IP Library › Granted Patent US 9,845,339

Granted Patent B2

US 9,845,339 · App. 14/369,116 · Granted Dec 19, 2017

Method of treating melanocortin-4 receptor-associated disorders in heterozygous carriers

Inventors: Louis A. Tartaglia (Newton, MA); Bart Henderson (Belmont, MA)

Assignee: RHYTHM PHARMACEUTICALS, INC.

C07K5/0802 A61K38/08 C07K7/06 C07K14/68 C07K14/723

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Quick Facts

Patent No.: US 9,845,339
App. No.: 14/369,116
Granted: Dec 19, 2017
Kind: B2

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Abstract

A method of treating a disorder in a subject. The method comprises administering to said subject an effective amount of an agonist of the melanocortin-4 receptor (MC4R). The subject is a heterozygous carrier of an MC4R mutation, and the disorder results from an attenuated response of MC4R to a-melanocortin stimulating hormone (a-MSH).

Claims (1408)

1. A method of treating a disorder in a subject in need thereof, comprising:

administering to said subject an effective amount of an agonist of the melanocortin-4 receptor (MC4R),

wherein the subject is a heterozygous carrier of an MC4R mutation, and the disorder results from an attenuated response of MC4R to α-melanocortin stimulating hormone (α-MSH).

2. The method of claim 1 , wherein the disorder is obesity.

3. The method of claim 1 , wherein the disorder is a metabolic syndrome.

4. The method of any one claims 1 to 3 , wherein the MC4R agonist is not an adrenocorticotropic hormone (ACTH).

5. The method of any one of claims 1 - 3 , wherein said MC4R agonist is Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 (SEQ ID NO: 140) or a pharmaceutically acceptable salt thereof.

6. The method of any one of claims 1 - 3 , wherein said MC4R agonist is Hydantoin(C(O)-(Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 (SEQ ID NO: 500) or a pharmaceutically acceptable salt thereof.

7. The method of any one of claims 1 - 3 , wherein said MC4R agonist is a tripeptide D-Phe-Arg-Trp (SEQ ID NO: 560) or a pharmaceutical salt thereof.

8. The method of any one of claims 1 - 3 , wherein said MC4R agonist is a peptide that includes D-Phe-Arg-Trp (SEQ ID NO: 560) or a pharmaceutical salt thereof.

9. The method of any one of claims 1 - 3 , wherein said MC4R agonist is a peptide that includes an acetylated tripeptide Ac-D-Phe-Arg-Trp-NH 2 (SEQ ID NO: 561) or a pharmaceutical salt thereof.

10. The method of any one of claims 1 - 3 , wherein said MC4R agonist is a peptide selected form:

(SEQ ID NO: 1)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-NH 2 ;

(SEQ ID NO: 2)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-A6c-Lys)-NH 2 ;

(SEQ ID NO: 3)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-NH 2 ;

(SEQ ID NO: 4)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 5)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 6)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 7)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-NH 2 ;

(SEQ ID NO: 8)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Apn-Lys)-NH 2 ;

(SEQ ID NO: 9)

Ac-A6c-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 10)

Ac-D-2-Nal-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 11)

Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 12)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 13)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 14)

Ac-Nle-c(Cys-β-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 15)

Ac-Nle-c(Cys-Gaba-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 16)

Ac-Nle-c(Cys-Aib-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 17)

Ac-Nle-c(Cys-Gly-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 18)

Ac-Nle-c(D-Cys-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 19)

Ac-Nle-c(D-Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 20)

Ac-Nle-c(D-Cys-β-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 21)

Ac-Nle-c(D-Cys-Gaba-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 22)

Ac-Nle-c(D-Cys-Aib-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 23)

Ac-Nle-c(D-Cys-Gly-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 24)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 25)

Ac-Nle-c(Cys-β-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 26)

Ac-Nle-c(Cys-Gaba-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 27)

