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    • 10. 发明授权
    • Cephalosporins
    • 头孢菌素
    • US4364944A
    • 1982-12-21
    • US323382
    • 1981-11-20
    • Bernd WetzelEberhard WoitunWolfgang ReuterRoland MaierUwe LechnerHanns Goeth
    • Bernd WetzelEberhard WoitunWolfgang ReuterRoland MaierUwe LechnerHanns Goeth
    • C07D501/06A61K20060101A61K31/545A61K31/546C07D20060101C07D501/00C07D501/20C07D501/22C07D501/24C07D501/34C07D501/36C07D501/46C07D501/56C07D501/57
    • C07D501/20Y02P20/55
    • 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.
    • 其中Y是氢或甲氧基的式“IMAGE”的化合物; A是,或者当Y是甲氧基时,3,4-二羟基 - 苯基的苯基,4-羟基 - 苯基,2-噻吩基,3-噻吩基; A'是氢,-COCH 2 Cl,-COCH 2 Br,-COOCH 2 CCl 3,甲酰基或三苯甲基; D是氢,乙酰氧基,氨基羰氧基,吡啶鎓,4-氨基羰基 - 吡啶鎓或-S-Het,其中Het是3-甲基-1,2,4-噻二唑-5-基,1,2,4-噻二唑-5-基, 1,3,4-噻二唑-5-基,2-甲基-1,3,4-噻二唑-5-基,4H-5,6-二氧代-1,2,4-三嗪-3-基, 4-甲基-5,6-二氧代-1,2,4-三嗪-3-基,1-乙烯基 - 四唑-5-基,1-烯丙基 - 四唑-5-基或n为1,2 或3; R1是羟基,氨基,二甲基氨基,乙酰基氨基,氨基羰基,氨基羰基氨基,氨基磺酰基,氨基磺酰基氨基,甲基羰基,甲基磺酰基氨基,氰基,羟基磺酰基氨基,甲基磺酰基,甲基亚磺酰基,羧酸基或磺酸基团。 或 - (CH 2)n R 1是1至4个碳原子的烷基或2,3-二羟基 - 丙基; R2是未取代的或单取代的3-吡啶基,5-嘧啶基,2-噻吩基,2-呋喃基 - 甲基,2-噻吩基 - 甲基,2-咪唑基 - 甲基,2-噻唑基 - 甲基,3-吡啶基 - 甲基或5-嘧啶基 甲基,其中取代基是氯,甲基,乙酰氨基,羟基,甲基亚磺酰基,甲基磺酰基,氨基羰基或氨基磺酰基; E是氢或羧基保护基,其在体外或体内容易除去; 和E是氢,与无机或有机碱形成的无毒的药理学上可接受的盐; 化合物及其盐可用作抗生素。