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Abstract

The present invention discloses that compounds having the formula: ##STR1## wherein Z represents the atoms necessary to complete a five-membered or six-membered heterocyclic ring; D is a 1-piperid-4-yl moiety, a --Q--NH-- moiety, or a --Q--S-- moiety; Q is a bridging group; R.sup.1 is H, R.sup.3 or R.sup.4 ; R.sup.2 is R.sup.3 ; each of A.sup.1 and A.sup.2 is H or A.sup.1 and A.sup.2 taken together form a second bond between the carbon atoms bearing A.sup.1 and A.sup.2 ; X is S, N--CN, CHNO.sub.2, O, or NH, provided that when D is a --Q--S--moiety, X is NH; R.sup.3 is selected from the group consisting of substituted or unsubstituted alkyls; substituted or unsubstituted 4-8-membered homocyclic rings; substituted or unsubstituted 4-8-membered heterocyclic rings; substituted or unsubstituted fused multicyclic rings; R.sup.4 is a moiety having the formula: --W--T --W-- is --O--, --S--, --S--S--, --C(O)--O--, --C(O)--S--, --C(O)--N(R.sup.5)--, --N(R.sup.5)--, or CH.dbd.N--; T is selected from the group consisting of substituted or unsubstituted alkyls, substituted or unsubstituted 4-8-membered homocyclic rings, substituted or unsubstituted 4-8-membered heterocyclic rings, substituted or unsubstituted fused multicyclic rings, and proteinaceous transport vectors; R.sup.5 is H, substituted alkyl, or an unsubstituted alkyl and pharmaceutically acceptable salts thereof have analgesic activity. Methods for using these compounds in reducing pain and formulations containing and brain-penetrating derivatives of these compounds are also described.

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First Claim