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公开(公告)号:US4482553A
公开(公告)日:1984-11-13
申请号:US484126
申请日:1983-04-12
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D333/60 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/57 , C07D501/59
CPC分类号: C07D333/60
摘要: 7-(2-Benzothienyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.
摘要翻译: 7-(2-苯并噻吩基)甘氨酰胺基头孢菌素具有良好的革兰氏阳性活性和有利的药代动力学,且口服有效。
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公开(公告)号:US4501741A
公开(公告)日:1985-02-26
申请号:US484125
申请日:1983-04-12
申请人: Bernard J. Graves , Stjepan Kukolja
发明人: Bernard J. Graves , Stjepan Kukolja
IPC分类号: A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/16 , C07D501/20 , C07D501/22 , C07D501/32 , C07D501/34 , C07D501/46 , C07D501/58 , C07D501/59
CPC分类号: C07D501/20
摘要: 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.
摘要翻译: 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。
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