C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/12 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01) C07D 413/14 (2006.01)
Patent
CA 2236677
This invention provides a novel oxazolidinone derivative represented by formula (I) or pharmaceutical acceptable salts thereof: wherein R1 is (a), (b), or (c); R2 is (a) hydrogen, or (b) C1-4 alkyl; R3 is (a) C1-4 alkyl, (b) C3-6 cycloalkyl, (c) C1-4 alkoxy, (d) C1-4 alkylamino, or (e) C1-4 dialkylamino; and X is (a) hydrogen, or (b) fluoro. This invention provides novel oxazolidinone derivatives useful as preventatives and therapeutics for infectious diseases. The compounds of this invention have excellent antimicrobial action against various human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast Mycobacterium tuberculosis and Mycobacterium avium.
La présente invention concerne un nouveau dérivé d'oxazolidinone représenté par la formule I, ou des sels de ce dérivé acceptables en pharmacie. Dans cette formule, R1 est (a), (b) ou (c); R2 est: (a) hydrogène ou (b) alkyle C1-4; R3 est: (a) alkyle C1-4, (b) cycloalkyle C3-6, (c) alcoxy C1-4, (d) alkylamino C1-4, ou (e) dialkylamino C1-4, et X est: (a) hydrogène ou (b) fluoro. Cette invention se rapporte à de nouveaux dérivés d'oxazolidinone utiles dans la prévention et la thérapie de maladies infectieuses. Les composés de la présente invention ont d'excellents effets antimicrobiens contre divers agents pathogènes humains et vétérinaires, dont les staphylocoques et les streptocoques multirésistants ainsi que les organismes anaérobies tels que Bacteroides et clostridia species et les Mycobacterium tuberculosis et Mycobacterium avium acidorésistants.
Brickner Steven Joseph
Tucker John A.
Ulanowicz Debra A.
Macrae & Co.
Pharmacia & Upjohn Company
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