3-Phosphonate carbapenems
    61.
    发明授权
    3-Phosphonate carbapenems 失效
    3-膦酸酯碳青霉烯

    公开(公告)号:US4565808A

    公开(公告)日:1986-01-21

    申请号:US529194

    申请日:1983-09-06

    IPC分类号: C07F9/6561 A61K31/675

    CPC分类号: C07F9/65611

    摘要: 3-Phosphonate carbapenems of the Formula: wherein R.sup.1 is hydrogen, alkyl, amino, --NHCO-alkyl, hydroxy, alkoxy, halo, hydroxyalkyl, carboxyl or trifluoromethyl; R.sup.2 is alkyl, substituted alkyl, heterocyclic or substituted heterocyclic; R.sup.3 is hydrogen, alkyl or substituted alkyl; and M is a metal cation of H.sup.+ are disclosed. The compounds are useful as antibiotics.

    摘要翻译: 其中R1是氢,烷基,氨基,-NHCO-烷基,羟基,烷氧基,卤素,羟基烷基,羧基或三氟甲基的3-膦酸酯碳青霉烯。 R2是烷基,取代的烷基,杂环或取代的杂环; R3是氢,烷基或取代的烷基; 并且M是H +的金属阳离子。 该化合物可用作抗生素。

    3-Substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acid
    63.
    发明授权
    3-Substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acid 失效
    3-取代的-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸

    公开(公告)号:US4369187A

    公开(公告)日:1983-01-18

    申请号:US176819

    申请日:1980-08-08

    摘要: Disclosed are 3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R is, inter alia, acyl, alkyl, and aralkyl. Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译: 公开了3-取代-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸(I):其中R特别是酰基,烷基和芳烷基。 这些化合物及其药学上可接受的盐,酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法,包含这些化合物的药物组合物和治疗方法,包括当指出抗生素作用时施用这些化合物和组合物。

    Substituted N-methylene derivatives of thienamycin
    65.
    发明授权
    Substituted N-methylene derivatives of thienamycin 失效
    噻吩霉素的取代的N-亚甲基衍生物

    公开(公告)号:US4335043A

    公开(公告)日:1982-06-15

    申请号:US84013

    申请日:1979-10-11

    CPC分类号: C07F7/10 C07D205/08

    摘要: Disclosed are substituted N-methylene derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR.sup.1 R.sup.2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R.sup.1 and R.sup.2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译: 公开了噻吩霉素的取代的N-亚甲基衍生物,其可以由以下结构式表示:其中X和Y选自氢,R,OR,SR和NR 1 R 2,其中除了其中R是 取代或未取代的:烷基,烯基,炔基,环烷基,环烷基烷基,芳基,芳烷基,杂芳基,杂芳烷基,杂环基和杂环基烷基; R1和R2是氢或R.这些化合物及其药学上可接受的盐,醚,酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法,包括当指出抗生素效应时施用这些化合物和组合物。

    3-Substituted
thio-6-amido-7-oxo-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid
s-oxides
    68.
    发明授权
    3-Substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid s-oxides 失效
    3-取代的硫代-6-氨基-7-氧代-1-氮杂双环[3.2.0] - 庚-2-烯-2-羧酸S-氧化物

    公开(公告)号:US4277482A

    公开(公告)日:1981-07-07

    申请号:US84934

    申请日:1979-10-15

    CPC分类号: C07D477/24

    摘要: Disclosed are S-oxides of 3-substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; R.sup.1 is hydrogen or acyl; and R.sup.8 is, inter alia, independently selected from the group consisting of alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译: 公开了具有以下结构的3-取代的硫代-6-氨基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸的S-氧化物:其中:n是1或 2; R1是氢或酰基; 并且R8特别地独立地选自烷基,烯基,芳基和芳烷基。 这些化合物及其药学上可接受的盐,酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法,包含这些化合物的药物组合物和治疗方法,包括当指出抗生素作用时施用这些化合物和组合物。

    2-, 5-, and 6-Substituted-1-carbadethiapen-2-em-3-carboxylic acids
    70.
    发明授权
    2-, 5-, and 6-Substituted-1-carbadethiapen-2-em-3-carboxylic acids 失效
    2-,5-和6-取代的1-碳氮杂环戊烯-2-烯-3-羧酸

    公开(公告)号:US4269873A

    公开(公告)日:1981-05-26

    申请号:US60552

    申请日:1979-07-25

    摘要: Disclosed are 2-, 5- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are, inter alia, independently selected from the group consisting of hydrogen, (R.sup.9 is not hydrogen), alkyl, alkenyl, aryl and aralkyl. Such compounds, as well as their pharmaceutically acceptable salt, ester and amide derivatives, are useful as antibiotics. Also disclosed are processes for the preparation of such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译: 公开了具有以下结构的2-,5-和6-取代-1-碳代二脱氧-2-烯-3-羧酸:其中R 6,R 7,R 8和R 9特别地独立地选自 由氢,(R9不是氢),烷基,烯基,芳基和芳烷基组成。 这些化合物及其药学上可接受的盐,酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法和治疗方法,包括当指示抗生素效果时施用这些化合物和组合物。