AU2007221964B2 - Peptide vectors - Google Patents

Description

\O

AUSTRALIA

Patents Act 1990 COMPLETE SPECIFICATION STANDARD PATENT Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.

Invention Title: PEPTIDE VECTORS The following statement is a full description of this invention, including the best method of performing it known to me/us: PEPTIDE VECTORS O FIELD OF THE INVENTION [0001] The present invention relates to therapeutic compositions and their use in the treatment of disease states. More particularly, the present invention provides compounds, compositions and methods for treating disease states associated with aberrant or undesirable cellular proliferation, migration, and/or physiological activity.

BACKGROUND OF THE INVENTION S[0002] Most cytotoxic drugs exhibit undesirable toxic side effects due to their lack of selective action toward the tissues or cells requiring therapeutic effect. Various approaches have been pursued to achieve the selective delivery of cytotoxic agents to a target cell type.

[0003] Using biological receptor ligands as carriers of drugs to target these drugs to the cells of interest can reduce toxic side-effects and greatly improve the efficiency drug delivery. For example, International Patent Publication No. WO97/19954 discloses conjugates of an anthracycline cytotoxic agent such as doxorubicin with a peptide hormone such as LHRH, bombesin or somatostatin. The cytotoxic agent is covalently attached to the peptide via a linker of formula -C(O)-(CH 2 n 0-7.

[0004] Similarly, European Patent Application No. EP1118336 discloses conjugates of somatostatin analogs, octreotide, lanreotide, and vapreotide, and a cytotoxic drug, such as paclitaxel, doxorubicin, or camptothecin, through a spacer, wherein the spacer is also indicated to have the structure: -C(O)-(CH 2 n 0- 7.

[0005] U.S. Patent Application Publication No. 2002/0115596 discloses conjugates of cytotoxic agents and oligopeptides in which the amino acid sequences of the peptides are indicated to be cleaved preferentially by free prostate specific antigen. Such conjugates are said to be useful for the treatment of prostate cancer and benign prostatic hyperplasia.

[0006] U.S. Patent Application Publication No. 2003/0064984 discloses conjugates of cytotoxic analogs of CC-1065 and the duocarmycins with cleavable 00 0 linker arms and a targeting agent such as an antibody or a peptide. The cN cytotoxic analogs are indicated to be released upon cleavage of the linker.

S[0007] International Patent Application No. W002/34237 discloses Sconjugates of active agents covalently attached directly to a polypeptide. The s polypeptide is said to stabilize the active agent, in the stomach, through conformational protection.

O [0008] There remains, however, a significant need for targeted cytotoxic cN drugs with improved properties in respect of targeting specificity, systemic toxicity, and pharmacokinetics.

N 10 SUMMARY OF THE INVENTION [0009] The instant invention provides a compound according to formula

X-B'-B

2

-B

3

B

4

-Z

(I)

wherein: X is selected from the group consisting of: {5-(R)-ethyl-9,10-difluoro-1,4,5,13-tetrahydro-3H, oxepino indolizino[1,2-b]quinoline-3,15-dione-5-O-; camptothecin or a camptothecin derivative; doxorubicin or a doxorubicin derivative; and paclitaxel or a paclitaxel derivative; each of B 1

B

2

B

3 and B 4 is, independently for each occurrence, (Doc)m, (Aepa)n, -(C(O)-A1-A2-A3-A4-A5-C(O))s- or (amino acid)p, wherein the amino acid is selected from the group consisting of Gly, Val, Abu, Gaba, and Sar; each of Al and A5 is, independently for each occurrence, CR'R 2 each of R 1 and R 2 is, independently for each occurrence, H; each of A2, A3, and A4 is, independently for each occurrence,

CR

6

R

7

(CH

2 )t or absent; each of R 6 and R 7 is, independently for each occurrence, H; -2- 0 m is, independently for each occurrence, 0, 1, 2, 3, 4, 5 or 6; cn is, independently for each occurrence, 1, or 2; c is, independently for each occurrence, 0,1, or 2; 0 p is, independently for each occurrence, 0, 1, or 2;

O

n s is, independently for each occurrence, 0, 1, or 2; t is, independently for each occurrence, 0, 1, 2 or 3; and Z is a peptide selected from the list: -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr- C NH 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 10 -DPhe-cyclo(Cys-31Tyr-DTrp-Lys-Val-Cys)-Thr-NH 2 -Gln-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 -DPhe-Gln-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 -Gln-Trp-Ala-Val-pAla-His-Leu-Nle-NH 2 -DCys-3Pal-DTrp-Lys-DCys-Thr-Tyr-NH 2 and -pGlu-His-Trp-Ser-Tyr-DLys[N'- ]-Leu-Arg-Pro-Gly-NH 2 provided that: when X is doxorubicin-, at least one of m and n is not 0, and at least one of B 1

B

2

B

3 and B 4 is (Doc)m or (Aepa)n; when X is paclitaxel-, B 1 is (amino acid)p selected from the list consisting of Sar, Gly, Val, and Gaba, and p is 1 or 2; and when X is paclitaxel-, at least one of B 1

B

2

B

3 and B 4 is (Doc)m, and m is not 0; or a pharmaceutically acceptable salt thereof.

[010] A first preferred embodiment features a compound according to formula wherein X is a cytotoxic moiety. More preferably X is an anthracycline. More preferably still X is camptothecin, a camptothecin derivative, paclitaxel, a paclitaxel derivative, doxorubicin, or a doxorubicin derivative; provided that: when X is doxorubicin or a doxorubicin derivative, at least one of m and n is not 0, and when X is paclitaxel or a paclitaxel derivative, then B 1 is (amino acid)p and p is 1 or 2; 00 0 [011] In a further preferred embodiment of said first preferred embodiment ci said the invention features compounds of formula wherein: O [012] X is camptothecin or a camptothecin derivative, wherein said t camptothecin derivative is:

N__

i CI N N N

N

N

O

S; or or X is paclitaxel or a paclitaxel derivative, wherein said paclitaxel derivative is:

H

3

C

H

3 C CH0 OH

HO

S/ HO H

H

3

C

or X is doxorubicin or a doxorubicin derivative, wherein said doxorubicin derivative is: PARAGRAPH [013] DELIBERATELY DELETED.

[014] In a further preferred embodiment of said second preferred to embodiment, the invention features compounds of formula wherein Z is: [015] a somatostatin analog according to the formula: -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Val-Cys)-Thr-NH 2 00 0 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 or a pharmaceutically acceptable salt thereof; O PARAGRAPH [016] DELIBERATELY DELETED.

[017] or a bombesin analog according to the formula: -Gln-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4); 0 -DPhe-Gln-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 Sor a pharmaceutically acceptable salt thereof.

S[018] A third preferred embodiment features a compound according to c formula wherein at least one of m and n is not 0.

[019] A fourth preferred embodiment features a compound the structure of which is specifically disclosed herein. More preferred are compounds and intermediates described in examples 1-79 herein. More preferred still are compounds of examples 19-25, 28-32, 40-42, 45-65, and 74-79.

[020] In a fifth preferred embodiment is featured a compound according to the formula: 0 [THIS PAGE DELIBERATELY BLANK] 0 O 0 -7- >Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 (Doc) 4 -Aepa-DPhe-cycto(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 ~-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -DPhe-GIn-Trp-Ala-Va-PAla-His-Leu-Leu-N

H

2 -8- Aepa-(Doc) 2-DPhe-GIn-Trp-AIa-VaI-~3AIa-His-Leu-Leu-N H 0 0 (SEQ ID NO: 4) -Aep c)2-~heGln-rp-la-al-P la-is-Lu-Lu-N 2 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-O3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) 0 1-yDPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 0 OH 0 0 O 0 O 0 pGlu-His-Trp-Ser-Tyr-N- Leu-Arg-Pro-Gly-NH, OH H, 0 0 H 0 0 OH 0*r N)(Q (D oc)..G aba -N ~O0 OHQ

H,C

H,C 0~ pGiu-His-Trp-Ser-Tyr-N Leu-Arg-Pro-Gly-NH, I H 0 0 0 O0

H.C

HNJH

OH

CH,

(SEQ ID NO: 6) -(Doc) 4 ,-Aepa-NpGlu-His-Trp-Ser-Tyr-N-"'>- Leu-Arg-Pro-Gly-NH, 0 Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH, (DoC) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 ,Lys- Lys- Lys-DTyr-DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys)-Thr- NH 2 (Doc), -D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 Aepa-DPhe-cyclo(Gys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 N 0 (Doc)-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 11 F N 0 F- N 0 F N

Q,

4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH, 00 00 F) C N

N

F NAepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp -Lys-Abu-Cys)-Thr-NH 2 0 F N 0 F0

N

0 (Doc) 4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp- Lys-Abu-Cys)-Thr-N H, 0 H 0 N' 0 (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H2 0 CH 0 0 Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Gys)-Thr-NH, 00 *0 CH 0

H,C

H,C HJ0 9

OH

0 N 2 0~ 0 0 N N 0 Aepa-(DoC) 4

-H

0

H

pGlu-His-Trp-Ser-Tyr -N Leu-Nrg-Pro-Gly-NH 2

H

12-

IN

H A epa-(D o H HOH I H 3 C

H

HOHC CFH 3 pGlu-H is-Trp-Ser-Tyr -N Leu-Arg-Pro-G Iy-l\ H-, 0 CHH 0 pGltI-H is-Trp-Ser-'rvr- N"1V Leu-Arg-Pro-Gly-NH, 0 Aepa-(Doc) 4 pGiI-H is-Trp-Ser-Tyr- -j -rLeU-Arg-Pro-G Iy-NH, 0 -13y'l) 0 (SEQ ID NO: 12)

'(DOC)

4 -Aepa-DPhe-Gn-Trp-Aa-Va-3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba-Gn-Trp-Ala-Va-3Ala-His-Leu-Nle-N

H

2 (SEQ ID NO: 12) (DoC) 4 -Aepa-Gaba-GIn-Trp-Ala-Va-3Ala-His-Leu-Nie-NH2 (SEQ ID NO: 12) 14- I h- (Doc) 4 -Aepa-Gaba-Gn-Trp-Aa-Va-P3Ala-His-Leu-Nle-N

H

2 0 (SEQ ID NO: 12) 0 OH 0 0 0 OH (Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-PAla-His-Leu-Nie-NH 2 01 0 ,0 0 OH 0 HC HC

Q)

OH

(SEQ ID NO: 12) (SEQ ID NO: 12) 4 -Aepa-DPhe-cycio(Cys-Tyr-DTrp- Lys-Abu-Cys)-Thr-N H 2 7Y) 0 0 cH, U(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 C -j O 0_ O OH N 0 HC CY2) OO, H 0O H 0 Noy--N (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp- Lys-Abu-Cys)-Thr-N H 2 9(4N0 0 0 0OH0

HC

OH

or a pharmaceutically acceptable salt thereof. More preferred are compounds according to the formula: F 0 F N' /oc)-Lys- DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 16-

(DOC)

4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 Doc) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H I i 0 (SEQ ID NO: 12) (SEQ ID NO: 12) or (SEQ ID NO: 12) 17or a pharmaceutically acceptable salt thereof. Even more preferred are compounds

O

Scomprising the formula: cl SN 0 a (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 or Nir- (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 r- r 0 C or a pharmaceutically acceptable salt thereof.

[021] In a sixth preferred embodiment is featured a compound selected from the compounds listed in Table A.

[022] In a seventh preferred embodiment is featured a compound selected from the compounds listed in Table B.

[023] In an eighth preferred embodiment is featured a compound selected from the compounds listed in Table C.

[024] In a ninth preferred embodiment is featured a compound selected from the compounds listed in Table D.

[025] In a tenth preferred embodiment is featured a compound selected from the compounds listed in Table E.

[026] In an eleventh preferred embodiment is featured a compound selected from the compounds listed in Table F.

[027] In a twelfth preferred embodiment is featured a compound selected from the compounds listed in Table G.

[028] In a thirteenth preferred embodiment is featured a compound selected from the compounds listed in Table H.

[0100] In a fourteenth preferred embodiment is featured a compound selected from the compounds listed in Table I.

18- [0101] In second aspect, the invention features a pharmaceutical composition Scomprising an effective amount of a targeted cytotoxic compound comprising a Scytotoxic moiety bound to a targeting moiety, such as, for example, a ligand of a 0 biological receptor, or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The two moieties are bound via a linker, e.g., as described by formula I defined herein.

[0102] In a third aspect, the invention features a method of treating a disease in a subject in need thereof, said method comprising administering to said subject a C therapeutically effective amount of a targeted cytotoxic compound according to formula I defined herein, or a pharmaceutically acceptable salt thereof, wherein said c disease is selected from the group consisting of fibrosis, benign prostatic hyperplasia, atherosclerosis, restenosis, breast cancer, colon cancer, pancreas cancer, prostate cancer, lung cancer, small cell lung cancer, ovarian cancer, epidermal cancer, and hematopoietic cancer.

[0103] In a fourth aspect, the invention features a method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a targeted cytotoxic compound according to formula I defined herein, or a pharmaceutically acceptable salt thereof, wherein said disease is selected from the group consisting of benign prostatic hyperplasia, restenosis, breast cancer, colon cancer, pancreas cancer, prostate cancer, lung cancer, small cell lung carcinoma, ovarian cancer, epidermal cancer, and hematopoietic cancer.

[0104] In a fifth aspect, the invention features a method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a targeted cytotoxic compound according to formula I defined herein, or a pharmaceutically acceptable salt thereof, wherein said disease is characterized by undesired proliferation of cells that express one or more somatostatin-type receptors.

[0105] In a sixth aspect, the invention features a method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a targeted cytotoxic compound according to formula I defined herein, or a pharmaceutically acceptable salt thereof, wherein said -19disease is characterized by undesired proliferation of cells that express one or more

O

0of bombesin-type receptors.

[0106] In a seventh aspect, the invention features a method of treating a disease O in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a targeted cytotoxic compound according to formula I defined herein, or a pharmaceutically acceptable salt thereof, wherein said Sdisease is characterized by undesired proliferation of cells that express one or more LHRH-type receptors.

N [0107] As used herein the term "amino acid" refers to any naturally occurring and 0 unnatural amino acids, including but not limited to a-amino acids, p-amino acids, y- C amino acids, and may be either D-amino acids or L-amino acids unless otherwise indicated. With the exception of the N-terminal amino acid, all abbreviations (e.g.

Ala) of amino acids in this disclosure stand for the structure of wherein R and R' each is, independently, hydrogen or the side chain of an amino acid R CH 3 and R' H for Ala), or R and R' may be joined to form a ring system. For the N-terminal amino acid, the abbreviation stands for the structure of

(R

2

R

3 wherein R 2 and R 3 are as defined in formula [0108] An exemplary list of preferred amino acids includes, but is not limited to, Ala, Arg, Asp, Asn, Cys, Glu, pGlu, Gin, Gly, His, lie, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val, p-Ala, Act, Apc, Gaba, Apn, Ahx, Ahp, Aoc, Anc, Adc, Aun, Ado, Acc, A3c, A4c, A5c, A6c, Aib, Orn, Dab, Dap, hArg, 4Pal, 3Pal, 2Pal, Abu, Cha, Cit, NIe, Nva, Taz, 2Thi, 3Thi, Dhp, Dmt, 2Fua, 3Hyp, 4Hyp, Inc, Inp, Ktp, hLeu. Oic, hPhe, Pip, Sar, Thz, Tic, Tie, Phg and Caeg.

[0109] The peptide portion of compounds of the invention may also be denoted herein by another format, (Tyr'l)Somatostatin(1-14)-NH 2 with the substituted amino acid(s) from the natural sequence placed between the first set of parentheses Tyr 1 for Phe' in somatostatin). The numbers between the second set of parentheses refer to the number of amino acids present in the peptide somatostatin(1-11) refers to amino acids 1 through 11 of the peptide sequence for somatostatin). The designation "NH 2 in (Tyr'')Somatostatin(1-14)-NH 2 indicates that the C-terminus of the peptide is amidated. (Tyr'')Somatostatin(1-14), or alternatively (Tyr'')Somatostatin(1-14)-OH, indicates that the C-terminus is the

O

Sfree acid.

c [0110] "Alkyl" refers to a hydrocarbon group containing one or more carbon atoms, O where multiple carbon atoms if present are joined by single bonds. The alkyl hydrocarbon group may be straight-chain or contain one or more branches or cyclic groups.

S[0111] "Substituted alkyl" refers to an alkyl wherein one or more hydrogen atoms of the hydrocarbon group are replaced with one or more substituents selected from N the group consisting of halogen, fluorine, chlorine, bromine, and iodine), -OH, S-CN, -SH, -NH 2

-NHCH

3

-NO

2 -C1- 2 alkyl substituted with 1 to 6 halogens, -CF 3

-OCH

3

-OCF

3 and -(CH 2 )o-4-COOH. In different embodiments 1, 2, 3 or 4 substituents are present. The presence of -(CH 2 )o-4-COOH results in the production of an alkyl acid. Examples of alkyl acids containing, or consisting of, -(CH2)o-4-COOH include 2-norbornane acetic acid, tert-butyric acid and 3-cyclopentyl propionic acid.

[0112] "Heteroalkyl" refers to an alkyl wherein one of more of the carbon atoms in the hydrocarbon group are replaced with one or more of the following groups: amino, amido, or carbonyl. In different embodiments 1 or 2 heteroatoms are present.

[0113] "Substituted heteroalkyl" refers to a heteroalkyl wherein one or more hydrogen atoms of the hydrocarbon group are replaced with one or more substituents selected from the group consisting of halogen, fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2

-NHCH

3

-NO

2 -C1- 2 alkyl substituted with 1 to 6 halogens, -CF 3

-OCH

3

-OCF

3 and -(CH 2 )o-4-COOH. In different embodiments 1, 2, 3 or 4 substituents are present.

[0114] "Alkenyl" refers to a hydrocarbon group made up of two or more carbons where one or more carbon-carbon double bonds are present. The alkenyl hydrocarbon group may be straight-chain or contain one or more branches or cyclic groups.

[0115] "Substituted alkenyl" refers to an alkenyl wherein one or more hydrogens are replaced with one or more substituents selected from the group consisting of halogen fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2

-NHCH

3 -21

-NO

2 -C1- 2 alkyl substituted with 1 to 6 halogens, -CF 3

-OCH

3

-OCF

3 and

-(CH

2 )o0-COOH. In different embodiments 1, 2, 3 or 4 substituents are present.

[0116] "Aryl" refers to an optionally substituted aromatic group with at least one O ring having a conjugated pi-electron system, containing up to two conjugated or fused ring systems. Aryl includes carbocyclic aryl, heterocyclic aryl and biaryl groups. Preferably, the aryl is a 5 or 6 membered ring. Preferred atoms for a heterocyclic aryl are one or more sulfur, oxygen, and/or nitrogen. Examples of aryl include phenyl, 1-naphthyl, 2-naphthyl, indole, quinoline, 2-imidazole, and 9-anthracene. Aryl substituents are selected from the group consisting of -C-4 alkyl, -C14 alkoxy, halogen fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH,

S-NH

2

-NO

2 -C1-2 alkyl substituted with 1 to 5 halogens, -CF 3

-OCF

3 and

-(CH

2 0 4 -COOH. In different embodiments the aryl contains 0, 1,2, 3, or 4 substituents.

[0117] "Alkylaryl" refers to an "alkyl" joined to an "aryl".

[0118] The term cycloalkyl is intended to include a mono-cycloalkyl group or a bicycloalkyl group of the indicated carbon number known to those of skill in the art.

[0119] The term heterocycle includes mono-cyclic and bi-cyclic systems having one or more heteroatoms, such as oxygen, nitrogen and/or sulfur. The ring systems may be aromatic, for example pyridine, indole, quinoline, pyrimidine, thiophene (also known as thienyl), furan, benzothiophene, tetrazole, dihydroindole, indazole, Nformylindole, benzimidazole, thiazole, and thiadiazole. The ring systems also may be non-aromatic, for example pyrrolidine, piperidine, morpholine and the like.

[0120] The chemist of ordinary skill will recognize that certain combinations of heteroatom-containing substituents listed in this invention define compounds which will be less stable under physiological conditions. Accordingly, such compounds are less preferred.