Ac-Nle-c(Cys-Aib-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 28)

Ac-Nle-c(Cys-Gly-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 29)

Ac-Nle-c(D-Cys-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 30)

Ac-Nle-c(D-Cys-D-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 31)

Ac-Nle-c(D-Cys-β-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 32)

Ac-Nle-c(D-Cys-Gaba-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 33)

Ac-Nle-c(D-Cys-Aib-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;

(SEQ ID NO: 34)

Ac-Oic-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 35)

Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 36)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 37)

Ac-D-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 38)

Ac-D-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 39)

Ac-Nip-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 40)

Ac-hPro-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 41)

Ac-hLeu-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 42)

Ac-Phe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 43)

Ac-D-Phe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 44)

Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 45)

n-butanoyl-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 46)

n-butyryl-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 47)

Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 48)

Ac-β-hMet-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 49)

Ac-Gaba-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 50)

Ac-Cha-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 51)

Ac-hCha-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 52)

Ac-Leu-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 53)

Ac-hLeu-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 54)

Ac-Phe-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 55)

Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-D-Ala-Lys)-NH 2 ;

(SEQ ID NO: 56)

Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-β-Ala-Lys)-NH 2 ;

(SEQ ID NO: 57)

Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 58)

Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-Aha-Lys)-NH 2 ;

(SEQ ID NO: 59)

Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-Apn-Lys)-NH 2 ;

(SEQ ID NO: 60)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-NH 2 ;

(SEQ ID NO: 61)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 62)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-NH 2 ;

(SEQ ID NO: 63)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-NH 2 ;

(SEQ ID NO: 64)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-D-Ala-Cys)-NH 2 ;

(SEQ ID NO: 65)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 66)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-2-Nal-Cys)-NH 2 ;

(SEQ ID NO: 67)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-1-Nal-Cys)-NH 2 ;

(SEQ ID NO: 68)

n-butanoyl-Nle-c(Cys-D-Ala-His-D-Phe-Arg-2-Nal-Cys)-NH 2 ;

(SEQ ID NO: 69)

n-butanoyl-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 70)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-2-Nal-Cys)-NH 2 ;

(SEQ ID NO: 71)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-1-Nal-Cys)-NH 2 ;

(SEQ ID NO: 72)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Bal-Cys)-NH 2 ;

(SEQ ID NO: 73)

Ac-Nle-c(Cys-D-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 74)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-D-Ala-Lys)-NH 2 ;

(SEQ ID NO: 75)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Bal-Cys)-NH 2 ;

(SEQ ID NO: 76)

Ac-Nle-c(Pen-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 77)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;

(SEQ ID NO: 78)

Ac-Nle-c(Pen-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;

(SEQ ID NO: 79)

D-Phe-c(Cys-His-D-Phe-hArg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 80)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 81)

D-Phe-c(Cys-His-D-Phe-Arg-Bip-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 82)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 83)

D-Phe-c(Cys-His-D-Phe-hArg-Bip-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 84)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-NH 2 ;

(SEQ ID NO: 85)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-NH 2 ;

(SEQ ID NO: 86)

Ac-Nle-c(Asp-D-Ala-His-D-Phe-Arg-Trp-Lys)-NH 2 ;

(SEQ ID NO: 87)

Ac-Nle-c(Asp-D-Ala-His-D-Phe-Arg-Bal-Lys)-NH 2 ;

(SEQ ID NO: 88)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-OH;

(SEQ ID NO: 89)

Ac-Nle-c(Cys-D-Abu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 90)

Ac-Nle-c(Cys-D-Val-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 91)

Ac-Nle-c(Cys-D-Ile-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 92)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 93)

Ac-Nle-c(Cys-D-Tle-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 94)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 95)

Ac-Nle-c(Pen-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 96)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;

(SEQ ID NO: 97)

Ac-Nle-c(Pen-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;

(SEQ ID NO: 98)

Ac-Leu-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 99)

