发明授权
- 专利标题: Cephalosporin derivatives
- 专利标题(中): 头孢菌素衍生物
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申请号: US191423申请日: 1980-09-26
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公开(公告)号: US4415566A公开(公告)日: 1983-11-15
- 发明人: Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
- 申请人: Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
- 申请人地址: DEX Ingelheim am Rhein
- 专利权人: Boehringer Ingelheim GmbH
- 当前专利权人: Boehringer Ingelheim GmbH
- 当前专利权人地址: DEX Ingelheim am Rhein
- 优先权: DEX2938344 19790713
- 主分类号: C07D499/66
- IPC分类号: C07D499/66 ; A61K31/43 ; A61K31/545 ; A61K31/546 ; A61P31/04 ; C07D239/36 ; C07D499/00 ; C07D499/64 ; C07D499/68 ; C07D499/70 ; C07D501/20 ; C07D501/22 ; C07D501/34 ; C07D501/36 ; C07D501/46
摘要:
Penicillins and cephalosporins of the formula ##STR1## wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohene-1-yl, cyclohexa-1,4-diene-1-yl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 3,4-disubstituted phenyl, where the substituents, which may be identical to or different from each other, are each chlorine, hydroxyl or methoxy;R.sub.1 is an unsubstituted or substituted 5- or 6-membered heterocycle comprising carbon atoms and 1 to 4, preferably 1 to 2, identical or different heteroatoms such as oxygen, sulfur or nitrogen;n is 0 or 1;X is ##STR2## D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-triadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,2,4-thiadiazol-5-yl, 2-acetylamino-1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-oxadiazol-5-yl, 1,2,3-triazol-4-yl or 1,2,4-triazol-3-yl; andE is hydrogen or a protective group which is easily removable in nitro or in vivo, especially an ester-forming group which can be removed under mild conditions by hydrogenation or hydrolysis or other treatments, or an ester-forming group which can easily be split off in the living organism;and, when E is hydrogen, their non-toxic, pharmacologically acceptable salts thereof, such as their alkali metal or alkaline earth metal salts, especially the sodium, potassium, magnesium or calcium salts; their ammonium salts; or their organic amine salts, especially the triethylamine or dicyclohexylamine salts. The compounds are useful as antibiotics.
公开/授权文献
- US5652755A Printer interface system 公开/授权日:1997-07-29
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