Substituted pyrimidobenzimidazole derivatives

Details Substituted pyrimidobenzimidazole derivatives Substituted pyrimidobenzimidazole derivatives

C - Chemistry, Metallurgy

07

D

167/220, 260/242

C07D 487/04 (2006.01) A61K 31/505 (2006.01) C07C 275/40 (2006.01) C07D 235/16 (2006.01) C07D 295/155 (2006.01) C07D 403/04 (2006.01) C07D 403/10 (2006.01)

Patent

CA 2028530

RAN 4410/221 Abstract The present invention is concerned with novel substituted pyrimidobenzimidazole derivatives of the general formula Image wherein R1 signifies hydrogen, halogen or amino, R2 signifies halogen, R signifies a lower alkyl-substituted 4-pyridyl group or a group R3R4N- in which R3 and R4 each signify hydrogen or lower alkyl or together signify a group of the formula -(CH2)n-X-(CH2)m- or -(CH2)p- which is unsubstituted or substituted by lower alkyl, amino, lower aminoalkyl, mono- or di(lower alkyl)- amino-lower alkyl, oxo or the group -COOR2 or -CONR'R", n and m each signify the number 1, 2 or 3, with the proviso that n + m is a maximum of 5. p signifies the number 4, 5 or 6, X signifies an oxygen or sulphur atom or the group -NR"'-, Ra signifies hydrogen, lower alkyl, lower alkenyl, phenyl or phenyl which is mono-, di- or trisubstituted by halogen, lower alkyl or hydroxy, R' and R" each signify hydrogen or lower alkyl, R"' signifies hydrogen, hydroxy, lower alkyl or lower aminoalkanoyl, R5 signifies hydrogen, halogen, lower alkoxy or amino, R6 signifies lower alkyl, lower cycloalkyl, lower haloalkyl, phenyl or phenyl which is mono-, di- or trisubstituted by halogen, lower alkyl, hydroxy or lower alkoxy, R7 signifies hydrogen, lower alkyl or carboxy, R8 signifies hydrogen, hydroxy, lower alkoxy, amino, lower alkylamino or di-lower alkylamino and Y signifies an oxygen or sulphur atom, and pharmaceutically acceptable salts thereof. The products have an inhibitory action on the DNA-gyrase activity in bacteria. They can accordingly be used for the prevention or control of bacterial infections.

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