Ac-Cha-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 100)

Ac-Ile-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 101)

Ac-Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 102)

Ac-Val-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 103)

Ac-2-Nal-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 104)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 105)

Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 106)

Ac-Nle-c(Cys-3-Pal-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 107)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-OH;

(SEQ ID NO: 108)

Ac-Nle-c(Cys-His-Phe-Arg-D-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 109)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 110)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-β-Ala-Lys)-NH 2 ;

(SEQ ID NO: 111)

Ac-Nle-c(Cys-His-D-2-Nal-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 112)

Ac-Nle-c(Cys-His-D-2-Nal-Arg-Trp-Ahx-Cys)-NH 2 ;

(SEQ ID NO: 113)

Ac-hPhe-c(Asp-His-D-2-Nal-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 114)

Ac-Cha-c(Asp-His-D-2-Nal-Arg-Trp-Gaba-Lys)-NH 2 ;

(SEQ ID NO: 115)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-OH;

(SEQ ID NO: 116)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-OH;

(SEQ ID NO: 117)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-Ala-D-Cys)-Thr-OH;

(SEQ ID NO: 118)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-OH;

(SEQ ID NO: 119)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-D-Cys)-Thr-OH;

(SEQ ID NO: 120)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-OH;

(SEQ ID NO: 121)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Apn-Lys)-OH;

(SEQ ID NO: 122)

Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 123)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 124)

Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 125)

Ac-D-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 126)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 127)

Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 128)

Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;

(SEQ ID NO: 129)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Gaba-Cys)-OH;

(SEQ ID NO: 130)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-OH;

(SEQ ID NO: 131)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-OH;

(SEQ ID NO: 132)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-D-Ala-Cys)-OH;

(SEQ ID NO: 133)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-OH;

(SEQ ID NO: 134)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-2-Nal-Cys)-OH;

(SEQ ID NO: 135)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-1-Nal-Cys)-OH;

(SEQ ID NO: 136)

Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Bal-Cys)-OH;

(SEQ ID NO: 137)

Ac-Nle-c(Pen-D-Ala-His-D-Phe-Arg-Trp-Cys)-OH;

(SEQ ID NO: 138)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-OH;

(SEQ ID NO: 139)

Ac-Arg-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 140)

Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 141)

Ac-D-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 142)

Ac-D-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;

(SEQ ID NO: 143)

Ac-D-Arg-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;

(SEQ ID NO: 144)

Ac-Arg-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;

(SEQ ID NO: 145)

Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;

(SEQ ID NO: 146)

Ac-D-Arg-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 147)

Ac-Arg-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-NH 2 ;

(SEQ ID NO: 148)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-NH 2 ;

(SEQ ID NO: 149)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-D-Ala-Cys)-NH 2 ;

(SEQ ID NO: 150)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-β-Ala-Cys)-NH 2 ;

(SEQ ID NO: 151)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;

(SEQ ID NO: 152)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Apn-Cys)-NH 2 ;

(SEQ ID NO: 153)

Ac-c(Cys-Glu-His-D-Phe-Arg-Trp-Ala-Cys)-NH 2 ;

(SEQ ID NO: 154)

Ac-c(Cys-Glu-His-D-Phe-Arg-2-Nal-Ala-Cys)-NH 2 ;

(SEQ ID NO: 155)

Ac-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Ala-Cys)-NH 2 ;

(SEQ ID NO: 156)

Ac-c(Cys-D-Ala-His-D-Phe-Arg-2-Nal-Ala-Cys)-NH 2 ;

(SEQ ID NO: 157)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Ala-Cys)-NH 2 ;

(SEQ ID NO: 158)

Ac-Nle-c(Asp-D-Ala-His-D-Phe-Arg-Bal-Ala-Lys)-NH 2 ;

(SEQ ID NO: 159)

Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -Nle-c(Asp-His-D-2-Nal-Arg-Trp-

