Potent and selective inhibitors of monoamine transporters; method of making; and use thereof
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsAmy Hauck Newman, Oluyomi M. Okunola-Bakare, Jianjing Cao
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Abstract
Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.
Claims17
A method for treating substance use disorders, comprising:
- providing a therapeutically effective amount of a compound of Formula V or salt thereof to a patient in need of such treatment
- wherein
- R5 is 3-phenylpropyl, -CH2CH(OH)CH3, or -CH2CH(OH)CH2Ph;
- X is independently chosen at each occurrence from halogen, hydroxyl, amino, nitro, cyano, C1-C6 alkyl, —COOH, —CHO, —CONH2, C1-C6alkoxy, C2-C6alkanoyl, mono- or di-C1-C2alkylamino, C1-C2haloalkyl, or C1-C2haloalkoxy;
- Y is S, S(O), or S(O)2;
- and
- Z is O, S, or 2H.
A method for treating substance use disorders, comprising:
- providing a therapeutically effective amount of a compound of Formula V or salt thereof to a patient in need of such treatment
- wherein
- R5 is 3-phenylpropyl, -CH2CH(OH)CH3, or -CH2CH(OH)CH2Ph;
- X is independently chosen at each occurrence from hydroxyl, amino, nitro, cyano, C1-C6 alkyl, —COOH, —CHO, —CONH2, C1-C6alkoxy, C2-C6alkanoyl, mono- or di-C1-C2alkylamino, C1-C2haloalkyl, or C1-C2haloalkoxy;
- Y is O, S, S(O), or S(O)2;
- and
- Z is O or S.
Dependencies are inferred from the claim text.