Meiji Seika Kaisha, Ltd.

Kazutaka Ueda

Kou Kumura

Eijirou Umemura

Yoshinari Wakiyama

Satomi Masaki

Takashi Watanabe

Yasuo Sato

Keiichi Ajito

Mikio Yamamoto

Chizuko Kaji

Hiroshi Kondo

Chika Kikuchi

Yoko Hirai

An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; Rrepresents N-optionally substituted Calkyl-N-optionally substituted Calkylamino-Calkyl; Rrepresents a hydrogen atom or optionally substituted Calkyl; Rrepresents optionally substituted Calkyl or Ccycloalkyl-Calkyl; 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, 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. 

Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient

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. 

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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Kitakami, Japan

Kazutaka Ueda