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16 条记录 (耗时 0.033 秒)

    Cephalosporins
    11.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US4401667A

    公开(公告)日：1983-08-30

    申请号：US323432

    申请日：1981-11-20

    申请人： Bernd Wetzel ,  Eberhard Woitun ,  Wolfgang Reuter ,  Roland Maier ,  Uwe Lechner ,  Hanns Goeth

    发明人： Bernd Wetzel ,  Eberhard Woitun ,  Wolfgang Reuter ,  Roland Maier ,  Uwe Lechner ,  Hanns Goeth

    IPC分类号： C07D501/06 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C20060101 ,  C07D20060101 ,  C07D501/00 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46 ,  C07D501/54 ,  C07D501/56

    CPC分类号： C07D501/36 ,  Y02P20/55

    摘要： Compounds of the formula ##STR1## wherein A is phenyl, 4-hydroxy-phenyl, 2-thienyl, 3-thienyl or 3,4-dihydroxy-phenyl;Het is 4H-5,6-dioxo-1,2,4-triazin-3-yl, 4-methyl-5,6-dioxo-1,2,4-triazin-3-yl, 1-vinyl-tetrazol-5-yl, 1-allyl-tetrazol-5-yl or ##STR2## where n is an integer from 1 to 3, inclusive,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 may also be alkyl of 2 to 4 carbon atoms or 2,3-dihydroxy-propyl;R.sub.2 is an unsubstituted or monosubstituted heterocyclic radical selected from the group consisting of 3-pyridyl, 5-pyrimidinyl, 2-thienyl, 2-furylmethyl, 2-thienylmethyl, 2-imidazolylmethyl, 2-thiazolylmethyl, 3-pyridylmethyl or 5-pyrimidinylmethyl, where the substituent is chlorine, methyl, acetylamino, hydroxyl, methylsulfinyl, methylsulfonyl, aminocarbonyl or aminosulfonyl; andE is hydrogen or a protective group which is easily removable in vitro or in vivo;and, when 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.

    摘要翻译： 其中A是苯基，4-羟基 - 苯基，2-噻吩基，3-噻吩基或3,4-二羟基 - 苯基的式 Het是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 - 其中n为1〜3的整数，包括1和3的整数，R1为羟基，氨基，二甲基氨基，乙酰氨基，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，或 - （CH 2）n -R 1也可以是2至4个碳原子的烷基或2,3-二羟基丙基; R2是选自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-嘧啶基甲基的未取代或单取代杂环基， 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是氢或在体外或体内容易除去的保护基; 并且当E是氢时，与无机或有机碱形成的无毒的药学上可接受的盐; 化合物及其盐可用作抗生素。

    Penicillins
    12.
    发明授权
    Penicillins 失效
    青霉素

    公开(公告)号：US4289775A

    公开(公告)日：1981-09-15

    申请号：US149839

    申请日：1980-05-14

    申请人： Bernd Wetzel ,  Eberhard Woitun ,  Wolfgang Reuter ,  Roland Maier ,  Uwe Lechner ,  Hanns Goeth

    发明人： Bernd Wetzel ,  Eberhard Woitun ,  Wolfgang Reuter ,  Roland Maier ,  Uwe Lechner ,  Hanns Goeth

    IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D239/48 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70

    CPC分类号： C07D239/48 ,  C07D499/00

    摘要： Compounds of the formula ##STR1## wherein A is phenyl, p-hydroxy-phenyl, 2-thienyl, 3-thienyl 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 is --NH--Z--X;Z is straight or branched alkylene of 1 to 6 carbon atoms or cycloalkylene of 3 to 6 carbon atoms;X is cyano, hydroxyl, mercapto, aminocarbonyl, aminosulfonyl, ##STR2## R.sub.1 is straight or branched alkyl of 1 to 4 carbon atoms or phenyl; R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms; and R.sub.1 and R.sub.2, together with an adjacent nitrogen atom to which they are attached, form a 3- to 6-membered heterocyclic ring;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases.

    摘要翻译： 其中A是苯基，对羟基 - 苯基，2-噻吩基，3-噻吩基或3,4-二取代的苯基的化合物，其中取代基可以相同或不同， 其他都是氯，羟基或甲氧基; R是-NH-Z-X; Z是1〜6个碳原子的直链或支链亚烷基或3〜6个碳原子的亚环烷基; X是氰基，羟基，巯基，氨基羰基，氨基磺酰基，+OR OR 1，OCOR 1，SR 1，SOR 1或SO 2 R 1; R1是1-4个碳原子的直链或支链烷基或苯基; R2是氢或1-4个碳原子的烷基; R1和R2与它们所连接的相邻氮原子一起形成3-至6-元杂环; 和与无机或有机碱形成的无毒的，药学上可接受的盐。

    Cephalosporins
    16.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US4316898A

    公开(公告)日：1982-02-23

    申请号：US151694

    申请日：1980-05-20

    申请人： Bernd Wetzel ,  Eberhard Waitun ,  Roland Maier ,  Wolfgang Rueter ,  Uwe Lechner ,  Hans Goeth

    发明人： Bernd Wetzel ,  Eberhard Waitun ,  Roland Maier ,  Wolfgang Rueter ,  Uwe Lechner ,  Hans Goeth

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D239/46 ,  C07D501/20 ,  C07D501/36 ,  C07D501/57

    CPC分类号： C07D239/47 ,  Y02P20/55

    摘要： Cephalosporins of the formula ##STR1## wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohexene-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;Y is hydrogen or methoxy;D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or the group S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 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, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,3,4-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;R is hydrogen, methyl, cyclopropyl, hydroxyl, methoxy, ethoxy, mercapto, morpholino, thiomorpholino, thiomorpholino-S-oxide, thiomorpholino-S,S-dioxide, ##STR2## E is hydrogen or a protective group which is easily removable in vitro or in vivo;and nontoxic, pharmacologically acceptable salts thereof.

    摘要翻译： 其中A为苯基，4-羟基苯基，环己基，环己烯-1-基，环己-1,4-二烯-1-基，2-噻吩基，3-噻吩基，2-呋喃基，3-甲氧基苯基， 呋喃基或3,4-二取代的苯基，其中可以相同或不同的取代基各自为氯，羟基或甲氧基; Y是氢或甲氧基; D是氢，羟基，乙酰氧基，氨基羰基氧基，吡啶鎓，氨基羰基 - 吡啶鎓或S-Het基团，其中Het是1-甲基 - 四唑-5-基，四唑-5-基，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，2-甲基氨基 -1,3,4-噻二唑-5-基，2-二甲基氨基-1,3,4-噻二唑-5-基，2-甲酰氨基-1,3,4-噻二唑-5-基，2-乙酰基氨基-1 ，3,4-噻二唑-5-基，2-甲基-1,3,4-恶二唑-5-基，1,2,3-三唑-4-基或1,2,4-三唑-3-基 ; R是氢，甲基，环丙基，羟基，甲氧基，乙氧基，巯基，吗啉代，硫代吗啉代，硫代吗啉代-S-氧化物，硫代吗啉代-S，S-二氧化物，E是氢或保护基， 体外或体内可去除; 和无毒的药学上可接受的盐。