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    Quaternary basic amides, method of preparing them and pharmaceutical compositions in which they are present
    22.
    发明授权
    Quaternary basic amides, method of preparing them and pharmaceutical compositions in which they are present 失效
    第四纪碱性酰胺，其制备方法和其存在的药物组合物

    公开(公告)号：US5712288A

    公开(公告)日：1998-01-27

    申请号：US734029

    申请日：1996-10-18

    申请人： Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto ,  Didier Van Broeck

    发明人： Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto ,  Didier Van Broeck

    IPC分类号： C07D453/02 ,  C07D487/08 ,  A61K31/44

    CPC分类号： C07D487/08 ,  C07D453/02

    摘要： The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl; Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-azoniabicyclo�2.2.2!octane optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

    摘要翻译： 本发明涉及式（I）的四元碱性酰胺，其中Ar是任选取代的单 - ，二 - 或三 - 环芳族或杂芳族基团; T是直接键，羟基亚甲基，烷氧基是C1-C4的烷氧基亚甲基或C1-C5-亚烷基; Ar'是未取代的或单取代或多取代的苯基，噻吩基，苯并噻吩基，萘基或吲哚基; R是氢或C 1 -C 4烷基或C 1 -C 4 - ω-烷氧基（C 2 -C 4）烷基或C 2 -C 4 - ω-烷酰氧基（C 1 -C 4）烷基; Q是氢; 或者Q和R一起形成1,2-亚乙基，1,3-亚丙基或1,4-亚丁基; Am（+）是其中X1，X2和X3与它们所键合的氮原子一起形成任选被苯基或苄基取代的1-氮鎓双环[2.2.2]辛烷的基团 并且A（ - ）是药学上可接受的阴离子。 这些化合物可用于制备用于治疗涉及速激肽系统的病理状况的药物。

    1-azoniabicyclo[2.2.1] heptanes and pharmaceutical compositions in which they are present
    23.
    发明授权
    1-azoniabicyclo[2.2.1] heptanes and pharmaceutical compositions in which they are present 失效
    1-氮杂双环[2.2.1]庚烷及其存在的药物组合物

    公开(公告)号：US5554763A

    公开(公告)日：1996-09-10

    申请号：US470249

    申请日：1995-06-06

    申请人： Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto ,  Didier Van Broeck

    发明人： Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto ,  Didier Van Broeck

    IPC分类号： C07D453/02 ,  C07D487/08 ,  C07D487/02

    CPC分类号： C07D487/08 ,  C07D453/02

    摘要： The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group;T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group;Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl;R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a .omega.-C.sub.1 -C.sub.4 -alkoxy(C.sub.2 -C.sub.4)alkyl, or a .omega.-C.sub.2 -C.sub.4 -alkanoyloxy (C.sub.1 -C.sub.4)alkyl;.Q is hydrogen;or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group;Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form an azabicyclic or azatricyclic system optionally substituted by a phenyl or benzyl group; andA.sup..crclbar. is a pharmaceutically acceptable anion.These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

    摘要翻译： 本发明涉及式（I）的四元碱性酰胺，其中Ar是任选取代的单 - ，二 - 或三 - 环芳族或杂芳族基团; T是直接键，羟基亚甲基，烷氧基是C1-C4的烷氧基亚甲基或C1-C5-亚烷基; Ar'是未取代的或单取代或多取代的苯基，噻吩基，苯并噻吩基，萘基或吲哚基; R是氢或C 1 -C 4烷基或ω-C 1 -C 4 - 烷氧基（C 2 -C 4）烷基或ω-C 2 -C 4 - 烷酰氧基（C 1 -C 4）烷基。 Q是氢; 或者Q和R一起形成1,2-亚乙基，1,3-亚丙基或1,4-亚丁基; Am（+）是其中X1，X2和X3与它们键合的氮原子一起形成任选被苯基或苄基取代的氮杂双环或氮杂三环体系的基团 并且A（ - ）是药学上可接受的阴离子。 这些化合物可用于制备用于治疗涉及速激肽系统的病理状况的药物。

    1-Phenacyl-3-phenyl-3-(piperidylethyl)piperidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them
    24.
    发明授权
    1-Phenacyl-3-phenyl-3-(piperidylethyl)piperidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them 失效
    1-苯甲酰基-3-苯基-3-（哌啶基乙基）哌啶衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US06642233B1

    公开(公告)日：2003-11-04

    申请号：US09913106

    申请日：2001-08-09

    申请人： Jean-Philippe Ducoux ,  Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto

    发明人： Jean-Philippe Ducoux ,  Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto

    IPC分类号： A61K31535

    CPC分类号： C07D211/34 ,  C07D211/26

    摘要： The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.

    摘要翻译： 本发明涉及对于物质P的人NK1受体具有强亲和力和高选择性的下式的化合物及其与无机或有机酸的盐，其溶剂合物和/或其水合物。本发明涉及 还涉及制备它们的方法，可用于制备的式（VII）的中间体化合物，含有它们的药物组合物及其保险丝，用于制造用于治疗任何病理学的药物，其中物质P和 涉及人NK1受体。