18-02-2016 дата публикации
Номер: US20160046688A1
Provided herein are stable peptide analogs of the native alpha-melanocyte stimulating hormone (α-MSH) having selectivity for the melanocortin 1 receptor (MC1R). Also provided herein are pharmaceutical preparations of the α-MSH peptide analogs, as well as methods of using these analogs in the treatment of medical and veterinary conditions involving MC1R. 1. A substantially pure compound that selectively binds melanocortin 1 receptor (MC1R) , said compound comprising a polypeptide having the sequence:{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12', '13, 'XaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaa,'}{'sub': '1', 'claim-text': [{'sub': '2', 'Xaais D-Pro, D-Ala or D-Lys;'}, {'sub': '3', 'Xaais D-Lys, D-Orn, D-Nle, D-Ala or D-Lys;'}, {'sub': '4', 'Xaais Gly, or D-Ala;'}, {'sub': '5', 'Xaais D-Trp, Trp, D-3-benzothienyl-Ala, D-5-hydroxy-Trp, D-5-methoxy-Trp, D-Phe, or D-Ala;'}, {'sub': '6', 'Xaais D-Arg, D-His, or D-Ala;'}, {'sub': '7', 'Xaais D-Cha, D-Phe, Phe, D-4-fluoro-Phg, D-3-pyridyl-Ala, D-Thi, D-Trp, D-4-nitro-Phe, or D-Ala;'}, {'sub': '8', 'Xaais D-His, His, D-Arg, Phe, or D-Ala;'}, {'sub': '9', 'Xaais D-Glu, D-Asp, D-citrulline, D-Ser, or D-Ala;'}, {'sub': '10', 'Xaais D-Met, D-buthionine, D-Ile, or D-Ala;'}, {'sub': '11', 'Xaais D-Ser, D-Ile or D-Ala;'}, {'sub': '12', 'Xaais D-Tyr, D-Ser, or D-Ala; and'}, {'sub': '13', 'Xaais D-Ser or D-Ala;'}], 'wherein Xaais D-Val, D-Ala or D-Lys;'}{'sub': 1-13', '1-3', '1-13, 'wherein no more than one Xaais D-Ala except when Xaaare all D-Ala, and no more than one Xaais an L-amino acid;'}or a pharmaceutically acceptable salt thereof.2. The compound of claim 1 , said compound comprising a polypeptide having the sequence:{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12', '13', '1, 'claim-text': [{'sub': '2', 'Xaais D-Pro;'}, {'sub': '3', 'Xaais D-Lys, D-Orn or D-Nle;'}, {'sub': '4', 'Xaais Gly;'}, {'sub': '5', 'Xaais D-Trp, Trp, D-3-benzothienyl-Ala, D-5-hydroxy-Trp, D-5-methoxy-Trp, or D-Phe ...
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