IP Library › Granted Patent US 7,589,058
Granted Patent B2
US 7,589,058 · App. 10/522,398 · Granted Sep 15, 2009

Ghrelin analogs

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Quick Facts
Patent No.
US 7,589,058
App. No.
10/522,398
Granted
Sep 15, 2009
Kind
B2
Abstract

The invention comprises peptidyl analogs that possess agonist or antagonist ghrelin activity, along with therapeutic and non-therapeutic uses thereof.

Claims (666)

1. A compound according to formula (I):

(R 2 R 3 )-A 1 -A 2 -A 3 -A 4 -A 5 -A 6 -A 7 -A 8 -A 9 -A 10 -A 11 -A 12 -A 13 -A 14 -A 15 -A 16 -A 17 -A 18 -A 19 -A 20 -A 21 -A 22 -A 23 -A 24 -A 25 -A 26 -A 27 -A 28 -R 1   (I),

or a pharmaceutically acceptable salt thereof, wherein:

A 1 is Gly, Aib, Ala, β-Ala, or Acc;

A 2 is Ser, Aib, Act, Ala, Acc, Abu, Ava, Thr, or Val;

A 3 is Ser, Ser(C(O)—R 4 ), Asp(O—R 8 ), Asp(NH—R 9 ), Dap(S(O) 2 —R 10 ), Dab(S(O) 2 —R 11 ), Glu(O—R 6 ), Glu(NH—R 7 ), Thr, Thr(C(O)—R 5 ), or HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O);

A 4 is Phe, Acc, Aic, Cha, 2Fua, 1Nal, 2Nal, 2Pal, 3Pal, 4Pal, hPhe, (X 1 , X 2 , X 3 , X 4 , X 5 )Phe, Taz, 2Thi, 3Thi, Trp, or Tyr;

A 5 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, or Val;

A 6 is Ser, Abu, Acc, Act, Aib, Ala, Gly, Thr, or Val;

A 7 is Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A 8 is Glu, Acc, Aib, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 9 is His, Apc, Aib, Acc, 2Fua, 2Pal, 3Pal, 4Pal, Taz, 2Thi, 3Thi, (X 1 , X 2 , X 3 , X 4 , X 5 -)Phe or deleted;

A 10 is Gln, Acc, Aib, Asn, Asp, Glu, or deleted;

A 11 is Arg, Apc, hArg, Dab, Dap, Lys, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 12 is Val, Abu, Acc, Aib, Ala, Cha, Nva, Gly, Ile, Leu, Nle, Tle, Cha, or deleted;

A 13 is Gln, Acc, Aib, Asn, Asp, Glu, or deleted;

A 14 is Gln, Acc, Aib, Asn, Asp, Glu, or deleted;

A 15 is Arg, hArg, Acc, Aib, Apc, Dab, Dap, Lys, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 16 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 17 is Glu, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 18 is Ser, Abu, Acc, Act, Aib, Ala, Thr, Val, or deleted;

A 19 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 20 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 21 is Pro, Dhp, Dmt, Inc, 3Hyp, 4Hyp, Ktp, Oic, Pip, Thz, Tic, or deleted;

A 22 is Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A 23 is Abu, Acc, Act, Aib, Ala, Apc, Gly, Nva, Val, or deleted;

A 24 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

A 25 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, Val, or deleted;

A 26 is Gln, Aib, Asn, Asp, Glu, or deleted;

A 27 is Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A 28 is Acc, Aib, Apc, Arg, hArg, Dab, Dap, Lys, Orn, HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O), or deleted;

R 1 is —OH, —NH 2 , —(C 1 -C 30 )alkoxy, or NH—X 6 —CH 2 -Z 0 , wherein X 6 is a (C 1 -C 12 )alkyl, (C 2 -C 12 )alkenyl, and Z 0 is —H, —OH, —CO 2 H or —C(O)—NH 2 ;

R 2 and R 3 each is, independently for each occurrence, H, (C 1 -C 20 )alkyl or (C 1 -C 20 )acyl;

R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 each is, independently for each occurrence, (C 1 -C 40 )alkyl, (C 2 -C 40 )alkenyl, substituted (C 1 -C 40 ) alkyl, substituted (C 2 -C 40 ) alkenyl, alkylaryl, substituted alklyaryl, aryl or substituted aryl;