[0121] Doc is 8-amino-3,6-dioxaoctanoic acid, represented by the structure: 0 O -22- [0122] Aepa is 4-(2-aminoethyl)-1-carboxy methyl-piperazine, represented by the structure: ,0 [0123] Suc or succ is succinyl, represented by the structure: o [0124] Glut or glutaryl has the structure of: 0 0 [0125] A camptothecin moiety has the structure of: [0126] Camptothecin derivative moieties include but are not limited to: -23-

HO

N

o0 r

N

0 ON1 0 N C 00 F N- 0 0 F N0 0 F N 011 [0127] A paclitaxel moiety has the structure of: I H3O 3 0 C1H 3 0 CH OH N N

OH

3 H -O 3 00 HO i H c-i-

IND

H 0

NH

OH H H0 0

NOHO

H 0

NH

2 [01 30] DLys(-) is represented by the structure:

HN

0 [0131] DOrn(-) is represented by the structure: 25 O fNH o [0132] DDab(-) is represented by the structure:

O

[0133] DDap(-) is represented by the structure:

HN

0 o [0133] DDap(-) is represented by the structure:

NHNH

H

0 [0134] DApa(-) is represented by the structure:

*\NH

H I [0135] Certain abbreviations used herein are defined as follows: Abu a-aminobutyric acid Acc 1-amino-1-cyclo(C 3

-C

9 )alkyl carboxylic acid A3c 1-amino-l-cyclopropanecarboxylic acid A4c 1-amino-1-cyclobutanecarboxylic acid 1-amino-l-cyclopentanecarboxylic acid -26- A6c 1 -amino-I1 -cyclohexanecarboxylic acid Act 4-amino-4-carboxytetrahydropyran, represented by the structure: 00 0 NAib a-aminoisobutyric acid Ala or A alanine N -Ala beta-alanine Apc denotes the structure:

H

N

0 Arg or R arginine hArg homoarginine Asn or N asparagine Asp or D aspartic acid Ava 5-aminovaleric acid; Cha Il-cyclohexylalanine Cys or C cysteine Dab 2,4-diaminobutyric acid Dap 2,3-diaminopropionic acid Dhp 3,4-dehydroproline Dint 5, 5-dimethylth iazolid ine-4-ca rboxylic acid 27 101001 11001Doc 8-amino-3, 6-dioxaoctanoic acid, denoted by the structure: H 0 2Fua Gin or 0 Glu or E pGlu or Gip Gly or G His or H 3Hyp carboxylic acid 4Hyp acid 9-(2-furyi)-ala nine giutamine glutamic acid pyroglutamnic acid glycine histidine trans-3-hydroxy-L-proline, (2S, 3S)-3-hydroxypyrrolidine-2- 4-hydroxyproline, (2S, 4R)-4-hydroxypyrrolidine-2-carboxylic lie or I Inc lnp Ktp Leu or L h Leu Lys or K Met or M Nie

NE

Nva Oic isoleucine indoline-2-carboxylic acid isonipecotic acid 4-ketoproline leucine homoleucine lysine methionine norleucine indicates that the entity within the brackets is coupled to the epsilon nitrogen of the Lysine sidechain norvaline octahydroindole-2-carboxylic acid 28 Orn ornithine 2Pal f-(2-pyridinyl)alanine 3Pal 9-(3-pyridinyl)alanine C0 N4Pal 9!-(4-pyridiny)alanine Phe or F phenylalanine hPhe homophenylalanine Pip pipecolic acid Pro or P proline Sar Sarcosine or N-methyl glycine Ser or S serine Taz (I-(4-thiazolyI)ala nine, denoted by the structure:

H

0 2Thi R-(2-thienyl)alanine 3Thi I-(3-thienyl)alanine Thr or T threonine Thz thiazolidine-4-carboxylic acid Tic 1 ,2,3,4-tetrahydroisoquinoline-3-carboxylic acid Tie tert-leucine Trp or W tryptophan Tyr or Y tyrosine Val or V valine Gaba 4-Aminobutyric acid 29 Apn Ahx Ahp Aoc Anc Adc Aun Ado Phg Caeg the structure: 5-Aminopentanoic acid 6-Aminohexanoic acid 7-Aminoheptanoic acid 8-Aminooctanoic acid 9-Aminononanoic acid lO-Aminodecanoic acid 11 -Aminoundecanoic acid 12-Aminododecanoic acid Phenyig lycine N-(2-am inoethyl)-N-(2-cytosinyl-l1-oxo-ethyl)-glycine, denoted by

NH

2

NO

0 [0136] Certain other abbreviations used herein are defined as follows: Aloc: Boc: Bhoc BzI: 0CM: Dde:

DIG:

DIEA:

Dmab: amino) benzyl

DMAP:

DMF:

Allyboxycarbonyl tert-butyloxycarbonyl benzhydryboxycarbonyl benzyl dich lorometha ne 1 ,4-d imethyl-2, 6-d ioxocyclo hex- 1 -ylid ine)ethyl] N, N-diisopropylcarbodiimide diisopropylethyl amine 1 ,4-dimethyl-2 ,6-d ioxocyclohexylidene)-3-methylbutyl)- 4-(dimethylamino)pyridine dimethylformamide 30 DNP: 2,4-dinitrophenyl Et: ethyl Fmoc: Fluorenylmethyloxycarbonyl O HBTU: 2-(1 H-benzotriazole-1 1,3,3-tetramethyluronium N hexafluorophosphate cHex cyclohexyl HOAT: O-(7-azabenzotriazol-1 -yl)-1l 1,3,3-tetramethyluronium hexafluorophosphate HOBt: 1-hydroxy-benzotriazole Mmt: 4-methoxytrityl NMP: N-methylpyrrolidone Pbf: 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl tBu: tert-butyl TIS: triisopropylsilane TOS: tosyl trt trityl TFA: trifluoro acetic acid TFFH: tetramethylfluoroforamidinium hexafluorophosphate Z: benzyloxycarbonyl The Greek letter psi is used herein to indicate that a peptide bond has been replaced by a psuedopeptide bond. In an amino acid sequence name, the format of the qp term is wherein A is the amino acyl radical whose carbonyl group has been modified to X and B the amino acyl radical whose a-amino groups has been modified to X'.

X and X are shown as strings of element symbols, separated by a bond; -Leu-(p-(CH 2 NH)-Leu.

DETAILED DESCRIPTION [029] The invention features targeted cytotoxic compounds comprising a cytotoxic moiety bound to a targeting moiety, such as, for example, a ligand of a biological receptor, and methods relating to their therapeutic use for the treatment of neoplasia, hyperplasia, and other conditions associated with undesired proliferation of cells.

-31 [030] Examples of somatostatin peptides useful in the present invention are O described herein. Further examples are those covered by formulae or those S specifically recited in the publications set forth below, each of which is hereby O incorporated by reference in its entirety: N PCT Application No. WO 03/057214 (2003) U.S. Application No. 20030191134 (2003) U.S. Application No. 20030083241 (2003) U.S. Patent No. 6,316,414 (2001) SPCT Application No. WO 02/10215 (2002) PCT Application No. WO 99/22735 (1999) PCT Application No. WO 98/08100 (1998) PCT Application No. WO 98/44921 (1998) PCT Application No. WO 98/45285 (1998) PCT Application No. WO 98/44922 (1998) EP Application No. P5 164 EU (Inventor: G. Keri); Van Binst, G. et al. Peptide Research 5:8 (1992); Horvath, A. et al. Abstract, "Conformations of Somatostatin Analogs Having Antitumor Activity", 22nd European peptide Symposium, September 13-19, 1992, Interlaken, Switzerland; PCT Application No. WO 91/09056 (1991); EP Application No. 0 363 589 A2 (1990); U.S. Patent No. 4,904,642 (1990); U.S. Patent No. 4,871,717 (1989); U.S. Patent No. 4,853,371 (1989); U.S. Patent No. 4,725,577 (1988); U.S. Patent No. 4,684,620 (1987); U.S. Patent No. 4,650,787 (1987); U.S. Patent No. 4,603,120 (1986); U.S. Patent No. 4,585,755 (1986); EP Application No. 0 203 031 A2 (1986); U.S. Patent No. 4,522,813 (1985); U.S. Patent No. 4,486,415 (1984); U.S. Patent No. 4,485,101 (1984); -32- U.S. Patent No. 4,435,385 (1984); U.S. Patent No. 4,395,403 (1983); U.S. Patent No. 4,369,179 (1983); U4 O U.S. Patent No. 4,360,516 (1982); 1 U.S. Patent No. 4,358,439 (1982); U.S. Patent No. 4,328,214 (1982); U.S. Patent No. 4,316,890 (1982); U.S. Patent No. 4,310,518 (1982); c U.S. Patent No. 4,291,022 (1981); Patent No. 4,238,481 (1980); U.S. Patent No. 4,235,886 (1980); U.S. Patent No. 4,224,199 (1980); U.S. Patent No. 4,211,693 (1980); U.S. Patent No. 4,190,648 (1980); U.S. Patent No. 4,146,612 (1979); U.S. Patent No. 4,133,782 (1979); U.S. Patent No. 5,506,339 (1996); U.S. Patent No. 4,261,885 (1981); U.S. Patent No. 4,728,638 (1988); U.S. Patent No. 4,282,143 (1981); U.S. Patent No. 4,215,039 (1980); U.S. Patent No. 4,209,426 (1980); U.S. Patent No. 4,190,575 (1980); EP Patent No. 0 389 180 (1990); EP Application No. 0 505 680 (1982); EP Application No. 0 083 305 (1982); EP Application No. 0 030 920 (1980); PCT Application No. WO 88/05052 (1988); PCT Application No. WO 90/12811 (1990); PCT Application No. WO 97/01579 (1997); PCT Application No. WO 91/18016 (1991); U.K. Application No. GB 2,095,261 (1981); and French Application No. FR 2,522,655 (1983).

-33- [0137] Examples of LHRH (leutinizing hormone releasing hormone) peptides useful in the present invention are described herein. Further examples are those covered by formulae or those specifically recited in the publications set forth below, O each of which is hereby incorporated by reference in its entirety: N EP Application No. 0 081 877 (1983) EP Application No. 0 328 089 (1989) EP Application No. 0 417 454 (1991)

IND

EP Application No. 0 626 170 (1994) SEP Application No. 0 832 107 (1998) EP Application No. 1 340 768 (2003) SU.S. Application No. 2003040482 (2003) U.S. Patent No. 4,317,815 (1982) U.S. Patent No. 4,431,635 (1984) U.S. Patent No. 4,581,169 (1986) U.S. Patent No. 4,628,044 (1986) U.S. Patent No. 4,642,332 (1987) U.S. Patent No. 4,656,247 (1987) U.S. Patent No. 4,721,775 (1988) U.S. Patent No. 5,075,224 (1991) U.S. Patent No. 5,140,009 (1992) U.S. Patent No. 5,484,592 (1996) U.S. Patent No. 5,885,966 (1999) U.S. Patent No. 6,284,733 (2001) U.S. Patent No. 6,559,282 (2003) PCT Application No. WO 00/24764 (2000) PCT Application No. WO 90/11298 (1990) PCT Application No. WO 92/15330 (1992) PCT Application No. WO 94/14841 (1994) PCT Application No. WO 94/25060 (1994) PCT Application No. WO 96/40757 (1996) [0138] Examples of bombesin peptides useful in the present invention are described herein. Further examples are those covered by formulae or those -34specifically recited in the publications set forth below, each of which is hereby incorporated by reference in its entirety: EP Application No. 0 309 297 (1989) O EP Application No. 0 339 193 (1989) EP Application No. 0 402 852 (1990) EP Application No. 0 434 979 (1991) EP Application No. 0 468 497 (1992) EP Application No. 0 835 662 (1998) M U.S. Application No. 2003050436 (2003) U.S. Application No. 2003166539 (2003) SU.S. Patent No. 5,084,555 (1992) U.S. Patent No. 5,100,873 (1992) U.S. Patent No. 5,217,955 (1993) U.S. Patent No. 5,369,094 (1994) U.S. Patent No. 5,410,018 (1995) U.S. Patent No. 5,620,955 (1997) U.S. Patent No. 5,723,578 (1998) U.S. Patent No. 5,843,903 (1998) U.S. Patent No. 5,877,277 (1999) U.S. Patent No. 6,156,725 (2000) U.S. Patent No. 6,307,017 (2001) PCT Application No. WO 90/03980 (1990) PCT Application No. WO 91/06563 (1991) PCT Application No. WO 91/17181 (1991) PCT Application No. WO 94/02018 (1994) PCT Application No. WO 94/21674 (1994) [0139] The methods for synthesizing somatostatin, LHRH, and bombesin peptides are well documented and are within the ability of a person of ordinary skill in the art.

Further synthetic procedures are provided in the following examples. The following examples also illustrate methods for synthesizing the targeted cytotoxic compounds of the present invention.

Example 1 H-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu- Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin O [0140] The titled protected peptide-resin was automatically synthesized on an Applied Biosystems (ABI) (Foster City, CA) model 433A peptide synthesizer by using Fluorenylmethyloxycarbonyl (Fmoc) chemistry. A Rink Amide MBHA (4methylbenzylhydrylamine) resin (Novabiochem, San Diego, CA) with substitution of 0.72 mmol/g was used. The following Fmoc amino acids (AnaSpec, San Jose, CA) were used: Fmoc-Thr(tBu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Lys(Boc)-OH, Fmoc- DTrp(Boc)-OH, Fmoc-Tyr(tBu)-OH, Fmoc-DTyr(tBu)-OH Fmoc-Phe-OH, Fmoc- Cys(Trt)-OH, Fmoc-Thr(tBu)-OH, and Fmoc-Abu-OH. The synthesis was carried out on a 0.25 mmol scale. The Fmoc groups were removed by treatment with piperidine in N-methylpyrrolidone (NMP) for 30 min. In each coupling step, the Fmoc amino acid (4 eq, 1 mmol) was first pre-activated in 2 mL of a solution containing 0.45M 2-(1 -H-benzotriazole-l -yl)-1,1,2,3-tetramethyluronium hexafluorophosphate (HBTU) and 0.45M 1-hydroxy-benzotriazole (HOBT) in N,N-dimethylformamide (DMF). The resulting activated amino acid ester, 1 mL of diisopropylethylamine (DIEA) and 1 mL of NMP were added to the resin. The ABI 433A peptide synthesizer was programmed to perform the following reaction cycle: washing with NMP, removing Fmoc protecting group with 20% piperidine in NMP for min, washing with NMP, coupling with pre-activated Fmoc amino acid for 1h.

The resin was coupled successively according to the sequence. After peptide chain was assembled, the Fmoc was removed and the resin was washed completely by using DMF and dichloromethane (DCM).

Example 2 H-Doc-Doc-Doc-Doc-Lys(Boc)-DTyr(tBu)-tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)- Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin [0141] The titled protected peptide-resin was synthesized substantially according to the procedure described in Example 1. Fmoc-8-amino-3, 6-dioxaoctanoic acid (Fmoc-Doc-OH) was purchased from Chem-Impex Internatoinal, Wood Dale, IL.

After the assembly of H-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)- Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin (0.45 mmol scale), the -36protected peptide-resin was transferred into a reaction vessel on a shaker for manual

O

Ssynthesis. The resin was shaken with a DMF solution of Fmoc-Doc-OH (1.5 eq, 0.75 Smmol), N, N-diisopropylcarbodiimide (DIC, 1.5 eq, 0.75 mmol) and HOBT (1.5 eq, O 0.75 mmol) for 2 h. The resin was washed with DMF and treated with 20% piperidine (C in DMF to remove Fmoc protecting group. The rest of the three Doc residues were sequentially coupled to the resin using the same manual operation procedure. After removing Fmoc protecting group with 20% piperidine in DMF, the protected peptideresin was washed with DMF and DCM.

Example 3 H-Doc-Doc-Doc-Doc-Doc- c--Doc-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)- C DTrp(Boc)-Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin [0142] The titled protected peptide-resin was synthesized substantially according to the procedure described in Example 2.

Example 4 H-Aepa-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu- Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin [0143] The titled protected peptide-resin was synthesized substantially according to the procedure described in Example 1. Fmoc-4-(2-aminoethyl)-1-carboxymethylpiperazine (Fmoc-Aepa-OH) was purchased from Neosystem, Strasbourg, France.

After the assembly of H-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)- Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin, the protected peptideresin was transferred into a reaction vessel on a shaker for manual synthesis. The Fmoc-Aepa-OH (1.5 eq, 0.75 mmol) was pre-activated with O-(7-azabenzotriazol-1yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HATU, 1.4 eq, 0.7 mmol) and 1-hydroxy-7-azabenzotriazole (HOAT, 1.4 eq., 0.7 mmol) in 2 mL of DMF for 2 min.

The resulting activated ester of Fmoc-Aepa-OH and 1 mL of DIEA were added into the reaction vessel and the mixture was shaken for 2h. The resin was washed with DMF and treated with 20% piperidine in DMF to remove Fmoc protecting group. The protected peptide-resin was washed with DMF and DCM.

Example 37- H-Doc-Doc-Doc-Doc-Aepa-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)- DTrp(Boc)-Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin [0144] The titled protected peptide-resin was synthesized substantially according O to the procedure described in Example 4. The couplings of Fmoc-Doc-OH were N performed according to the corresponding procedure described in Example 2.

Example 6 SH-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin N [0145] The titled protected peptide-resin was synthesized substantially according to the procedure described in Example 1. Fmoc-DPhe-OH was purchased from (N AnaSpec, San Jose, CA.

Example 7 H-Aepa-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin [0146] The titled protected peptide-resin was synthesized substantially according to the procedure described in Example 4.

Example 8 5-O-tBoc-glycyl-5-(R)-ethyl-9, 1 0-difluoro-1,4,5,13-tetrahydro-3H,15Hoxepino[3',4':6'7]indolizino[1,2-b]quinoline-3,1 0 F 0 I 0 N NNLo 0 [0147] 5-(R)-Ethyl-9,1 O-difluoro-1,4,5, 1 3-tetrahydro-5-hydroxy-3H, oxepino[3',4':6,7]indolizino[l ,2-b]quinoline-3,15-dione (300 mg), Boc-Gly-OH (923 mg, 7eq.) and 4-(dimethylamino)pyridine (DMAP) (560.4 mg, 6 eq.) were dissolved in a mixed solvent system of DCM and DMF (30 mL, v/v, 30/0.5). To the solution was added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) (1.08 g, The mixture was stirred overnight at room temperature and the solvents were removed under reduced pressure. The residue was dissolved in 100 mL of DCM and washed successively with 10% citric acid aqueous solution (20 mL x 2), saturated NaHCO 3 (20 mL x 2) and brine (10 mL x The organic layer was dried -38over MgSO 4 filtered and evaporated under reduced pressure. The crude product was purified by a flash chromatography on a silica gel column using 10% methanol in DCM as the eluent to give a pure product of 5-O-tBoc-glycyl-5-(R)-ethyl-9, 0 ~difluoro-1 13-tetrahydro-3H, 15H-oxepino[3',4':6,7indolizino[1 ,2-b]quinoline-3, CI dione. 330 mg, TLC (silica gel, DCM/MeOH: Rf=0.43. Electro-spray ionization mass spectrometry (ESI MS) analysis gave the molecular weight at 556.4 (in agreement with the calculated molecular weight of 555.5).

Example 9 (Ni 5-O-glycyl-5-(R)-Ethyl-9, 10-difluoro-1 13-tetrahydro-3H, 1 oxepino[3',4':6,7]indolizino1 ,2-b]quinoline-3, 15-dione TFA salt F 0 F

N

Oy'N.NH, TFA 0 [0148] 5-O-tBoc-glycyl-5-( R)-ethyl-9, 1 0-difluoro-1 ,4 ,5,1 3-tetrahyd ro-3H, 1 oxepino[3',4':6,7]indolizino[1 ,2-b]quinoline-3, 15-dione (330 mg) was treated with trifluoroacetic acid (TFA) solution in DCM under nitrogen for 1h. TFA and solvent were removed under reduced pressure. The residue was triturated with cold ether to give a light yellow powder. TLC (silica gel, DCM/MeOH: RfO0.13. ESI MS analysis gave the molecular weight at 456.0 (in agreement with the calculated molecular weight of 455.4).

Example 5-O-(N-glutaryl-glycyl)-5-(R)-Ethyl-9, 1 0-difluoro-1 13-tetrahydro-3H, 1 oxepino[3',4':6,7]indolizino[1 ,2-blquinoline-3, 0 F:O N" 0 OH F N O r

-A

0 [0149] A mixture of 5-O-glycyl-5-(R)-ethyl-9, 1 0-d ifluoro-1 .4,5,1 3-tetrahydro- 3H, 15H-oxepino[3',4':6,7]indolizino[1 ,2-b]quinoline-3, 15-dione (208 mg, 0.37 mmol), glutaric anhydride (66 mg, 0.58 mmol, 1.5 eq.) and triethylamine (243 mL) in DMF (7 mL) was stirred at room temperature for 3h. The solvent was removed under reduced pressure. The residue was dissolved in water (10 mL) and the pH of the 39 solution was adjusted to 3 by adding 0.5N HCI solution at 0 OC. The precipitate 0formed was collected by filtration and washed with cold water and ether. After drying under reduced pressure, a solid was obtained (160 mg). Yield was 77%. ESI MS O analysis gave the molecular weight at 570.0 (in agreement with the calculated C molecular weight of 569.5). Purity was 98% based on analytical HPLC analysis.

Example 11 0 5-O-(N-succinyl-glycyl)-5-(R)-Ethyl-9,10-difluoro-1,4,5,13-tetrahydro-3H, oxepino[3',4':6,7]indolizino[1,2-b]quinoline-3,15-dione 0 0 OH F NOH o [0150] The titled compound was synthesized substantially according to the procedure described in Example 10 by using succinic anhydride. The yield was 86%. ESI MS analysis gave the molecular weight at 556.2 (in agreement with the calculated molecular weight of 555.50). Purity was 96% based on the analytical HPLC analysis.

Example 12 0 N 0 o [0151] Camptothecin (0.79 g, 2.2 mmol), Boc-Gly-OH (1.2 g, 6.8 mmol, 3 eq.) and DMAP (0.83 g, 6.8 mmol, 3 eq.) were dissolved in a mixed solvent system of DCM and THF (18 mL, v/v, The mixture was cooled in an ice-water bath. To it was added 1,3-diisopropylcarbodiimide (DIC) (1.1 mL, 6.8 mmol, 3.1 After stirring at 0 °C for 0.5h, the mixture was warmed to room temperature and stirred overnight.

The solution was diluted with 50 mL of DCM and washed successively with citric acid aqueous solution (20 mL x saturated NaHCO 3 (20 mL x 2) and brine mL x The organic layer was dried over MgSO 4 filtered and evaporated under reduced pressure to dryness. The crude product was purified by a flash chromatography on a silica gel column using 4% methanol in DCM as the eluent to give a pure product of camptothecin-20-(S)-(O-tBoc-glycyl) (1.07 g, white solid). TLC 0(silica, DCM/MeOH: Rf=0.6. MS ESI analysis gave the molecular weight at 506.3 (in agreement with the calculated molecular weight of 505.53).

