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    • 9. 发明授权
    • Tetrahydro-.beta.-carboline derivatives and treatment of liver diseases
    • 四氢-β-咔啉衍生物和肝脏疾病的治疗
    • US4628057A
    • 1986-12-09
    • US666481
    • 1984-10-30
    • Ikuo IijimaYutaka SaigaToshikazu MiyagishimaYuzo MatsuokaMamoru Matsumoto
    • Ikuo IijimaYutaka SaigaToshikazu MiyagishimaYuzo MatsuokaMamoru Matsumoto
    • A61K31/435A61P1/16A61P3/06C07D471/04C07D498/18A61K31/395C07D471/02
    • C07D471/04
    • Novel tetrahydro-.beta.-carboline derivatives of the formula: ##STR1## wherein R.sup.1 is carboxyl, a lower alkoxycarbonyl, carbamoyl, an N,N-di-lower alkylcarbamoyl, an N-(phenyl-substituted lower alkylidenamino)carbamoyl, a [N,N-di(lower alkyl)amino]-lower alkyl, or a nitrogen-containing monocyclic heterocyclic group;R.sup.2 is hydrogen atom, a lower alkyl, or a hydroxy-lower alkyl group, or R.sup.2 is combined with R.sup.1 to form a group: --CO--O--CH.sub.2 --;R.sup.3 is hydrogen atom, a lower alkyl, a phenyl-lower alkyl, or a group: --CSS--R.sup.4 ;R.sup.4 is hydrogen atom, an alkyl, or a group: --(CH.sub.2).sub.n Y.sup.1 ;n is 0, 1 or 2,Y.sup.1 is a lower alkenyl, a phenyl-substituted lower alkenyl, an N,N-di(lower alkyl)amino, a lower alkylmercapto, a lower alkoxycarbonyl, benzoyl, naphthyl, a cycloalkyl, a monocyclic heterocyclic group, or a substituted or unsubstituted phenyl, which have excellent activities for alleviating, curing and preventing hepatic damages and are useful as a therapeutic or prophylactic agent for hepatic diseases,and processes for the preparation thereof, and a pharmaceutical composition containing the above compound as an active ingredient.
    • 其中R 1是羧基,低级烷氧基羰基,氨基甲酰基,N,N-二低级烷基氨基甲酰基,N-(苯基取代的低级亚烷基氨基)氨基甲酰基,[N ,N-二(低级烷基)氨基] - 低级烷基或含氮单环杂环基; R2是氢原子,低级烷基或羟基 - 低级烷基,或R2与R1结合形成基团:-CO-O-CH 2 - ; R3是氢原子,低级烷基,苯基 - 低级烷基或基团:-CSS-R4; R4是氢原子,烷基或基团: - (CH2)nY1; n是0,1或2,Y1是低级烯基,苯基取代的低级烯基,N,N-二(低级烷基)氨基,低级烷基巯基,低级烷氧基羰基,苯甲酰基,萘基,环烷基,单环 杂环基或取代或未取代的苯基,其具有优异的缓解,固化和预防肝损伤的活性,并且可用作肝脏疾病的治疗或预防剂及其制备方法,以及含有上述化合物的药物组合物 作为活性成分。