R 12 and R 13 each is, independently for each occurrence, H, (C 1 -C 40 )alkyl, (C 1 -C 40 )acyl, (C 1 -C 30 )alkylsulfonyl, or —C(NH)—NH 2 , wherein when R 12 is (C 1 -C 40 )acyl, (C 1 -C 30 )alkylsulfonyl, or —C(NH)—NH 2 , then R 13 is H or (C 1 -C 40 )alkyl;

n is, independently for each occurrence, 1, 2, 3, 4, or 5;

X 1 , X 2 , X 3 , X 4 , and X 5 each is, independently for each occurrence, H, F, Cl, Br, I, (C 1-10 )alkyl, substituted (C 1-10 )alkyl, aryl, substituted aryl, OH, NH 2 , NO 2 , or CN;

provided that the peptide contains at least one amino acid selected from the groups consisting of:

A 2 is Aib, Acc, or Act;

A 3 is Dap(S(O) 2 —R 10 ), Dab(S(O) 2 —R 11 ), or Glu(NH-Hexyl);

A 5 is Abu, Acc, Aib, Cha, hLeu, Nle, Nva, or Tle;

A 6 is Abu, Acc, Act, or Aib;

A 7 is Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz or Tic;

A 8 is Acc, Aib, Asn, Asp, Dab, Dap, Orn, or HN—CH((CH 2 ) n —N(R 12 R 13 ))—C(O);

A 9 is Aib, Acc, Apc, 2Fua, 2Pal, 3Pal, 4Pal, Taz, 2Thi, 3Thi, or (X 1 , X 2 , X 3 , X 4 , X 5 -)Phe; and

A 10 is Acc or Aib;

and further provided that the peptide is not (Lys 8 )hGhrelin(1-8)-NH 2 or (Arg 8 )hGhrelin(1-8)-NH 2 .

2. The compound of claim 1 , wherein

A 1 is Gly or Aib;

A 2 is Ser, Aib, A5c, Act, or Ava;

A 3 is Ser(C(O)—R 4 ), Glu(O—R 6 ), Glu(NH—R 7 ), Dap(S(O) 2 —R 10 ), or Dab(S(O) 2 —R 11 );

A 4 is Phe;

A 5 is Leu, Acc, Aib, Cha, or hLeu;

A 6 is Ser, Abu, Act, Aib, or Thr;

A 7 is Pro, Dhp, Dmt, 4Hyp, Ktp, Pip, Tic, or Thz;

A 8 is Glu or Aib;

A 9 is His, Aib, Apc, 2Fua, 2Pal, 3Pal, 4Pal, Taz, or 2Thi;

A 10 is Gln or Aib;

A 11 is Arg;

A 12 is Aib, Val or Acc;

A 13 is Gln;

A 14 is Gln;

A 15 is Arg or Orn;

A 16 is Lys or Apc;

A 17 is Glu;

A 18 is Ser;

A 19 is Lys;

A 20 is Lys;

A 21 is Pro;

A 22 is Pro;

A 23 is Ala;

A 24 is Lys;

A 25 is Leu;

A 26 is Gln;

A 27 is Pro; and

A 28 is Arg;

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 2 , wherein

R 2 and R 3 each is, independently, H, Acyl, n-butyryl, isobutyryl, or n-octanoyl;

R 4 is octyl;

R 6 is hexyl;

R 7 is hexyl;

R 10 is octyl; and

R 11 is octyl, wherein

Acc is, independently for each occurrence, A5c or A6c;

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 3 , selected from:

(Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:1)

(Aib 2 , A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Aib 2,6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , A5c 12 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:5)

(Aib 2 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:6)

(Aib 2 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:7)

(Aib 2 , Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Dmt 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(A5c 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Act 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Aib 2 , A5c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2,5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , hLeu 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2,6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 ,Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ktp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:11)

(Aib 2 , 2Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 2Fua 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Apc 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2,9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2,10 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:12)

(Aib 2 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:13)

(A5c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:13)

(3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Dmt 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Aib 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(hLeu 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:13)

(4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Ktp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:16)

(2Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(2Fua 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Apc 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Aib 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Aib 10 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:17)

(Aib 2 , Dap 3 (Octanesulfonyl), A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:18)

(Dap 3 (Octanesulfonyl), A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:19)

(Aib 2,6 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:67)

(Aib 2 , Dap 3 (Octanesulfonyl), A5c 12 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:68)

(Aib 2 , Dap 3 (Octanesulfonyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:69)