0 Example 13 TFA salt /NH, TFA [0152] Camptothecin-20-(S)-[O-(Boc-glycyl)] (1.07g, 2.1 mmol) was treated with 50% TFA in DCM under N 2 for 1h. TFA and the solvent were removed under reduced pressure. The residue was triturated with cold ether. The precipitate formed was collected by filtration and washed with cold ether, yielding a light yellow powder (0.9 g, 1.78 mmol). Yield= 83%, TLC (silica gel, DCM/MeOH: Rf =0.23. ESI MS analysis gave the molecular weight at 406.2 (in agreement with the calculated molecular weight of 405.41).

Example 14 0 VN 0 ^H -0 H [0153] A mixture of camptothecin-20-(S)-(O-glycyl) TFA (0.9 g, 1.7 mmol), succinic anhydride (0.35g, 3.5 mmol, 2 and triethylamine (0.72 mL, 3eq.) in DMF mL) was stirred at room temperature for 5 min. The precipitate formed was collected by filtration. The solid collected was suspended in cold water (10 mL). The pH of the water suspension was adjusted to 2 by adding 5% aqueous citric acid solution. After stirring at 0 OC for 0.5 h, the precipitate was filtered, washed with cold water and ether, and dried under reduced pressure. 0.88 g (1.58 mmol) of a solid was obtained.

The yield was 99 ESI MS analysis gave the molecular weight at 505.7 (in agreement with the calculated molecular weight of 505.49). Purity was 99% based on analytical HPLC analysis.

Example -41

OOH

0 H C [0154] The titled compound was synthesized substantially according to the procedure described in Example 14 by using glutaric anhydride. The yield was ESI MS analysis gave the molecular weight at 520.5 (in agreement with the C0\ calculated molecular weight of 519.52). Purity was 98% based on analytical HPLC CN analysis.

0Example 16 0 N Camptothecin-20-(S)-[O-(Boc-Valyl)] N 0

N

0 0 [0155] To a suspension of camptothecin (350 mg) and DMAP(180 mg) in DCM mL) at 0 OC was added a DCM solution of Boc-Val-F (2 which was prepared by using a literature method (Carpino et al., J.Org.Chem., 56, 2611, 1991).

After stirring at 0-5 oC for 30 minutes, the mixture was warmed to room temperature and the stirring continued overnight. The mixture was diluted with chloroform mL), washed with water, 10% citric acid aqueous solution and saturated NaHCO 3 dried over MgSO 4 and filtered. After removing the solvents under reduced pressure, the residue was purified by a chromatography on a silica gel column eluting with chloroform/acetone The fractions containing the desired product were pooled and concentrated under reduced pressure, resulting in a solid.

Example 17 TFA salt o NH.

N AO NH. TFA -42- [0156] Camptothecin-20-(S)-[O-(Boc-Valinyl)] obtained in Example 16 was treated with 35% TFA in chloroform (10 mL) for 30 min. TFA and solvent were removed in vacuo, yielding a solid. ESI MS analysis gave the molecular weight at 448.4 (in 0 agreement with the calculated molecular weight of 447.50).

Example 18 N 0 N 0 H [0157] To a mixture of camptothecin-20-(S)-(O-Valyl) TFA salt (150 mg), succinic anhydride (4 and OMAP (2 eq.) in chloroform (10 mL) was added triethylamine (6 After stirring at room temperature overnight, the mixture was diluted with chloroform (20 mL). The resulting solution was washed with water and aqueous citric acid solution, dried over MgSO 4 and filtered. Solvent was removed in vacuo and the residue was triturated with acetone. 120 mg of the titled compound was obtained.

TLC (silca gel, chloroform/methanol=9:1):- Rf=0.22. ESI MS analysis gave the molecular weight at 548.2 (in agreement with the calculated molecular weight of 547.57).

Example 19 {5-(R)-Ethyl-9, 1 0-difluoro-1 13-tetrahydro-3H, 1 oxepino[3',4':.6,7]indolizino[1 ,2-b]quinoline-3, 15-dione-5-O-glycyl-glutaryl}-(DOC)6- Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys-)-Th r-N H 2 0 F 0 a Nr D0-Ls ~r ~rccoCy-y-~p y-b-y)Tr F Do) 6 Ly-Dy-Dyrcylocs-yrD~p-ysAu-ys-TfHH 0 (0158] H- Doc 6 Lys (Boc) -DTy r(t Bu)- DTyr(tB u)-C ys (Trt)-Tyr(t Bu)- DTrp (Boc)- Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin (0.196 mmol) of Example 3 was mixed with 5-O-(N-glutaryl-g lycyl)-5-(R)-ethyl-9, 1 0-d ifluoro- 1,4,5,13tetrahydro-3H, 15H-oxepino[3',4':6,7indolizino[1 ,2-b]quinoline-3, 15-dione (0.123 g, 0.22 mmol, 1.1 eq.) (Example 10), DIC (136 aL-, 0.88 mmol, 4.4 eq.) and 1-hydroxy- 7-azabenzotriazol (HOAT) (30 mg, 0.22 mmol, 1.1 eq.) in 5 mL of DGM. The mixture 43 was shaken for 2 days. The resin was washed successively with DMF, methanol 0and DCM. After drying in the air, the resin was treated with a mixture of TFA, H 2 0 and triisopropylsilane (TIS) (9.5 mL 0.85 mL /0.8 mL) for 2h. The resin was filtered O off and the filtrate was poured into 100 mL of cold ether. The precipitate was N collected after centrifuge. The crude product was dissolved in 100 mL of 5% AcOH aqueous solution, to which iodine methanol solution was added dropwise until yellow color maintained. The reaction solution was stirred for additional 1h. 10% Na 2

S

2 03 \0 water solution was added to quench the excess iodine. The crude product in the C- solution was purified on preparative HPLC system with a column (4 x 43 cm) of C18 DYNAMAX-100 AO (Varian, Walnut Creek, CA). The column was eluted with a linear 0 gradient from 80% A and 20% B to 55%A and 45% B in 50 min., where A was 0.1% TFA in water and B was 0.1% TFA in acetonitrile. The fractions were checked by an analytical HPLC. Those containing pure product were pooled and lyophilized to dryness. Yield: 25%. The purity was 99.9% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2761.1 (in agreement with the calculated molecular weight of 2761.04).

Example {5-(R)-Ethyl-9,10-difluoro-1,4,5,13-tetrahydro-3H, oxepino[3',4':6,7]indolizino[1,2-b]quinoline-3,15-dione-5-O-glycyl-glutaryl}-(Doc)4- Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2

FN

*N (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH, O

M

0 [0159] The titled compound was synthesized substantially according to the procedure described in Example 19 by using H-Doc-Doc-Doc-Doc-Lys(Boc)- DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)- Rink Amide MBHA Resin of Example 2. Yield was 21.4 Purity: 99% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2471.2 (in agreement with the calculated molecular weight of 2471.727).

Example 21 -44- {5-(R)-Ethyl-9, 1 0-difluoro-1 13-tetrahydro-3H, 1 oxepino[3',4'-6,7]indolizino[1 ,2-b]quinoline-3, 15-dione-5-O-glycyl-succinyl}-Aepa- DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 N0 00 N N Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 [0160] The titled compound was synthesized substantially according to the procedure for Example 19 by using 5-O-(N-succinyl-glycyl)-5-(R)-ethyl-9, 1,4,5,1 3-tetrahydro-3H, 1 5H-oxepino[3',4':6,7indolizino[1 ,2-blquinoline-3, (Example 11) and H-Aepa -D Phe-Cys (Trt)-Tyr(tB DTrp (B oc)- Lys (B oc)-Abu Gys(Trt)-Thr(tBu)-Rink Amide MBHA Resin (Example Yield was 48 Purity: 99.9% based on analyical HPLC analysis. ESI MS analysis gave the molecular weight at 1739.8 (in agreement with the calculated molecular weight of 1740.14).

Example 22 Cam ptotheci n-2 lycyl-succi nyl- Doc-Doc- Doc-Doc-Aepa-D Phe-cyclo(Cys- Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 N N N 0 0 N (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0N 0 [0161] The titled compound was synthesized substantially according to the procedure for Example 19 by using (Example 14) and H-Doc-Doc-Doc-Doc-Aepa-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)- Lys (Boc)-Abu-Cys(Trt)-Th r(tB Rink Amide MBHA Resin. Yield was 32 Purity was 99 based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2269.0. (in agreement with the calculated molecular weight of 2269.8).

Example 23 C am ptotheci n-2 0- lycyl-glIuta ryl-Ae pa- Lys- DTy r- DTyr-cyclo (C ys-Tyr- DTrp-Lys- Abu-Cys)-Thr-NH 2 0 Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr- DTrp-Lys-Abu-Gys)-Thr- NH 2 45 [0162] The titled compound was synthesized substantially according to the procedure in Example 19 by using camptothecin-20-(S)-[O-(glutaryl-glycyl)] (Example N_ 15) and H-Aepa-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)-DTrp(Boc)- U Lys(Boc)-Abu-Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin (Example Yield was c-i 11 Purity was 95% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2008.9 (in agreement with the calculated molecular weight of 2009.2).

Example 24 N- N DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

NOH

[0163] The titled compound was synthesized substantially according to the procedure in Example 19 by using (Example 18) and H-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu-Gys(Trt)- Thr(tBu)-Rink Amide MBHA Resin (Example 145 mg of a pale yellow solid was obtained. ESI MS analysis gave the molecular weight at 1562.4 (in agreement with the calculated molecular weight of 1561.8).

Example {5-(R)-Ethyl-9, 1 0-difluoro-1 13-tetrahydro-3H, 1 oxepino[3',4':6,7]indolizino[1 ,2-b]quinoline-3, 15-dione-5-O-glycinyl-succinyl}-DPhecyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 F 0_ F- N 0 DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 [0164] The titled compound was synthesized substantially according to the procedure for Example 19 by using 5-(R)-ethyl-9, 10-difluoro-1 13-tetrahydro- 3H, 1 5H-oxepino[3',4':6,7]indolizino[1 ,2-b]quinoline-3, 15-dione-5-O-(N-succinylglycyl) (Example 11) and H-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Boc)-Abu- Cys(Trt)-Thr(tBu)-Rink Amide MBHA Resin (Example A yellow solid was 46 obtained. ESI MS analysis gave the molecular weight at 1570.2 (in agreement with

O

Sthe calculated molecular weight of 1569.72).

c Example 26

O

SH-Aepa-(Doc) 4 -Gln(Trt)-Trp(Boc)-Ala-Val-pAla -His(Trt)-Leu-Leu-Rink Amide MBHA resin (SEQ ID NO: 4) [0165] The titled protected peptide-resin was synthesized substantially according D to the procedure described for Example 5. Fmoc-His(Trt)-OH, Fmoc-Gln(Trt)-OH, SFmoc-Leu-OH, Fmoc-Ala-OH, and Fmoc-Ala -OH were purchased from AnaSpec (San Jose, CA).

0Example 27 H-Aepa-(Doc) 4 -DPhe-Gln(Trt)-Trp(Boc)-Ala-Val-pAla-His(Trt)-Leu-Leu-Rink Amide MBHA resin [0166] The titled protected peptide-resin was synthesized substantially according to the procedure described for Example 26.

Example 28 4 -Gln-Trp-Ala-Val-pAla -His- Leu-Leu-NH 2 (SEQ ID NO: 4) 0 N Aepa-(Doc) 4 -GIn-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) [0167] A mixture of H-Aepa-(Doc) 4 -Gln(Trt)-Trp(Boc)-Ala-Val-pAla-His(Trt)-Leu- Leu-Rink Amide MBHA resin (0.125 mmol) of Example 26, (N-glycyl-succinyl)] (Example 14) (0.138 mmol, 1.1 DIC (0.55 mmol, 4.4 eq.), and HOBt (0.275 mmol, 2.2 eq.) in DCM (7 mL) and DMF (7mL) was shaken at room temperature for 5 days. The peptide was cleaved off from the resin using a solution of TFA, H 2 0 and TIS (9.5 mL 0.85 mL /0.8 mL) for 2 hours. The resin was filtered off and the peptide was precipitated using diethyl ether. After centrifuging the suspension, a pellet of crude peptide was obtained. The crude product was purified on a preparative HPLC system with a Microsorb C 18 column, eluting with a linear gradient from 100% A and 0% B to 20%A and 80% B in 80 min. A was 0.1% TFA in -47water and B was 0.1% TFA in acetonitrile The fractions were checked by an analytical HPLC. The fractions containing the desired product were pooled and N_ lyophilized to dryness. Purity was 96.1 based on analytical HPLC analysis. ESI O MS analysis gave the molecular weight at 2172.9 (in agreement with the calculated CN molecular weight of 2173.44).

Example 29 4 -DPhe-Gln-Trp-Ala-Val-pAla- His-Leu-Leu-NH 2 0 N C O 0 Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 [0168] The titled peptide was synthesized substantially according to the procedure described for Example 28. Purity was 99.9 based on analytical HPLC analysis.

ESI MS analysis gave the molecular weight at 2321.1 (in agreement with the calculated molecular weight of 2320.62).

Example Cam ptothecin-20-(S)-O-glycinyl-succinyl-Aepa-(Doc) 2 -Gln-Trp-Ala-Val-3Ala-His-Leu- Leu-NH 2 (SEQ ID NO: 4) 0 VN 0H -Aepa-(Doc) 2 -Gln-Trp-Ala-Val-pAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) [0169] The titled peptide was synthesized substantially according to the procedure described for Example 28. Purity was 99.9 based on analytical HPLC analysis.

ESI MS analysis gave the molecular weight at 1882.8 (in agreement with the calculated molecular weight of 1883.13).

Example 31 2 -DPhe-Gln-Trp-Ala-Val-PAla- His-Leu-Leu-NH 2 -48- N_ Iea-Do)-DPhe-Gln-Trp-Ala-Va-P3Ala-His-Leu-Leu-N 2 0[0170] The titled peptide was synthesized substantially according to the procedure described for Example 28. Purity was 99.9 based on analytical HPLC analysis.

ESI MS analysis gave the molecular weight at 2030.7 (in agreement with the calculated molecular weight of 2030.30).

Example 32 4 -Gaba-Gln-Trp-Ala-Val-pAla His-Leu-Nle-NH 2 (SEQ ID NO: 12) C'0 2 0H 0 (SEQ ID NO: 12) [0171] The titled peptide is synthesized substantially according to the procedure described for Example 28 by using Aepa-(Doc) 4 -Gaba-Gln(Trt)-Trp(Boc)-Ala-Valf3Ala-His(Trt)-Leu-Nle-Rink Amide MBHA resin (SEQ ID NO: 12).

Example 33 pG lu-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLys[N'-Aepa]-Leu-Arg (Pbf)-Pro-Gly-Rink Amide MBHA resin [0172] The titled peptide resin was synthesized substantially according to the procedure described in Example 1. Fmoc-Arg(Pbf)-OH, Fmoc-Ser(tBu)-OH, Fmoc- His(Trt)-OH, Fmoc-Pro-OH, Fmoc-Gly-OH, Fmoc-Leu-OH, Fmoc-DLys(Dde)-OH were purchased from Novabiochem, San Diego, CA. pGlu-OH was from Chem- Impex Internatoinal, Wood Dale, IL. The synthesis was carried out on a 0.25 mmol scale. The Fmoc groups are removed by treatment with 20% piperidine in Nmethylpyrrolidone (NMP) for 30 min After finishing the assembly of pGlu-His(Trt)- Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLys(Dde)-Leu-Arg(Pbf)-Pro-Gly-Rink Amide MBHA resin, the protected peptidle-resin was transferred into a reaction vessel on a shaker for manual synthesis. The Dde protecting group on DLys residue was removed by using 2% hydrazine in DMF for 0.5 h. The resin was washed completely with DMF, 49 MeOH and DCM and shaken for 2h with the pre-activated Fmoc-Aepa-OH ester solution (described in Example 4) in DMF containing 0.5 mL of DIEA. The resin was washed with DMF and treated with 20% piperidine in DMF to remove Fmoc 0protecting group on Aepa residue. The protected peptide-resin was washed CI completely by using DMF and DCM.

Example 34 pGlu-H is(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLys[N'-(Aepa-(DOC) 4 -)]-Leu-Arg(Pbf)-Pro- Gly-Rink Amide MBHA resin (Ni [0173] The titled protected peptide resin was synthesized substantially according to the procedure in Example 2 by using pGlu-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)- DLys[NF--Aepa]-Leu-Arg(Pbf)-Pro-Gly-Rink Amide MBHA resin (Example 33).

Example

H-(DOC)

4 -Aepa-Caeg-DCys(Trt)-3Pa I-DTrp(Boc)-Lys(Boc)-DCys(Trt)-Thr(BzI)- Tyr(tBu)-Rink Amide MBHA resin [0174] The titled protected peptide resin is synthesized substantially according to the procedure for Example 5. Fmoc-Thr(Bzl)-OH, Fmoc-DCys(Trt)-OH, and Fmoc- 3Pal-OH are from Chem-Impex Internatoinal, Wood Dale, IL. Fmoc-DTrp(Boc)-OH, Fmoc-Lys(Boc)-OH and Fmoc-Tyr(tBu)-OH are from AnaSpec, San Jose, CA.

Fmoc-Caeg(Bhoc)-OH is from PepSeptive Biosystems, Framingham, Mass.

Example 36

H-(DOC)

4 -Aepa-D Phe-Cys(Trt)-3 IlTyr- DTrp(Boc)- Lys(Boc)-ValI-Cys(Trt)-Thr(tB u)-R ink Amide MBHA resin [0175] The titled protected peptide resin is synthesized substantially according to the procedure for Example 5. Fmoc-3ITyr-OH and Fmoc-DPhe-OH are from Chem- Impex Internatoinal, Wood Dale, IL.

Example 37 Paclitaxel-2'-O-g lycyl

I

0 0 NH 0 0 o H 0 2 HC HO C CH

SCH,

0 C [0176] To a solution of Boc-Gly-OH (53 mg) and paclitaxel (215 mg) in 10 mL of r dichloromethane was added 4-dimethylaminopyridine (DMAP, 10 mg) followed by SEDC (58 mg). After stirring at room temperature overnight, the reaction mixture was diluted with 20 mL of dichloromethane and the mixture was washed with aqueous citirc acid, saturated NaHCO 3 and water, dried over MgSO 4 and filtered.

The solvent was removed in vacuo. The crude product was treated with 30% TFA in dichloromethane for 45 min at room temperature. TFA and the solvent were removed in vacuo, yielding a solid. 0.256 g, ESI MS analysis gave the molecular weight at 911.0 (in agreement with the calculated molecular weight of 911.1).

Example 38 Paclitaxel-2'-O-(N-glycyl-succinyl) 0 9O HO HC CH 3 0 0 [0177] A mixture of paclitaxel-2'-O-glycyl TFA salt (127 mg, 1 eq.) and succinic anhydride (150 mg, 12 eq) in 5 mL of pyridine was stirred overnight at room temperature. The solvent was removed in vacuo. The residue was triturated with water for 1 hour and the precipitate was collected by filtration, washed with water -51 and dried, yielding a solid (94.8 mg). ESI MS analysis gave the molecular weight at 01010.9 (in agreement with the calculated molecular weight of 1011.06).

Example 39

O

Paclitaxel-2'-O-(N-valyl-succinyl)

CH

3 ,o OH O0=f, 0 HN O H

H

3 C 0- O o cH 0 oH O CH, [0178] The titled compound was synthesized substantially according to the procedures described in Examples 37 and 38 by using Boc-Val-OH. ESI MS analysis gave the molecular weight at 1052.5 (in agreement with the calculated molecular weight of 1053.27).

Example Paclitaxel-2'-O-Gly-Succinyl-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu- Cys)-Thr-NH 2 j0 y-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH, o0

HC

[0179] A mixture of H-Aepa-Lys(Boc)-DTyr(tBu)-DTyr(tBu)-Cys(Trt)-Tyr(tBu)- DTrp(Boc)-Lys(Boc)-Abu-Cys(Trt)-Rink Amide MBHA resin (0.1 mmol) (Example 4), paclitaxel-2'-O-(N-glycyl-succinyl) (Example 39) (1.1 DIC (136 [IL, 4.4 and mg, 1.1 eq.) in 5 mL of DCM was shaken for 2 days. The resin was washed successively with DMF, methanol and DCM. After drying in the air, the resin was treated with a mixture of TFA, H 2 0 and triisopropylsilane (TIS) (9.5 mL 0.85 mL /0.8 mL) for 2 h. The resin was filtered off and the filtrate was poured into 100 mL of cold ether. The precipitate was collected after centrifuge. The crude product was dissolved in a mixed solution system (100 mL of 5% acetic acid aqueous solution -52and 30 mL of acetonitrile). To the solution was added dropwise iodine methanol solution until the yellow color maintained. The reaction solution was stirred for additional 45 min. 10% Na 2

S

2 03 water solution was added to quench excess iodine.

O The crude product in the solution was purified on a preparative HPLC system with a N column (4x43cm) of C 18 DYNAMAX-100 Ao (Varian, Walnut Creek, CA). The column was eluted with a linear gradient from 80% A and 20% B to 55%A and 45% B in min., where A was 0.1% TFA in water and B was 0.1% TFA in acetonitrile. The S fractions were checked by an analytical HPLC. Those containing pure product were C pooled and lyophilized to dryness. The purity was 98% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2500.9 (in agreement with 0the calculated molecular weight of 2501.0).

Example 41 Paclitaxel-2'-O-Val-Succinyl-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 C H' DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 o- P 0 H 2o o 1 0 r HC

N

MC HOH.C CH, 0 0 0 [0180] The titled peptide was synthesized substantially according to the procedure described in Example 40. The purity was 99% based on analytical HPLC analysis.

ESI MS analysis gave the molecular weight at 2066.2 (in agreement with the calculated molecular weight of 2067.4).

Example 42 Paclitaxel-2'-O-Val-Succinyl-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)- Thr-NH 2 -53- [0181] The titled peptide was synthesized substantially according to the procedure O described in Example 40. The purity was 95% based on analytical HPLC analysis.

c ESI MS analysis gave the molecular weight at 2544.3 (in agreement with the O calculated molecular weight of 2543.9).

