发明授权
US4321194A N-Substituted aziridine-2-carboxylic acid derivatives for immuno
stimulation
失效
N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激
- 专利标题: N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation
- 专利标题(中): N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激
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申请号: US59863申请日: 1979-07-23
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公开(公告)号: US4321194A公开(公告)日: 1982-03-23
- 发明人: Elmar Bosies , Herbert Berger , Wolfgang Kampe , Uwe Bicker , Alfred Grafe
- 申请人: Elmar Bosies , Herbert Berger , Wolfgang Kampe , Uwe Bicker , Alfred Grafe
- 申请人地址: DEX Mannheim
- 专利权人: Boehringer Mannheim GmbH
- 当前专利权人: Boehringer Mannheim GmbH
- 当前专利权人地址: DEX Mannheim
- 优先权: DEX2833986 19780803
- 主分类号: C07D203/08
- IPC分类号: C07D203/08 ; A61K31/395 ; A61K31/396 ; A61K31/40 ; A61K31/44 ; A61K31/4427 ; A61K31/443 ; A61K31/4433 ; A61P37/04 ; C07D203/06 ; C07D401/04 ; C07D403/06 ; C07D405/04 ; C07D409/04 ; C07D203/10 ; C07D203/12 ; C07D203/14
摘要:
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.