(Aib 2 , Dap 3 (Octanesulfonyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:23)

(Aib 2 , Dap 3 (Octanesulfonyl), Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:20)

(Aib 2 , Dap 3 (Octanesulfonyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), Dmt 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:25)

(Aib 2 , Dap 3 (Octanesulfonyl), Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:25)

(A5c 2 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:26)

(Act 2 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:26)

(Aib 2 , Dap 3 (Octanesulfonyl), A5c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:27)

(Aib 2,5 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:27)

(Aib 2 , Dap 3 (Octanesulfonyl), hLeu 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:27)

(Aib 2 , Dap 3 (Octanesulfonyl), Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:27)

(Aib 2,6 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:20)

(Aib 2 , Dap 3 (Octanesulfonyl), Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:20)

(Aib 2 , Dap 3 (Octanesulfonyl), Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:20)

(Aib 2 , Dap 3 (Octanesulfonyl), 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:25)

(Aib 2 , Dap 3 (Octanesulfonyl), Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:25)

(Aib 2 , Dap 3 (Octanesulfonyl), Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:25)

(Aib 2 , Dap 3 (Octanesulfonyl), Ktp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:25)

(Aib 2,8 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:28)

(Aib 2 , Dap 3 (Octanesulfonyl), 2Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), 2Fua 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2 , Dap 3 (Octanesulfonyl), Apc 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2,9 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:24)

(Aib 2,10 , Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:29)

(Dap 3 (Octanesulfonyl), A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:19)

(Dap 3 (Octanesulfonyl), Aib 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:30)

(Dap 3 (Octanesulfonyl), A5c 12 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:31)

(Dap 3 (Octanesulfonyl), A5c 12 ,Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:32)

(Dap 3 (Octanesulfonyl), A5c 12 ,Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:33)

(Dap 3 (Octanesulfonyl), Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:30)

(Dap 3 (Octanesulfonyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), Dmt 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:35)

(Dap 3 (Octanesulfonyl), Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:35)

(Dap 3 (Octanesulfonyl), A5c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:19)

(Dap 3 (Octanesulfonyl), Aib 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:19)

(Dap 3 (Octanesulfonyl), hLeu 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:19)

(Dap 3 (Octanesulfonyl), Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:19)

(Dap 3 (Octanesulfonyl), Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:30)

(Dap 3 (Octanesulfonyl), Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:30)

(Dap 3 (Octanesulfonyl), 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:35)

(Dap 3 (Octanesulfonyl), Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:35)

(Dap 3 (Octanesulfonyl), Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:35)

(Dap 3 (Octanesulfonyl), Ktp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:35)

(Dap 3 (Octanesulfonyl), Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:36)

(Dap 3 (Octanesulfonyl), 2Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), 2Fua 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), Apc 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), Aib 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:34)

(Dap 3 (Octanesulfonyl), Aib 10 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:37)

(Dap 3 (Octanesulfonyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:32)

(Dab 3 (Octanesulfonyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:32)

(Aib 2 , A6c 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:38)

(A6c 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:39)

(Aib 2 , Act 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:40)

(Aib 2 , Act 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:40)

(Aib 2 , 3Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , Dmt 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:42)

(Aib 2 , Thz 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:42)

(Aib 2 , A5c 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:38)

(Aib 2,5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:38)

(Aib 2 , hLeu 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:38)

(Aib 2 , Cha 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:38)

(Aib 2,6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:40)

(Aib 2 , Thr 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:40)

(Aib 2 , Abu 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:40)

(Aib 2 , 4Hyp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:42)

(Aib 2 , Pip 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:42)

(Aib 2 , Dhp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:42)

(Aib 2 , Ktp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:42)

(Aib 2,8 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:43)

(Aib 2 , 2Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , 3Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , 4Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , Taz 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , 2Thi 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , 2Fua 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2 , Apc 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2,9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:41)

(Aib 2,10 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:44)

(Dap 3 (Octanesulfonyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:33)

(Dab 3 (Octanesulfonyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:33)

(Aib 2 , A6c 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:45)

(A6c 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:46)

(Aib 2,6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:47)

(Aib 2 , Act 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:47)

(Aib 2 , 3Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:48)

(Aib 2 , Dmt 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , Thz 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , A5,12, Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:45)

(Aib 2,5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:45)

(Aib 2 , hLeu 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:45)

(Aib 2 , Cha 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:45)

(Aib 2,6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:47)

(Aib 2 , Thr 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:47)