C Example 43 N-Boc-Doxorubicin-14-O-(Fmoc-glycine) ester SOH OO 0 0 OH 0 0 N 0 C o H H, 0 0 OH

O

[0182] To a solution of doxorubicin-HCI (190 mg) in DMF (5 mL) is added

(BOC)

2 0 (1.2 eq), followed by diisopropylethylamine (2.5 After stirring for 3 hours, volatile substances are removed in vacuo and the residue is treated with water. The solid is collected by filtration, washed with water and dried. The resulting product is dissolved in DMF (10 mL). To it are added Fmoc-Gly-OH (1.2 DMAP (0.2 eq.) and EDC (1.2 eq). The mixture is stirred at room temperature for 4h. After evaporation of the solvent, the residue is partitioned between chloroform-methanol and water. Organic layer is dried over MgSO 4 and filtered. Solvents are removed in vacuo and the residue is chromatographed on silica gel eluting with chloroformmethanol The fractions containing the desired product are pooled and solvents are evaporated in vacuo.

Example 44 N-BOC-Doxorubicin-14-O-[(N-succinyl)glycine] ester 0 H 0 0 o o OOH SOr OH 0 OH 0 H,C

H

SH3C [0183] To a solution of Boc-doxorubicin-14-O-(Fmoc-glycine) ester (100 mg) in DMF (5 mL) is added 1 mL of piperidine. After stirring for 2 hours at room temperature, the mixture is diluted with chlorofom (20 mL). The mixture is washed -54with brine, dried over MgSO 4 and filtered. The solvents are removed in vacuo to a small volume mL). To the mixture are added succinic anhydride (4 DMAP (2 eq.) and triethylamine (4 The solution is stirred at room temperature overnight.

C0 Volatile substances are removed in vacuo. The residue is triturated with 5% aqueous (N citric acid. Precipitate is collected by filtration, washed with water, and dried.

Example INO pGlu-His-Trp-Ser-Tyr-DLys[N':-(doxorubicin- 1 4-O-g lycyl-succinyl-Aepa-(DOC) 4 Arg-Pro-Gly-NH 2 Aepa-(Doc) 4 OH 0 O [0184] The titled compound is synthesized substantially according to the procedure for Example 28 by using pGlu-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)- D~sN-Ap-DC4)-LuAgP PoGyRn Amide MBHA resin (Example 34) and Boc-doxorubicin-14-O-[(N-succinyl)glycine] ester (Example 44).

Example 46 pGlu-H is-Trp-Ser-Tyr-DLys[NK.(doxorubicin 1 4-O-Gly-Succinyl-(DOC) 4 -Gaba-]-Leu- Arg-Pro-Gly-NI-H 2 0 OH 0 0 I H 0 H 0 0 0 0 H ,CC pGlu-His-Trp-Ser-Tyr-j N- rLeu-Arg-Pro-Gly-NH 2 OH '0 [0185] The titled compound was synthesized substantially according to the procedure for Example 45. Fmoc-Gaba-OH was from Novabiochem, San Diego,

CA.

Example 47 Doxorubicin- 14-O-g lycyl-succinyl-(Doc) 4 -Aepa-Caeg-cyclo(DCys-3Pal-DTrp-Lys- DCys)-Th r(Bzl)-Tyr-N H 2 55 09H9 0

OH

0[0186] The titled compound is synthesized substantially according to the procedure for Example 19. The H-(Doc) 4 -Aepa-Caeg-DCys(Trt)-3Pal-Trp(Boc)- Lys(Boc)-D~ys(Trt)-Thr(Bzl)-Tyr(tBu)-Rink Amide MBHA resin (Example 35) and BOC-doxorubicin-14-O-[(N-succinyl)glycine] ester (Example 44 are used.

Example 48 Paclitaxel-2'-O-glycyl-succinyl-(DOC) 4 -Aepa-DPhe-cyclo[Cys-3Tyr-DTrp-Lys-Val- Cys]-Thr-NH 2 (Doc)-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-N

H

2 0 0

OHH

?9O O..YN

Q)

[08]Tette cmon ssnhsie usatalyacrigt h prcdr o xml 4-00b sn -Dc 4 Ap-~e-y(r)3~rDr(o Hyoc)VlC Tt-h~~)Rn Amid MBHA rei0Eape3)adpciae 0 N [0188] The titled compound is synthesized substantially according to the procedure for Example 28 by using H-Aepa)-ADoc)-Gln(Trt)-Tr(t)-la-Val-f3Ala- 56 His(Trt)-Phe-Nle-Rink Amide MBHA resin (SEQ ID NO: 6) and paclitaxel-2'-O-(Nglycyl-succinyl) (Example 38).

Example Arg-Pro-Gly-NH- 2 ~K 0 HN A-Th 1 -Aepa-(Doc) 4 1 OQ 0 0 0 H [0189] The titled compound was synthesized substantially according to the procedure for Example 45 by using pGlu-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)- DLys[N':-(Aepa-(Doc) 4 -)]-Leu-Arg (Pbf)-Pro-Gly-R ink Amide M BHA resin (Example 34) and 2'-O-(N-succinyl-glycyl)-paclitaxeI (Example 38).

Example 51 pG lu-H is-Trp-Ser-Tyr-D Lys [N'-(camptotheci n-20-(S)-O-g lycin yl-s uccinyl-(DOC) 4 Aepa-)]-Leu-Arg-Pro-Gly-N

H

2 0 0 pGIu-His-Trp-Ser-Tyr-Nf~--- Leu-Arg-Pro-Gly-NH 2 0 [0190] The titled compound is synthesized substantially according to the procedure for Example 50 by using camptothecin-20-(S)-[O-(N- succinyl-glycyl)] (Example 14).

Example 52 Abu-Cys)-Thr-NH 2 57 [0191] The titled compound was synthesized substantially according to the 0procedure described in Example 19. Yield= 11 Purity was 99.9% based on N_ analytical HPLC analysis. ESI MS analysis gave the molecular weight at 1891.8 (in O agreement with the calculated molecular weight of 1891.1).

Example 53 Camptothecin-Gly-glutaryl-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-

SNH

2 0 c:i r. N o 1 0 H N Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0192] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield= 23 Purity was 99 based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 1841.9 (in agreement with the calculated molecular weight of 1841.1).

Example 54 Camptothecin-Gly-succinyl-(Doc) 6 -DPhe-c(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 c(Doc) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0193] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=18 Purity was 98 based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2390.0 (in agreement with the calculated molecular weight of 2390.7).

Example Camptothecin-Gly-gluta ryl-Lys-Lys-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu- Cys)-Thr-NH 2 0 S Lys-Lys-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 I N t- 0 [0194] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=12 Purity was 100% based on -58analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2097.0 (in agreement with the calculated molecular weight of 2097.4).

Example 56 Camptothecin-Gly-succinyl-(Doc) 4 -DPhe-c(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 r N j (Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0195] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=31%. Purity was 100% based on Sanalytical HPLC analysis. ESI MS analysis gave the molecular weight at 2100.9 (in agreement with the calculated molecular weight of 2100.3).

Example 57 Camptothecin-Gly-succinyl-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 N- Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 0 [0196] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=21%. Purity was 97% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 1688.0 (in agreement with the calculated molecular weight of 1688.9).

Example 58 Camptothecin-Abu-succinyl-(Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu- Cys)-Thr-NH 2 S N 0 IN 1, I o -(Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 [0197] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=23%. Purity was 95% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2435.2 (in agreement with the calculated molecular weight of 2435.8).

-59- Example 59 0 0 Camptothecin-glutaryl-(Doc)2-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr- SNH2 O0 hnN-ro -(Doc) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0198] The titled compound was synthesized substantially according to the Sprocedure described in Example 19. Yield=11%. Purity was 95% based on c1 analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2074.0 (in l'- 0 agreement with the calculated molecular weight of 2074.4).

Example Camptothecin-gluta ryl-Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-

NH

2 00N 0 °-Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0199] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=16%. Purity was 95% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 1929.5 (in agreement with the calculated molecular weight of 1929.2).

Example 61

NH

2 N DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0200] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=15.6%. Purity was 94% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 1520.1 (in agreement with the calculated molecular weight of 1519.71).

Example 62 {5-(R)-Ethyl-9, 1 0-difluoro-1,4,5,1 3-tetrahydro-3H, oxepino[3',4':6,7]indolizino[1 ,2-b]quinoline-3,1 5-dione-5-O-glycyl-succinyl}-(Doc) 4 0 Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -0 N, 00 (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 [0201] The titled compound was synthesized substantially according to the cI procedure described in Example 19. Yield=25%. Purity was 97% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2320.0 (in agreement with the calculated molecular weight of 2319.6).

Example 63 {5-(R)-Ethyl-9,1 0-difluoro-1,4,5, 13-tetrahydro-3H, 1 oxepino[3',4':6,7]indolizino[1 ,2-bjquinoline-3,1 DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 N" 0 Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-cys)-Thr-NH 2 0 [0202] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=24%. Purity was 95% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2059.4 (in agreement with the calculated molecular weight of 2060.3).

Example 64 {5-(R)-Ethyl-9, 1 O-difluoro-1,4,5,1 3-tetrahydro-3H, oxepino[3',4':67]indolizino[1 ,2-b]quinoline-3,1 5-dione-5-O-glycyl-succinyl}-(Doc) 4 Aepa-Lys-DTyr-DTyr-c(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 0 F N- (Doc),-Aepa-Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0 0 [0203] The titled compound was synthesized substantially according to the procedure described in Example 19. Yield=48. Purity was 99.9% based on analytical -61 HPLC analysis. ESI MS analysis gave the molecular weight at 2626.0 (in agreement with the calculated molecular weight of 2626.9).

Example 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)- Thr-NH 2 0 So (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 [0204] The titled compound was synthesized substantially according to the 0procedure described in Example 19. Yield=10%. Purity was 98.9% based on analytical HPLC analysis. ESI MS analysis gave the molecular weight at 2365.0 (in agreement with the calculated molecular weight of 2365.0).

Example 66 H-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Aloc)-Abu-Cys(Trt)-Thr(tBu)-Rink-Amide- MBHA-Resin [0205] The titled peptide was automatically synthesized on an Applied Biosystems (Foster City, CA) model 433A peptide synthesizer based on Fluorenylmethyloxycarbonyl (Fmoc) chemistry. A Rink Amide MBHA resin (Nova Biochem, San Diego, CA) with substitution of 0.72 mmol/g was used. The Fmoc amino acids (AnaSpec, San Jose, CA) were used with the following side chain protection: Fmoc-Thr(tBu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Lys(Aloc)-OH, Fmoc- DTrp(Boc)-OH, Fmoc-Tyr(OtBu)-OH, Fmoc-DPhe-OH, and Fmoc-Abu-OH. The synthesis was carried out on a 0.25 mmol scale. The Fmoc groups were removed by treatment with 20% piperidine in N-methylpyrrolidone (NMP) for 30 min. In each coupling step, the Fmoc amino acid (4 eq, 1 mmol) was first pre-activated by 0.45M 2-(1-H-benzotriazole-1-yl)-1,1,2,3-tetramethyluronium hexafluorophosphate 1hydroxy-benzotriazole (HBTU/HOBT) in DMF. This activated amino acid ester with 1ml of diisopropylethylamine (DIEA) and (NMP were added to the resin. The ABI 433A peptide synthesizer was programmed to perform the following reaction cycles: washing with NMP, removing Fmoc protecting group with 20% piperidine in NMP for 30 min, washing with NMP, coupling with pre-activated Fmoc amino -62acid for 1h. Single couplings were applied to the Cys(Trt) 2 ,Tyr(tBu) 3 and 0 DTrp(Boc) 4 For all other amino acids double coupling was used. The resin was Scoupled successively according to the sequence. After peptide chain was O assembled, the Fmoc was removed and washed completely by DMF and DCM.

Example 67 Fmoc-Aepa-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Aloc)-Abu-Cys(Trt)-Thr(tBu)- 0 Rink-Amide-MBHA-Resin S[0206] The titled peptide was synthesized starting with the peptide from Example C1 66. The Fmoc-Aepa-OH (Neosystem Laboratoire, Gennevilliers, France. 1.5 eq, S0.75mmol) was pre-activated with [O-(7-azabenzotriazol-1-yl)-1,1,3,3- (I tetramethyluronium hexafluorophosphate] (HATU, 1.4 eq, 0.7 mmol) and 1-hydroxy- 7-azabenzotriazole(HOAT,1.4 eq, 0.7 mmol) in 2ml of DMF for 5 min. The above resin was transferred into a small reaction vessel and shaken with this activated ester of Fmoc-Aepa-OH and 1 ml of DIEA on a shaker for 2h. The resin was washed thoroughly with DMF and DCM.

Example 68 H-Doc-Doc-Doc-Doc-Aepa-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Aloc)-Abu- Cys(Trt)-Thr(tBu)-Rink-Amide-MBHA-Resin [0207] The titled peptide was synthesized starting with the peptide from Example 68. The resin was washed with DMF and treated with 25% piperidine in DMF to remove Fmoc. The resin was mixed with a DMF solution of Fmoc-Doc-OH (Chem- Impex Internatoinal, Wood Dale, IL.,1.5 eq, 0.75 mmol) N, N-diisopropylcarbodiimide (DIC, 1.5 eq, 0.75 mmol), and HOBT (1.5 eq, 0.75 mmol) for 2h. The second through fourth Fmoc-Doc-OH were coupled to the resin using the same procedure as described in coupling of the first Fmoc-Doc-OH. The process was repeated until the assembly of peptide chain was completed.

[0208] The final Fmoc was removed with 25% piperidine in DMF. The resin was washed with DMF and DCM.

Example 69 H-Doc-Doc-Doc-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys(Aloc)-Abu-Cys)-Thr-NH 2 -63- [0209] The peptide was cleaved from the Resin using 19 mL of TFA O (Trifluoroacetic Acid, Halocarbon Products Corp. River Edge, NJ), 1.6 mL of TIS S (Triisopropylsilane, Aldrich) and 1.7 mL of water for 2 hours. The resin was filtered O and the peptide precipitated by pouring into ether. Dissolve the precipitate in 150 mL C of 5% acetic acid and 30 mL of acetonitrile. 12 (20 mg/ml in MeOH) was added dropwise till there was a persistent red color. The flask was placed in a bath of hot tap water and stirred for 2 hours. The reaction was quenched using 10% Na 2

SSO

s NO^ The peptide was purified using a Phenomenex C 18 column with a gradient 5-60%

CH

3 CN where Buffer A is 0.1%TFA in water and Buffer B is 0.1% TFA in CH 3

CN

over 60 minutes. The fractions containing product were freeze dried to give 186 0mg(40% yield) of white powder. MS (Electro Spray): 1722.2 Example H-Doc-Doc-Doc-Aepa-DPhe-Cys(Trt)-Tyr(tBu)-DTrp(Boc)-Lys(Aloc)-Abu-Cys(Trt)- Thr(tBu)-Rink-Amide-MBHA-Resin [0210] The titled peptide was synthesized starting with the peptide from Example 67. The resin was washed with DMF and treated with 25% piperidine in DMF to remove Fmoc. The resin was mixed with a DMF solution of Fmoc-Doc-OH (Chem- Impex International, Wood Dale, IL.,1.5 eq, 0.75 mmol) N, N-diisopropylcarbodiimide (DIC, 1.5 eq, 0.75 mmol), and HOBT (1.5 eq, 0.75 mmol) for 2h. The second and third Fmoc-Doc-OH were coupled to the resin using the same procedure as described in coupling of the first Fmoc-Doc-OH. The process was repeated until the assembly of peptide chain was completed.The final Fmoc was removed with piperidine in DMF. The resin was washed with DMF and DCM.

Example 71 H-Doc-Doc-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys(Aloc)-Abu-Cys)-Thr-NH 2 [0211] The peptide was cleaved from the Resin using 19 mL of TFA (Trifluoroacetic Acid, Halocarbon Products Corp. River Edge, NJ), 1.6 mL of TIS (Triisopropylsilane, Aldrich) and 1.7 mL of water for 2 hours. The resin was filtered and the peptide precipitated by pouring into ether. Dissolve the precipitate in 150 mL of 5% acetic acid and 30 mL of acetonitrile. 12 (20 mg/mL of MeOH) was added dropwise till there was a persistent red color. The flask was placed in a bath of hot tap water and stirred for 2 hours. The reaction was quenched using 10% Na 2

SSO

3 -64- The peptide was purified using a Phenomenex Cl8 column with a gradient 5-60% 0CH 3 CN where Buffer A is 0.1 %TFA in water and Buffer B is 0.1 %TFA in CH 3 CN over 60 minutes. The fractions containing product were freeze dried to give 180mg(42% O yield) of white powder. MS (Electro Spray):1722.2, Example 72 Paclitaxel-2'-glutarate oCH 3

OH

0 0 Hor o o

OH

H

3 C 0 N

HOH

3 C CH 3 0 0 0 OH [0212] To a solution of Paclitaxel (HandeTech USA,lnc, Houston, Texas, lg.,1.17 mmol) in 10 mL of pyridine was added glutaric anhydride (Aldrich, 1.6 g, 14.1 mmol, 12 The resulting solution was stirred at room temperature for 4 hours and then evaporated at reduced pressure. 20 mL of water was added. The sticky solid was collected by filtration. Recrystallization from acetone/water gave 0.842 g of white solid, 0.869mmole, 74% yield. MS (Electro Spray): 969.0.

Example 73 Paclitaxel-2'-Doc-Suc-OH 0 0 0

OH

HO H C CH3 0 or SCH, O O N-Suc-OH 0 o o O OJ H H QC O H H3C N

HOH

3 C CH 3 0 0 0 [0213] To a solution of paclitaxel (1 1.17 mmol) and the Boc-Doc-OH (0.31g., c- 1.17 mmol) in 25 mL of DCM was added DIC (0.241 mL,1.54 mmol) followed by SDMAP (50 mg. 0.4 mmol). The resulting solution was stirred at room temperature for N 4 hours. The solution was washed with 3 X 10% citric acid, 3 X saturated NaHCO 3 1 x saturated NaCI and dired over MgSO 4 filtered and evaporated. The resulting residue was dissolved in EtOAc and then precipitated with hexane. The product was collected by filtration and dried under reduced pressure. Solid (1.19 g, 1.08 mmol) was obtained. Yield was 92%. MS (Electro Spray): m/e=1099.7(+1), Purity was by HPLC. The resulting Boc-Doc-paclitaxel (1.19 g, 1.08 mmol) was dissolved in mL of formic acid, stirred for 30 minutes and then evaporated. The product was dissolved in 15 mL of pyridine. To the solution was added succinic anhydride (1.29 g, 13 mmol). The mixture was stirred at room temperature overnight. Pyridine was removed by evaporation under reduced pressure. The residue was triturated with water and collected (0.99 g, 0.91mmole, 84% yield). MS (Electo Spray) gave 1099.4(+1), 1121.6 Purity was 75% by HPLC.

Example 74 Paclitaxel-2'-glutaryl-(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 e C, (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 oH

H

3 C N HC O

CH,

[0214] To a DMF (10 mL) solution of the peptide (125 mg, 0.067 mmol) from Example 69 was added paclitaxel-2'-Glut-OH (Example 72, 65 mg, 0.067 mmol), -66- HOBT (20 mg, 0.147 mmol), BOP (Benzotriazole-1-yl-oxy-tris-(dimethylamino)-

O

0phosphonium hexafluorophosphate; 29 mg, 0.067mmol) and DIEA (8 eq., 93 The solution was stirred overnight and then evaporated under reduced pressure. The O residue was dissolved in minimal MeOH and precipitated with ether. A solid was (1 obtained (108 mg, 0.04 mmol). Yield was 60% y. MS (Electro Spray) showed 1409.5(+2). To remove the Aloc from the Lys, the peptide was dissolved in DCM/THF (anhydrous, 15mL/5mL). To is were added glacial acetic acid (15 pL, 0eq.), Pd(PPh 3 4 (Tetrakis (triphenylphosphine) palladium 12 mg, 0.3 eq.) and CN Bu 3 SnH(Tributyltin hydride; 2x31 l-L, 3eq) at 0 OC. After stirring 1 hour, the solution was quenched using 0.5M HCI in ether (0.7mL, 10 The peptide was precipitated 0 with ether. The crude peptide was purified on a PLRP-S column (Polymer Labs, 100A, 8 pt) using a gradient of 5-90% over 1 hour where solvent A was 5%MeOH in water and solvent B was CH 3 CN. Pure fractions were combined and lyophilized, yielding 42 mg of the peptide. MS (Electro Spray) gave 2731.4 (in agreement with the calculated molecular weight of 2732.1). Purity was 99.9% based on HPLC analysis.

Example Paclitaxel-2'-Doc-Suc-(Doc) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 c, 0 o N° Suc-(Doc) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2

OH

H0SC 0'i' o 0 0 "r0 0 [0215] To a DMF (10ml) solution of the peptide (200 mg, 0.12 mmol) from Example 71 was added paclitaxel-2'-Doc-Suc-OH (Example 73, 140 mg, 0.128 mmol), HOBT (39 mg, 0.281 mmol), BOP (74 mg, 0.166 mmol) and DIEA (8 eq., 177 The solution was stirred overnight and evaporated under reduced pressure. A solid was obtained (355 mg, 0.126 mmol).

[0216] To remove the Aloc from the Lys, the product was dissolved in DCM/THF (anhydrous, 15mL/5mL). To it were added glacial acetic acid (19 pL, 5 eq.), Pd(PPh 3 4 (12 mg, 0.3 eq.) and Bu 3 SnH (2x54 pL, 3eq) at 0 OC. The solution was stirred for 1hour and then quenched using 0.5M HCI in ether (0.7 mL, 10 The -67product was precipitated with ether. Purify was done on a PLRP-S column (Polymer Labs, 100A, using a gradient of 5-90% over 1 hour where solvent A was N_ MeOH in water and solvent B was CH 3 CN. Pure fractions were combined and

C.)

