Growth hormone releasing peptides
Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs: R 1 -A 1 -A 2 -A 3 -A 4 -A 5 -R 2 (I) wherein: A 1 is Aib, Apc or Inp; A 2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A 3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A 4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A 5 is Apc, Dab, Dap, Lys, Orn, or deleted; R 1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R 2 is OH or NH 2 ; and pharmaceutical compositions and methods of use thereof.
1. A compound selected from the group consisting of:
H-Inp-D-Bal-D-Trp-Phe-Apc-NH 2 ;
H-Inp-D-Bal-D-Trp-Phe-Lys-NH 2 ;
H-Inp-D-2Nal-D-Trp-Phe-Apc-NH 2 ;
H-Inp-D-Bal-D-Trp-Taz-Apc-NH 2 ;
H-Inp-D-Bal-D-Trp-2Thi-Apc-NH 2 ; and
pharmaceutically acceptable salts thereof.
2. A compound which is H-Inp-D-Bal-D-Trp-Phe-Apc-NH 2 , or a pharmaceutically acceptable salt thereof.
3. A compound which is H-Inp-D-Bal-D-Trp-Phe-Lys-NH 2 , or a pharmaceutically acceptable salt thereof.
4. A compound which is H-Inp-D-2Nal-D-Trp-Phe-Apc-NH 2 , or a pharmaceutically acceptable salt thereof.
5. A compound which is H-Inp-D-Bal-D-Trp-Taz-Apc-NH 2 , or a pharmaceutically acceptable salt thereof.
6. A compound which is H-Inp-D-Bal-D-Trp-2Thi-Apc-NH 2 , or a pharmaceutically acceptable salt thereof.
7. A pharmaceutical composition comprising the compound of any one of claims 1 to 6 , and a pharmaceutically acceptable carrier.