2-(Iminoethylidene)-pyrrolidines and tautomeric
2-(aminoethenyl)-1-pyrrolines
    75.
    发明授权
    2-(Iminoethylidene)-pyrrolidines and tautomeric 2-(aminoethenyl)-1-pyrrolines 失效
    2-(亚氨基亚乙基) - 吡咯烷和互变异构的2-(氨基乙烯基)-1-吡咯啉

    公开(公告)号:US4130652A

    公开(公告)日:1978-12-19

    申请号:US771294

    申请日:1977-02-23

    摘要: The present invention provides new imino compounds having the formula I ##STR1## wherein R.sub.1 represents an aliphatic or cycloaliphatic hydrocarbon radical, unsubstituted or substituted phenyl, or phenyl-lower alkyl or diphenyl-lower alkyl, which radicals are unsubstituted or substituted in the phenyl ring(s),R.sub.2 represents unsubstituted or substituted phenyl, unsubstituted or substituted monocyclic heteroaryl or lower alkyl,R.sub.3 represents hydrogen, lower alkyl, a carbonyl group linked with R.sub.2 to form a five-membered ring, or the group R.sub.6 --CO wherein R.sub.6 represents lower alkyl or unsubstituted or substituted phenyl,R.sub.4 represents, if present, hydrogen or lower alkyl which is independent or is linked with R.sub.1 to form a five- to seven-membered ring which can contain as ring members two aromatic ring carbon atoms of an unsubstituted or substituted phenyl or phenyl-lower-alkyl radical R.sub.1, and as a six- or seven-membered ring also epoxy or lower alkylimino which is separated by two, or at least two, carbon atoms from the nitrogen atom given in the formula I,R.sub.5 represents, if present, hydrogen or lower alkyl,A represents a straight- or branched-chain lower alkylene having 2 to (5-n.sub.1 -n.sub.2) chain members,Z represents epoxy, epithio, imino or lower alkylimino, andM.sub.1 and m.sub.2 represent 0 or 1 and together always represent 1,N.sub.1 represents 1 or, if Z represents imino or lower alkylimino and n.sub.2 represents 1, can also represent 0,N.sub.2 represents 0 or 1,And wherein two additional bonds, either corresponding to the dashed lines or corresponding to the dotted lines, are present, with m.sub.1 representing 0 in the former case and m.sub.2 representing 0 in the latter case, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, particularly hypoglycaemic activity.

    摘要翻译: 本发明提供具有式I 的新的亚氨基化合物

    Indolylimidoylheterocyclics
    78.
    发明授权
    Indolylimidoylheterocyclics 失效
    吲哚维林型杂环

    公开(公告)号:US3886165A

    公开(公告)日:1975-05-27

    申请号:US30606572

    申请日:1972-11-13

    申请人: MEAD JOHNSON & CO

    摘要: Heterocyclic bases such as quinolines, isoquinolines, benzoquinolines and phenanthridine react with indole and carboxamides in the presence of phosphorus oxychloride to provide indolylimidoylheterocyclic derivatives. Derivatives incorporating a dihydroquinoline, dihydroisoquinoline or dihydrobenzoquinoline moiety can be reduced to provide corresponding tetrahydro analogs. Typical examples of indolyl derivatives are 1,2-dihydro6-methoxy-2-(5-methoxy-3-indolyl)-1-(5-methyl-1-pyrrolin -2yl)quinoline and 1-(5,5-dimethyl-1-pyrrolin-2-yl)-1,2,3,4tetrahydro-6-methoxy-2-(5-methoxy-3 -indolyl)quinoline. The indolyl derivatives are useful as diuretic and antithrombogenic agents.

    摘要翻译: 诸如喹啉,异喹啉,苯醌和苯胺之类的杂环碱在三氯氧化磷存在下与吲哚和甲酰胺反应以提供吲哚维酰胺基杂环衍生物。 引入二氢喹啉,二氢异喹啉或二氢苯并喹啉部分的衍生物可以被还原以提供相应的四氢类似物。 吲哚基衍生物的典型实例是1,2-二氢-6-甲氧基-2-(5-甲氧基-3-吲哚基)-1-(5-甲基-1-吡咯啉-2-基)喹啉和1-(5- (5-甲基-1-吡咯啉-2-基)-1,2,3,4-四氢-6-甲氧基-2-(5-甲氧基-3-吲哚基)喹啉。 吲哚基衍生物可用作利尿剂和抗血栓形成剂。