发明名称 SUBSTITUTED OXAZINE AND THIAZINE OXAZOLIDINONE ANTIMICROBIALS.
摘要 A COMPOUND OF STRUCTURAL FORMULA I FORMULA I 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 OPTINALLY 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, CO2H. CO2R OR ( CH2 ) MR11 ( M IS 1 OR 2 );@R2 IS INDEPENTLY H, F OR C1;@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 ( ) - TOLUENESULFONYL;@R11 IS HYDROGEN, OH, OR, OCO, NH2, NHCOR OR N ( R 10 ) ; AND N IS 0, 1 OR 2. THE IXAZINE AND THIAZINE OXAZOLIDINONE DERIVATIVES ARE USEFUL ANTIMICROBIAL AGENTS, EFFECTIVE AGENTS A NUMBER OF HUMAN AND VETERINARY PATHOGENS, INCLUDING GRAMPOSITIVE AEROBIC BACTERIA SUCH AS MULTIPLY - RESISTANT STAPHYLOCOCCI, STREPTOCOCCI AND ENTEROCOCCI AS WELL AS ANAEROBIC ORGANISM SUCH AS BACTEROIDES SPP. AND CLOSTRIDIA SPP. SPECIES, AND ACID - PAST ORGANISMS SUCH AS MYCOBACTERIUM TUBAERCULLOSIS, MYCOBACTERIUM AVIUM AND MYCOBACTERIUM SPP..
申请公布号 MY115155(A) 申请公布日期 2003.04.30
申请号 MY1994PI02115 申请日期 1994.08.13
申请人 PHARMACIA & UPJOHN COMPANY 发明人 MICHAEL R. BARBACHYN.;STEVEN J. BRICKNER.;DOUGLAS K. HUTCHINSON.
分类号 C07D263/10;C07D263/20;A61K31/42;A61K31/421;A61K31/54;A61P31/00;A61P31/04;C07D413/10;C07D417/10 主分类号 C07D263/10
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