Melanocortin receptor ligands

摘要

The present invention is directed to compounds according to formula,
(R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1,
and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.

主权项

1. A compound according to formula (I):
(R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1 wherein:
A1 is Arg, D-Arg, Cha, hCha, Chg, D-Chg, Ile, Leu, 2-Nal, Nle, Phe, D-Phe, hPhe, Val or deleted; A2 is Cys, Pen or Asp; A3 is D-Ala, D-Abu, D-Cha, D-Ile, D-Leu, D-Tle, or D-Val; A4 is His or 3-Pal; A5 is D-Phe, D-2-Nal or D-(Et)Tyr; A6 is Arg or hArg; A7 is Trp, 2-Nal, Bal, Bip or D-Trp; A8 is Gly, Ala, β-Ala, Gaba, Apn, Ahx or deleted; A9 is Cys, D-Cys, Pen or Lys; A10 is Thr or deleted; and R2 and R3 is, independently for each occurrence, H or acyl; R1 is —OH or —NH2;
provided that(I). when A2 is Cys or Pen, then A9 is Cys, D-Cys, or Pen;(II). when A2 is Asp, then A9 is Lys;(III). when A1 is deleted, then R2 and R3 cannot both be H;or a pharmaceutically acceptable salt thereof.