Novel 1,3 - dihydro - 2H - imidazo[4,5 - b]quinolin - 2 - one derivatives of formula
wherein R is hydrogen, C1-6 alkyl, C3-6cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C1-6alkyloxy, C5-6cycloalkyloxy, C1-6alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C1-6alkyl; and
C=X is a radical of formula
or
the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.
式中的新型 1,3 - 二氢 - 2H -
咪唑并[4,5 - b]
喹啉 - 2 - 一衍
生物
其中 R 是氢、C1-6 烷基、C3-6 环烷基、任选被 1 至 3 个各自独立选自卤代、羟基、C1-6 烷氧基、C5-6 环烷氧基、C1-6 烷基或三
氟甲基的取代基取代的苯基;
吡啶基;任选被卤代或 C1-6 烷基取代的
噻吩基;以及
C=X 是式中的一个自由基
或
药学上可接受的加成盐及其立体异构体形式,所述化合物是
磷酸二酯酶 III 和 IV 的强效
抑制剂,可用于治疗过敏性疾病、特应性疾病和相关疾病。其制备过程中的中间体。含有上述化合物作为活性成分的药物组合物。制备所述化合物和药物组合物的方法。