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    • 107. 发明授权
    • 2-azacycloalkylthiopenem derivatives
    • 2-氮杂环烷基硫代青霉烯衍生物
    • US4772597A
    • 1988-09-20
    • US649516
    • 1984-09-13
    • Ernest S. Hamanaka
    • Ernest S. Hamanaka
    • C07D207/12C07D207/26C07D207/273C07D207/277C07D207/40C07D207/416C07D211/54C07D211/76C07D263/20C07D265/06C07D265/10C07D277/14C07D499/88C07F7/18C07D499/00A61K31/425
    • C07D207/273C07D207/12C07D207/277C07D207/416C07D211/54C07D211/76C07D263/20C07D265/06C07D265/10C07D277/14C07D499/88C07F7/186
    • Certain 2-azacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R is ##STR2## A is alkylene having 2-4 carbon atoms, alkylene having 2-4 carbon atoms wherein a carbon atom has an oxo substituent or alkylene having 2-4 carbon atoms wherein a methylene is replaced by oxygen, S(O).sub.m, or N--R.sub.3 ;B is carbonyl, thiocarbonyl, methylene or imine;R.sub.1 is hydrogen or forms an ester group which is hydroyzed in vivo;R.sub.2 is hydrogen, formyl, alkylcarbonyl, N-alkylaminocarbonyl, N-alkylaminosulfonyl, aminosulfonyl, aminocarbonyl, alkoxycarbonyl having 2-5 carbon atoms, alkylsulfonyl, alkyl, or alkyl substituted by aminocarbonyl, alkyl--S(O).sub.m --, hydroxyl, amino, alkylcarbonylamino, formamido or alkylsulfonylamino, wherein each alkyl has 1-4 carbon atoms;R.sub.3 is hydrogen, methyl, formyl, methylcarbonyl or methylsulfonyl;alk is alkylene having 1-4 carbon atoms;n is zero or one; andm is zero, 1 or 2.
    • 某些2-氮杂环烷基硫代-2-青霉烯-3-羧酸化合物可用作治疗哺乳动物的抗细菌剂,并且具有式I或其药学上可接受的盐,其中:R为A为2-4的亚烷基 碳原子,具有2-4个碳原子的亚烷基,其中碳原子具有氧取代基或具有2-4个碳原子的亚烷基,其中亚甲基被氧,S(O)m或N-R 3取代; B是羰基,硫代羰基,亚甲基或亚胺; R1是氢或形成在体内水解的酯基; R2是氢,甲酰基,烷基羰基,N-烷基氨基羰基,N-烷基氨基磺酰基,氨基磺酰基,氨基羰基,具有2-5个碳原子的烷氧基羰基,烷基磺酰基,烷基或被氨基羰基取代的烷基,烷基-S(O)m - ,羟基,氨基 烷基羰基氨基,甲酰氨基或烷基磺酰基氨基,其中每个烷基具有1-4个碳原子; R3是氢,甲基,甲酰基,甲基羰基或甲基磺酰基; 烷基是具有1-4个碳原子的亚烷基; n为零或一; m为零,1或2。