SHI YI-QUN,SHARMA SHUBH D,DODD JOHN H,YANG WEI,CHEN XIN
申请号:
NZ59661710
公开号:
NZ596617A
申请日:
2010.06.07
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
596617 Disclosed are melanocortin receptor(MC4-R)-specific cyclic peptides. For treating MC4-R mediated conditions such as erectile disfunction. The melanocortin receptor-specific cyclic peptides are of the formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes. The cyclic peptides also conform to the formula Z-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Y, which is an amino acid sequence as defined in the specification, with exemplified compounds including: Ac-Arg-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-NH2 Ac-Arg-cyclo(Asp-Ser-D-Phe-Arg-Trp-Lys)-NH2 Ac-Arg-cyclo(Asp-Ala- D-Phe-Cit-Trp-Lys )-NH2 Ac-Arg-cyclo(Asp-His-D-Phe-Lys-Trp-Lys)-NH2 Ac-Arg-cyclo(Asp-Lys- D-Phe-Lys-Trp-Lys)- NH2 Ac-Arg-cyclo(Asp-Nle- D-Phe-Arg-Trp-Lys)- NH2 Ac-Arg-cyclo(Asp-Thr(Bzl)-D-Phe-Arg- Trp-Lys)-NH2 and Ac-Arg-cyclo(Asp-lle-D-Phe-Arg-Trp-Lys)-NH2