O lyophilized. MS (Electro Spray) gave 2717.3 (in agreement with the calculated NC molecular weight of 2718.1). Purity was 99.9% based on HPLC analysis.

EXAMPLE 76 SPaclitaxel-Sar-Suc-(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 IC 0 0-=c 0N (Doc),-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 0 Q 0

H

OH

H,01 0 N 0 ,C Y [0217] The titled compound was synthesized substantially according to the procedure described in Example 28 by using 2'-O-(N-succinyl-N-methyl-glycyl)paclitaxel (Example 38) and H-Doc-Doc-Doc-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp- Lys(Aloc)-Abu-Cys)-Thr-NH 2 (Example 69). The yield was 18.8%, and the purity was based on HPLC analysis. The molecular weight was determined to be 2789.2.

Example 77 Paclitaxel-Suc-(Doc) 4 -Gaba-Gln-Trp-Ala-Val-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) 0 P -(Doc) 4 -Gaba-Gln-Tp-Aa-Al-Val-PAla-His-Leu-Nle-NH 0 I0 HC

YO

HO H3C CH, O 0

OP

yCH (SEQ ID NO: 12) [0218] The titled compound was synthesized substantially according to the procedure described in Example 28 by using paclitaxel-2'-succinyl, prepared as in Example 72, using succinic anhydride instead of glutaric anhydride and H-Doc-Doc- Doc-Doc-Gaba-Gn-Trp-Ala-Val-13Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) in which the -68peptide was prepared substantially as described in Example 1, then coupled to four 0Doc residues as substantially described in Example 2. The yield was 12.1%, and the purity was 97% based on HPLC analysis. The molecular weight was determined to O be 2537.8.

Example 78 Paclitaxel-Sar-Suc-(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-IAla-His-Leu-Nle-NH 2

(SEQ

SID NO: 12) O N o -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-pAla-His-Leu-Nle-NH 2 0 Q0 0

-H

HOH,C CH,0 CHo 0 (SEQ ID NO: 12) [0219] The titled compound was synthesized substantially according to the procedure described in Example 28 by using paclitaxel-2'-O-(N-succinyl-N-methylglycyl) prepared substantially as described in Example 38, using Boc-Sar-OH for Boc-Gly-OH) and H-(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-BAla-His-Leu-Nle-NH 2

(SEQ

ID NO: 12), in which the peptide was synthesized substantially as Example 1, then coupled to an Aepa residue as described in Example 4, followed by coupling to four Doc residues as described in Example The yield was 13.4%, and the purity was 98% based on HPLC analysis. The molecular weight was determined to be 2778.1 Example 79 Camptothecin-Gly-Suc-(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Val- Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 0 S N_ 1 0-(Doc) 4 -Aepa-Gaba-GIn-Trp-Ala-Val-pAla-His-Leu-Nle-NH 2 12) o (SEQ ID NO: 12) -69- [0220] The titled compound was synthesized substantially according to the procedure described in Example 28 by using cam ptothecin-20-(S)-[O-(N-suiC nylglycyl)] (Example 14) and H-(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-la-H is-Leu-Nleo NH 2 (Example 78, SEQ ID NO: 121. The yield was 14.4%, and the purity was 99.4% (1 based on HPLC analysis. The molecular weight was determined to be 2258 by mass spectrometry.

Synthesis of Other Compounds [0221] The compounds listed below in Tables A-I can be synthesized according to the procedures described above.

TABLE A 0 -00 0 0 0 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Val-RAla-His-Leu-Nle-NH2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Val-RlAla-His-Leu-Nle-NH2 (SEQ ID NO: 12) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gn-Trp-Ala-Val-BAla-His-Leu-Nle-NH2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -Gln-Trp-Ala-Val-BAla-His-Phe-Nle-NH2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-Ala-BAla-His-Phe-NIe-NH2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-VaI-RlAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) DoC) 4 -Aepa-Gaba-

N_)

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 70 -Aepa-(Doc) 4 -Gaba pGlu-His-Trp-Ser-Ty -N-h 1 Leu-Arg-Pro-Gly-NH 2 H0 -(DoC) 4 -Gaba pGlu-His-Trp-Ser-Ty N Tr- Leu-Arg-Pro-Gly-NH 2 H 0

H

-(DoC) 4 -Aepa-Gaba -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N H 2 H 0

H

-Aepa-(Doc) 4 -Gaba npGlu-His-Trp-Ser-Tyr N ~r-Leu-Arg-Pro-Gly-NH 2 H 0 Doc-DPhe-Gln-Trp-Ala-VaI-QAla-His-Leu-Leu-N H 2 -Doc-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-N H 2 -Doc-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2 -Doc- DAla-G In-Trp-Ala-Va I- RAla- His-Phe-N le-N H 2 -Doc- DPhe-G In-Trp-Ala-Ala-Ila- H is- Phe-N le- N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va I-RAa-His-Leu-Leu-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-Aepa-DAla-Gln-Trp-Aa-Va-1Ala-H is-Phe-N Ie-N H 2 -Doc-Aepa-DPhe-GIn-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-N Ie-N H 2 -Aepa-(DoC) 3 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-[eu-NH2 -Aepa-(DOC) 3 -DAla-Gln-Trp-Ala-VaI-BAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Ala-Ila-H is-Phe-N Ie-N H 2

-(DOC)

3 -Aepa-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 3 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) 71

-(DOC)

3 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9)

-(DOC)

3 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-N Ie-N H 2 (SEQ ID NO:

-(DOC)

3 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) o -Aepa-Doc-DPhe-GIn-Trp-Ala-Ala-gAla-His-Phe-N Ie-N H 2 ci -Aepa-Doc-DAla-Gln-Trp-Ala-Va-IgAla-His-Phe-Nle-NH 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N

H

2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-Rla-His-Leu-Nle-N

H

2 IND -Aepa-Doc-DPhe-GIn-Trp-Ala-Va-BAla-His-Leu-Leu-N

H

2 c-i -Doc-DPhe-GIn-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -Doc- DAla-G In-Trp-Ala-Va1-fAla-H is-Phe-N Ie-N H 2 -Doc- DPhe-G In-Trp-Ala-Va I-Gly-H is-Leu-Leu-N H 2 -Doc-DPhe-Gln-Trp-Ala-Va-tla-His-Leu-Nle-N

H

2 -Doc- DPhe-G In-Trp-Ala-Va1-flAla-H is-Le u-Leu- N H 2

-(DOC)

2 -GIn-Trp-Ala-Ala-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 1)

-(DOC)

2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

2 -Gln-Trp-Ala-VaI-tla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 2 -Gln-Trp-Ala-Va-2Aa-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Gln-Trp-Ala-Va-Gly-His-Leu-TP (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Val-Gly-His-Leu-- (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-V (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

-(DOC)

4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'v (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13)

-(DOC)

4 -Aepa-Gaba-Gn-Trp-Aa-Va-Gy-His-Leu-(GH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-P (CH 2 NH)-Leu-NH 2 (SEQ ID NO:13) -(Doc) 4 -Gaba-Gln-Trp-Ala-Va-'Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DoC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO:. 14) -Aepa-(DOC) 4 -Gaba-GIn-Trp-Ala-Va-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va43Ala-His-Leu-NIe-NH 2 (SEQ ID NO: 12) 72 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-N Ie-N H 2 (SEQ ID NO: 12)

-(DOC)

2 -Gln-Trp-Ala-Ala-f3Ala-His-Phe-Nle-N H 2 (SEQ ID NO: 1)

-(DOC)

2 -Gln-Trp-Ala-VaI-fla-His-Phe-Nle-N H 2 (SEQ ID NO: 6) 0 -(DOC) 2 -GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) (Ni -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

2 -Gln-Trp-Ala-ValIBAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nie-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 6) N1 -(DoC) 4 -Aepa-DPhe-GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-NIe-NH 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Ala-IlAIa-H is-Phe-Nle-N H 2 -Aepa-(Doc) 4 -DAla-GIn-Trp-Ala-VaI-ila-H is-Phe-NIe-N H 2 -Aepa-(Doc) 4 -DPhe-GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-G In-Trp-Ala-VaI-BAla-His-Leu-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-N H 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Ala-BIAla-His-Phe-N Ie-N H 2 -(Doc) 4 -DAla-Gln-Trp-Ala-Val-flAIa-His-Phe-Nle-NH 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-VaI-aAla-His-Leu-Nle-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2

-(DOC)

4 -Aepa-DAla-Gln-Trp-Ala-Va-t3Ala-His-Phe-Nle-NH 2 -(Doc) 4 -Aepa-GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO:- 9)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-BlAla-His-Leu-Nle-NH 2 (SEQ ID -(Doc) 4 -Aepa-Gln-Trp-Ala-ValIBAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -Gln-Trp-Ala-Ala-(lAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-RAla-His-Leu-N le-N H 2 (SEQ ID NO: -Aepa-(DOC) 4 -Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Gln-Trp-Ala-Ala-SAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -GIn-Trp-Ala-Val-BAla-His-Phe-Nle-NH 2 (SEQ ID NO:- 6) 73

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -GIn-Trp-Ala-VaI-i3Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) o -(DOC) 4 -Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) Ni -(DOC) 4 -Aepa-G In-Trp-Ala-VaI-Ila-His-Phe-Nle-N H 2 (SEQ ID NO: 6) -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N H 2 -Aepa-DPhe-GIn-Trp-Ala-Va-3Ala-H is-Leu-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 N- -Aepa-(DOC) 2 -DPhe-GIn-Trp-Ala-Ala-RSAla-His-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -DAla-Gln-Trp-Ala-Val-RAla-His-Phe-N Ie-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Val-G Iy-H is-Leu-Leu-N H 2 -Ap-DC2DhcGnTpAaVl-il-i-e-i-H -Aepa-(DOC) 2 -DPhe-GIn-Trp-Ala-Va-IIlia-H is-Leu- eu-N H 2 -Ap-(Doc) 2 -DPhe-Gn-Trp-Aa-a-lAa-His-e-leu-N 2

-(DOC)

2 -D~he-Gln-Trp-Ala-Val-fBAa-His-Phe-Nle-NH 2

-(DOC)

2 -DAha-Gln-Trp-Ala-Va-GlAy-His-e-Neu-NH 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-VaI-Iy~-His-Leu-Le-NH 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-VaIAla-His-Leu-te-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-NH 2 -Aepa-DAla-Gln-Trp-Ala-VaI-RAIa-His-Phe-Nle-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaIBAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Ala-Nle-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-RAla-His-Ala-N Ie-N H 2

-(DOC)

2 -Gln-Trp-Ala-VaI-flAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Va-Rla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(Doc) 2 -Aepa-DPhe-G In-Trp-Ala-Va I-BAla-H is-Ala-N le-N H 2

-(DOC)

2 -Aepa-G In-Trp-Ala-Va I-BAla-His-Ala-N Ie-N H 2 (SEQ ID NO:- 7)

-(DOC)

4 -DPhe-G In-Trp-Ala-ValI-BAla-His-Ala-N le-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Va-la-His-Ala-Nle-NH 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Val IAla-H is-Ala-N Ie-N H 2

-(DOC)

4 -Gln-Trp-Ala-VaI-(lAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) 74

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-la-His-Ala-Nle-N H 2 (SEQ ID NO: 7) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-la-His-Ala-N Ie-N H 2 (S EQ ID NO: 7) -Aepa-Gln-Trp-Ala-ValI-BAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7) 0 -(DOC) 2 -Gln-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) Cl -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BSAla-His-Ala-N Ie-N H 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Va-la-His-Ala-NIe-N H 2 C \-Aepa-(DOC) 4 -Gln-Trp-Ala-Va-la-His-Ala-Nie-N H 2 (SEQ ID NO: 7) c-i -(DOC) 4 -Aepa-GIn-Trp-Ala-Va-RAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7)

-(DOC)

4 -Gln-Trp-Ala-Val-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 4 -DPhe-GIn-Trp-Ala-Va-la-H is-Ala-Nle-N H 2

-(DOC)

4 -Aepa-DPhe-GIn-Trp-Aa-Va-RAla-His-Ala-Nle-N H 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Va-2Ala-His-Ala-N Ie-N H 2

-(DOC)

2 -Aepa-Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7)

DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-Nle-N H 2 -Aepa-(DOC) 3 -Gln-Trp-Ala-Va-LRAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 3 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(Doc) 3 -Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-RllAa-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 3 -GIn-Trp-Ala-Ala-R'la-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gn-Trp-Ala-Va-Rla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Va-3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-ValI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Doc-Gln-Trp-Ala-Ala-Rl3Aa-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

3 -Gln-Trp-Ala-ValI%Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

3 -Gln-Trp-Ala-Va-LRAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

3 -Gln-Trp-Ala-VaI-RIla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 3 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

3 -DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-N H 2 -(Doc) 3 -DAla-GIn-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 -(Doc) 3 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 75

-(DOC)

3 -DPhe-GIn-Trp-Ala-ValI-fAla-His-Leu-NIe-N

H

2

-(DOC)

3 -DPhe-GIn-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -(DoC) 3 -Aepa-DPhe-GIn-Trp-Ala-Ala-rlAla-His-Phe-Nle-N

H

2 o -(DOC) 3 -Aepa-DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 Ni -(DOC) 3 -Aepa-DPhe-GIn-Trp-Ala-VaI-G Iy-His-Leu-Leu-NH 2

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-VaIfla-H is-Leu-N Ie-N H 2

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-N H 2 -Doc-GIn-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) c-i -Doc-Aepa-Gln-Trp-Ala-Ala-tla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Aepa-Gln-Trp-Ala-Va-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) 0 -Doc-Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -DcAp-c-rpAaVl-l-HsLuNeN2(E -Doc-Aepa-Gln-Trp-Ala-Va-RAla-His-Leu-NLe-NH 2 (SEQ ID NO: -Doc-A-Gn-Trp-AAa-VAlAa-His-e-leu-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-Va-aAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -DcGnTpAaVl-l-i-e-e-H (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-Iy~-His-Leu-le-NH 2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-VaI-RAla-His-Leu-NLe-NH 2 (SEQ ID NO: -(DOC)-A-Tp-a-VaIe-cyAla-Hs-LeuDr-Lu- 2 (SEQ ID N 4

-(DOC)

4 -Aepa--D~ye~ y-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N 2 -Aepa-

N\

pGlu-His-Trp-Ser-Tyr -N -'--Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 -Aepa-N\, pGlu-His-Trp-Ser-Tyr N >Leu-Arg-Pro-Gy-NH 2 H 0 76 -(DoC) 4 -Aepa -pGiu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H H 0 0 -Aepa-Doc-N-) pGiu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2

-N\

pGiu-His-Trp-Ser-Tyr-N>- Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DoC) 3 pGlu-His-Trp-Ser-Tyr N- -Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -N\ pGlu-His-Trp-Ser-Tyr N-Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0

-(DOC)

2 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N

H

2 H 0 -(DoC) 3 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr-N>- Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc

H

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 77 -(DoC) 4 -Aepa -N-t c-i pGlu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0 0 -Aepa-(Doc) 2 pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 3

-N-

HK

c-I pG Iu-His-Trp-Ser-Tyr- N >"-Leu-Arg-Pro-Gly-NH 2 -Aepa-(Doc) 4 -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Doc pGlu-His-Trp-Ser-Tyr-N> Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 NpGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 H 0 -(Doc) 3

-N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -NpGlu-His-Trp-Ser-Tyr- N ~--Leu-Arg-Pro-Gly-N

H

2 H 0 -Doc -N pGlu-His-Trp-Ser-Tyr- N>r- Leu-Arg-Pro-Gly-N H 2 H 0 78 -(DoC) 2 -N -1

HK

Cl pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 0 -(DOC) 3

-N

H1 pGIlu-His-Trp-Ser-Tyr-N>)-Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4

-N

2H pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N H H 0 2

H

c-i -Aepa -N pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-N H 2 H 0

H

-(Doc) 2 -Aepa -N pGlu-His-Trp-Ser-Tyr N r- Leu-Arg-Pro-G Iy-NH 2 H 0

H

-(DoC) 3 -Aepa -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 4 -Aepa -N pGtu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0

H

-Aepa-Doc -N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 H 0 79

H

-Aepa-(Doc) 2 -N opGlu-His-Trp-Ser-Tyr -N)T--e-r-r-l-H CI H -Aepa-(DoC) 3

N

pGlu-His-Trp-Ser-Tyr Le-rPoGlNH H 0 LuAgPoGNH CI H c-i -Aepa-(Doc) 4 -N CI pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 0 F -'WkN 0 F N 0

-N

0

H

-(DOC)

2 -Gln-Irp-Ala-Ala-fRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 2 -Gln-Trp-Ala-ValIfAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 2 -Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

2 -Gln-Trp-Ala-VaI-fla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-GIn-Trp-Ala-Ala-fRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-Va-LRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-GIn-Trp-Ala-VaI-f Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-R.Ala-His-Phe-Nie-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-aAla-His-Leu-NIe-NH 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) 80

-(DOC)

4 -DPhe-GIn-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 -(Doc) 4 -DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-NIe-N

H

2

-(DOC)

4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N

H

2 o -(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-aAla-His-Leu-NIe-N

H

2 c-I -(DoC) 4 -DPhe-GIn-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-N

H

2

-(DOC)

4 -Aepa-DAla-Gln-Trp-Ala-VaI-aAla-His-Phe-Nle-NH 2

IND-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Va I-Gly-H is-Leu-Leu-N H 2 c-I -(DOC) 4 -Aepa-DPhe-Gn-Trp-Ala-Va-BlAla-H is-Leu-N Ie-N H 2 -(DoC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Ala-la-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-Val-aAla-His-Phe-N Ie-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gn-Trp-Ala-Va-3Ala-H is-Leu-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-IAla-H is-Leu-Leu-N H 2 -(Doc) 4 -Gln-Trp-Ala-Ala-RAla-His-Phe-NIe-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Gln-Trp-Ala-Val-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

4 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Gln-Trp-Ala-Va-fRAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Ala-IlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Val-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6)

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Aepa-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -Gln-Trp-Ala-Ala-i3Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(Doc) 4 -GIn-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

2 -DPhe-Gln-Trp-Ala-Ala-Ila-His-Phe-N Ie-N H 2 -(Doc) 2 -DAla-Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 81 -(DOC)2-DPhe-Gn-Trp-Ala-Val-la-His-Leu-Nle.N

H

2 -(Doc)2-DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Leu-NH 2 -Aepa-DPhe-Gn-Trp-Ala-Ala-BAla-His-Phe.Nle-NH 2 o -Aepa-DAla-Gln-Trp-Ala-Val-RiAla-His-Phe.N Ie-N H 2 c-i -Aepa-DPhe-Gln-Trp-Ala-Val-Gly.His-Leu-eu.NH 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Ala-His-LeuNle.NH 2 -Aepa-DPhe-Gln-Trp-Ala-Val-Ala-His-Leu-Leu-NH 2 ID-Aepa-(Doc)2-DPhe-Gn-Trp-Aa-Aa-Ala-H is-Phe-N e-N H 2 -Aepa-(DOC) 2 -DAla-Gln-Trp-Ala-Val-BlAla-H is-Phe-Nle-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Val.Gly..His-Leu-Leu-N

H

2 -Aepa-(Doc) 2 -DPhe-Gn-Trp-Ala-Val-RAla-H is-Leu-N Ie-N H 2 -Aepa-(Doc) 2 -DPhe-Gn-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -(DOC)2-Aepa-DPhe-Gln-Trp-Ala-Ala-Rla-His-Phe-N le-N H 2 -(Doc)2-Aepa-DAla-Gln-Trp-Ala-VaI-R3Ala-His-Phe-N le-N H 2

-(DOC)

2 -Aepa-DPhe-GIn-Trp-Ala-Va I-Gly-H is-Leu-Leu-N H 2 -(DOC)2-Aepa-DPhe-Gln-Trp-Aa-Va-Aa-His-LeuNle.NH 2 -(Doc)2-Aepa-DPhe-Gln-Trp-Aa-Va-RAla-H is-Leu-Leu.N H 2 -(Doc)2-Aepa-DPhe-Gln-Trp-Ala-Va-Aa-His-AaNle.NH 2 -(DOC)2-Aepa-Gln-Trp-Ala-Va-la-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC)4-DPhe-Gln-Trp-Ala-Va-lAla-His-Ala-Nle-N

H

2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-AIa-Va I-fAla-H is-Ala-Me-N H 2 -Aepa-(DoC) 4 -DPhe-Gln-Trp-Ala-Val-Rla.}is.Ala..NleNH 2

-(DOC)

4 -Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC)4-Aepa-Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DoC) 4 -Gln-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7)

-(DOC)

2 -DPhe-G In-Trp-Ala-VaI-RAla-His-Ala-N Ie-N H 2 -Aepa-DPhe-GIn-Trp-Ala-Va-RAla-His-Ala-N Ie-N H 2 -Aepa-(Doc) 2 -DPhe-Gn-Trp-Aa-Va-RAla-His-Ala-Nle.N

H

2 -(DOC)2-Gln-Trp-Ala-VaI-Ila-His-Ala-Nie-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 2 -Gln-Trp-Ala-ValI-BAla-H is-Ala-N Ie-N H 2 (S EQ ID NO: 7) -Aepa -Lys- DTyr- DTy r-cyclo(C ys-Tyr- DTrp- Lys-Ab u-.C ys)-Th r- N H 2 82 -Aepa

-NA

__pGlu-His-Trp-Ser-Tyr N" Leu-Arg-Pro-Gly-NH 2 o~ H 0 0-(Doc) 2 -Aepa pGlu-His-Trp-Ser-Tyr N >F-Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 2 -Aepa-(Doc) 4

