申请人:Sanofi
公开号:US05679693A1
公开(公告)日:1997-10-21
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\x9b2.2.1!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.
该发明涉及公式为##STR1##的四元碱性酰胺,其中Ar是一个可选择取代的单环、双环或三环芳香或杂芳基团;T是直链键,羟甲亚基,烷氧甲亚基,其中烷氧基是C.sub.1 -C.sub.4,或C.sub.1 -C.sub.5-烷基亚基;Ar'是未取代或单取代或多取代的苯基,噻吩基,苯噻吩基,萘基或吲哚基;R是氢或C.sub.1 -C.sub.4-烷基,或C.sub.1 -C.sub.4-ω-烷氧基(C.sub.2 -C.sub.4)烷基,或C.sub.2 -C.sub.4-ω-烷酰氧基(C.sub.1 -C.sub.4)烷基;Q是氢;或者Q和R一起形成1,2-乙烯,1,3-丙烯或1,4-丁烯基团;Am.sup..sym.是基团##STR2##其中X.sub.1、X.sub.2和X.sub.3与它们连接的氮原子一起形成一个1-AZONIABICYCLO\x9b2.2.1!HEPTANE,该环可选择由苯基或苄基取代;A.sup..crclbar.是一种药用可接受的阴离子。这些化合物可用于制备用于治疗涉及Tachykinin系统的病理条件的药物。