| 摘要 |
Melanocortin receptor-specific cyclic peptides of the formula;
where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes. |
| 主权项 |
1. A cyclic peptide of the formula:
Z-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Y or a pharmaceutically acceptable salt thereof, wherein: Z is H or an N-terminal group; Xaa1 is an amino acid with a side chain including a linear or branched alkyl, cycloalkyl, cycloheteroalkyl, aryl or heteroaryl; Xaa2 and Xaa6 are L- or D-isomer amino acids wherein the side chains thereof comprise a cyclic bridge; Xaa3 is L- or D-Pro, optionally substituted with hydroxyl, halogen, sulfonamide, alkyl, —O-alkyl, aryl, alkyl-aryl, alkyl-O-aryl, alkyl-O-alkyl-aryl, or —O-aryl, or Xaa3 is an L- or D-isomer of an amino acid with a side chain including at least one primary amine, secondary amine, alkyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, ether, sulfide, or carboxyl; Xaa4 is an L- or D-isomer amino acid with a side chain including phenyl, naphthyl or pyridyl, optionally substituted with one or more substituents independently selected from halo, (C1-C10)alkyl-halo, (C1-C10)alkyl, (C1-C10)alkoxy, (C1-C10)alkylthio, aryl, aryloxy, nitro, nitrile, sulfonamide, amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, and alkoxy-carbonyl; Xaa5 is L- or D-Pro or Xaa5 is an L- or D-isomer amino acid with a side chain including at least one primary amine, secondary amine, guanidine, urea, alkyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, or ether; Xaa7 is optionally present, and if present is from one to three L- or D-isomer amino acid residues; and Y is a C-terminal group. |