Lys)-NH 2 ;

(SEQ ID NO: 160)

Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -Doc-Nle-c(Asp-His-D-2-Nal-Arg-

Trp-Lys)-NH 2 ;

(SEQ ID NO: 161)

Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 162)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys) 2 -

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 163)

Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 164)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro) 2 -Lys-Asp-Tyr-Gly-Arg-

(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 165)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro) 2 -Lys-Asp-Tyr-Gly-

Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 166)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala) 2 -Tyr-Gly-Arg-(Lys) 2 -

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 167)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro) 2 -Lys-Asp-Doc-Tyr-Gly-

Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 168)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro) 2 -Lys-Asp-Doc-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 169)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 170)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-Doc-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 171)

Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-Arg-(Lys) 2 -

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 172)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 173)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 174)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 175)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 176)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -Arg-Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 177)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -Gln-(Arg) 5 -NH 2 ;

(SEQ ID NO: 178)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-Lys-Gln-Lys-(Arg) 5 -NH 2 ;

(SEQ ID NO: 179)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 4 -Gln-Arg-NH 2 ;

(SEQ ID NO: 180)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Aib-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 181)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 182)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 183)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 184)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 185)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 186)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 187)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 188)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 189)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 6 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 190)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 3 -Gln-(Arg) 2 -NH 2 ;

(SEQ ID NO: 191)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-Gln-(Lys) 2 -(Arg) 5 -NH 2 ;

(SEQ ID NO: 192)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 5 -Gln-NH 2 ;

(SEQ ID NO: 193)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 194)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 195)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 196)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Arg-

Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 197)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 198)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 199)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 200)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 201)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 202)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 203)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 204)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 205)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 206)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Arg-

Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 207)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 208)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 2 -

Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 209)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Arg-

Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 210)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 211)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 212)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 213)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-

Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 214)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 215)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 216)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 217)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 218)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 219)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 220)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 221)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 222)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 223)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 224)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 225)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 226)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 227)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 228)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 229)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 230)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 231)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 232)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 233)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 234)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 235)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 236)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 237)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 238)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 239)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 240)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 241)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 242)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 243)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 244)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 245)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-

Gly-(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 246)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-

Gly-(Arg) 6 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 247)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-Arg-(Lys) 2 -

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 248)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys) 2 -

Arg-Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 249)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys) 2 -

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 250)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 251)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 252)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 253)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 254)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 2 -Lys-

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 255)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-

(Arg) 3 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 256)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg) 2 -Lys-

(Arg) 2 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 257)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg) 3 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 258)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 2 -Lys-(Arg) 2 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 259)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg) 3 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 260)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 261)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 262)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 263)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 264)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 265)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 266)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 267)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 268)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 269)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 270)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 271)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 272)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 273)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 274)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 275)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 276)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 277)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 278)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 279)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 280)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 281)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 282)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 283)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 284)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 285)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 286)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 287)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 288)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 289)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 290)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 291)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 292)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 293)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 294)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 295)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 296)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 297)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 298)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 299)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 300)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 301)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 302)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 303)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 304)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 305)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 306)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 307)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 308)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 309)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 310)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 311)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 312)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 313)

D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 314)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 315)

Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 316)

Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 317)

Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 318)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 319)

Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 320)

Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 321)

Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 322)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 323)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 324)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 325)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 326)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 327)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 328)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 329)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 330)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 331)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 332)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 333)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 334)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 335)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 336)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 337)

Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 338)

Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 339)

Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 340)

Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 341)

Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 342)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 343)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 344)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 345)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 346)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 347)

Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 348)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 349)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 350)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 351)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 352)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 353)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 354)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 355)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 356)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 357)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 358)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc) 2 -Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 359)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 360)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 361)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 362)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 363)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 364)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 365)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 366)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 367)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 368)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 369)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 370)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 371)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 372)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 373)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 374)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 375)

