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19 条记录 (耗时 0.025 秒)

    Pyrrolo [2,1-b][1,3]benzothiazepines with atypical antipsychotic activity
    2.
    发明授权
    Pyrrolo [2,1-b][1,3]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] [1,3]苯并硫氮杂

    公开(公告)号：US06391870B2

    公开(公告)日：2002-05-21

    申请号：US09769740

    申请日：2001-01-26

    申请人： Giuseppe Campiani ,  Vito Nacci ,  Patrizia Minetti ,  Maria Assunta Di Cesare

    发明人： Giuseppe Campiani ,  Vito Nacci ,  Patrizia Minetti ,  Maria Assunta Di Cesare

    IPC分类号： C07D51300

    CPC分类号： C07D513/04

    摘要： Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) where the groups are defined as in the description are disclosed. As compared to known antipsychotic agents, these compounds present substantial activity associated with a simultaneous reduction in unwanted extrapyramidal symptoms. These compounds can be formulated in pharmaceutical compositions for the treatment of psychoses such as, for example, schizophrenia.

    摘要翻译： 公开了具有如描述中定义的基团的下式（I）的吡咯[2,1-b] [1,3]苯并硫氮杂结构的缩聚杂环。 与已知的抗精神病药相比，这些化合物具有与同时减少不需要的锥体外系症状相关的显着活性。 这些化合物可以配制在用于治疗精神病例如精神分裂症的药物组合物中。

    Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity
    5.
    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。

    Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines
    8.
    发明授权
    Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines 失效
    制备9-氨基取代的9,10-二氢吡咯并[2,1-b] [1,3]苯并氮杂的方法

    公开(公告)号：US07078521B2

    公开(公告)日：2006-07-18

    申请号：US10343629

    申请日：2001-07-20

    申请人： Patrizia Minetti ,  Domenico Mastrojanno

    发明人： Patrizia Minetti ,  Domenico Mastrojanno

    IPC分类号： C07D513/04

    CPC分类号： C07D513/04

    摘要： A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R1H to give the corresponding enamine, which is subsequently transformed into the final compound

    摘要翻译： 描述了用于制备具有下式的化合物的方法，其中基团如下所定义; 特别地，R 1是取代的胺; 所述方法基本上包括吡咯并苯并硫氮杂-9-酮与胺R 1 H的反应，得到相应的烯胺，随后将其转化为最终化合物