Monoamine reuptake inhibitors
AssigneeResearch Triangle Institute
InventorsFrank Ivy Carroll, Bruce Edward Blough, Philip Abraham
Life of this patent
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Abstract
The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.
Claims41
A compound according to the structure:
- wherein:
- R1-R5 are each independently selected from H, OH, optionally substituted C1-4 alkyl, optionally substituted C1-3 alkoxy, optionally substituted C2-4 alkenyl, optionally substituted C2-4 alkynyl, halo, amino, acylamido, CN, CF3, NO2, N3, CONH2, CO2R12, CH2OR12, NR12R13, NHCOR12, NHCO2R12, CONR12R13;
- C1-3 alkylthio, R12SO, R12SO2, CF3S, and CF3SO2;
- R6 and R7 are each independently H or optionally substituted C1-10alkyl, or R6 and R7 together constitute ═O or ═CH2;
- R8 and R9 are each independently H or optionally substituted C1-10alkyl, wherein at least one of R8 and R9 is optionally substituted C2-C7 alkyl;
- R10, R11, R12, and R13 are each independently H or optionally substituted C1-10alkyl, wherein at least one of R10 and R11 is optionally substituted C3-C10 cycloalkyl;
- and wherein R1 and R8 may be joined to form a cyclic ring;
- or a pharmaceutically acceptable ester, amide, salt, solvate, prodrug, or isomer thereof.
A method for treating or delaying the progression of a disorder responsive to inhibition of monoamine reuptake in a patient, the method comprising administering, to a patient in need thereof, a therapeutically effective amount of at least one compound according to the structure:
- wherein:
- R1-R5 are each independently selected from H, OH, optionally substituted C1-4 alkyl, optionally substituted C1-3 alkoxy, optionally substituted C2-4 alkenyl, optionally substituted C2-4 alkynyl, halo, amino, acylamido, CN, CF3, NO2, N3, CONH2, CO2R12/CH2OR12, NR12R13, NHCOR12, NHCO2R12, CONR12R13;
- C1-3 alkylthio, R12SO, R12SO2, CF3S, and CF3SO2;
- R6 and R7 are each independently H or optionally substituted C1-10alkyl, or R6 and R7 together constitute ═O or ═CH2;
- R8 and R9 are each independently H or optionally substituted C1-10alkyl;
- R10, R11, R12, and R13 are each independently H or optionally substituted C1-10alkyl, wherein at least one of R10 and R11 is optionally substituted C3-C10 cycloalkyl;
- and wherein R1 and R8 may be joined to foam a cyclic ring;
- or a pharmaceutically acceptable ester, amide, salt, solvate, prodrug, or isomer thereof.
Dependencies are inferred from the claim text.