申请人:A. H. Robins Company, Incorporated
公开号:US04950674A1
公开(公告)日:1990-08-21
A method of inhibiting Type 1 allergic responses in a living animal body with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain known compounds: ##STR1## wherein P is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, CH.sub.2 -- or ##STR2## n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the .alpha. carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one,4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one, 1,4-benzodioxanloweralkyl-2-yl or 1,1'-biphenyl-4-yl and the pharmaceutically acceptable salts thereof.
揭示了一种利用取代杂环胺抑制活体动物体内的1型过敏反应的方法,其中活性剂通常由以下公式表示:其中P为零、一或二;m为一到六(包括六);A选自氢、羟基或氰基;d为零或一;Q为--CH--、CH.sub.2--或n为零或一,当Q为--CH--且n为一时,与相邻碳之一形成双键,但不同时与两个相邻碳形成双键;当n和d同时为零时,在中心杂环胺环的α碳和一个碳之间形成双键;Ar、D和R选自苯基、取代苯基、吡啶基、噻吩基、呋喃基或萘基,此外,R可能具有苄基、取代苄基、环烷基或较低烷基的值,D还可能具有以下值:2H-1-苯并吡喃-2-酮、4-氧代-4H-1-苯并吡喃-2-羧酸较低烷基酯、2,3-二氢-4H-1-苯并吡喃-4-酮、1,4-苯并二氧杂环较低烷基-2-基或1,1'-联苯基-4-基,以及其药学上可接受的盐。