发明授权
- 专利标题: Cephalosporins
- 专利标题(中): 头孢菌素
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申请号: US323382申请日: 1981-11-20
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公开(公告)号: US4364944A公开(公告)日: 1982-12-21
- 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 Biberach
- 专利权人: Dr. Karl Thomae Gesellschaft mit beschrankter Haftung
- 当前专利权人: Dr. Karl Thomae Gesellschaft mit beschrankter Haftung
- 当前专利权人地址: DEX Biberach
- 优先权: DEX3045330 19801202; DEX3045331 19801202
- 主分类号: C07D501/06
- IPC分类号: C07D501/06 ; A61K20060101 ; A61K31/545 ; A61K31/546 ; C07D20060101 ; C07D501/00 ; C07D501/20 ; C07D501/22 ; C07D501/24 ; C07D501/34 ; C07D501/36 ; C07D501/46 ; C07D501/56 ; C07D501/57
摘要:
Compounds of the formula ##STR1## wherein Y is hydrogen or methoxy;A is ##STR2## or, when Y is methoxy, also phenyl, 4-hydroxy-phenyl, 2-thienyl, 3-thienyl of 3,4-dihydroxy-phenyl;A' is hydrogen, --COCH.sub.2 Cl, --COCH.sub.2 Br, --COOCH.sub.2 CCL.sub.3, formyl or trityl;D is hydrogen, acetoxy, aminocarbonyloxy, pyridinium, 4-aminocarbonyl-pyridinium or -S-Het, where Het is 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 4H-5,6-dioxo-1,2,4-triazine-3-yl, 4-methyl-5,6-dioxo-1,2,4-triazin-3-yl, 1-vinyl-tetrazol-5-yl, 1-allyl-tetrazol-5-yl or ##STR3## n is 1, 2 or 3; R.sub.1 is hydroxyl, amino, dimethylamino, acetylamino, aminocarbonyl, aminocarbonylamino, aminosulfonyl, aminosulfonylamino, methylcarbonyl, methylsulfonylamino, cyano, hydroxysulfonylamino, methylsulfonyl, methylsulfinyl, a carboxylic acid group or a sulfonic acid group; or--(CH.sub.2).sub.n R.sub.1 is alkyl of 1 to 4 carbon atoms or 2,3-dihydroxy-propyl;R.sub.2 is unsubstituted or monosubstituted 3-pyridyl, 5-pyrimidinyl, 2-thienyl, 2-furyl-methyl, 2-thienyl-methyl, 2-imidazolyl-methyl, 2-thiazolyl-methyl, 3-pyridyl-methyl or 5-pyrimidinyl-methyl, where the substituent is chlorine, methyl, acetylamino, hydroxyl, methylsulfinyl, methylsulfonyl, aminocarbonyl or aminosulfonyl; andE is hydrogen or a carboxyl-protective group which is easily removable in vitro or in vivo;and, E is hydrogen, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as antibiotics.
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