(Aib 2 , Abu 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:47)

(Aib 2 , 4Hyp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , Pip 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , Dhp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , Ktp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2,8 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:50)

(Aib 2 , 2Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:48)

(Aib 2 , 3Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , 4Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , Taz 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , 2Thi 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , 2Fua 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2 , Apc 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2,9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:49)

(Aib 2,10 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:51)

(Aib 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:39)

(Aib 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:52)

(Act 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:52)

(3Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(Dmt 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:54)

(Thz 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:54)

(A5c 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:39)

(Aib 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:39)

(hLeu 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:39)

(Cha 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:39)

(Aib 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:52)

(Abu 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:52)

(4Hyp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:54)

(Pip 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:54)

(Dhp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:54)

(Ktp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:54)

(Aib 8 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:55)

(2Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(3Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(4Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(Taz 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(2Thi 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(2Fua 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(Apc 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(Aib 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:53)

(Aib 1 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:56)

(Aib 6 , A5c 12 , Apc 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:57)

(A5c 5 , A5c 12 , Apc 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:46)

(Act 6 , A5c 12 , Apc 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:57)

(3Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(Dmt 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:59)

(Thz 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:59)

(Aib 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:46)

(hLeu 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:46)

(Cha 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:46)

(Abu 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:57)

(4Hyp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:59)

(Pip 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:59)

(Dhp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:59)

(Ktp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:59)

(Aib 8 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:60)

(2Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(3Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(4Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(Taz 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(2Thi 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(2Fua 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(Apc 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(Aib 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:58)

(Aib 10 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:61)

(Aib 2 , Glu 3 (NH-Hexyl), A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:62)

(Glu 3 (NH-Hexyl), A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:63)

(Aib 2,6 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:64)

(Aib 2 , Glu 3 (NH-Hexyl), Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:64)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), Dmt 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2 , Glu 3 (NH-Hexyl), Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2 , Glu 3 (NH-Hexyl), A5c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:62)

(Aib 2,5 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:62)

(Aib 2 , Glu 3 (NH-Hexyl), hLeu 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:62)

(Aib 2 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2,6 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:64)

(Aib 2 , Glu 3 (NH-Hexyl), Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:64)

(Aib 2 , Glu 3 (NH-Hexyl), Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:64)

(Aib 2 , Glu 3 (NH-Hexyl), 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2 , Glu 3 (NH-Hexyl), Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2 , Glu 3 (NH-Hexyl), Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2 , Glu 3 (NH-Hexyl), Ktp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2,8 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:67)

(Aib 2 , Glu 3 (NH-Hexyl), 2Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), 2Fua 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), Apc 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2,9 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:68)

(Glu 3 (NH-Hexyl), Aib 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:69)

(Glu 3 (NH-Hexyl), A5c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:63)

(Glu 3 (NH-Hexyl), Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:69)

(Glu 3 (NH-Hexyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), Dmt 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:71)

(Glu 3 (NH-Hexyl), Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:71)

(Glu 3 (NH-Hexyl), Aib 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:63)

(Glu 3 (NH-Hexyl), hLeu 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:63)

(Glu 3 (NH-Hexyl), Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:63)

(Glu 3 (NH-Hexyl), Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:69)

(Glu 3 (NH-Hexyl), Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:69)

(Glu 3 (NH-Hexyl), 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:71)

(Glu 3 (NH-Hexyl), Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:71)

(Glu 3 (NH-Hexyl), Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:71)

(Glu 3 (NH-Hexyl), Ktp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:71)

(Glu 3 (NH-Hexyl), Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:36)

(Glu 3 (NH-Hexyl), 2Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), 2Fua 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), Apc 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), Aib 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:70)

(Glu 3 (NH-Hexyl), Aib 10 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:37)

(Aib 2 , Glu 3 (NH-Hexyl), A6c 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:72)

(A6c 5 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:73)

(Aib 2,6 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:74)

(Aib 2 , Glu 3 (NH-Hexyl), Act 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:74)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), Dmt 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:76)

(Aib 2 , Glu 3 (NH-Hexyl), Thz 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:76)

(Aib 2 , Glu 3 (NH-Hexyl), A5c 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:72)

(Aib 2,5 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:72)

(Aib 2 , hLeu 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:38)

(Aib 2 , Glu 3 (NH-Hexyl), Cha 5 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:72)

(Aib 2,6 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:74)

(Aib 2 , Glu 3 (NH-Hexyl), Thr 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:74)

