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    • 4. 发明授权
    • Ergot derivatives
    • Ergot衍生物
    • US4252941A
    • 1981-02-24
    • US72289
    • 1979-09-04
    • Sergio ManteganiGiuliana ArcariAnna M. CaravaggiGermano Bosisio
    • Sergio ManteganiGiuliana ArcariAnna M. CaravaggiGermano Bosisio
    • C07D457/04A61K31/48A61P9/12C07D457/02
    • C07D457/02
    • Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents a methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR" R"' (wherein R" and R"' both represent alkyl groups having from 1 to 4 carbon atoms);R.sub.2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, or a phenyl group;R.sub.3 represents a fluorine atom, a cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl, or sulphonamido group, an alkoxy group having from 1 to 4 carbon atoms, an acyl group having from 2 to 4 carbon atoms, or a benzoyl group;R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.5 represents a hydrogen atom or a methoxy group;R.sub.6 represents a hydrogen or halogen atom or a methyl group; andR.sub.7 represents a hydrogen atom or a methyl group.The 2-cyano derivatives are especially preferred.
    • 公开了化合物及其制备方法,具有式(I)的化合物:其中R 1表示甲基,苯基,哌啶子基,1-吡咯烷基,吗啉代或4-甲基-1-哌嗪基, 具有1至4个碳原子的烷基或烷氧基,氨基,式NHR'的取代氨基(其中R'表示具有1至4个碳原子的烷基,环烷基,苄基或 苯基)或式NR“R”'的取代氨基(其中R“和R”“均表示具有1至4个碳原子的烷基); R2表示氢原子,具有1至4个碳原子的烷基或苯基; R 3表示氟原子,氰基,二氟甲基,二氟溴甲基,三氟甲基,甲硫基,甲磺酰基或磺酰胺基,具有1至4个碳原子的烷氧基,具有2至4个碳原子的酰基或苯甲酰基; R4表示具有1至4个碳原子的烃基; R5表示氢原子或甲氧基; R6表示氢或卤素原子或甲基; 并且R 7表示氢原子或甲基。 2-氰基衍生物是特别优选的。