Nonpeptide kappa opioid receptor antagonists
AssigneeThe Board of Trustees of the University of Illinois
InventorsWilliam Dunn, Ludwig Bauer, Hemendra N. Bhargava
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Abstract
The compounds of structural formulae (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents, is disclosed. A compound of formula (I) or (II) is an agonist for the μ and δ opioid receptors, an antagonist for the κ opioid receptor, and has high affinity at all three receptors. A compound of formula (I) or (II) has utility in a variety of therapeutic and research areas where κ opioid receptor antagonism is beneficial, including the treatment of opiate addiction or pain, or in a method of stimulating an immune system of a human.
Claims19
A compound of formula (I) or (II)
- wherein R1 is selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C3-8cycloalkyl, and aryl, and
- R3 is selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, and C2-6alkynyl;
- a pharmaceutically acceptable salt or hydrate thereof.
A compound having a formula (I) or (II)
17-Methyl-6,7-dehydro-3,14-hydroxy-4,5α-epoxy-6,7:5′,4′(6,7:3′,4′)-pyrazolomorphinan, a physiologically acceptable salt or hydrate thereof.
Dependencies are inferred from the claim text.