(Aib 2 , Glu 3 (NH-Hexyl), Abu 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:74)

(Aib 2 , Glu 3 (NH-Hexyl), 4Hyp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:76)

(Aib 2 , Glu 3 (NH-Hexyl), pip 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:76)

(Aib 2 , Glu 3 (NH-Hexyl), Dhp 7 , A5c 12 , OM1,5)hGhrelin(1-28)-NH 2 ; (SEQ ID NO:76)

(Aib 2 , Glu 3 (NH-Hexyl), Ktp 7 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:76)

(Aib 2,8 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:77)

(Aib 2 , Glu 3 (NH-Hexyl), 2Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), 4Pal 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), Taz 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), 2Thi 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), 2Fua 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2 , Glu 3 (NH-Hexyl), Apc 9 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2,9 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:75)

(Aib 2,12 , Glu 3 (NH-Hexyl), 4Pal 9 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:143)

(Aib 2,10 , Glu 3 (NH-Hexyl), A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:78)

(Aib 2 , Glu 3 (NH-Hexyl), A6c 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:79)

(Glu 3 (NH-Hexyl), A6c 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:80)

(Aib 2,6 , Glu 3 (NH-Hexyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:81)

(Aib 2 , Glu 3 (NH-Hexyl), Act 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:81)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), Dmt 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:83)

(Aib 2 , Glu 3 (NH-Hexyl), Thz 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:83)

(Aib 2 , Glu 3 (NH-Hexyl), A5c 5,12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:79)

(Aib 2,5 , Glu 3 (NH-Hexyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:79)

(Aib 2 , Glu 3 (NH-Hexyl), hLeu 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:79)

(Aib 2 , Glu 3 (NH-Hexyl), Cha 5 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:79)

(Aib 2,6 , Glu 3 (NH-Hexyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:81)

(Aib 2 , Glu 3 (NH-Hexyl), Thr 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:81)

(Aib 2 , Glu 3 (NH-Hexyl), Abu 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:81)

(Aib 2 , Glu 3 (NH-Hexyl), 4Hyp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:83)

(Aib 2 , Glu 3 (NH-Hexyl), Pip 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:83)

(Aib 2 , Glu 3 (NH-Hexyl), Dhp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:83)

(Aib 2 , Glu 3 (NH-Hexyl), Ktp 7 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:83)

(Aib 2,8 , Glu 3 (NH-Hexyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:84)

(Aib 2 , Glu 3 (NH-Hexyl), 2Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), 4Pal 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), Taz 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), 2Thi 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), 2Fua 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2 , Glu 3 (NH-Hexyl), Apc 9 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2,9 , Glu 3 (NH-Hexyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:82)

(Aib 2,10 , Glu 3 (NH-Hexyl), A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:85)

(Aib 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:85)

(Aib 2 , Glu 3 (O-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:87)

(Aib 2 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:87)

(Dap 3 (1-Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:1)

(Aib 2 , Dap 3 (1-Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:89)

(Aib 1 , Dap 3 (1-Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:88)

(Ava 2 , Dap 3 (1-Octanesulfonyl))hGhrelin(2-28)-NH 2 ; (SEQ ID NO:144)

(Ac-Gly 1 , Aib 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-Hexyl))hGhrelin(1-5)-NH 2 ; (SEQ ID NO:94)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-Hexyl))hGhrelin(1-6)-NH 2 ; (SEQ ID NO:95)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-Hexyl))hGhrelin(1-7)-NH 2 ; (SEQ ID NO:96)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:97)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-Hexyl), Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-Hexyl), Lys 8 )hGhrelin(1-8)-NH 2 ; and (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:99)

(n-Octanoyl-Gly 1 )hGhrelin(1-28)-NH 2 (SEQ ID NO:100):

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 4 , selected from:

(4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:16)

(Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(4Pal)hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Aib 2 , Glu 3 (NH-Hexyl), Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:103)

(Aib 2 , Glu 3 (NH-Hexyl), 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Thr 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:104)

(Aib 2 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:106)

(Aib 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:109)

(Aib 2,6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 ,Act 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(A5c 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Act 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Aib 2 , A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(A6c 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Aib 2 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Dap 3 (Octanesulfonyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:1)

(Aib 2 ,Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:11)

(Aib 2 , Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Glu 3 (NH-Hexyl), 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:66)

(Aib 2,8 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:67)

