Importance

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Abstract

Compounds of formula (I), ##STR1## wherein {character pullout} is a single or double bond; Z is NH, methylene, a (C.sub.2 -C.sub.6)alkylene chain optionally branched and/or unsaturated and/or interrupted by a (C.sub.5 -C.sub.7)cycloalkyl residue; A is phenyl or heterocycle optionally substituted or a COR.sub.4 group wherein R.sub.4 is hydroxy, (C.sub.1 -C.sub.6)-alkoxy, amino optionally substituted; R is a (C.sub.1 -C.sub.6)alkyl or polyfluoro(C.sub.1 -C.sub.6)alkyl group; R.sub.1 is absent when {character pullout} is a double bond or, when {character pullout} is a single bond, is (a) hydrogen; (b) (C.sub.1 -C.sub.6)alkyl optionally substituted; (c) --COR.sub.6 wherein R.sub.6 is hydrogen, aryl, aryl-(C.sub.1 -C.sub.6)alkyl, amino optionally alkylated or monohydroxylated, hydroxy, (C.sub.1 -C.sub.4)alkoxy, carboxy, (C.sub.1 -C.sub.4)alkoxycarbonyl, formula (1), or (C.sub.1 -C.sub.4)alkyl optionally substituted by heterocycle; (d) (C.sub.1 -C.sub.4)-alkylsulfonyl; R.sub.2 represents two hydrogen atoms or a group --O when {character pullout} is a single bond, or, when {character pullout} is a double bond, R.sub.2 is hydrogen, cyano, (C.sub.1 -C.sub.4)alkoxycarbonyl, amido, optionally substituted aryl or heterocycle, (C.sub.1 -C.sub.8)alkyl, (C.sub.2 -C.sub.8)alkenyl or (C.sub.2 -C.sub.8)alkynyl optionally branched and/or substituted; aryloxy, heterocyclyloxy, aryl-(C.sub.1 -C.sub.4)alkoxy, heterocyclyloxy-(C.sub.1 -C.sub.4)alkoxy, amino substituted by one or two (C.sub.1 -C.sub.4)-alkyl group(s), arylamino, heterocyclylamino, aryl-(C.sub.1 -C.sub.4)alkylamino, heterocyclyl-(C.sub.1 -C.sub.4)-alkylamino; R.sub.3 is hydrogen, or a (C.sub.1 -C.sub.8)alkyl, (C.sub.2 -C.sub.8)alkenyl or (C.sub.2 -C.sub.8)alkynyl group optionally substituted, and optionally interrupted; the N.fwdarw.O derivatives of the compounds of formula (I) and the pharmaceutically acceptable salts thereof are PDE 4 inhibitors.

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First Claim