摘要 |
The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R<SUP>1 </SUP>is H, alkyl, cycloalkyl, cylcoalkylalkyl-, -CH<SUB>2</SUB>F, -CHF<SUB>2</SUB>, -CF<SUB>3</SUB>, -C(O)alkyl or -C(O)NR<SUP>18</SUP>R<SUP>19</SUP>; R<SUP>3 </SUP>and R<SUP>4</SUP>H, alkyl, hydroxyalkyl or -C(O)Oalkyl; R<SUP>5 </SUP>and R<SUP>6 </SUP>are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, -CH<SUB>2</SUB>F, -CHF<SUB>2</SUB>, -CF<SUB>3</SUB>, -C(O)OH or -C(O)Oalkyl; R<SUP>7 </SUP>is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R<SUP>17</SUP>-phenyl)alkyl or -CH<SUB>2</SUB>-C(O)-O-alkyl; and R<SUP>8 </SUP>comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R<SUP>7 </SUP>and R<SUP>8 </SUP>and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.
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