D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 376)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 377)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 378)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 379)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 380)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 381)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 382)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 383)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 384)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 385)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 386)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 387)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 388)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 389)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 390)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc) 2 -(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 391)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 392)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 393)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 394)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 395)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala) 2 -(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 396)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 397)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-

(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 398)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 399)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc) 2 -Tyr-Gly-

(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 400)

D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc) 2 -(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 401)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 402)

Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 403)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 404)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 405)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 406)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 407)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 408)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 409)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 410)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 411)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 412)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 413)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 414)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 415)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 416)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 417)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 418)

Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 419)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 420)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 421)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 422)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 423)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 424)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 425)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 426)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 427)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 428)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 429)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 430)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 431)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 432)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 433)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 434)

Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 435)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 436)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 437)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 438)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 439)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 440)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 441)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 442)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 443)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 444)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 445)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 446)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 447)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 448)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 449)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -

Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 450)

Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 451)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 452)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 453)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 454)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 455)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 456)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 457)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 458)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 459)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -

NH 2 ;

(SEQ ID NO: 460)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 461)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 3 -NH 2 ;

(SEQ ID NO: 462)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;

(SEQ ID NO: 463)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -

NH 2 ;

(SEQ ID NO: 464)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 465)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-

(Arg) 4 -NH 2 ;

(SEQ ID NO: 466)

Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;

(SEQ ID NO: 467)

Ac-c(Cys-Glu-His-D-4-Br-Phe-Arg-Trp-Gly-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 468)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 469)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 470)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 471)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 472)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 473)

Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;

(SEQ ID NO: 474)

c[Hydantoin(C(O)-(Cys-D-Ala))-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 475)

c[Hydantoin(C(O)-(hCys-D-Ala))-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 476)

c[Hydantoin(C(O)-(Cys-D-Ala))-His-D-2-Nal-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 477)

c[Hydantoin(C(O)-(hCys-D-Ala))-His-D-2-Nal-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 478)

c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 479)

c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Orn]-NH 2 ;

(SEQ ID NO: 480)

c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Dab]-NH 2 ;

(SEQ ID NO: 481)

c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Dap]-NH 2 ;

(SEQ ID NO: 482)

c[Hydantoin(C(O)-(Asp-His))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 483)

c[Hydantoin(C(O)-(Asp-His))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 484)

c[Hydantoin(C(O)-(Asp-A3c))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 485)

c[Hydantoin(C(O)-(Asp-A5c))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 486)

c[Hydantoin(C(O)-(Asp-A6c))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 487)

c[Hydantoin(C(O)-(Asp-A3c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 488)

c[Hydantoin(C(O)-(Asp-A5c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 489)

c[Hydantoin(C(O)-(Asp-A6c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 490)

c[Hydantoin(C(O)-(Asp-Aic))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 491)

c[Hydantoin(C(O)-(Asp-Apc))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 492)

c[Hydantoin(C(O)-(Asp-Aic))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 493)

c[Hydantoin(C(O)-(Asp-Apc))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 494)

c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Orn]-NH 2 ;

(SEQ ID NO: 495)

c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Dab]-NH 2 ;

(SEQ ID NO: 496)

c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Dap]-NH 2 ;

(SEQ ID NO: 497)

c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 498)

c[Hydantoin(C(O)-(Glu-His))-D-Phe-Arg-Trp-Dap]-NH 2 ;

(SEQ ID NO: 499)

c[Hydantoin(C(O)-(Glu-His))-D-Phe-Arg-Trp-Lys]-NH 2 ;

(SEQ ID NO: 500)

Hydantoin(C(O)-(Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 501)

Hydantoin(C(O)-(Nle-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 502)

Hydantoin(C(O)-(Gly-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 503)

Hydantoin(C(O)-(Nle-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 504)

Hydantoin(C(O)-(Gly-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 505)

Hydantoin(C(O)-(Nle-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;

(SEQ ID NO: 506)

Hydantoin(C(O)-(Gly-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;

