Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient
申请人:Meiji Seika Kaisha, Ltd.
公开号:US07879808B2
公开(公告)日:2011-02-01
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 C1-6 alkyl 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.
本发明的目标是提供符合公式(1)或其药理学上可接受的盐或溶剂的化合物,其中A代表芳基;R1代表N-可选取代的C1-6烷基-N-可选取代的C1-6烷基氨基-C1-6烷基;R2代表氢原子或可选取代的C1-6烷基;R3代表可选取代的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,对最近在感染疾病治疗中出现问题的耐药性肺炎链球菌具有强效活性。此外,这些化合物可用作抗微生物剂,有助于预防或治疗细菌感染性疾病。