Meiji Seika Kaisha, Ltd.

Chizuko Kaji

Takashi Watanabe

Keiichi Ajito

Mikio Yamamoto

Kou Kumura

Eijirou Umemura

Satomi Masaki

Yoshinari Wakiyama

Kazutaka Ueda

Yasuo Sato

This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, Rrepresents a halide, nitro, substituted Calkyl, optionally substituted amino, Calkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, Rrepresents a hydrogen atom or Calkyl, Rrepresents Calkyl, all of R, R, and Rrepresent a hydrogen atom, Rrepresents Calkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases. 

Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient

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 Rrepresents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while Rrepresents aryl or a five- or six-membered monocyclic heterocyclic group; Rrepresents a hydrogen atom or Calkyl; Rrepresents Calkyl or Ccycloalkyl-Calkyl; R, R, and Rrepresent a hydrogen atom; Rrepresents Calkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases. 

Lincosamide derivatives and antimicrobial agents comprising the same as active ingredient

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Kawasaki, Japan

Chizuko Kaji