Substituted oxazine and thiazine oxazolidinone antimicrobials
Patent 5688792 Issued on November 18, 1997. Estimated Expiration Date: 
March 5, 2016. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
March 5, 2016. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent ReferencesN-Aryl oxazolidinones, oxazolidinethiones, pyrrolidinones, pyrrolidines and thiazolidinones Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents Patent #: 4921869 InventorsAssigneeApplicationNo. 617877 filed on 03/05/1996US Classes:514/235.5, Ring nitrogen in the additional hetero ring514/236.8, Ring chalcogen in the additional hetero ring (e.g., oxazole, etc.)514/376, Chalcogen bonded directly to ring carbon of the oxazole ring544/137The five-membered hetero ring has at least oxygen and nitrogen as ring hetero atomsExaminersPrimary: Shah, Mukund J.Assistant: Bucknum, Michael Attorney, Agent or FirmForeign Patent References
International ClassA61K 031/535AbstractA compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO2, SNR10 or S(O)NR10 ;R is (a) hydrogen,(b) C1 -C8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C1 -C8 alkoxy, C1 -C8 acyloxy or --O--CH2 --Ph,(c) C3 -C6 cycloalkyl,(d) amino,(e) C1 -C8 alkylamino,(f) C1 -C8 dialkylamino or(g) C1 -C8 alkoxy;R1 is H, except when X is O then R1 can be H, CH3, CN, CO2 H, CO2 R or (CH2)m R11 (m is 1 or 2);R2 is independently H, F or Cl;R3 is H except when X is O and R1 is CH3 then R3 can be H or CH3 ;R10 is independently H, C1 -C4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C1 -C8 alkoxy, amino, C1 -C8 alkylamino, or C1 -C8 dialkylamino) or p-toluenesulfonyl;R11 is hydrogen, OH, OR, OCOR, NH2, NHCOR or N(R10)2 ; and n is 0, 1 or 2. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Other References
|
| ||||||||||||||
