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    • 34. 发明授权
    • 2-(heterocyclylthio) carbapenem derivatives, their preparation and their
use as antibiotics
    • 2-(杂环硫基)碳青霉烯衍生物,其制备及其作为抗生素的用途
    • US5242914A
    • 1993-09-07
    • US831070
    • 1992-02-04
    • Isao KawamotoTeruo TanakaRokuro EndoMasayuki IwataMasao Miyauchi
    • Isao KawamotoTeruo TanakaRokuro EndoMasayuki IwataMasao Miyauchi
    • C07D477/20
    • C07D477/20
    • Compounds of formula (I): ##STR1## in which R.sup.a is a group of formula (II): ##STR2## where one of R' is a bond to the remainder of the compound, one more of R' is R.sup.2 and the others of R' are all hydrogen, R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen, optionally substituted alkyl, halogen, hydroxy, alkoxy, amino, alkanoylamino, alkanoyloxy, alkanoyl, carboxy, alkoxycarbonyl, cyano, --S(O).sub.j R.sup.9 where j is 0, 1 or 2 and R.sup.9 is alkyl, or --CONR.sup.6 R.sup.7 which is optionally substituted carbamoyl or heterocyclyl-carbonyl, --NR.sup.3 R.sup.4 is optionally substituted amino or heterocyclic, and --COOR.sup.5 is carboxy, --COO.sup.-, --COOM.sub.x, where M is a cation and x is the reciprocal of the valence of the cation M or protected carboxy and, where --COOR.sup.5 is carboxy, --COOM.sub.x or protected carboxy, the compound of formula (I) also contains an anion; l, m and n are independently 0, 1, 2 or 3, provided that (m+n) is an integer from 2 to 6; p is 0, 1 or 2; Y is a single bond, oxygen, sulfur or ##STR3## wherein R.sup.8 is hydrogen, alkyl or alkanoyl, and pharmaceutically acceptable salts and esters thereof. Such compounds are useful as antibiotics.
    • 式(I)的化合物:其中R a是式(II)的基团:其中R'中的一个与化合物的其余部分键合,R 1是R '是R 2,其余的R'都是氢,R 1是氢或甲基,R 2是氢,任选取代的烷基,卤素,羟基,烷氧基,氨基,烷酰基氨基,烷酰氧基,烷酰基,羧基,烷氧基羰基,氰基,-S O)j R 9其中j为0,1或2,R 9为烷基或-CONR 6 R 7,其为任选取代的氨基甲酰基或杂环基 - 羰基,-NR 3 R 4为任选取代的氨基或杂环,-COOR 5为羧基,-COO - , - COOMx 其中M是阳离子,x是阳离子M或保护的羧基的价数的倒数,并且其中-COOR 5是羧基,-COOM x或被保护的羧基,式(I)化合物还含有阴离子; l,m和n分别为0,1,2或3,条件是(m + n)为2至6的整数; p为0,1或2; Y是单键,氧,硫或其中R8是氢,烷基或烷酰基,及其药学上可接受的盐和酯。 这些化合物可用作抗生素。