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    N-Substituted aziridine-2-carboxylic acid derivatives
    1.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives 失效

    公开(公告)号：US4517183A

    公开(公告)日：1985-05-14

    申请号：US495548

    申请日：1983-05-17

    Applicant: Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    Inventor： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

    IPC: A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

    CPC classification number: C07D203/22 ,  Y10S514/885

    Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

    Adenosine-5'-carboxylic acid amides
    9.
    发明授权
    Adenosine-5'-carboxylic acid amides 失效
    腺苷-5'-羧酸酰胺

    公开(公告)号：US4224438A

    公开(公告)日：1980-09-23

    申请号：US161338

    申请日：1971-07-09

    Applicant: Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Karl Dietmann ,  Wolfgang Juhran

    Inventor： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Karl Dietmann ,  Wolfgang Juhran

    IPC: C07H19/16 ,  A61K31/70 ,  C07H19/18

    CPC classification number: C07H19/16

    Abstract: Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.

    Abstract translation: 具有以下通式的腺苷-5'-羧酸衍生物：其中Z为两个氢原子或二价低级亚烷基，其中R 1和R 2独立为 氢，羟基，氨基，低级烷基，低级烯基，任选N-烷基化的低级氨基烷基，环烷基，羟基烷基或哌啶基，或者R 1和R 2一起是含有4-7个碳原子的任选被氧或硫中断的二价亚乙基 或亚氨基，亚氨基亚氨基或芳基亚氨基或其药理学上相容的盐。 这些酯令人惊奇地可以通过在硫酸存在下酯化酸而不水解糖基来制备。 虽然酯具有一些活性，但它们可用于制备以标记的冠状动脉为特征的酰胺。

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