申请人:Taiho Pharmaceutical Company Limited
公开号:US04668514A1
公开(公告)日:1987-05-26
This invention provides a penicillin derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, C.sub.1-6 hydroxyalkyl, C.sub.3-9 acyloxyalkyl, C.sub.8-13 benzyloxyalkyl, C.sub.2-7 alkoxyalkyl, C.sub.2-7 alkoxycarbonyl, C.sub.3-8 alkenyloxycarbonyl, C.sub.3-8 alkynyloxycarbonyl, phenyl, amino, cyano, formyl, trifluoromethyl, C.sub.2-6 acyl, carbamoyl, C.sub.2-7 alkylcarbamoyl, benzyloxycarbonylamino, C.sub.2-7 alkoxycarbonylamino; and R.sub.3 is hydrogen, a group for forming a pharmaceutically acceptable salt, or a penicillin carboxyl protecting group, with the proviso that both of R.sub.1 and R.sub.2 are not hydrogen or C.sub.2-7 alkoxycarbonyl at the same time and that when one of R.sub.1 and R.sub.2 is hydrogen, the other is not C.sub.2-7 alkoxycarbonyl, or a pharmaceutically acceptable acid addition salt, process for preparing the derivative, and a pharmaceutical composition containing the derivative.
这项发明提供了一种青霉素衍生物,其化学式为##STR1##其中R.sub.1和R.sub.2相同或不同,代表氢、C.sub.1-6烷基、C.sub.1-6羟基烷基、C.sub.3-9酰氧基烷基、C.sub.8-13苄氧基烷基、C.sub.2-7烷氧基烷基、C.sub.2-7烷氧羰基、C.sub.3-8烯氧羰基、C.sub.3-8炔氧羰基、苯基、氨基、氰基、甲酰基、三氟甲基、C.sub.2-6酰基、氨基甲酰基、C.sub.2-7烷基氨基甲酰基、苄氧羰基氨基、C.sub.2-7烷氧羰基氨基;以及R.sub.3为氢、用于形成药学上可接受的盐的基团,或者青霉素羧基保护基团,但条件是R.sub.1和R.sub.2中没有两者同时是氢或C.sub.2-7烷氧羰基,且当R.sub.1和R.sub.2中的一个是氢时,另一个不是C.sub.2-7烷氧羰基,或者药学上可接受的酸盐,制备该衍生物的方法,以及含有该衍生物的药物组合物。