Tri-substituted (aryl or heteroaryl) derivatives and pharmaceuti

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514252, 514255, 514256, 514277, 514332, 514340, 514367, 514383, 514374, 514394, 514427, 514438, 514544, 544242, 544335, 546266, 546339, 5462691, 5462701, 5462717, 5462724, 5462711, 5462697, 5462714, 5462734, 5462727, 5462781, 5462884, 5462811, 5462834, 5462841, 5482686, 5482678, 548179, 548239, 5483101, 5483411, 548562, 549 78, 560104, A61K 3144, C07D40510, C07D40910, C07D21304

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056229771

ABSTRACT:
Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.

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