1-azoniabicyclo�2.2.1!heptanes, method of preparing them and
pharmaceutical compositions in which they are present
    7.
    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

    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。