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Abstract

Compounds of the formula: ##STR1## are provided, which are selective kappa opioid receptor antagonists, wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans (C.sub.4 -C.sub.5) alkenyl, allyl or furan-2-ylalkyl; R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H or (C.sub.1 -C.sub.5)alkyl; R.sup.4 is CH.sub.2 (methylene) or C.dbd.O (carbonyl), R.sup.5 is CH.sub.2, C.dbd.O or C.dbd.NH (imino) and R.sup.6 is (C.sub.1 -C.sub.4)alkyl or NH(C.sub.1 -C.sub.4)alkyl, optionally substituted by a non-terminal (C.sub.1 -C.sub.2)alkyl group or by N(R.sup.7) (R.sup.8) wherein R.sup.7 and R.sup.8 are individually H or (C.sub.1 -C.sub.3) alkyl, with the proviso that one of R.sup.4 or R.sup.5 is CH.sub.2, and the pharmaceutically acceptable salts thereof.

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First Claim