-N-

pGlu-His-Trp-Ser-Tyr N rr-Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa

-N

pGlu-His-Trp-Ser-Tyr 'Leu-Arg-Pro-NH Et H 0 -(Doc) 2 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -(Doc) 4 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr N-r-Leu-Arg-Pro-NHEt H 0 -Aepa-(Doc) 2 N pGlu-His-Trp-Ser-Tyr N '-1TLeu-Arg-Pro-NH Et H 0 83 -(Doc) 2

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-NHEt o~ H 0 0-Aepa-(DoC) 4 -N

A

pGlu-His-Trp-Ser-His -Nt-rTyPoGlNH __-Aepa H 0 -(Doc) 2 -Aepa -N

H

pGlu-His-Trp-Ser-His N-)-Trp-Tyr-Pro-Gly-N

H

2 -(Doc) 4 -Aepa -N H

A

pGlu-His-Trp-Ser-His N 1 Trp-Tyr-Pro-Gly-N

H

2 H 0 -Aepa-(Doc 2 pGlu-His-Trp-Ser-His N 'r-Trp-Tyr-Pro-Gy-NH 2 H 0 N 0 I 0 Y i 0 0 0 -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Va-la-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-NIe-NH 2 (SEQ ID NO: 12) 84 -(Doc) 4 -Aepa-Gaba

-N-

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H0 -Aepa-(Doc) 4 -Gaba pGlu-His-Trp-Ser-Tyr -WN>-Leu-Arg-Pro-Gly-NH 2 H 0 (DoC) 4 -Gaba pGlu-His-Trp-Ser-Tyr N ~'-Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 4 -Aepa-Gaba N:r pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N

H

2 H 0

H

-Aepa-(DoC) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 0 N 00 O H -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-.Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba

N

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N

H

2 H 0 85 -Aepa-(DoC) 4 -Gaba pGlu-His-Trp-Ser-Tyr N-'Leu-Arg-Pro..GyNH 2 H 0 0 -(Doc) 4 -Gaba pGtu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0

H

-(DOC)

4 -Aepa-Gaba N pGlu-His-Trp-Ser-Tyr -N -r Leu-Arg-Pro-Gly-NH2 H 0

H

-Aepa-(DOC) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr N Th-Leu-Arg-Pro-Gly-NH 2 H 0 -DPhe-cyclo(Cys-Tyr- DTrp-Lys-Abu-Cys)-Thr-N H 2 0 N 0 0 0

DOC)

4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 TABLE B 0 F jiN F N0

H

86

H

-Doc -N p~luHis-rp-Sr-T >rN" Leu-Arg-Pro-Gly-NH 2 H H 0

H

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 3

-N

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0

H

-(OC)

4 -N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 H 0

-(DOC)

4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)6-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc) 5 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Val-Cys)-Th r-N H 2

-(DOC)

4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2

-(DOC)

3 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2

-(DOC)

2 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -Doc-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-3ITyr- DTrp-Lys-VaI-Cys)-Thr-N H 2

-(DOC)

6 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2

-(DOC)

5 -Ae pa- D Phe-cycl o(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(Doc) 3 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-N H 2

-(DOC)

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-N H 2 Doc-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 87 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 -Aepa-(DOC) 3 DPhe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 __-Aepa-(DOC) 2 -D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r-N H 2 o-Aepa- Doc- DPhe-cyclo (Gys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 c-i -(DOC) 6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -(DOC)5-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DoC)4-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -(DOC)3-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -(Doc)2-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 Do-DPecco( s-31Tr -p y-T -y)T -NH -(Doc) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 OC)-ep -he-cyclo(Cys-3 Tr-yIrp-Cys)-Th r-N ys-H 2 rN -(D5Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -(Doc) 6 -Ae pa-D Phe-cyclo(Cys- 3I1Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC)3-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-NH 2 -(DOC)2-Aepa-D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2 -(Doc)-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 DcApa Ph e-cyclo(C ys-3 I Tyr- DTrp- Lys-Th r-C ys)-Ih r-NH 2 Aepa- D Phe-cyclo (Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2 -Aepa-(Doc)2-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Aepa-(Doc)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Aepa-(DoPhc-Doh(Ccyclo(ICyr-3ITr-D Lys-Th r-C y) -Th H2NH -Apo-DPhe-cyclo(Cys-3 I~yr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(Dep)-DePaDPhe-cyclo(Cys-3 Tr-sTr-ys-Th r-N ys-H 2 r -()-DPhe-cyclo(Cys-3Tyr-DTrp-Lys- -Cys)-Thr-NH 2 -(Doc) 4 -p-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-hr-Cys)-Th r-N H 2 -(DOC)4-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)3-DPhe-cyclo(Cys-3IlTyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)2-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 2 D Phe-cyclo(C ys-3 ITyr- DTrp- Lys-Abu -Cys)-Th r-N H 2 -(DOC)6A-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 88 -(Doc) 5 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Gys)-Thr-NH 2 -(o)-eaDh-ycoCs3-rDr-LsAuCs-h-H __-(DOC)2-Aepa-D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -DcAp-Ce-yl(y.)yrDr-y-buCs-h-H o -(Doc)(-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Ae p-a-c(Aepa-D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Ab u-Cys)-Thr- NH 2 -Ae pa- (Doc)2-D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa D Phe-cyclo (C ys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -Aepa-()-DPhe-cyclo(Cys-3ITyr-DTrp-Lys- a b-Cys)-Thr-N H 2 c-i Ap-D c-Phe-cyclo(Cys-3 ITyr-DTrp-Lys- Abu-Cys)-Thr-N H 2 h-yl Cs3ITy-Dr-LsV -Cy)Thr -Aepa)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-VAI-Cys)-Thr-N H 2 Phe-cyclo(Cys-Tyr-DTrp-Lys-A-Cys)-Thr-N H2 ecyl( y -y-D r-y -b -C s-h-H -(Doc) 4 -p-DPhe-cyclo(Cys-ITyr-DTrp-Lys- aI-Cys)-Thr-NH 2 -(Doc)2-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-ys)-Thr-N

H

2 -(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)6-e-DPhe-cyclo(Cys-Tyr-DTrp-ys-Abu-Cys)-Th r-N H2 -(Doc) 2 -e-DPhe-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H2 -(DOC)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N 2 -(D2Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc) 5 ,-Ae pa D~ye~-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Thr-N H 2 y-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)4-Aepa D~y -e -cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Thr-N H 2 -(Doc)-Ae pa -Ly- ~he -cyclo(Cys-Tyr-DTrp-bbu-Cys)-Th r- 2

H

-(DOC)2-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc)-Aepa -Lys- DTyr-DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- H 2 -DcAp-Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- NH 2 -(Doc)-AaLys-DTyr- DTyr-cyclo(ys-Tyr- DTrp- Lys-Ab u-Cys)-ThrN H 2

-(DOC)

2 -AeLys- DTyr- DTy r-cyclo(Cys-Tyr- DTrp- Lys-Abu-C ys) -Ihr-N H 2 89

-(DOC)

3 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DoC) 4 Lys- DTyr- DTyr-cyc lo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- NH 2

-(DOC)

5 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(O)-y-0rDy-yl(y-y-~pLsAuCs-h-H o -(DOC) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 c-i Ap-(Doc)-DyrDe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Aepa-(DOC)2-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 IND-Aepa-(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Ae pa-(Doc- Lys-cDyl(- Tyr-Dcorpy-Ty-rLys-Abu-Cys)-Thr- H-N 2 -Aepa-(DOC) 3-Lys- DTy r- DTyr-cyclo(C ys-Tyr-DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Ap-DC2 y-Dcr -rccoCs-y-Dr-LsAu Cs-hr -Aepa-(Doc)-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(Doc 2 PysD r-ey-cyclo (Cys-3ITyr- DTrp- Lys-Ab u-C ys)-Thrr-N H 2 -Ae-oLy-yrDy-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -()-Aepa-DPhe-cyclo(Cys-3 lTyr-DTrp-Lys-Abu-ys)-Thr-N H 2 -D(e )--cyclo(3yrD r-ys-a- rpLyDCys)-Th H 2 z)-yr -(DOC)6-Aepa-Dae-cyclo(DCys-3 PI- DTrp- Lys-ADC ys)-Th (z1Tr-N N -(Aep)-e-Caeg-cyclo( Cys- 3Pa I-DTrp- Lys- DC y)-Th r( BzI)-Ty r-N H 2 -(DOC)4-Aepa-C aeg-cyclo( DCys-3 Pa I-DTrp- Lys- D Cys)-Th r(Bz1)-Ty r- N H 2 DOC)3-Aepa-C aeg -cyclo( DCys-3 PaI- DTrp- Lys- D Cys)-Th r(Bz I)-Tyr- N H 2 -(Doc)2-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(Doc)-Aepa-C aeg-cyclo (DC ys-3 Pa DTrp-Lys- DCys)-Th r(Bz)-Tyr- N H 2

-(DOC)

2 -CAepa-cacyclD (D y-3Pa -D~rp.Lys-sDyss)-Th r( yr- N H 2 -(DOC-Ae-C aeg -cyclo(DCys-3 P aI-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 -(Doc)4-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr- N H 2 -(Doc)3-Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Thr(BzI)-Tyr-N H 2 -(Doc)2-C aeg-cyclo(D Cys- 3P a I- DTrp-[Lys- DCys)-Th r(Bz I)-Tyr- NH 2 -(Doc)-C aeg-cyclo(DC ys- 3Pa I- DTrp-Lys- DC ys)-Thr(Bz) -Tyr- N H 2 -(eDoc-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -Doc-D)-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N 2 -Ae pa-DOC)-Caeg-cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz )-Tyr-N H 2 -Ae pa-(Doc) 2 -C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DC ys)-Th r(Bz1) -Ty r- N H 2

(DOC)

6 -Ae pa- Lys- DTy r- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu Cys)-Th r- N H 2 90

-(DOC)

4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(o)-eaDh-ycoCsTrDr-)sAuCs-h-H 0 -(DOC)4-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 Cl -(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ihr-N

H

2 -(D-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(D2Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-NH 2 -(DOC)4-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 c-i -(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

-(DOC)

8 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Aepa)HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -(Aepa)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Aepa)HSDAVFTDNYTRLRKQMAVKKFLNSILN-NH 2 (SEQ ID NO: 17) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) -(Aepa)HSDAVFTDNYTRLRKQ(Ne)AVKKYLNSILN-NH 2 (SEQ ID NO: 19)

-HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH

2 (SEQ ID NO:

-HSDAVFTDNYIRLRKQMAVKKALNSILN-NH

2 (SEQ ID NO: 16)

-HSDAVFTDNYTRLRKQMAVKKFLNSILN-NH

2 (SEQ ID NO: 17)

-HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH

2 (SEQ ID NO: 18) -HSDAVFTDNYTRLRKQ(Nle)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-N

H

2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2

-(DOC)

4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 0 F N0

NN

0

H

2 (SEQ ID NO: -91 -(Aepa)HSDGI FTDSYSRYRKQ MAVKKYLAAVLGKRYKQR(A6c)KNK-NH 2 (SEQ ID NO: 21) -(Aepa)HSDGI FTDSYSRYRKQ MAVKKYLAAVL(Ava)KRYKQ RVKN K-NH 2 (SEQ ID NO: 22) N- -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(f&Ala)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) 2 (SEQ ID NO: IND -HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A6c)KNK-NH 2 (SEQ ID NO: 21) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(BAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -Ae pa -Lys- DTyr-DTyr-cyclo(C ys-Tyr- DTrp- Lys-Abu-Cys)-Th r-N H 2 Lys- DTyr- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2

DOC)

4 Lys- DTy r- DTyr-cyclIo(C ys-Ty r- DTrp-Lys-Ab u-C ys)-Th r- N H 2 -(DOC)6-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -D Phe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2

DOC)

4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Ihr-N H 2

-(DOC)

6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Ihr-N

H

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2

DOC)

4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2

-(DOC)

6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Th r-NH 2 -(Ae pa) 2 Lys- DTyr- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-C ys)-T h r- N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Gys)-Thr-N

H

2 -(Aepa) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ihr-N

H

2

-(DOC)

6 -Aep a- Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 Doc) 4 -Ae pa- Lys- DTy r-DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 2 -Ae pa- Lys- DTy r- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-T hr- N H 2 -Ae pa- Lys- DTyr- DTy r-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 92 -Lys- DTyr- DTyr-cyclo (Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 -Aepa-(Doc)6-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Aepa-(Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

DOC)

2 Lys- DTyr- DTy r-cyclo (Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r-N H 2 CI -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -Caeg-cyclo(DCys-3Pa.-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2

-(DOC)

4 -C aeg -cyclo (D Cys- 3Pa I-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2

-(DOC)

6 -C aeg -cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 No aa

N_

0 N

H

-DcGl-rpAa-l-Bl-HsPh-leN2 SQ DN0-1 -Doc-Gln-Trp-Ala-Val-IIAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Gln-Trp-Ala-VaI-GlAy-His-e-Le-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-G~ly-His-Leu-le-NH 2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-VaI-BAla-His-Leu-NLe-NH 2 (SEQ ID NO -Doc-G~GIn-Trp-Ala-VaBA la-H is-Leu-Leu-N (SQH2 N:4 -Doc-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-le-N

H

2 -Doc- DPhe-G In-Irp-Ala-Va I- ly- H is- Leu-Le-N H 2 -Doc- D~he-GI n-Trp-Ala-Va I-g~l-H is-e-Nle-N H 2 -Doc-DAha-Gln-Trp-Ala-Va-Lla-His-Phe-Nle-N

H

2 -Doc-AeDPhe-Gln-Trp-Aa-la-a-His-Phe-Nl

H

2 -Doc-Aepa-D~he-Gln-Trp-Ala-Va-RAla-His-Phe-Nle-NH 2 -Doc-Aepa-DAha-Gln-Trp-Ala-Va-BAla-His-e-Neu-N

H

2 -Doc-Aepa-DPhe-G In-Trp-Ala-VaI-G~ly-His-Leu-Le-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-f Ala-His-Leu-Le-NH 2 -Aepa-(Doc) 3 -DPhe-GIn-Trp-Ala-Ala-IAla-His-Phe-Nle-NH 2 -Aepa-(Doc) 3 -DAla-GIn-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 93 -Aepa-(Doc) 3 -DPhe-GIn-Trp-Ala-Va-BAla-His-Leu-Nle-N H 2 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Leu-N

H

2 -(DOC)3-Aepa-Gln-Trp-Ala-Ala-flAIa-His-Phe-NIe-N H 2 (SEQ ID NO: 1) o -(DOC) 3 -Aepa-Gin-Trp-Ala-VaI-RAla-His-Phe-Nle-N H 2 (SEQ ID NO: 6) c-i -(DOC) 3 -Aepa-GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DOC)3-Aepa-Gln-Trp-Ala-ValIfAa-His-Leu-N Ie-N H 2 (SEQ ID NO:

-(DOC)

3 -Aepa-Gln-Trp-Ala-VaI-rlAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-N Ie-N H 2 N- -Aepa-Doc-DAla-Gln-Trp-Ala-Va I-RAla-H is-Phe-N Ie-N H 2 -Aepa-.Doc-DPhe-Gln-Trp-Ala-Va I-Gly-His-Leu-Leu-NH 2 C) -Aepa-Doc-DPhe-Gin-Trp-Ala-Va-RAla-His-Leu-NIe-N H 2

N-

-Aepa-Doc-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-+' (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Y (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Ap-DC4GnTpAl-a-l-i-e-- (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

-(DOC)

4 -Gaba-GIn-Trp-Ala-VaI-Gly-His-Leu-T+ (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DoC) 4 -Aepa-Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'P (GH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Aa-Va-Gy-His-Leu-,P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(Doc) 4 -Gaba-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Gaba-Gln-Trp-Ala-Va-flAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Aepa-(Doc) 4 -Gaba-GIn-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Gln-Trp-Ala-ValI-fAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-PIla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-RlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-PiAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va I-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) 94 -Aepa-(DOC) 2 -Gln-Trp-Ala-ValI-rla-His-Leu-Nle-NH 2 (SEQ ID NO: C) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-BlAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

2 -Gln-Trp-Ala-Ala-afla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) C0 -(DOC) 2 -Gln-Trp-Ala-ValIIA~a-His-Phe-Nle-N H 2 (SEQ ID NO: 6)

-(DOC)

2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

2 -Gln-Trp-Ala-VaI-aIla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DoC) 2 -Gln-Trp-Ala-Val-Pila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) 2 (E DN:1 ci -Aepa-Gln-Trp-Ala-Vla-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Ap(lNr-i-alR l-i-h -l-N 2( E DN :6 -(DoC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-VaIBAla-His-Leu-NIe-N

H

2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-VaIIAla-His-Leu-Leu-N

H

2 -Aepa-(Doc) 4 -DPhe-GIn-Trp-Ala-Ala-aAla-His-Phe-NIe-N

H

2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-Va-3Ala-H is-Phe-NIe-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-RlAIa-His-Leu-Nle-NH 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-RlAla-His-Leu-Leu-NH 2

-(DOC)

4 -DPhe-G In-Trp-Ala-Ala- 4Aa-His-Phe-N Ie-N H 2

-(DOC)

4 -DAla-Gin-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Va-aAla-His-Leu-N Ie-N H 2

-(DOC)

4 -DPhe-GIn-Trp-Ala-Val-PlAla-His-Leu-Leu-NH 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2

-(DOC)

4 -Aepa-DAla-Gln-Irp-Ala-Va-RAla-His-Phe-Nle-NH 2

-(DOC)

4 -Aepa-GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 4 -Aepa-GIn-Trp-Ala-Va-RlAIa-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Aepa-Gln-Trp-Ala-VaIRAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -GIn-Trp-Ala-Ala-aAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-aAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -GIn-Trp-Ala-Va-RAla-H is-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO. 4) -(Doc) 4 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) 95 -(DoC) 4 Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DoC) 4 -GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) O)(lNr-l-Vlil-i-e -leN 2(E DN

-(DOC)

4 -Gln-Trp-Ala-VaI-B3AIa-H is-Leu-Leu-N H 2 (SEQ ID NO: (1 -(DOC) 4 -Aepa-Gln-Trp-Ala-Ala-'Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-IRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-DAla-Gin-Trp-Ala-VaI-RAla-His-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 ci -(DOC) 2 -DPhe-Gln-Trp-Ala-ValIRAla-His-Leu-Leu-N H 2 r- -(DOC) 2 -DPhe-Gln-Tp-Ala-Va-2Ala-His-Leu-Nle-NH 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2

-(DOC)

2 -DAla-Gln-Trp-Ala-VaI-Bl3Aa-His-Phe-N Ie-N H 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Ala-RIAla-His-Phe-Nle-N H 2 TABLE C >N o cl N 0

-(DOC)

2 -DPhe-Gln-Trp-Ala-Ala-rlAla-His-Phe-Nle-NH 2

-(DOC)

2 -DAla-Gln-Trp-Ala-Val-f3Ala-His-Phe-N Ie-N H 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2

-(DOC)

2 -DPhe-GIn-Trp-Ala-VaIAla-His-Leu-Nle-NH 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-3Ala-H is-Phe-N Ie-N H 2 -Aepa-DA~a-Gln-Trp-Ala-Va I-BAla-His-Phe-Nle-N H 2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Ala-RIAla-His-Phe-Nle-NH 2

-(DOC)

2 -Aepa-DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-N Ie-N H 2 -(Doc) 2 -Aepa-DPhe-G In-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2

-(DOC)

2 -Aepa-DPhe-G In-Trp-Ala-VaI-fRAla-His-Leu-N Ie-N H 2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-ValI-IAla-His-Leu-Leu-NH 2 96 -Aepa-(DOC) 2 -GIn-Trp-Aia-Va-BAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7) 0 -Aepa-Gln-Trp-Ala-Val-BAla-His-Ala-N le-N H 2 (SEQ ID NO: 7)

-(DOC)

2 -Gln-Trp-Ala-ValIBAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) 0 -Aepa-(DoC) 2 -DPhe-GIn-Trp-Ala-Va-IIla-His-Ala-N Ie-N H 2 -Aepa-DPhe-GIn-Trp-Ala-Va-la-His-Ala-Nle-N H 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Va-BlAla-H is-Ala-Nle-N H 2 ,'I--Aepa-(DOC) 4 -Gln-Trp-Ala-Va-fAIa-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DoC) 2 -Aepa-DPhe-Gln-Trp-Ala-ValI-BAla-His-Ala-Nle-N H 2 (1 -(Doc) 2 -Aepa-Gln-Trp-Ala-Val-BIAla-H is-Ala-NIe-N H 2 (SEQ ID NO: 7) -(DoC) 4 -DPhe-Gln-Trp-Ala-Va-PiAla-His-Ala-Nle-NH 2 -(DoC) 4 -Aepa-DPhe-Gln-Trp-Ala-VaIBAla-H is-Ala-N Ie-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-RAla-H is-Ala-N le-N H 2

-(DOC)

4 -Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7)

-(DOC)

4 -Aepa-Gn-Trp-Ala-VaIAla-His-Ala-Nle-NH 2 (SEQ ID NO:7) -Aepa-Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-Val-BAla-His-Leu-Ne-NH 2 (SEQ ID NO: -Aepa-Doc-GIn-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 3 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 3 -Gln-Trp-Ala-Val-R2Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 3 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO:9 -Aepa-(DOC) 3 -Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 3 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

3 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 3 -Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DoC) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

3 -GIn-Trp-Ala-VaI-BAla-His-Leu-Nie-NH 2 (SEQ ID NO:

-(DOC)

3 -Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Ala-PiAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Va I-Gly-H is-Leu-Leu-N H 2

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-VaI-tRAa-His-Leu-Nle-N H 2

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2

-(DOC)

3 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 97

-(DOC)