(SEQ ID NO: 507)

Hydantoin(C(O)-(Ala-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 508)

Hydantoin(C(O)-(D-Ala-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 509)

Hydantoin(C(O)-(Aib-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 510)

Hydantoin(C(O)-(Val-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 511)

Hydantoin(C(O)-(Ile-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 512)

Hydantoin(C(O)-(Leu-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 513)

Hydantoin(C(O)-(Gly-Gly))-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 514)

Hydantoin(C(O)-(Nle-Gly))-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 515)

Hydantoin(C(O)-(D-Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 516)

Hydantoin(C(O)-(D-Arg-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 517)

Hydantoin(C(O)-(Arg-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 518)

Hydantoin(C(O)-(D-Arg-Gly))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 519)

Hydantoin(C(O)-(Arg-Gly))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 520)

Hydantoin(C(O)-(Ala-Nle))c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 521)

Hydantoin(C(O)-(Val-Nle))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 522)

Hydantoin(C(O)-(Gly-Nle))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 523)

Hydantoin(C(O)-(A6c-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 524)

Hydantoin(C(O)-(Gly-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 525)

Hydantoin(C(O)-(Ala-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 526)

Hydantoin(C(O)-(D-Ala-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 527)

Hydantoin(C(O)-(Val-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 528)

Hydantoin(C(O)-(Leu-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 529)

Hydantoin(C(O)-(Cha-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 530)

Hydantoin(C(O)-(Aib-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 531)

Hydantoin(C(O)-(Gly-Arg))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 532)

Hydantoin(C(O)-(Gly-Arg))-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 533)

Hydantoin(C(O)-(Gly-Arg))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 534)

Hydantoin(C(O)-(Gly-Arg))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 535)

Hydantoin(C(O)-(Gly-D-Arg))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 536)

Hydantoin(C(O)-(Gly-D-Arg))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 537)

Hydantoin(C(O)-(Gly-D-Arg))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 538)

Hydantoin(C(O)-(Nle-Ala))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 539)

c[Hydantoin(C(O)-(Nle-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 540)

c[Hydantoin(C(O)-(Ala-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 541)

c[Hydantoin(C(O)-(D-Ala-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 542)

c[Hydantoin(C(O)-(Aib-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 543)

c[Hydantoin(C(O)-(Val-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 544)

c[Hydantoin(C(O)-(Abu-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 545)

c[Hydantoin(C(O)-(Leu-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 546)

c[Hydantoin(C(O)-(Ile-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 547)

c[Hydantoin(C(O)-(Cha-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 548)

c[Hydantoin(C(O)-(A6c-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 549)

c[Hydantoin(C(O)-(Phe-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 550)

c[Hydantoin(C(O)-(Nle-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 551)

c[Hydantoin(C(O)-(Gly-Cys))-Glu-His-D-Phe-Arg-Trp-Cys]-NH 2 ;

(SEQ ID NO: 552)

Ac-Tyr-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 553)

Ac-2-Nal-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 554)

Ac-1-Nal-Arg-c(Cys-D-Ala-His-DPhe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 555)

Ac-Phe-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 556)

Ac-Trp-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 557)

Ac-Pff-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

(SEQ ID NO: 558)

H-His-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

and

(SEQ ID NO: 559)

Ac-His-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;

or a pharmaceutically acceptable salt thereof.

Assignments (2)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 23, 2020

From: VAN DER PLOEG, LEONARDUS H.T.

To: RHYTHM PHARMACEUTICALS, INC.

Reel/Frame 051604/0488 →

CHANGE OF NAME Recorded Nov 12, 2015

From: RHYTHM METABOLIC, INC.

To: RHYTHM PHARMACEUTICALS, INC.

Reel/Frame 037108/0044 →

Continuity (2)

Provisional Application 61581391 · Dec 29, 2011

Related Publication 20140329743A1 · Nov 6, 2014