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    Dealkylated Derivatives of Pyrrolo[2,1-B]Benzothiazepines with Atypical Antipsy-Chotic Activity
    1.
    发明申请
    Dealkylated Derivatives of Pyrrolo[2,1-B]Benzothiazepines with Atypical Antipsy-Chotic Activity 失效
    吡咯并[2,1-B]苯并硫氮杂脱烷基衍生物与非典型抗胆碱活性

    公开(公告)号：US20070270402A1

    公开(公告)日：2007-11-22

    申请号：US11579806

    申请日：2005-04-28

    申请人： Paolo Carminati ,  Maria Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    发明人： Paolo Carminati ,  Maria Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    IPC分类号： A61K31/554 ,  A61P25/18 ,  C07D281/02

    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： 具有式（I）的吡咯并[2,1-b]苯并硫氮杂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 1 -C 4烷基，C 5 -C 6环烷基，C 1 -C 4烷基，C 5 -C 6环烷基， R 1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烷基， C 1 -C 4烷基，C 1 -C 4烷基，CHO，CH-NOH，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。

    Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity
    2.
    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

    申请人： Paolo Carminati ,  Maria Assunta Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    发明人： Paolo Carminati ,  Maria Assunta Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    IPC分类号： A61P25/18 ,  A61K31/407 ,  C07D513/04

    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。