Triterpene saponins having anti-inflammatory, mucolytic and antiedemic
activities, process for the preparation thereof and pharmaceutical
compositions containing them
    7.
    发明授权
    Triterpene saponins having anti-inflammatory, mucolytic and antiedemic activities, process for the preparation thereof and pharmaceutical compositions containing them 失效
    具有抗炎,粘液溶解和抗血清活性的三萜皂苷,其制备方法和含有它们的药物组合物

    公开(公告)号:US4879376A

    公开(公告)日:1989-11-07

    申请号:US67948

    申请日:1987-06-26

    IPC分类号: C07H15/256

    CPC分类号: C07H15/256

    摘要: Triterpene saponins of formula ##STR1## wherein R.sub.1 is H or OH and R.sub.2 is a tetrasaccharide, or alternatly pentasaccharide, chain have antiinflammatory, mucolytic and antiedemic activities. Said saponins are isolated from roots and bark of Crossopteryx febrifuga, for instance by precipitating them, in form of a complex with cholesterol or sytosterol, from an alcoholic extract of the vegetal material and by partitioning the precipitate between an apolar solvent, which subtracts the complexing agent and a polar solvent in which saponins are soluble.

    摘要翻译: 其中R1是H或OH,R2是四糖,或者五糖,链的三萜皂苷具有抗炎,粘液溶解和抗血清活性。 所述皂甙是从Crossopteryx febrifuga的根和树皮中分离出来的,例如通过从植物材料的酒精提取物中沉淀出与胆固醇或sytosterol的复合物形式,并通过将沉淀物分配在非极性溶剂之间,从而减去络合物 助剂和皂苷可溶的极性溶剂。

    Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity
    10.
    发明授权
    Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity 失效
    具有非典型抗精神病活性的吡咯并[2,1-b]苯并硫氮杂的脱烷基衍生物

    公开(公告)号:US07713956B2

    公开(公告)日:2010-05-11

    申请号:US11579806

    申请日:2005-04-28

    CPC分类号: C07D513/04

    摘要: Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH—CH2C═CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH═NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.

    摘要翻译: 吡咯并[2,1-b]苯并硫氮杂与式(I)的衍生物,其中A是CH-CH 2 C = CH; R是氢,卤素,C 1 -C 4烷氧基,C 1 -C 4烷硫基,C 1 -C 4烷基,C 5 -C 6环烷基; R1是1-哌嗪基,1-高哌嗪基和1-哌啶基; R 2是氢,C 1 -C 4烷氧基,C 1 -C 4烷硫基,C 1 -C 4烷基,CHO,CH = NH,CH 2 OH。 式(I)化合物具有特征性非典型抗精神病活性,因此可用作药物,特别是用于治疗和预防精神分裂症,偏执状态,躁狂抑郁状态,情感障碍,社会回归, 人格回归和幻觉。 所述化合物还表现出有利的药代动力学性质。