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33 条记录 (耗时 0.034 秒)

    Thiophene-2-carboxamide derivatives, preparation thereof and therapeutic use thereof
    3.
    发明授权
    Thiophene-2-carboxamide derivatives, preparation thereof and therapeutic use thereof 有权
    噻吩-2-甲酰胺衍生物，其制备及其治疗用途

    公开(公告)号：US08410137B2

    公开(公告)日：2013-04-02

    申请号：US13057043

    申请日：2009-07-30

    申请人： Francis Barth ,  Jean-Philippe Ducoux ,  Patrick Gueule ,  Murielle Rinaldi-Carmona ,  Arnaud Rouquette

    发明人： Francis Barth ,  Jean-Philippe Ducoux ,  Patrick Gueule ,  Murielle Rinaldi-Carmona ,  Arnaud Rouquette

    IPC分类号： A61K31/445 ,  C07D409/06

    CPC分类号： C07D409/06 ,  C07D409/14

    摘要： The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n′—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).

    摘要翻译： 本发明的主题是对应于式（I）的化合物，其中：R 1和R 2与它们所连接的氮原子一起构成含有4至7个原子的饱和杂环基团，其优选被取代; 两个取代基R 3和R 6中的一个是Y-A-R 9基团; Y是氧原子或-S（O）n'-或-OSO 2基团; A是未取代的（C 1 -C 4）亚烷基; R9是-OR19，-CH3，-NR19R20，-CONR19R20，-NR15COR19，-S（O）nR21或-NR13SO2R21基团; -R10是氢原子或（C1-C4）烷基。 本发明还涉及式（I）化合物的制备方法和治疗用途。

    1-azoniabicyclo�2.2.1!heptanes, method of preparing them and pharmaceutical compositions in which they are present
    10.
    发明授权
    1-azoniabicyclo�2.2.1!heptanes, method of preparing them and pharmaceutical compositions in which they are present 失效
    1-氮杂双环[2.2.1]庚烷，其制备方法和其中存在的药物组合物

    公开(公告)号：US5679693A

    公开(公告)日：1997-10-21

    申请号：US685489

    申请日：1996-07-24

    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 tricyclic 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�2.2.1!HEPTANE 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-亚烷基亚氨基C [2.2.1]庚烷的基团 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。