Vinylogous phenethylamines as neurotransmitter releasers
AssigneeResearch Triangle Institute
InventorsBruce Blough, Ann Decker, Richard Rothman
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Abstract
The disclosure provides monoamine neurotransmitter releaser and/or monoamine uptake inhibitor compounds having biogenic amine transporter activity but lacking substantial activity at 5-HT2 receptor subtypes. The phenethylamine or vinylogous phenethylamine compounds of the disclosure are useful in treating diseases, conditions and/or disorders mediated by activity of one or more of the monoamine neurotransmitters.
Claims12
A method of mediating dopamine transporter (DAT) and norepinephrine transporter (NET) activity with a substrate type releaser, said method comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to the structure of Formula I:
- wherein A is C3-4 alkynyl or C2-4 alkenyl;
- R1-R5 and R9 are each independently selected from H, OH, optionally substituted C1-3 alkyl, optionally substituted C1-2 alkoxy, optionally substituted C2-3 alkenyl, optionally substituted C2-3 alkynyl, halo, amino, CN, CF3, and NO2;
- and R10 and are H or C1-3 alkyl;
- or a pharmaceutically acceptable ester, amide, salt, solvate, prodrug, or stereoisomer thereof.
A method of mediating dopamine transporter (DAT) and norepinephrine transporter (NET) activity with a substrate type releaser, said method comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to the structure of Formula II:
- R1-R5 and R9 are each independently selected from H, OH, optionally substituted C1-3 alkyl, optionally substituted C1-2 alkoxy, optionally substituted C2-3 alkenyl, optionally substituted C2-3 alkynyl, halo, amino, CN, CF3, and NO2;
- R6 and R7 are each independently selected from H or C1-3 alkyl;
- R8 is selected from H, OH, optionally substituted C1-3 alkyl, optionally substituted C1-2 alkoxy, optionally substituted C2-3 alkenyl, optionally substituted C2-3 alkynyl, halo, amino, CN, CF3, and NO2;
- and R10 and R11 are H or C1-3 alkyl;
- or a pharmaceutically acceptable ester, amide, salt, solvate, prodrug, or stereoisomer thereof.
Dependencies are inferred from the claim text.