3 -DAla-Gln-Trp-Ala-VaI-BiAla-His-Phe-Nle-NH 2

-(DOC)

3 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2

-(DOC)

3 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-NIe-N H 2 0 -(Doc) 3 -DPhe-GIn-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 Cl -Doc-Gln-Trp-Ala-Ala-BAla-His-Phe-NIe-N H 2 (SEQ ID NO: 1) -Doc-Gin-Trp-Ala-VaI-BlAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) -Doc-GIn-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) C \-Doc-GIn-Trp-Ala-VaI-BAla-H is-Leu-Nle-N H 2 (SEQ ID NO: CI -Doc-Gln-Trp-Ala-VaI-fRAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-Aepa-Gln-Trp-Ala-Ala-3Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Aepa-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Doc-Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Doc-Aepa-Gln-Trp-Ala-Val-BAla-His-Leu-NIe-NH 2 (SEQ ID NO: -Doc-Aepa-GIn-Trp-Ala-Va-lAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -(DoC) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 1 0 -(Doc) 3 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N- Le-rPoGlNH -(DoC) 4 -Aepa N-

H

pGlu-His-Trp-Ser-Tyr N r Leu-Arg-Pro-Gly-NH 2 0 98 0 0 -Aepa-Doc N

H

pGlu-His-Trp-Ser-Tyr N e-rPoGlNH H 0 -Aepa-(Doc) 2 N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H2 0 -Aepa-(Doc) 3

N

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4

N

H

H Leu-Arg-Pro-Gly-NH 2 0 pGlu-His-Trp-Ser-Tyr N ILeu-Arg-Pro-Gly-NH 2 H 0 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 1 0 -(Doc) 2 -Aepa

H

pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2

H

0 -(Doc) 3 -Aepa pG~uHis-rp-Sr-T H I4 Leu-Arg-Pro-Gly-NH 2 0 99 -(DoC) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH, H 0 -Aepa-Doc N-

H

pG lu-H is-Trp-Ser-Tyr Leu-Arg- Pro-G ly-N H 2 H i 0 -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr e-r-r-l-H H 6 e-r-r-l-H -Aepa-(Doc) 3 N Hf pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4

N

H I pGlu-His-Trp-Ser-Tyr -Doc N

H

pGlu-His-Trp-Ser-Tyr -(DoC) 2

N

H

pGlu-His-Trp-Ser-Tyr -(DoC) 3

N-'

H

Leu-Arg-Pro-Gly-NH 2 H 61 H 0 -Leu-Arg-Pro-Gly-NH 2 H 0 pGiu-His-Trp-Ser-Tyr--- -LuAgPoGyN H u-rg1o- yN 2 0 100 -(Doc) 4

N

H

O pGlu-His-Trp-Ser-Tyr N L o ~H 0 uAg-r-GyN 2 -DocN N

H

pGlu-His-Trp-Ser-Tyr 0 -(DoC) 2 H pGlu-His-Trp-Ser-Tyr -WFLuAN-r-l-H H 0 -(Doc) 3

-N

H

pGlu-His-Trp-Ser-Tyr N'>Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4

N

pGlu-His-Trp-Ser-Tyr e-r-r-l-H H 0

H

-Aepa N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2

H

-(Doc) 2 -Aepa N pGlu-His-Trp-Ser-Tyr N" Leu-Arg-Pro-Gly-NH 2 H 0 101

H

-(Doc) 3 -Aepa N pGlu-His-Trp-Ser-Tyr -N 'f-Leu-Arg-Pro-Gly-NH 2 02

H

-(Doc) 4 -Aepa pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc

HN

_N

pGlu-His-Trp-Ser-Tyr N_ Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DoC) 2

H

N

pG Iu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N

H

2 Ho -Aepa-(Doc) 3

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0

HH

-Doc N pGlu-His-Trp-Ser-Tyr N

H

FLe u-Arg-Pro-Gly-NH 2 0 102-

H

-(DoC) 2

N

opGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0

H

pGlu-His-Trp-Ser-Tyr ij Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 4

N

pGlu-His-Trp-Ser-Tyr -N'ILeu-Arg-Pro-Gly-NH 2 H 0 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Gys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2

-(DOC)

4 -Aepa-D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2

-(DOC)

4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2

-(DOC)

4 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2

-(DOC)

6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Val-Cys)-Thr-N H 2 -(Doc) 2 -Aepa-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2

-(DOC)

3 -Aepa-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Th r-N H 2

-(DOC)

5 -Aepa-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Ihr-N H 2

-(DOC)

6 -Aepa-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Gys)-Th r-N H 2 -(Aepa) 2 -DPhe-cyclo(Gys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC)2-D Phe-cyclo (C ys-3 ITyr- DTrp- Lys-Va I-C ys)-Th r- N H 2

-(DOC)

3 -D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-VaI-Cys)-Th r- N H 2

-(DOC)

5 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Val-Cys)-Thr-N H 2 103 -Aepa-(DOC) 4 DPh e-cyclo(Cys-3 I Tyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 __-Aepa-(DOC) 2 DPh e-cyclo(Cys-3 I Tyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 o -Aepa-Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 c-i -(DOC)5-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-NH 2 -(DOC)4-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-NH 2 -(DOC)3-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DoC)2-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Doc)- D Phe-cyclo(C ys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(ea2 ecco(y- y-Dr-ysT -y)T -NH -(Doc)-epDPhe-cyclo- (CI 31Tyr- DTrp-T-ys-Th r-N y-H r NH -(D5Aepa-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(o)-eaDheccoCs3-y-ipLsTr-y)TrNH -(DOC)2-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc)-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -(Doc)(-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(Doc)(-Aepa-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 AepaO)-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Aepa-(Doc)-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Aepa-()-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -Aea(c 2 DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -()-Aepa-DDPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Aepa- DP he-cyc lo(C ys-3 I Tyr- DTrp-Lys-Th r-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-NH 2

DOC)

4 -A-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-r-Cys)-Thr-N 2 -Aepa)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-h r-Cys)-Thr-N H 2 -()-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys--Cys)-Th r-N 2 -(Doc)5-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 DOC)4-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Ihr-N H 2 -(DOC)3-DPhe-cyclo(Cys-3 I Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 -(DOC)2-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 104 -(Aepa) 2 D Phe-cyclo (Cys-3 ITyr- DTrp-Lys-Ab u-Cys)-Th r- NH 2

-(DOC)

6 -Ae pa-D Ph e-cyclo(C ys-3 ITyr- DTrp- Lys-Abu-Cys)-Th r- N H 2 -(DOC) 5 -Aepa- D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Ab u-Cys)-Th r- N H 2 ecco(y- Tr 0p y-buCs-hr N -(DOC)2-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 CI -(Doc)-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 D-Ae pa-D -P he-cyclo(Cys-3 I Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 -Ae pa-(Doc)3-D Ph e-cyclo (Cys-3 I Tyr- D~rp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(DOC)2-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 cI-Aepa-(Doc)- DP he-cyclo (Cys- 3 Tyr-DTrp-Lys-Abu-Cys) -Th r-N H 2 -Ap-Ceccl(y-ly-Dr-y-b-Cs-h-H -Apo-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -()-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ap- h-ycoCs3-y-Dr-y-b-Cs-hrNH -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2

DOC)

4 -A-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N 2 -Aepa)-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -()-DPhe-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)5-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)4-D Phe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)2-D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)6-e-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) -Aep-yDiP(Cy-yrl(C-r-DTrp-Auys-Tru-N C -H 2 r NH -(D3Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)2-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(D-Aepa2 y- D~yhe~-cyclo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2 -(DOC)6-Aepa--D~ye~ y-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 -(DOC)-Aepa-ysD~he ~-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 -(D4Aepa-Lys-DTyr-DTyr-cyclo(ys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 105 r- -(DOC) 3 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(Doc) 2 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Doc-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 0-Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-N H 2 (SEQ ID NO: 6)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9)

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-RAla-H is-Leu-N Ie-NH 2 (SEQ ID NO: C -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-R3Ala-His-Leu-Leu-NH 2 (SEQ ID NO:- 4) CI -Aepa-(DOC) 4 -Gtn-Trp-Ala-Ala-Rla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Ap-DC4Gn(rNlia-~a-i-e-l-H2(E -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Ila-H is-Leu-N eu-N H 2 (SEQ ID NO: -Ap-(Doc) 4 -Gn-Trp-Aa-aI-BAa-His-eu-e-NH 2 (SEQ ID NO: 4) -(Doc) 4 -Gln-Irp-Ala-AVal-RAa-His-Phe-NIe-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 4 -Gln-Trp-Ala--VaI-i2Ala-His-Leu-Nle-NH 2 (SEQ ID NO.- -(Doc) 4 -GIn-Trp-Ala-VaI-RAAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Ala-2Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 6 Lys- DTyr- DTyr-cyc lo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2 -(Doc) 5 Lys- DTyr- DTy r-cyc lo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2

DOC)

4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ih r-N H 2

DOC)

3 Lys- DTy r- DTyr-cyc lo(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2

DOC)

2 Lys- DTy r- DTyr-cyc lo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr- DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-( DOC) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(DOC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-Doc-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ihr-N

H

2 -Aepa-(DOC) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(Doc) 3 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Ae pa -(Doc) 2 Lys- DTyr- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Aepa-Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 106

-(DOC)

6 -Aepa-Caeg-cyclo(DCys-3Pal-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Doc) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -Aep a-C aeg-cyclo(DCys-3 Pa I-DTrp- Lys- D Cys)-Thr(Bz)-Tyr- N H 2 0-C aeg-cyclo(D DCys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2

CI-(DOC)

4 -C aeg -cyclo(D Cys-3Pa I- DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2

-(DOC)

6 -C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(Aepa) 2 -Caeg-cyclo( DCys-3 Pal- DTrp- Lys-DCys)-Thr(Bz)-Tyr-N H 2

-(DOC)

6 -Ae pa-C aeg-cyclo(DC ys- 3Pa I- DTrp- Lys- D Cys)-Th r(Bz I)-Tyr- N H 2 ci-(DOC) 5 -Aepa-C aeg-cycl o(DC ys-3 Pa I-DTrp- Lys- D Cys)-Th r(Bz I)-Tyr- N H 2

-(DOC)

4 -Aepa-Caeg-cyclo(DCys-3 Pai-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 3 -Aepa-C aeg-cyclo(DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Tyr- N H 2

-(DOC)

2 -Aep a-C aeg -cyclo(DC ys-3 Pa I-DTrp- Lys- D Cys)-Th r(Bz)-Tyr- N H 2 Doc-Ae pa-C aeg-cyclo (D Cys-3 Pa I-DT rp- Lys- DCys)-Th r(Bz)-Tyr- N H 2

OC)

6 -Caeg -cyclo(D Cys- 3Pa I-DTrp- Lys- DC ys)-Th r(Bz)-Tyr- N H 2 -(Doc) 5 -Ca eg -cyclo (D Cys- 3Pa I-DTrp- Lys- DCys)-Th r(BzI)-Tyr-N H 2

DOC)

4 -Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2

-(DOC)

3 -Caeg-cyclo(DCys-3 PaI-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-N H 2

-(DOC)

2 -Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(BzI)-Iyr-N H 2 -Doc-C aeg-cyclo(DC ys- 3Pa I-DTrp- Lys- DC ys)-Th r(Bz I)-Tyr- N H 2 -Aepa-(Doc) 4 -Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Aepa-(DOC) 3 -Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(Bz)-Tyr-N H 2 -Aepa-( Doc) 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r( BzI)-Tyr-N H 2 -Aepa-Doc-Caeg-cyclo(DCys-3 PaI-DTrp-Lys-DCys)-Thr( BzI)-Tyr-N H2 0 F N F 0 0

H

-Ae pa- (DOC) 2 -Caeg-cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Iy r- N H 2 -Ae pa-Caeg-cyclo(DC ys-3 Pal-DTrp-Lys- DCys)-Th r(BzI)-Tyr-N H 2 -Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(BzI)-Tyr- N H 2 -Aepa-(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 107 -(Doc) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Tr-NH 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 0- 00 0 o NI H 0 -Aepa-(Doc) 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr( BzI)-Tyr-N H 2 -Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Caeg -cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 -Aepa-(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2

DOC)

4 -Ae pa- D Ph e-cyclo(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-NH 2 TABLE D 0 N0 0 0 H 0 -108-

-(DOC)

2 -GIn-Trp-Ala-Ala-ila-His-Phe-NIe-N H 2 (SEQ ID NO: 1) C) -(DoC) 2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) C0 -(Doc) 2 -GIn-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: Cl -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-I3Aa-His-Phe-NIe-NH 2 (SEQ ID NO: 1) -Aepa-GIn-Trp-Ala-VaI-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) Nl -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-GIn-Trp-Ala-ValItla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-BlAIa-H is-Phe-N le-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-lAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-tlAia-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(Doc) 2 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

2 -Gln-Trp-Aia-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

2 -Gln-Irp-Ala-VaIBAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(OC)

2 -Gln-Trp-Aia-VaI-RIla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-I3Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-BlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Gln-Trp-Ala-Va-RlAla-His-Leu-NIe-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-RlAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-IBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-flAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-RlAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -GIn-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -DPhe-Gln-Trp-Ala-Ala-i3Aia-His-Phe-Nle-NH 2 -(Doc) 4 -DAla-G ln-Trp-Ala-Va -IAa-His-Phe-Nle-N H 2 109

-(DOC)

4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N

H

2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-N Ie-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-N

H

2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N

H

2 CI -(DoC) 4 -Aepa-DA~a-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-N

H

2

-(DOC)

4 -Aepa-DPhe-Gln-rp-Ala-Va-Gly-H is-Leu-Leu-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-rp-Ala-Va-BiAla-His-Leu-Nle-N

H

2 -(DOC)4-Aepa-DPhe-Gln-Trp-Ala-VaI-ila-His-Leu-Leu-N

H

2 c-i -Aepa-(DOC) 4 -DPhe-Gln-Trp-Aia-Ala-tla-His-Phe-N ie-N H 2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-Val-Ila-His-Phe-N Ie-NH 2 -Aepa-(DOC) 4 -DPhe-GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -A p -D C 4 D h -G n T p A a Vl-il i e l H -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu- eu-N H 2 -Ap-(Doc) 4 -D -Gn-Trp-Af a-ais-A-H2 SLEu-LID-NO. 1

-(DOC)

4 -GIn-Trp-Ala-AVal-Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 4 -Gln-Trp-Ala-VaI-lyi-His-e-Ne-NH 2 (SEQ ID NO: -(Doc) 4 -Gin-Trp-Ala-Val-G~ly-His-Leu-le-NH 2 (SEQ ID NO:

-(DOC)

4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Le-NH 2 (SEQ ID NO:

-(DOC)

4 -GepGn-Trp-Aa-Ala-R~His-u e-N 2 -(SEQ ID NO: -(Doc) 4 -Aepa-Gln-Trp-Ala-AVa-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-RAl-His-e-Ne-NH 2 (SEQ ID NO: 6) -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-G~ly-His-Leu-Le-NH 2 (SEQ ID NO: 9)

-(DOC)

4 -Aepa-GIn-Trp-Ala-Va-QRAla-His-Leu-Leu-NH 2 (SEQ ID NO: -(Doc)-Aepa)-Gln-Trp-Ala-VaI-BAla-His-e-NLe-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 4 -GIn-Trp-Ala-Va-'Ala-His-Phe-Nle-NH 2 (SEQ ID NO:- 6) -Aepa-(DOC) 4 -GIn-Trp-Ala-AVal-BAl-His-e-Ne-NH 2 (SEQ ID NO: -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-G~ly-His-Leu-le-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-IRAla-His-Leu-Leu-NH 2 (SEQ ID NO: -Aepa-(DOC)2-G~hGn-Trp-Ala-VaJ~A a-His-Leu-Leu-NH 2 E DN:4 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-Ila-His-Leu-le-N

H

2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N

H

2 -Aepa-(DOC) 2 -DAla-G In-Trp-Ala-Val-RAa-His-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -DPhe-Gn-Trp-Aa-Aa-2Ala-His-Phe-Nle-N

H

2 -110- -Aepa-DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Leu-N

H

2 -Aepa-DPhe-Gln-Trp-Ala-Val-BIAla-His-Leu-N le-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N

H

2 -Ap-0aGnTpAaVlBl-i-h-l-H o -Aepa-DAha-GIn-Trp-Ala-a-BAla-His-Phe-Ne-NH 2 c-i -Aepa)-DPhe-Gln-Trp-Ala-VAl-Ala-His-he- e-N H 2 -(DoC) 2 -DPhe-Gln-Trp-Ala-Val-RAla-H is-Leu-Le-N H 2

IND-(DOC)

2 -DPhe-Gln-Trp-Ala-Val-ly-H is-Leu-N e-N H 2 -(DoC) 2 -D~he-Gln-Trp-Ala-Val-Gly-His-e-Nle-N

H

2 c-i -(DOC) 2 -DAha-GlIn-Trp-Ala-Val-RAla-H is-Phe-N le-N H 2 -(DoC) 2 -A-DPhe-Gln-Trp-Ala-ala~a-His-eu-Nle-NH 2 -(DoC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va I-GlAy-His-Leu-Leu-N H 2 -(O)-eaDcaGnTpAl-a-iaHi-h-l-H -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-VlaI-BAa-His-he-N le-N H 2 -()-Aepa-D e-Gn-Trp-Ala-Va I-y-H is-l-Nleu-N H 2 QI N:7 -()-Aep-Aa-Gln-Trp-Aa-Va-IlAa-H is-Phe-N le-NH(E IDNO 2 7

-(DOC)

2 AeDh-Gln-Trp-Ala-Ala-llAla-His-Phe-Nle-N H 2 QI N:7 -Aepa-(DOC) 2 -G~hGn-Trp-Ala-Val-RAla-His-Ala-Nle-NH 2 E DN:7 -Aepa-D-Gln-Trp-Ala-Val-la-His-Ala-Nle-NH 2 DN:7

-(DOC)

2 -G~hGn-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 E DN:7 -Aepa-( DOC) 2 -4-Gn-Trp-Ala-Va-RAa-H is-Ala-N Ie-N H 2 QI N:7 -()-Aepah-Gn-Trp-Ala-Val-Ala-His-Ala-N Ie-N H 2 (E DN:7 -(Doc) 2 -4-Gln-Trp-Aia-Va-RAa-H is-Ala-N Ie-N(E H 2 NO 7 -Aepa-(Doc) 4 -G~hGn-Trp-Ala-Val- la-His-Ala-Nle-NH 2 E DN:7

-(DOC)

4 -Aepa-G~hGn-Trp-Ala-Val Ala-His-Ala-Nle-NH 2 E DN:7

-(DOC)

4 -G~hn-rp-ra-a-Val-HisAla-Ni-l-N 2 (eQ NO 7 -Ap-(DOC) 4 -DheG n-Trp-Ala-VaI-RAa-H is-Ala-N H SE-N HDNO 2 7 -(DOC)2-Aepa-D Phe-Gln-Trp-Ala-VaI-RAla-His-Ala-N le-N H 2 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-QAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Aa-Va-Gly-His-Leu-T(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -111l

-(DOC)

4 -Gaba-GIn-Trp-Ala-Va-flAa-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'v (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) 0 -(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'p (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) Cl -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Y (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DoC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-'v (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-T+ (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(O)-eaGb(GnTpAaVNi~aHsLuNeNH SQI O 2 -(DOC)4-A-Gaba-Gn-Trp-Aa-Va-BAa-Hs-Leu-Ne-NH 2 (SEQ ID NO: 12) -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 -Aepa N

H>

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 3 -Aepa N-

H

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gy-NH 2

H-'

0 -(DoC) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr ri~ Leu-Arg-Pro-Gly-NH 2 -Aepa-Doc

N-

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N

H

2 H 0 -112- -Aepa-(Doc) 2

H-

pGlu-His-Trp-Ser-Tyr N- -Leu-Arg-Pro-Gly-NH 2 02 -Aepa-(Doc) 3

N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(DoC) 4

N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 N Leu-Arg-Pro-Gly-NH 2 H 2f 0 -Aepa -N

HL

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 1 0 -(Doc) 2 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr iLeu-Arg-Pro-Gly-NH 2 0 -(Doc) 3 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -(Doc) 4 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr N~ Leu-Arg-Pro-Gly-NH 2 0 NLeu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc N-

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2

H

0 -113- -Aepa-(Doc) 2

-N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(.DOC) 3

N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(DOC) 4

-N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 Leu-Arg-Pro-Gly-NH 2 H 0 -DOC

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 (Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr -(Doc) 3

N-

H

pGlu-His-Trp-Ser-Tyr H0 Leu-Arg-Pro-Gly-NH 2

K

N

H

0 Leu-Arg-Pro-Gly-NH 2 -(Doc) 4

N

H

pGlu-His-Trp-Ser-Tyr H ii u-Arg-Pro-Gly-NH 2 0 -114- 7- -Doc---N-

H

__pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH, H H 0 -(Doc) 2

N--

H

pGlu-His-Trp-Ser-Tyr N H I r Leu-Arg-Pro-Gly-NH 2 INO 0 -(DoC) 3

N

HL

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H2 0

-(DOC)

4

N

HL

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH, H 0

H

-Aepa N pGlu-His-Trp-Ser-Tyr N- Leu-r-r-l-H H 0

H

-(Doc) 2 -AepaN pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 HO0

H

-(Doc) 3 -Aepa N T pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -115-

H

-(DOC)

4 -Aepa N OpGlu-His-Trp-Ser-Tyr N __Leu-Arg-Pro-Gly-NH 2

H

-Aepa-Doc---NNpGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

-Aepa-(Doc) 2

N

pGlu-His-Trp-Ser-Tyr N-r Leu-Arg-Pro-Gly-NH 2 H 0

H

-Aepa-(Doc) 3

N.;

pGlu-His-Trp-Ser-Tyr N ll Leu-Arg-Pro-Gly-NH 2 H 0

H

-Aepa-(Doc) 4

NN~

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -DocN pGlu-His-Trp-Ser-Tyr N V F Leu-Arg-Pro-Gly-NH 2 HO0

