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CEPHALOSPORINS HAVING CATECHOL GROUP

机译:头孢泊灵拥有卡奇醇集团

摘要

Disclosed is a cephem compound represented by formula (I) [wherein X represents N, CH, or C-Cl; T represents S, or the like; A and G independently represent a lower alkylene, or the like; B represents a single bond, or the like; D represents a single bond, -NR-CO, -CO-NR-, -NR-CO-NR-, or the like; E represents a lower alkylene which may be substituted; F represents a single bond, or a phenylene which may be substituted; R, R, Rand Rindependently represent a hydrogen, a halogen, a nitrile, or -OR; Rrepresents a hydrogen, or the like; and a group represented by formula (II) represents a saturated or unsaturated monocyclic or ring-fused quaternary ammonium group which has at least one N atom and may be substituted, wherein the dashed line represents a bond in the ring], an ester of the cephem compound, a protected product of the cephem compound in which an amino group located on the ring in the chain on the 7-position side is protected, a pharmaceutically acceptable salt of the cephem compound, the ester or the protected product, or a solvate of the cephem compound, the ester, the protected product or the pharmaceutically acceptable salt, which has a broad antibacterial spectrum and particularly has a potent antibacterial activity against -lactamase-producing Gram-negative bacteria. Also disclosed is a pharmaceutical composition comprising the cephem compound, the ester, the protected product, the pharmaceutically acceptable salt or the solvate.
机译:公开了由式(I)表示的头孢烯化合物[其中X代表N,CH或C-Cl; T表示S等。 A和G独立地表示低级亚烷基等。 B表示单键等。 D表示单键,-NR-CO,-CO-NR-,-NR-CO-NR-等。 E表示可以被取代的低级亚烷基; F表示单键或可以被取代的亚苯基; R,R,R和R分别独立地表示氢,卤素,腈或-OR; R表示氢等。式(II)表示的基团表示具有至少一个N原子并且可以被取代的饱和或不饱和的单环或环稠合的季铵基,其中虚线表示环中的键。头孢烯化合物,头孢烯化合物的被保护产物,其中头孢烯化合物的药学上可接受的盐,酯或被保护产物,或溶剂化物,其中所述头孢烯化合物的保护基位于7位侧链上的环上的氨基。头孢烯类化合物,酯,被保护的产物或药学上可接受的盐具有广谱的抗菌谱,特别是对产生β-内酰胺酶的革兰氏阴性细菌具有有效的抗菌活性。还公开了包含头孢烯化合物,酯,被保护的产物,药学上可接受的盐或溶剂化物的药物组合物。

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