申请人:Yoshitomi Pharmaceutical Industries, Ltd.
公开号:US04889857A1
公开(公告)日:1989-12-26
A quinolonecarboxylic acid compound of the formula: ##STR1## wherein R.sup.1 is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a phenyl group substituted by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R.sup.2 is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxycarbonyl group, R.sup.3 is a hydrogen atom, an alkyl group or an aralkyl group, or R.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a heterocyclic ring, R.sup.4 is a hydrogen atom or an alkyl group, R.sup.5 is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is interger of 1 to 3, and a salt thereof, and pharmaceutical use thereof. The compounds exhibit antibacterial activites and are useful for the treatment of various infectious diseases.
一种喹诺酸类化合物,其化学式为:##STR1## 其中,R1为烷基、环烷基、卤代烷基、烯基、单烷基或双烷基氨基、苯基或苯基上取代基中的1-3个取自卤素原子、烷基、烷氧基、羟基、硝基或氨基的基团,R2为氢原子、烷基、环烷基、酰基或烷氧羰基,R3为氢原子、烷基或芳基烷基,或R2和R3与相邻的氮原子一起形成杂环环,R4为氢原子或烷基,R5为氢原子、烷基、芳基烷基或易于在体内水解的酯基,X为氢原子、卤素原子或烷基,n为1-3的整数,以及其盐,以及其在制药上的用途。这些化合物表现出抗菌活性,适用于治疗各种传染病。