(Aib 2,12 ,Glu 3 (NH-Hexyl), 4Pal 9 , Orn 15 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:111)

(Aib 2 , Glu 3 (NH-Hexyl), 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2 , Glu 3 (NH-Hexyl), 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:65)

(Aib 2,10 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:12)

(Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:68)

(Ac-Gly 1 , Aib 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-5)-NH 2 ; (SEQ ID NO:94)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-6)-NH 2 ; (SEQ ID NO:95)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-7)-NH 2 ; (SEQ ID NO:96)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:97)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl), Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl), Lys 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; and (SEQ ID NO:99)

(n-Butyryl-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:101)

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 5 , selected from:

(Aib 2 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:11)

(Aib 2,8 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:112)

(Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:113)

(Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:114)

(Ac-Gly 1 , Aib 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-5)-NH 2 ; (SEQ ID NO:94)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-6)-NH 2 ; (SEQ ID NO:95)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-7)-NH 2 ; (SEQ ID NO:96)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:97)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl), Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl), Lys 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; and (SEQ ID NO:99)

(n-Butyryl-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:101)

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 6 , selected from:

(Aib 2 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:11)

(Aib 2,8 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:115)

(Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:114)

(Ac-Gly 1 , Aib 2 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-5)-NH 2 ; (SEQ ID NO:94)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-6)-NH 2 ; (SEQ ID NO:95)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-7)-NH 2 ; (SEQ ID NO:96)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:97)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl), Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2 , Glu 3 (NH-hexyl), Lys 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:98)

(Ac-Gly 1 , Aib 2,10 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; and (SEQ ID NO:99)

(n-Butyryl-Gly 1 , Aib 2 , Glu 3 (NH-hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:101)

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 1 , selected from:

(Aib 2 )hGhrelin(1-28)-NH 2 ; and (SEQ ID NO:10)

(Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:106)

or a pharmaceutically acceptable salt thereof.

9. A compound according to the formula:

(des-Ser 2 )hGhrelin(1-28)-NH 2 or

(des-Gly 1 , des-Ser 2 )hGhrelin(1-28)-NH 2 , or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 , selected from:

(Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Aib 2,6 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(A5c 5 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Aib 2 , Ser 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Ser 3 , Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ser 3 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , Ser 3 , Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , Ser 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ser 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2,4 , Ser 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:117)

(Aib 2 , Ser 3 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:11)

(Aib 2 , Ser 3 , Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Ac-Gly 1 , Aib 2,0 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:118)

(Aib 2,10 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:12)

(n-Butyryl-Gly 1 , Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:119)

(Ac-Gly 1 , Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Aib 2 , Ser 3 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Ac-Gly 1 , Aib 2 , Ser 3 , Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:120)

(Ser 3 , Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:121)

(Ser 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Aib 2 , Ser 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Ser 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15)

(Aib 2 , Ser 3 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:123)

(Aib 2,6 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:124)

(A5c 5 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:125)

(Aib 2 , Thr 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:126)

(Aib 2 , Thr 3 , Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:127)

(Aib 2 , Thr 3 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:128)

(Aib 2 , Thr 3 , Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:124)

(Aib 2 , Thr 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:127)

(Aib 2 , Thr 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:126)

(Aib 2,4 , Thr 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:129)

(Aib 2 , Thr 3 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:127)

(Aib 2,8 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:130)

(Aib 2 , Thr 3 , Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:127)

(Ac-Gly 1 , Aib 2,10 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:131)

(Aib 2,10 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:131)

(n-Butyryl-Gly 1 , Aib 2 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:133)

(Ac-Gly 1 , Aib 2 , Thr 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:133)

(Aib 2 , Thr 3 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:127)

(Ac-Gly 1 , Aib 2 , Thr 3 , Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:134)

(Thr 3 , Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:135)

(Thr 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:136)

(Thr 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:136)

(Thr 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:136)

(Aib 2 , Thr 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:126)

(Thr 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:136)

(Thr 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:137)

(Aib 2 , Thr 3 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:127)

(Aib 2 , Tic 7 )hGhrelin(1-28)-NH 2 ; and (SEQ ID NO:9)

(Ac-Gly 1 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:138)

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , selected from:

(Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Aib 2,6 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(A5c 5 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Aib 2 , Ser 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Ser 3 , Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ser 3 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , Ser 3 , Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , Ser 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ser 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2,4 , Ser 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:117)

(Aib 2 , Ser 3 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:117)

