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    • 1. 发明授权
    • Cephalosporin antibiotics
    • 头孢菌素类抗生素
    • US4501741A
    • 1985-02-26
    • US484125
    • 1983-04-12
    • Bernard J. GravesStjepan Kukolja
    • Bernard J. GravesStjepan Kukolja
    • A61K20060101A61K31/545A61K31/546A61P31/04C07D20060101C07D501/00C07D501/16C07D501/20C07D501/22C07D501/32C07D501/34C07D501/46C07D501/58C07D501/59
    • C07D501/20
    • 7.beta.-[2-Amino-2-(benzothien-4,5,6, and 7-yl)acetylamino]-3-substituted-3-cepham-4-carboxylic acids and 7.beta.-[2-amino-2-(2,3-dihydrobenzothien-4,5,6, and 7 yl)acetylamino]-3H- or 3-substituted-3-cephem-4-carboxylic acids (1), e.g. 7.beta.-[2-amino-2-(benzothien-4-yl)acetylamino]-3-methyl-3-cephem-4-carboxylic acid, are orally effective antibiotics. Also provided are benzothienyl oximino compounds, the corresponding 2,3-dihydro compounds (2) useful as intermediates to (1) and as antibiotics, as well as 7.beta.-(2,2-dialkyl-5-oxo-4-benzothienyl-1-imidazolidinyl)-3H-(3-substituted)-3-cephem-4-carboxylic acids and the corresponding 2,3-dihydro compounds (3) useful as antibiotics, and prepared with (1) by condensation with ketones. Pharmaceutical formulations of antibiotic compounds (1), (2), and (3) are provided.
    • 7β-[2-氨基-2-(苯并噻吩-4,5,6和7-基)乙酰氨基] -3-取代-3-头孢烯-4-羧酸和7β-[2-氨基-2- (2,3-二氢苯并噻吩-4,5,6和7基)乙酰氨基] -3H-或3-取代-3-头孢烯-4-羧酸(1),例如 7β-[2-氨基-2-(苯并噻吩-4-基)乙酰氨基] -3-甲基-3-头孢烯-4-羧酸是口服有效的抗生素。 还提供了苯并噻吩基肟基化合物,可用作(1)的中间体和作为抗生素的相应的2,3-二氢化合物(2),以及7β-(2,2-二烷基-5-氧代-4-苯并噻吩基 - 1-(3-咪唑烷基)-3H-(3-取代的)-3-头孢烯-4-羧酸和可用作抗生素的相应的2,3-二氢化合物(3),并用(1)与酮缩合制备。 提供了抗生素化合物(1),(2)和(3)的药物制剂。