Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists
AssigneeNova Pharmaceutical Corporation
InventorsWaclaw J. Rzeszotarski, Babu J. Mavunkel
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Abstract
A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a longacting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R.sub.1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.
Claims22
A potent, selective opioid kappa receptor agonist or a delta or mu antagonist compound of the formula:
- ##STR3## wherein R is cyclopropylmethyl and R.sub.1 is selected from the group consisting of phenylethyl, naphthyl, tetrahydronaphthyl, phenylpropyl, cyclohexyl, cyclopentyl, iminoaminomethylphenyl, dimethylphenyl, t-butyl, trifluormethylphenyl, cyanophenyl, 4-benzimidazolyl, 5-benzimidazolyl, or ##STR4## wherein R.sub.2 is selected from the group consisting of hydrogen, halogen, hydroxy, nitro, methoxy, methyl, trifluormethyl or amino and the pharmaceutically acceptable salts thereof.
A process of relieving pain in an animal in need thereof which comprises administering said compound of claim 1 or 15 parenterally, nasally, orally, rectally or a combination thereof to said animal in need thereof.
The potent, kappa selective opioid receptor agonist compound of the formula:
- ##STR5## wherein R is cyclopropylmethyl and wherein R.sub.1 is 2-phenylethyl or 3-phenylpropyl and the pharmaceutically acceptable salts thereof.
A potent, delta selective opioid receptor antagonist compound having the formula:
- ##STR6## wherein R is cyclopropylmethyl and R.sub.1 is t-butyl, cyclohexyl or cyclopentyl and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.