Oxazolidinone antimicrobials containing substituted diazine...

C - Chemistry – Metallurgy – 07 – D

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C07D 413/10 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07D 263/20 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2133079

A compound of structural formula (I) or pharmaceutically acceptable salts thereof wherein: Y is chosen from a-n as defined herein; wherein each occurrence of said C1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR1, CO2R1, CN, SR1, or R1 (where R1 is a hydrogen or C1-4 alkyl); X and Z are independently C1-6 alkyl, C3-12 cycloalkyl or hydrogen, or X and Z form a C0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C1-6 alkyl, F, Cl, Br, hydrogen or a C1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C1-12 alkyl, C3-12 cycloalkyl, C1-6 alkoxy, C1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and d is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimic-robial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobac- terium tuberculosis and Mycobaeterium avium.

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