申请人:SUMITOMO CHEMICAL COMPANY, LIMITED
公开号:EP0108627A2
公开(公告)日:1984-05-16
A compound of the general formula:
wherein A represents an unsubstituted thiazolyl or substituted thiazolyl residue having at least one substituent which is halogen, alkyl, amino or acylamido; R' represents hydrogen or alkyl, carboxymethyl or alkoxycarbonylmethyl, R2 represents hydrogen or methyl, hydroxymethyl, acyloxymethyl or alkylthiomethyl, or represents thiadiazolylthiomethyl optionally alkyl substituted, or represents tetrazolylthiomethyl residue optionally substituted by alkyl, alkylaminoalkyl or carboxymethyl; and R3 represents unsubstituted allyl or substituted allyl having at least one substituent which is halogen, alkyl, cycloalkyl, haloalkyl, acyloxy alkyl, alkoxycarbonyl, phenyl or substituted phenyl, or salts thereof have excellent chemical stability and are very satisfactorily absorbed to exhibit an excellent therapeutic effect on the patients having bacterial infectious diseases when administered by a method other than injection, such as oral administration. Various methods are disclosed for the preparation and formulation of the new compounds.
通式如下的化合物
其中 A 代表未取代的
噻唑基或取代的
噻唑基残基,其上至少有一个取代基为卤素、烷基、
氨基或酰
氨基;R'代表
氢或烷基、羧
甲基或烷
氧基羰基
甲基,R2 代表
氢或
甲基、
羟甲基、酰
氧基
甲基或烷基
硫甲基,或代表任选被烷基取代的
噻二唑硫甲基,或代表任选被烷基、烷基
氨基烷基或羧
甲基取代的
四唑硫甲基残基;和 R3 代表未取代的
烯丙基或至少有一个取代基为卤素、烷基、
环烷基、卤代烷基、酰
氧基烷基、烷
氧基羰基、
苯基或取代
苯基的取代
烯丙基,或其盐具有极好的
化学稳定性,通过注射以外的方法(如口服给药)给药时,吸收非常令人满意,对细菌感染性疾病患者有极好的治疗效果。新化合物的制备和配制方法多种多样。