New 3,7-Di:substd.-3-cephem-4-carboxylic acid(s) and analogues

摘要

Cephems and analogues of formula (I) and, when no positive charge present, acid-addn. salts, and with COOH base-addn. salts are new. X= S,O, CH2 or SO R1= R9-CH(SO3H)CO, p-HOC6H4CH(NH-COR10)CO, R11-C(=NOR12)CO or a gp. or (III); R5,R6= e.g. H, halogen, CN, OH or COOH or 2-6C alkoxycarbonyl, R7= e.g. COOH, or 2-6C alkoxycarbonyl, R8= e.g. H, 1-4C alkyl, 1-4C alkoxy, 2-5C alkanoyl, 1-4C alkylthio and 1-4C alkanesulphinyl, R9= H, or 1-6C alkyl, R10= gp. of e.g. formulae (IV); R11= e.g. 2-aminothiazol-4-yl, R12= e.g. H, 1-6C alkyl, or 3-8C cycloalkyl, R13= e.g. piperidino or pyrrolidino, m= 0,1,2 or 3; W= S or a direct bond; R14= e.g. Ph or pyridinio-(1-4C) alkylene, R15= 1-4C alkyl, Ph or PhCH2; R16 e.g. H, 1-4C alkyl or 1-4C haloalkyl, R17= phthalimido; R18-R20= 1-4C alkyl; or R18= 1-4C alkyl and CR19R20= 3-6C carbocyclic ring, R21, R22= H or 1-4C alkyl; R23 e.g. OH, 1-4C alkoxy, or 2-8C dialkylamino, R24 e.g. 1-4C alkyl or 1-4C alkoxy, R25,R26= OH or 1-4C alkoxy; R27= 1-4C alkyl; R28= H or 1-6C alkyl; m= 0-3; R29=H, 1-3C alkyl or MeS; R30 e.g. H, 1-3C alkyl, or 3-7C cycloalkyl, R31 e.g. OH, NH2 or 1-4C alkoxy, R32 e.g.H or 1-4C alkyl, R2= H or OMe; R3 e.g. COOH, R4 e.g. N=CR32-NR33R34, N=C(NR35R36)(NR37R38) R32 e.g. H, 1-6C alkyl, Ph or naphthyl R41= H or 1-6Calkyl, R33,R34 = H, 1-6C alkyl, OH or CN, R35,R37 e.g.H, 1-6C alkyl or Ph-(1-6C)alkyl q= 1-6; R41= H or 1-6C alkyl; R36,R38 e.g. H, 1-6C alkyl, Ph or naphthyl; ring Y e.g. pyridine, or pyrimidine, R39 e.g. H, NH2, 1-6C alkyl or 3-6C cycloalkyl, R42= 1-6C alkyl or 1-6C alkoxy; R43-R45= H or 1-4C alkyl; R4-= e.g. H, NH2 or NO2.