US 11,041,010 B2 · Hybrid peptidomimetics for use in neuropathic pain

Abstract

The invention pertains to novel hybrid peptidomimetics, pharmaceutical composition comprising thereof and use thereof in the treatment of neuropathic pain. The hybrid peptidomimetics according to the invention are comprised of two components: an opioid receptor agonist (OP) and a MC4 receptor antagonist, connected by a linker. The compounds of such a structure will allow to activate opioid receptors with simultaneous blocking of melanocortin type 4 receptors (MC4), which results in enhancing efficiency of the opioid therapy in neuropathic pain.

Claims5

Dependent claims

A compound of the general formula:

A1-A2-A3-A4-X-Nle-cyclo[Asp-His-D-Nal(2′)-Arg-Trp-Lys]-NH2wherein:
A1 is a Tyr, DMT (2,6-dimethyltyrosine), or N-Me-Tyr (N-methyltyrosine) residue
A2 is a D-Ala, D-Thr, D-Ser, D-Leu, D-Arg, D-Lys, or D-Pro residue
A3 may be absent or is a Gly or Phe residue
A4 is a Phe or Trp residue
X is-NH—(CH2)n—CO—, or —NH—(CH2)n—CO—NH—(CH2)m—CO—, wherein n and m are integers from 1 to 8;
or a pharmaceutically acceptable salt or hydrate thereof.

4 more elements

Dependencies are inferred from the claim text.

Hybrid peptidomimetics for use in neuropathic pain

Life of this patent

Hybrid peptidomimetics for use in neuropathic pain

Life of this patent

Abstract

Claims5