(Aib 2 , Ser 3 , Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Ac-Gly 1 , Aib 2,0 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:139)

(Aib 2,10 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:12)

(n-Butyryl-Gly 1 , Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:140)

(Ac-Gly 1 , Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Aib 2 , Ser 3 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Ac-Gly 1 , Aib 2 , Ser 3 , Arg 8 )hGhrelin(1-8)-NH 2 ; (SEQ ID NO:120)

(Ser 3 , Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:121)

(Ser 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Aib 2 , Ser 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Ser 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15) and

(Aib 2 , Ser 3 , Tic 7 )hGhrelin(1-28)-NH 2 (SEQ ID NO:9);

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 1 , selected from:

(Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:10)

(Aib 2,6 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(A5c 5 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:3)

(Aib 2 , Ser 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2 , Ser 3 , Thz 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ser 3 , Cha 5 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:2)

(Aib 2 , Ser 3 , Abu 6 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:4)

(Aib 2 , Ser 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2 , Ser 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Aib 2,4 , Ser 3 , 4Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:117)

(Aib 2 , Ser 3 , Dhp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Aib 2,8 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:11)

(Aib 2 , Ser 3 , Pip 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Ac-Gly 1 , Aib 2,10 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:139)

(Aib 2,10 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:12)

(n-Butyryl-Gly 1 , Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:119)

(Ac-Gly 1 , Aib 2 , Ser 3 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:93)

(Aib 2 , Ser 3 , Tic 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:9)

(Ac-Gly 1 , Aib 2 , Ser 3 , Arg 1 )hGhrelin(−8)-NH 2 ; (SEQ ID NO:120)

(Ser 3 , Aib 8 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:121)

(Ser 3 , Taz 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 3Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 4 Pal 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Aib 2 , Ser 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:8)

(Ser 3 , 2Thi 9 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:14)

(Ser 3 , 4Hyp 7 )hGhrelin(1-28)-NH 2 ; (SEQ ID NO:15) and

(Aib 2 , Ser 3 , Tic 7 )hGhrelin(1-28)-NH 2 (SEQ ID NO:9);

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 , selected from:

(Aib 2 , Tic 7 )hGhrelin(1-28)-NH 2 ; and (SEQ ID NO:9)

(Ac-Gly 1 , Glu 3 (NH-Hexyl))hGhrelin(1-28)-NH 2 ; (SEQ ID NO:138)

or a pharmaceutically acceptable salt thereof.

14. A compound selected from (Thr 6 )hGhrelin(1-28)-NH 2 (SEQ ID NO:13), (Thr 6 , A5c 12 , Orn 15 )hGhrelin(1-28)-NH 2 (SEQ ID NO:52) or (Thr 6 , A5c 12 , Apc 16 )hGhrelin(1-28)-NH 2 (SEQ ID NO:57) or a pharmaceutically acceptable salt thereof.

15. A pharmaceutical formulation comprising a compound from any one of claims 1 - 13 and 14 with a pharmaceutically acceptable carrier.

16. A method of treating cachexia in an individual in need thereof comprising administering to said individual a compound selected from any one of claims 1 - 13 and 14 or a pharmaceutically acceptable salt thereof in an amount sufficient to treat cachexia.

Assignments (5)
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNOR NAME PREVIOUSLY RECORDED ON REEL 296336 FRAME 0777. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jan 5, 2016
From: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.
To: IPSEN PHARMA S.A.S.
Reel/Frame 037430/0194 →
CORRECTIVE ASSIGNMENT TO CORRECT THE ADDRESS PREVIOUSLY RECORDED ON REEL 023034 FRAME 0251. ASSIGNOR(S) HEREBY CONFIRMS THE ADDRESS SHOULD BE 65 QUAI GEORGES GORSE, 92100 BOULOGNE-BILLANCOURT, FRANCE. Recorded Jan 16, 2013
From: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S.)
To: IPSEN PHARMA S.A.S.
Reel/Frame 029636/0777 →
CHANGE OF NAME Recorded Jul 31, 2009
From: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S.)
To: IPSEN PHARMA S.A.S.
Reel/Frame 023034/0251 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2005
From: BIOMEASURE, INCORPORATED
To: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.
Reel/Frame 016048/0501 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2005
From: DONG, ZHENG XIN; SHEN, YEELANA
To: BIOMEASURE, INCORPORATED
Reel/Frame 016048/0684 →