GYRASE INHIBITORS AND APPLICATION THEREOF Russian patent published in 2009 - IPC C07D403/14 C07D401/14 C07D405/14 C07D403/04 C07D413/14 C07D417/14 C07D471/04 C07D487/04 C07D491/04 A61K31/4184 A61P31/04 

Abstract RU 2350612 C2

FIELD: chemistry; pharmacology.

SUBSTANCE: new compounds of formula (I) and its pharmaceutically acceptable salts. Offered compounds possess properties of bacterial gyrase and Topo-IV activity inhibitor. In general formula (I) , W is chosen from CH or CF; X represents CH; Z represents O or NH; R1 represents phenyl or 5-6-merous heteroaryl ring containing 1-3 nitrogen atoms where R1 is substituted with 0-3 groups independently chosen from -(T)y-Ar, R', oxo, C(O)R', OR', N(R')2, SR', CN or C(O)N(R')2; R2 is chosen from C1-3alkyl and C3-7-cycloalkyl; and ring A represents 5-6-merous heteroaryl ring containing 1-3 heteroatoms, independently chosen of nitrogen, oxygen or sulphur provided the specified ring has hydrogen bond acceptor in position adjacent to that of joining to B ring where ring A is substituted with 0-3 groups independently chosen from R', oxo, CO2R', OR', N(R')2, halogen, CN, C(O)N(R')2, NR'C(O)R', or NR'SO2R', and where two substitutes in adjacent positions of ring A, together can form 6-merous saturated heterocyclic or heteroaryl ring containing 1-2 nitrogen atoms.

EFFECT: pharmaceutical compositions with properties of bacterial gyrase and Topo-IV activity inhibitor containing disclosed compound as active component, method of gyrase and/or Toro IV-activity inhibition, method of bacteria number reduction.

25 cl, 3 tbl, 4 dwg, 29 ex

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RU 2 350 612 C2

Authors

Charifson Pol S.

Dejnindzher Dehvid D.

Grijo Ann-Lor

Liao Jusheng

Ronkin Stiven M.

Stamos Din

Perola Ehmmanuehl'

Van Tjan'Shehn

Letiran Arno

Dramm Dzhozef

Dates

2009-03-27Published

2004-01-29Filed