Oxazolidinone antimicrobials containing substituted diazine moieties

US5700799A · kind A · utility

Assignee

• Pharmacia & Upjohn Company LLC · US

Inventors

• Douglas K. Hutchinson · Antioch, US
• Michael R. Barbachyn · Kalamazoo, US
• Steven J. Brickner · Ledyard, US
• Ronald B. Gammill · Portage, US
• Mahesh Vithalbhai Patel · Aurangabad, IN

Key dates

• Filing date: Mar 4, 1996
• Grant date: Dec 23, 1997
• Expiry date: Mar 4, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 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, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial 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 …