烷基,未取代或取代苯基,其中取代基为氟,氯,C.sub.1 -C.sub.3烷基或C.sub.1 -C.sub.3烷氧基;每个n独立地为3,4或5;以及其药学上可接受的盐和溶剂合物; 前提是R和R.sup.1中至少有一个为##STR4## 本发明还涉及使用式I化合物的方法和包含式I化合物的药物组合物。