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    Basic derivatives of benz[e] isoindol-1-ones and pyrrolo[3,4-c] quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use
    1.
    发明授权
    Basic derivatives of benz[e] isoindol-1-ones and pyrrolo[3,4-c] quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use 失效
    苯并[e]异吲哚-1-酮和具有5-HT3拮抗活性的吡咯并[3,4-c]喹啉-1-酮的基本衍生物及其制备及其治疗用途

    公开(公告)号：US06413978B1

    公开(公告)日：2002-07-02

    申请号：US09967972

    申请日：2001-10-02

    申请人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    IPC分类号： A61K31437

    CPC分类号： C07D451/04 ,  C07D453/02

    摘要： Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.l]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.

    摘要翻译： 可以由下列通式（I）表示的苯并[e]异吲哚-1-酮和吡咯并[3,4-c]喹啉-1-酮的新型碱性衍生物被描述为：其中X是CH或N， R是H，Cl或OR1，其中R 1是H或具有1至3个碳原子的烷基，Het是3-内丙基（即8-甲基-8-氮杂双环[3.2.1] （即，1-氮杂双环[2.2.2]辛-3-基））或3-奎宁环基（即，1-氮杂双环[2.2.2]辛-3-基）。 已经发现这些化合物是5-HT3血清素样受体的有效和选择性拮抗剂，因此可以用作例如抗遗传学以及中枢神经系统的各种病理状况，以及作为镇咳药。

    Basic derivatives of benz[E]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use
    3.
    发明授权
    Basic derivatives of benz[E]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use 失效
    苯并[E]异吲哚-1-酮和具有5-HT3拮抗活性的吡咯并[3,4-c]喹啉-1-酮的基本衍生物及其制备及其治疗用途

    公开(公告)号：US06323216B1

    公开(公告)日：2001-11-27

    申请号：US09417098

    申请日：1999-10-13

    申请人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    IPC分类号： A61K31439

    CPC分类号： C07D451/04 ,  C07D453/02

    摘要： Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.1]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.

    摘要翻译： 可以由下列通式（I）表示的苯并[e]异吲哚-1-酮和吡咯并[3,4-c]喹啉-1-酮的新型碱性衍生物被描述为：其中X是CH或N， R是H，Cl或OR 1，其中R 1是H或具有1至3个碳原子的烷基，Het是3-内丙基（即8-甲基-8-氮杂双环[3.2.1] （即，1-氮杂双环[2.2.2]辛-3-基））或3-奎宁环基（即，1-氮杂双环[2.2.2]辛-3-基）。 已经发现这些化合物是5-HT3血清素样受体的有效和选择性拮抗剂，因此可以用作例如抗遗传学以及中枢神经系统的各种病理状况，以及作为镇咳药。