LINCOSAMIDE DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
申请人:Umemura Eijirou
公开号:US20100184746A1
公开(公告)日:2010-07-22
An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R
1
represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R
1
represents aryl or a five- or six-membered monocyclic heterocyclic group; R
2
represents a hydrogen atom or C
1-6
alkyl; R
3
represents C
1-6
alkyl or C
3-6
cycloalkyl-C
1-4
alkyl; R
4
, R
5
, and R
6
represent a hydrogen atom; R
7
represents C
1-6
alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant
Streptococcus pneumoniae
. 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式(I)的化合物或其药理学上可接受的盐或溶剂,其中A代表芳基,而R1代表五元或六元单环杂环基,或A代表四至六元单环杂环基,而R1代表芳基或五元或六元单环杂环基;R2代表氢原子或C1-6烷基;R3代表C1-6烷基或C3-6环烷基-C1-4烷基;R4、R5和R6代表氢原子;R7代表C1-6烷基;m为1至3。这些化合物是新型的林可霉素衍生物,对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,对预防或治疗细菌感染性疾病有用。