Importance

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Abstract

Compounds of formula 1, ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, CF.sub.3, NO.sub.2, CN, halogen, C.sub.1 -C.sub.8 -alkyl, or C.sub.1 -C.sub.8 -alkoxy; R.sup.2, R.sup.3, and R.sup.4 independently of one another are hydrogen, C.sub.1 -C.sub.8 -alkyl, hydroxy, NO.sub.2, CN, C.sub.1 -C.sub.8 -alkoxyl, CF.sub.3, or halogen; R.sup.5 and R.sup.6 independently of one another are hydrogen or a group consisting of C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl, C.sub.3 -C.sub.8 -alkynyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.6 -alkylene, C.sub.5 -C.sub.8 -cycloalkenyl, C.sub.5 -C.sub.8 -cycloalkenyl-C.sub.1 -C.sub.6 -alkylene, C.sub.6 -C.sub.10 -aryl, and C.sub.6 -C.sub.10 -aryl-C.sub.1 -C.sub.6 -alkylene, each optionally substituted by a group consisting of C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, halogen, C.sub.1 -C.sub.6 -alkyloxy, --NH.sub.2, --NH(C.sub.1 -C.sub.4 -alkyl), --N(C.sub.1 -C.sub.4 -alkyl).sub.2, hydroxy, .dbd.O, --COOH, --CO--OC.sub.1 -C.sub.4 -alkyl, --CONH.sub.2, --CONH(C.sub.1 -C.sub.4 -alkyl), --CON(C.sub.1 -C.sub.4 -alkyl).sub.2, and CF.sub.3, or R.sup.5 and R.sup.6 together with the nitrogen atom are a saturated or unsaturated 5-, 6-, 7-, or 8-membered heterocyclic group optionally containing one or two further heteroatoms consisting of sulfur, oxygen, and nitrogen, and optionally mono-, di-, or trisubstituted by a group consisting of C.sub.1 -C.sub.4 -alkyl, hydroxy, .dbd.O, --COOH, --CO--OC.sub.1 -C.sub.4 -alkyl, --CONH.sub.2, --CONH(C.sub.1 -C.sub.4 -alkyl), --CON(C.sub.1 -C.sub.4 -alkyl).sub.2, halogen, and benzyl; X is oxygen, --NH--, --N(CHO)--, --N(CO--C.sub.1 -C.sub.6 -alkyl), --N(C.sub.1 -C.sub.6 -alkyl), or --N(C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkylene); and A is a group consisting of C.sub.1 -C.sub.6 -alkylene, C.sub.2 -C.sub.6 -alkenylene, and C.sub.3 -C.sub.6 -alkynylene, each optionally substituted by a group consisting of halogen, .dbd.O, and hydroxy, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of making such compounds; pharmaceutical compositions thereof, and their use in treating or preventing certain diseases.

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First Claim