申请人:Lilly Industries Limited
公开号:US05021441A1
公开(公告)日:1991-06-04
There are disclosed pharmaceutical compounds of the formula: ##STR1## in which R.sup.1 is halo-substituted alkyl; X is alkenylene; and R.sup.1 --X-- contains 6 to 34 carbon atoms; R.sup.2 is C.sub.1-5 alkyl substituted by (i) optionally protected carboxyl, nitrile, optionally protected tetrazolyl or --CONR'R", in which R' and R" are each hydrogen or C.sub.1-4 alkyl, ##STR2## (ii) in which R' and R" are each hydrogen or C.sub.1-4 alkyl, or ##STR3## (iii) in which R', R" and R'" are each hydrogen or C.sub.1-4 alkyl, or R.sup.2 is a group of the formula ##STR4## in which R' is hydrogen or an optionally protected amino acid residue, and R" is --OH or an optionally protected amino acid residue; and R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, optionally protected carboxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro or --CONR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl; and salts thereof.
公开了化学式为:##STR1##的药物化合物,其中R.sup.1是卤代烷基;X是烯烃基;R.sup.1 --X-- 包含6到34个碳原子;R.sup.2是C.sub.1-5烷基,被(i) 可选择保护的羧基,腈基,可选择保护的四唑基或--CONR'R"取代,其中R'和R"各自是氢或C.sub.1-4烷基,##STR2##(ii)其中R'和R"各自是氢或C.sub.1-4烷基,或##STR3##(iii)其中R',R"和R'"各自是氢或C.sub.1-4烷基,或R.sup.2是公式##STR4##的基团,其中R'是氢或可选择保护的氨基酸残基,R"是--OH或可选择保护的氨基酸残基;R.sup.3,R.sup.4和R.sup.5各自是氢,可选择保护的羧基,C.sub.1-4烷基,C.sub.1-4烷氧基,羟基,可选择保护的四唑基,卤素,三氟甲基,腈基,硝基或--CONR'R",其中R'和R"各自是氢或C.sub.1-4烷基;以及其盐。