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    • 2. 发明授权
    • N-Substituted aziridine-2-carboxylic acid derivatives for immuno
stimulation
    • N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激
    • US4321194A
    • 1982-03-23
    • US59863
    • 1979-07-23
    • Elmar BosiesHerbert BergerWolfgang KampeUwe BickerAlfred Grafe
    • Elmar BosiesHerbert BergerWolfgang KampeUwe BickerAlfred Grafe
    • C07D203/08A61K31/395A61K31/396A61K31/40A61K31/44A61K31/4427A61K31/443A61K31/4433A61P37/04C07D203/06C07D401/04C07D403/06C07D405/04C07D409/04C07D203/10C07D203/12C07D203/14
    • C07D203/06Y10S514/885
    • Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals, or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.
    • 其中X是羧基,腈,烷氧基羰基或氨基甲酰基的氮杂环丁烷-2-羧酸衍生物,R和R 1是各种有机基团或其药理学上可接受的盐,具有显着的免疫刺激活性,特别是与 添加化学治疗剂如青霉素,头孢菌素,硝基呋喃或氯霉素。 那些化合物是新的,其中X是氰基或烷氧基羰基,R 1是氢原子,但R'不是未取代的烷基或被羟基,烷氧基,二烷基氨基,苯基,4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基,或环烷基,苯基,4-氯苯基,4-甲氧基苯基,s-三嗪基或吡啶基; 或其中X为氨基甲酰基,R 1为氢原子,R'为未取代的环己基,烷基或苄基; 或其中X为氰基或烷氧基羰基,R 1为苯基,R'不为异丙基,环己基,苯基,苄基或对氯苄基; 或其中R 1是甲基,R 1不是苄基,对氯或对甲氧基苄基。
    • 7. 发明授权
    • N-Substituted aziridine-2-carboxylic acid derivatives and
immuno-stimulation composition and method
    • N-取代的氮丙啶-2-羧酸衍生物和免疫刺激组合物和方法
    • US4409236A
    • 1983-10-11
    • US268964
    • 1981-06-01
    • Elmar BosiesHerbert BergerWolfgang KampeUwe BickerAlfred Grafe
    • Elmar BosiesHerbert BergerWolfgang KampeUwe BickerAlfred Grafe
    • C07D203/08A61K31/395A61K31/396A61K31/40A61K31/44A61K31/4427A61K31/443A61K31/4433A61P37/04C07D203/06C07D401/04C07D403/06C07D405/04C07D409/04C07D333/30
    • C07D203/06Y10S514/885
    • Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals; or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl, a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.
    • 其中X是羧基,腈,烷氧基羰基或氨基甲酰基,R和R 1是各种有机基团; 或其药理学上可接受的盐具有显着的免疫刺激活性,特别是与添加的化学治疗剂如青霉素,头孢菌素,硝基呋喃或氯霉素结合使用。 那些化合物是新的,其中X是氰基或烷氧基羰基,R 1是氢原子,但R'不是未取代的烷基或被羟基,烷氧基,二烷基氨基,苯基,4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基,或环烷基,苯基,4-氯苯基,4-甲氧基苯基,s-三嗪基或吡啶基; 或其中X为氨基甲酰基,R 1为氢原子,R'为未取代的环己基,烷基或苄基; 或其中X为氰基或烷氧基羰基,R 1为苯基,R'不为异丙基,环己基,苯基,苄基或对氯苄基; 或其中R 1是甲基,R 1不是苄基,对氯或对甲氧基苄基。