Dopamine D3 receptor selective antagonists/partial agonists and uses thereof
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsAmy Hauck Newman, Vivek Kumar, Anver Basha Shaik
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Abstract
Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.
Claims17
A method of treating pain, comprising providing to a human in need thereof a therapeutically effective amount of an opioid analgesic or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of a compound of Formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof
- wherein
- Ar is a heteroaryl which may be optionally substituted with 1, 2, or 3 substituents where each substituent independently is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, —OH, —COOH, amino, nitro, C2-C3alkanoyl group, mono- or di- C1-C3alkylamino, or halogen, or Ar is a 3,4-methylenedioxy-phenyl group;
- n is 1 or 2;
- m is 1 or 2;
- R1 is H or halogen;
- R2 is H, C1-C3alkoxy, or halogen;
- R3 is H, halogen or C1-C3alkoxy;
- R4 is H, —OH, or halogen;
- R5 is H, —OH, or halogen;
- and
- is a single bond or a double bond,
- with the provisos a) and b) for Formula (I)
- a) when R1 is H then at least one of R2 and R3 is not H;
- and
- b) when one or both of R2 and R3 is H then R1 is not H.
Dependencies are inferred from the claim text.