LINCOMYCIN DERIVATIVES AND ANTIBACTERIAL AGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
申请人:Meiji Seika Kaisha Ltd.
公开号:EP2151447A1
公开(公告)日:2010-02-10
An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 represents N-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
本发明的目的是提供式(1)化合物或其药理学上可接受的盐或溶液,其中 A 代表芳基;R1 代表 N-任选取代的 C1-6 烷基-N-任选取代的 C1-6 烷基氨基-C1-6 烷基;R2 代表氢原子或任选取代的 C1-6 烷基;R3 代表任选取代的 C1-6 烷基或 C3-6 环烷基-C1-4 烷基;m 为 1 至 3;n 为 0;p 为 0 至 2。这些化合物是新型的林可霉素衍生物,在治疗传染性疾病方面对耐药性肺炎链球菌有很强的活性,而耐药性肺炎链球菌近来已造成了一些问题。此外,这些化合物还可用作抗菌剂,用于预防或治疗细菌性传染病。