Delta opioid receptor-selective benzylidene-substituted morphinans
AssigneeRegents of the University of Minnesota
InventorPhilip S. Portoghese
Life of this patent
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Abstract
A delta-selective opioid receptor antagonist is provided of the formula: wherein R1 is (C1-C3)alkyl, C3-C6(cycloalkyl)alkyl, C5-C7(cycloalkenyl)alkyl, aryl, aralkyl, trans-(C4-C5)alkenyl, allyl or furan-2-ylalkyl, R2 is H, OH or O2C(C1-C5)alkyl; R3 is H, (C1-C5)alkyl; or ((C1-C5)alkyl)-C═O; and R4 and R5 are individually H, F, Cl, Br, NH2, NO2, (C1-C5)alkyl or (C1-C5)alkoxy, or R4 and R5 together are benzo or dioxymethylene; and the pharmaceutically acceptable salts thereof.
Claims1
A method for blocking δ-opioid receptors in mammalian tissue comprising contacting said receptors with an amount of a compound of the formula:
- wherein R1 is (C1-C5)alkyl, C3-C6(cycloalkyl)alkyl, C5-C7(cycloalkenyl)alkyl, (C6-C10)aryl, (C6-C10aryl(C1-C5)alkyl, trans(C4-C5)alkenyl, allyl or furan-2-ylalkyl;
- R2 is H, OH or O2C(C1-C5)alkyl;
- R3 is H, (C1-C5)alkyl, or ((C1-C5)alkyl)C═O;
- and R4 and R5 are individually H, F, Cl, Br, NH2, NO2, (C1-C5)alkyl or (C1-C5)alkoxy, or R4 and R5 together are benzo or dioxymethylene;
- and the pharmaceutically acceptable salts thereof, wherein the amount is effective to block δ-opioid receptors in said tissue.
Dependencies are inferred from the claim text.