The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 28, 2024

Filed:

May. 23, 2019
Applicant:

Provincial Health Services Authority, Vancouver, CA;

Inventors:

François Bénard, Vancouver, CA;

Kuo-Shyan Lin, Vancouver, CA;

Chengcheng Zhang, Vancouver, CA;

Zhengxing Zhang, Vancouver, CA;

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 51/00 (2006.01); A61K 47/08 (2006.01); A61K 51/04 (2006.01); A61K 51/08 (2006.01); A61M 36/14 (2006.01); A61P 35/00 (2006.01);
U.S. Cl.
CPC ...
A61K 51/088 (2013.01); A61K 47/08 (2013.01); A61K 51/0482 (2013.01); A61P 35/00 (2018.01);
Abstract

A compound is provided comprising a melanocortin 1 receptor (MC1R) targeting peptide (MC1RTP), a radiolabeling group, and a linker joining the MC1RTP to the radiolabeling group. The MC1RTP is linear or cyclized, and comprises a sequence of Formula I or Formula II: Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa(I) or Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa(II). Xaais L-/D-Nle, L-/D-Nle, L-/D-Ala, L-/D-Leu, L-/D-Ile, D-Ile, L-/D-Cys, L-/D-Met, L-/D-Phe, L-/D-Trp, L-/D-Val, L-/D-Nal, L-/D-2-Nal, Gly, L-/D-α-aminobutryic acid, L-/D-norvaline, or L-/D-homonorleucine. Xaaand Xaaare L-/D-Cys, L-/D-Asp, L-/D-Glu, L-/D-2-Aad, L-/D-3-Aad, L-/D-Pra, L-/D-Hpg, or L-/D-Bpg. Xaaand Xaaare L-/D-Cys, L-/D-Lys, L-/D-Orn, L-/D-Dab, L-/D-Dap, L-/D-Lys(N), L-/D-Orn(N), L-/D-Dab(N), L-/D-Dap(N), L-/D-2-(5'-azidopentyl)alanine, or L-/D-2-(6′-azidohexyl)alanine. Xaais L-/D-His, Pro, beta-(1,2,3-triazol-4-yl)-L-alanine, beta-(1,2,3-triazol-4-yl)-D-alanine, 1,2,4-triazole-3-alanine, or 1,2,4-triazole-3-D-alanine. Xaais L-/D-Phe, L-/D-2-Nal, L-/D-Phe(4-F), L-/D-Phe(4-Cl), L-/D-Phe(4-Br), L-/D-Phe(4-I), L-/D-Phe(4-NH2), or L-/D-Phe(4-NO2). Xaais L-/D-Arg, L-/D-hArg), Leu, L-/D-Agb, or L-/D-Agp. Xaais L-/D-Trp, L-/D-Phe, L-/D-Trp(5-Br), L-/D-Trp(5-OCH3), L-/D-Trp(6-F), L-/D-Trp(5-OH) or L-/D-Trp(CHO). One or more amino acid residues of the MC1RTP is alpha N-methylated, wherein 1, 2, 3 or 4 of Xaa, Xaa, Xaaand Xaais alpha N-methylated or wherein 1, 2, 3 or 4 of Xaa, Xaa, Xaaand Xaais alpha N-methylated. The linker comprises an albumin-binding group.


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