Esters of substituted-hydroxyacetyl piperazine phenyl...

Details Esters of substituted-hydroxyacetyl piperazine phenyl... Esters of substituted-hydroxyacetyl piperazine phenyl...

C - Chemistry, Metallurgy

07

D

C07D 413/10 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/675 (2006.01) C07D 263/20 (2006.01) C07D 263/24 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2174107

A compound of structural Formula (1) or pharmaceutically acceptable salts thereof wherein: R is -C(O)-R1, -PO3= or -P(O)(OH)2; R1 is C1-6 alkyl, -N(R4)2, C1-6 alkyl-N(R4)2, -phenyl-N(R4)2, -phenyl- NHC(O)CH2NH2,-C2H4-morpholinyl, pyridinyl, C1-6 alkyl-OH, C1-6 alkyl-OCH3, C1-6 alkyl C(O)CH3, -O-C1-6 alkyl-OCH3, C0-3 alkyl-piperazinyl (optionally substituted with C1-3 alkyl), imidazolyl, C1-6 alkyl-COOH, -C(CH2OH)2CH3; R2 and R3 are independently selected from hydrogen or F except at least one of R2 or R3 is F; R4 are independently selected from hydrogen or C1-6 alkyl. The compounds are water soluble and are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci, enterococci and streptococci, as well as anaerobic organisms such as bacteriodes and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis.

L'invention concerne un composé ayant la formule (I), ainsi que des sels de celui-ci acceptables sur le plan pharmaceutique. Dans cette formule, R est un groupe -C(O)-R<1>, -PO3= ou -P(O)(OH)2; R<1> est un groupe C1-6 alkyle, -N(R<4>)2, C1-6 alkyle-N(R<4>)2, -phényle-N(R<4>)2, -phényle-NHC(O)CH2NH2, -C2H4-morpholinyle, pyridinyle, C1-6 alkyle-OH, C1-6 alkyle-OCH3, C1-6 alkyle C(O)CH3, -O-C1-6 alkyle-OCH3, C0-3 alkyle-pipérazinyle (le cas échéant substitué par un C1-3 alkyle), imidazolyle, C1-6 alkyle-COOH, -C(CH2OH)2CH3; R<2> et R<3> sont choisis d'une manière indépendante parmi l'hydrogène ou F, sauf qu'au moins un des éléments R<2> et R<3> est un F; R<4> est choisi d'une manière indépendante parmi l'hydrogène ou un C1-6 alkyle. Ces composés sont hydrosolubles et ils sont utiles comme agents antimicrobiens, efficaces contre un certain nombre d'agents pathogènes de l'homme et des animaux, en particulier les staphylocoques les entérocoques et les streptocoques à résistance multiple aux médicaments, ainsi que des organismes anaérobies tels que les espèces bactéroïdes et clostridium ainsi que des micro-organismes acidorésistants tels que Mycobacterium tuberculosis.

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