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    • 1. 发明申请
    • AROMATIC HYDROXYETHERS
    • 芳香羟基
    • WO1996031476A1
    • 1996-10-10
    • PCT/GB1996000854
    • 1996-04-04
    • RHONE-POULENC RORER LIMITEDCOX, Paul, JosephNEWTON, Christopher, GregoryPALFREYMAN, Malcolm, Norman
    • RHONE-POULENC RORER LIMITED
    • C07D213/75
    • C07D213/75C07D213/61C07D213/81C07D213/89
    • This invention is directed to physiologically active compounds of formula (I), wherein R is optionally substituted alkyl, R is optionally substituted aryl or heteroaryl, A is cycloalkyloxy, cycloalkylalkoxy or alkoxy carrying one or more hydroxy moieties, the cycloalkyl moieties optionally further substituted by one or more methylene or lower alkyl groups, Q , Q and Q each represents CH or CX or nitrogen, Z is oxygen or sulphur, Z is an NH or methylene and X is halogen and N-oxides thereof, and their esters, and prodrugs, pharmaceutically acceptable salts, and solvates (e.g. hydrates), thereof. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions containing compounds of formula (I), their pharmaceutical use and methods for their preparation.
    • 本发明涉及式(I)的生理活性化合物,其中R 1是任选取代的烷基,R 2是任选取代的芳基或杂芳基,A是环烷氧基,环烷基烷氧基或含有一个或多个羟基部分的烷氧基, 任选进一步被一个或多个亚甲基或低级烷基取代的环烷基部分,Q 1,Q 2和Q 3各自表示CH或CX或氮,Z 1为氧或硫,Z 2为氧或硫, 是NH或亚甲基,X是卤素及其N-氧化物及其酯及其前药,药学上可接受的盐和溶剂合物(例如水合物)。 这些化合物抑制TNF的产生或生理作用并抑制环AMP磷酸二酯酶。 本发明还涉及含有式(I)化合物的药物组合物,其药物用途及其制备方法。