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US 11,141,452 B2Granted
Bifunctional compounds for relief of pain comprising an opioid receptor agonist moiety and a NK1 receptor antagonist moiety and methods for treating pain
AssigneeArizona Board of Regents on Behalf of the University of Arizona
InventorsVictor J. Hruby, Aswini K. Giri
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Abstract
A compound for treatment of pain comprising a single multivalent/multifunctional ligand with agonist activity at opioid receptors and with antagonist activity at NK-1 receptors, joined by a linker. Also disclosed is a pharmaceutical compound comprising the above compound in a pharmaceutically acceptable carrier.
Claims15
A compound comprising an opioid receptor agonist moiety that is linked to a NK1 receptor antagonist moiety, wherein said compound is of the formula:
- A-B
- wherein A is said opioid receptor agonist moiety, and wherein B is said NK1 receptor antagonist moiety of the formula:
- and wherein said opioid receptor agonist moiety A is a moiety of the formula:
- H-Tyr′-D-NRAla-NRGly-Phe′-[AA]a-,
- wherein
- each of R′ is independently H, CH3, or CF3;
- X is NH or NMe;
- a is 0 or 1;
- AA is Nle, β-Ala, γ-Abu, Ahx, 4-Amb, 4-Abz, 4-Apac, or 4-Ampa;
- Tyr′ is Tyr or Dmt;
- Phe′ is N-methylated Phe, or Phe(4-F);
- and
- R is H or methyl provided at least one of R on said opioid receptor agonist is methyl or Phe′ is N-methylated Phe.
10 more elements
Dependencies are inferred from the claim text.