H

-(Doc) 2

-N

N.-

pGlu-His-Trp-Ser-Tyr N -rLeu-Arg-Pro-Gly-NH 2 H 0 -116-

H

-(Doc) 3

N

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4

-NH

pGtu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H0 -HSDGIFTDSYSRYRKQMAVKKYLAAVL(RAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22)

-HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A

6 c)KNK-NH 2 (SEQ ID NO: 21)

-HSDGIFTDSYSRYRKQMA(A

5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO: -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Aa)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -(AePa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO:- 22) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 c)KNK-NH 2 (SEQ ID NO: 21) -(Aepa)HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO: -Aepa-.Doc-Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bzl)-Tyr-N H 2 -Aepa-(DOC)2-Caeg-cyclo(DCys-3PaI-DTrp-LysDCys)Thr(Bzl)jTyr-NH 2 -Aepa-(Doc) 3 -Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Aepa-(DOC)4-Caeg-cyclo(DCys-3Pa[.DTrpLys..DCys)-Thr(Bzl)qTyr-NH 2 -(Doc)6-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Thr-NH 2

-(DOC)

4 DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Va I- Cys)-Th r-NH 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Ae pa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-C ys)-Th r-N H 2

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Val-Cys)-Tr-N

H

2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-N H 2 117- -Doc-Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Val-Cys)-Thr-NH 2 -(DOC)2-Aepa -D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Tr-N H 2 __-(DOC)3-Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-LysVaICys)-Thr-NH 2 Cy- ITrDr-LsV -y)T -NH o -(DOC)6-Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-LysakCys)-Thr-NH 2 -(Doc)e-D Phe-cyclo (Cys-3 ITyr-DTrp- Lys-VaI-Cys) -Th rN H 2 -(Aea-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-ThrN

H

2 -(Doc)-D Phe-cycl o(Cys-3 ITyr- DTrp-Lys-Va I-Cys)-Thr N H 2 -(Doc)2-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2

-(DOC)

3 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc)4-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-hr-N

H

2 -(DOC)6- DPh e-cyclo(C ys- 3I1Tyr- DTrp- Lys-Va I-Cys)-Th r-N H 2 -(eDoc-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Thr-NH 2 -Aepa-(Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaCys)ThrN

H

2 -Aepa-(Doc)3-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-NH 2 -Aepa-(Doc)4-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-Val-Cys)-Thr-N

H

2 Aepao)-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Thr-N

H

2 -(Doc)-Aepa-D Phe-cyclo(Cys-3 Iyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)3-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 D Phe-cyclo (Cys -3 1ITyr- DTrp- Lys-Th r- Cys)-Th r- N H 2 -(DOC)6-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(D-Aepa-DPhe-cycio(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(Aea-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)-DPhe-cyco(Cys-3Tyr-DTrp-Lys-Thr-Cys)ThrN

H

2 -(DOC)3-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)4-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)5-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(Doc)6-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(eDoc-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -Aepa-(Doc-D Ph e-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2 -Aepa-(Doc) 2 -DPhe-cyclo(Cys-3lTyr-DTrp-.LysTh r-Cys)-Thr-N H 2 -Aepa-(Doc)4-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Ap-(D o) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -118-

-(DOC)

4 -DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Thr-Cys)-Thr-NH 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 __-Aepa- DPhe-cyclo(Cys-3I yr- DTrp-Lys-Th r-C ys)-Th r-NH 2 -(O)-eaDh-yl(y0ly-~pLsTrCs-h-H o -Do)-ep-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -A-DPhe-cyclo(Cys-3lTyr-Drp-Lys-Thr-Cys)-Thr-NH 2 -Ae pa-D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-r-Cys)-Th r- 2 -(DOC)-Aepa- D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)3-Ae pa- D Phe-cyclo(Cys-3 I Tyr- D~rp-Lys-Ab u-Cys)-Th r-N H 2 D Phe-cyclo (Cys-3 I Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -(DOC)6-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(D-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Aea-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-ys)-Thr-N H 2 -(DOC)-D Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(DOC)3-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(DOC)4-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)5-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)6- D Phe-cycl o(C ys-3 [Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(eDoc-D Phe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa-(Doc)- DPh e-cyclo (Cys-3 ITyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 -Aepa-(Doc)3-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc)4-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ap-(DOC)6--he-cyclo(C ys-3 I Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2 -(DOC)4-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -()-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -A-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-ys)-Th r-N H -()-Aepa-D Phe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Th r-N 2 (DcAp-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -A-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Thr-N H -A-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -A-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

-Aepa)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ihr-N

H

2 -(DOC)6-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -119-

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 -(Aepa) 2

-(DOC)

2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 o -(Aep) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cy)-Thr-N 2 -(Aepa)-(DOC)-DPhe-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(Doc)a-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -A-(Doc)4-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cy)-Thr-N 2 c-i Ap-(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N 2 -(O)-Ap)-Dh-yl(y-TrDr-y-buCs-h-H -(Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc) 2 -Aepa)-DPhe-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th-N H 2 -DOC)-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 (DOC)5-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

-(D

5 Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc)-A-DPhe-cyclo(Cys-Tyr-DT-L-ys-bU-y)Th H2 -(Aep) 2 -DPhe-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)4-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 r-N H 2 -(Doc)6-DPhe-cyclo(Cys-Iyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 Dh-cyclo(Cys-Tyr- DTrp-Lys-Ab u-C ys)-Th r-N H 2 -(Doc)-Dep-y-yDr-cyclo(Cys-Tyr-DTrp-Lys-Abu- )-Thr-NH2 -DC3p-Lys- DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cy)-Thr-N

H

2 -(Doc)4Aepa- LysDTyr-DTyr-cyco(Cys-Tyr- DTrp-Lys-Abu-Cys)-Th r-N H 2 oc)5-Ae pa- Lys- D~yr- DTyr-cyclo (C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 4 -Ae pa -Lys- DTyr-DTyr-cyclo(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Thr- N H 2 (Docp)2-ApLys- Dr-DTyr-rcyclo(Cys-Ty r-DT rp-Lys-Ab u-Cys) -Thr-N H 2 -Dpoc- Lys- DTy r-DTyr-cycl o(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 Doc)- Lys- DTyr-DTyr-cyclo (Cys-Tyr-DTrp- Lys-Abu-C ys)-Th r- N H 2 120

-(DOC)

3 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 DoC) 5 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 o DoC) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 N- -Aepa-Doc- Lys-- DTyr-DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(Doc) 2 Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(Doc) 3 Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-T hr- N H 2 IND ~-Aepa-(DOC) 4 Lys- DTyr- DTyr-cyclo(C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa- Doc- D Phe-cyclo (C ys-Iyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Ap-Dc2Dh-ycoCsTrDr-ysAuCs-h-H 0 -Aepa-(DOC)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc)4-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 0 (N 0 0 00 H -Aepa N

H

pGlu-His-Trp-Ser-Tyr NLeu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 2 -Aepa- N--

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N

H

2 H 0 -(DoC) 4 -Aepa N--

H

pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 121 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N [-Leu-Arg-Pro-NHEt H 0 -Aepa-(DOC) 4

N--

H

pGlu-His-Trp-Ser-Tyr -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H0 Nw Leu-Arg-Pro-NHEI H 0 -(DoC) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-N HEt 0 -Aepa-(Doc) 2

-N*

H

pGlu-His-Trp-Ser-Tyr N--,Leu-Arg-Pro-NHEt H0 -(Doc) 2

N

H

Gip-His-Trp-Ser-Tyr

N

H

Leu-Arg-Pro-NHEt -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 122 -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N -'rLeu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa N--

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4

N

H

pGlu-His-Trp-Ser-Tyr H -'-jLeu-Arg-Pro-Gly-NH 2 H0 N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -(Doc) 3 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -(Doc) 4 -Aepa N

H

pG Iu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt 0 N -Leu-Arg-Pro-NHEt H

I-

0 1 Leu-Arg-Pro-NHEt H I 0 -Aepa-(DOC) 4 N

H

pGlu-His-Trp-Ser-Tyr N v 1-Leu-Arg-Pro-NHEt H 0 123

-(DOC)

4

N

H

Glp-His-Trp-Ser-Tyr N -Leu-Arg-Pro-NHEt H 0 -Aepa-(DoC) 4

N

H

pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H0 -Aepa N-

H

pGlu-His-Trp-Ser-His H0 Do C) 2 -Ae pa pGlu-His-Trp-Ser-His -(Ooc) 4 -Aepa N

H

pGlu-His-Trp-Ser-His -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H01 N> Trp-Tyr-Pro-Gly-NH 2 H 0

N

H0 Trp-Tyr-Pro-Gly-NH 2 -Aepa-(Doc) 4 N

H

pGlu-His-Trp-Ser-His i-jTrp-Tyr-Pro-Gly-NH 2 0 124 -Aepa-(Doc) 3 N

A

H

OpGiu-His-Trp-Ser-His Trp-Tyr-pro-Gly-NH 2 o H0 -Aepa N-

H

pGlu-His-Trp-Ser-His N -Trp-Tyr-Pro-Gly-NH 2 0 -(Doc) 3 -Aepa N

H

pGlu-His-Trp-Ser-His N H ii FTrp-Tyr-Pro-Gly-NH 2 0 -(DoC) 4 -Aepa N

H

pGlu-His-Trp-Ser-His N'j Trp-Tyr-Pro-Gly-N H 2 0 Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r- N H 2 Lys- Lys- Lys- DTyr- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -Ae pa- Lys- DTyr- DTy r-cyclo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Aepa-(DOC) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

(DOC)

2 Lys- DTyr- DTyr-cyc lo(C ys-Tyr- DTrp- Lys-Ab u-C ys) -Th r- N H 2

-(DOC)

4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)r 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

8 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Ae pa -(DOC) 2 Lys- DTyr- DTyr-cyclo (Cys-Tyr- D~rp- Lys-Ab u -Cys)-Th r- N H 2 -(Aepa) 2 Lys- DTyr- DTyr-cyclo (Cys-Ty r- DTrp- Lys-Ab u-C ys)-Th r- N H 2

-(DOC)

2 -Aepa- Lys- DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r- N H 2

(DOC)

4 -Ae pa- Lys- DTyr- DTy r-cyclIo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-T hr- N H 2 -(Doc) 6 -Ae pa- Lys- DTyr- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Ae pa-(DOC) 2 Lys- DTyr- DTyr-cycl o(Cys-Tyr-DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Ae pa-(Doc) 4 Lys- DTyr- DTyr-cyclo (C ys-Tyr- D~rp- Lys-Ab u-Cys)-Th r- N H 2 125 -Aepa-(DOC)6-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r- NH 2 -Lys-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 00 N 00 0

N.

0/ D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa- Lys- DTyr- DTyr-(Cys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 oc) 2 -Ae pa -Lys- DTyr- DTyr- (C ys-Tyr- DTrp-Lys-Ab u-C ys)-Th r- N H 2 -Aepa -(Doc) 2 -Ae pa -Lys- DTyr-DTyr- (C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(Doc)r 6 -Ae pa -Lys- DTyr- DTyr- (C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Doc-Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 0 N 0 0 -(Doc) 4 -Lys-DTyr-DTyr-cyclo(Gys-Tyr-DTrp-Lys-Abu-Cys)-Ih r-N H 2 Doc-Ae pa- Lys- DTyr- DTyr-(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2

-(DOC)

2 -Aepa-Lys-DTyr-DTyr-(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

-(DOC)

3 -Aepa-Lys-DTyr-DTyr-(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

DOC)

4 -Aepa-Lys-DTyr-DTyr-(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-Doc-Aepa-Lys-DTyr-DTyr-(Cys-Tyr- DTrp-Lys-Abu-Cys)-Thr- NH 2

-(DOC)

2 Lys- DTy r- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-C ys)-T h r- N H 2 -Doc- Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 0 N 0 H 0 o~N- 0 0O/ -126-

-(DOC)

4 -Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- NH 2 Lys- DTyr- DTy r-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r-NH 2

TABE

00 N- 0 N- 0 H NT 0 0 c-I -(Doc) 6 -Caeg-cyclo(DCys-3 PaI-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Doc) 4 -Caeg-cyco(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 c-I -Caeg-cyclo( DCys-3PaI-DTrp-Lys-DCys)-Thr(Bzl)-Iyr-N

H

2 -Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Thr(BzI)-Iyr-N H 2

-(DOC)

4 -Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(Doc) 6 -Aepa-Caeg-cyclo(DCys-3Pa-Drp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Aepa-Caeg-cyclo(DCys-3 PaI-DTrp-Lys-DCys)-Thr( BzI)-Tyr-N H 2 -Doc-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(BzI)-Iyr-N

H

2

-(DOC)

2 -Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(Doc) 3 -Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(Bz!)-Tyr-N H 2

-(DOC)

4 -Aepa-Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2

-(DOC)

5 -Aepa-Caeg-cyclo(DCys-3 Pa I-D~rp-Lys-DCys)-Thr(Bz)-Tyr- NH 2

-(DOC)

6 -Aepa-C aeg-cyclo(DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(Aepa) 2 -Caeg-cyclo( DCys-3PaI-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Doc-Caeg-cyclo(DCys-3Pa I-D~rp-Lys-DCys)-Th r(BzI)-Tyr-N H 2

-(DOC)

2 -Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2

-(DOC)

3 -C aeg -cyc lo(D Cys-3 Pa I-DTrp- Lys- DCys)-T h r(BzI)-Tyr- N H 2

-(DOC)

4 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(Doc) 5 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2

-(DOC)

6 -Caeg-cyclo(DCys-3Pa-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(Aepa) 2

-(DOC)

2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -127- -Doc-Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2

-(DOC)

2 -DPhe-cyclo(Cys-Iyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Aepa) 2

-(DOC)

4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 0 -Aepa-(Doc) 6 -D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 CI -(DOC) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DoC) 6 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2

-(DOC)

2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 ci -HSDAVFTDNYTRLRKQ(Nle)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -HDVTNTRRNAKYNSL-H(EQI O 8

-HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH

2 (SEQ ID NO: 18)

-HSDAVFTDNYIRLRKQMAVKKFLNSILN-NH

2 (SEQ ID NO: 17) -HDVTNTLKQAKLNINN2 SQI O -(eHSDAVFTDNYTRLRKQ eAVKK LNSILN-NH 2 (SEQ ID NO: 1 -(eHSDAVFTDNYTRLRKQMAVKKLNSILN-NH 2 (SEQ ID NO -(Aepa)HSDAVFTDNYTRLRKQNeAVKKLNSILN-NH 2 (SEQ ID NO 1) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) -(Aepa)HSDAVFTDNYTRLRKQMAVKKFLNSILN-NH 2 (SEQ ID NO: 17) 0 0/ N O H 0ON< 00 -Ap-Do)-y-Dy-~r-yl(ysTrD~pLsAb-y)T0rNH oc)-Lys- DTyr-DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab Cys) -Th r- N H 2 -(Doc)2- Lys- DTyr- DTy r-cyclo (C ys-Tyr- DT rp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC)4-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)6- Lys- DTyr- DTy r-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -Ap-(DOC)8-Lys- y-DTy r-DcycloC ys-Tyr- DTrp- L ysb y) -Th r- H 2 -(Aepa-() 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Docp) 2 -AeLys- DTyr- DTyr-cyc lo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc)2-Ae pa- Lys- DTy r- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 128

-(DOC)

6 -Aep a- Lys- DTyr- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r- N H 2 -Aepa-(Doc) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 -Ap-Dc4 y-Dcr -rccoCs-y-Dr-LsA uCs-hr -Aepa-(DoC)6-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 L-Aepa- Lys- DTyr-DTyr-cyclo(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 0 N 0 H/0 c-i 0 c-I -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

2 -Ae pa- Lys- DTy r- DTyr-cyc lo (Cys-Tyr- Drp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(DOC) 2 -Ae pa- Lys- DTyr- DTyr-cyclIo(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 (Doc) 6 -Ae pa- Lys- DTyr- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 0 ~N~<0 0

-(DOC)

2 -Aepa- Lys- DTyr-DTyr-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r-N H 2 Doc-Aepa -Lys- DTyr- DTyr-cyclo (C ys-Ty r- DTrp- Lys-Ab u-C ys) -Th r- N H 2

-(DOC)

3 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Iyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

4 -Ae pa -Lys- DTyr- DTyr-cyc lo(C ys-Ty r- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-Doc-Aepa- Lys- DTyr-DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r-N H 2 0 OH 0 0

~NX

I F "OH 0: NH O 0 OHO0 INH2 OH 2 -Doc-DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 -Doc-DPhe-Gln-rp-Ala-Va-Rla-His-Leu-Nle-NH 2 -129r- -Doc-DPhe-GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-Nle-NH 2 -D c A p-Ce G a a- i e e H 0 -Doc-Aepa-D Phe-GIn-Trp-Ala-VaI-IRAla-His-Leu-le-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-Aepa-DAla-Gln-Trp-Ala-Va-3Ala-H is-Phe-N Ie-N H 2 C -Doc-Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-NIe-N H 2 Ni -Aepa-(DOC) 3 -DPhe-GIn-Trp-Aa-Va-RAla-H is-Leu-Leu-N H 2 r- ~-Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-ValI-RAla-His-Leu-N le-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-(DoC) 3 -DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-N Ie-NH 2 -Aepa-(DoC) 3 -DPhe-Gln-Trp-Ala-Ala-RAla-H is-Phe-N Ie-N H 2

-(DOC)

3 -Aepa-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO:- 4) -(Doc) 3 -Aepa-GIn-Trp-Ala-Va4Aa-His-Leu-NIe-NH 2 (SEQ ID NO: -(Doc) 3 -Aepa-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

3 -Aepa-Gln-Trp-Ala-Val-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

3 -Aepa-Gln-Trp-Ala-Ala-IBAta-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 -Aepa-Doc-DPhe-Gin-Trp-Ala-Va-BAla-His-Leu-N Ie-N H 2 -Aepa-Doc-DPhe-G In-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 -Aepa-Doc-DAla-Gln-Trp-Ala-ValItla-His-Phe-N Ie-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Ala-la-H is-Phe-NIe-N H 2 -Aepa-(DOC) 2 -Gln-Trp-Ala-Val-aAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gln-Trp-Ala-Val-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -GIn-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Va-3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-GIn-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-I3Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -130 -Aepa-(DOC) 2 -Gln-Trp-Ala-VaIAla-His-Leu-NIe-NH 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -GIn-Trp-Ala-ValIBAla-His-Phe-Nle-N H 2 (SEQ ID NO: 6) 0 -Aepa-(DOC) 2 -GIn-Trp-Ala-Ala-RAla-His-Phe-N Ie-N H 2 (SEQ ID NO: 1) Cl -Aepa-Gln-Trp-Ala-VaI-IAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) C -Aepa-Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO.- 6) CI -Aepa-Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

2 -GIn-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

2 -Gln-Trp-Ala-VaI-Ila-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

2 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Gaba-Gln-Trp-Ala-Va-RlAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(DoC) 4 -Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-Y1- (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-+' (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13)

-(DOC)

4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-T (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-Gly-His-Leu--P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(Doc) 4 -Aepa-Gln-Trp-Ala-Va-Gly-His-Leu-+' (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

-(DOC)

4 -Gln-Trp-Ala-Val-Gly-His-Leu-V (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-VaIBAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-la-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -131 0 OH 00 0 OHO0 OH 2 -Doc-DPhe-G In-Trp-Ala-Va IfAa-His-Leu-Leu-NH 2 'No-Doc-DPhe-Gln-Trp-Ala-VaI-ISla-H is-Leu-N Ie-N H 2 c-i -Doc-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-DAla-Gln-Trp-Ala-Va -IAla-H is-Phe-Nle-N H 2 -Doc-DPhe-Gln-Trp-Ala-Ala-fRAla-His-Phe-N Ie-N H 2 -Aepa-Gln-Trp-Ala-Ala-fBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

2 -Gln-Trp-Ala-VaI-I3Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

2 -G In-Trp-Ala-VaI- RAI a-H is- Phe-N le-N H 2 (SEQ ID NO: 6)

-(DOC)

2 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-VaIAla-His-Leu-Nle-NH 2 -Aepa-(DOC) 4 -D Phe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-Va-I3Ala-His-Phe-Nle-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-N Ie-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-N H 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2

-(DOC)

4 -Aepa-DAla-.Gln-Trp-Ala-ValIBAla-His-Phe-Nle-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -(DoC) 4 -DPhe-Gln-Trp-Ala-Val-RAla-His-Leu-Leu-NH 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 -(Doc) 4 -DAla-Gln-Trp-Ala-VaI-RAla-H is.-Phe-N Ie-N H 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Ala-Rfla-His-Phe-Nle-N

H

2 -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-I'la-His-Leu-Leu-NH 2 (SEQ ID NO: 4) 132- -Aepa-(DOC) 4 -GIn-Trp-Ala-VaI-BAla-His-Leu-Nle-N H 2 (SEQ ID NO: C) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -Gln-Trp-Ala-Val-Ila-His-Phe-Nle-N H 2 (SEQ ID NO: 6) C0 -Aepa-(Doc) 4 -Gin-Trp-Ala-Ala-3Ala-H is-Phe-N Ie-N H 2 (SEQ ID NO: 1)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-gAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) C -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-IlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) CI DOC) 4 -Aepa-Gln-Trp-Ala-Ala-BAla-H is-Phe-NIe-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Gln-Trp-Ala-VaI-RAia-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Gln-Trp-Ala-VaI-IRAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

4 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 4 -Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Leu-NH 2 -Aepa-(DOC) 2 -DPhe-G In-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 -Aepa-(Doc) 2 -DPhe-G In-Trp-Ala-Va I-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 2 -DAla-Gln-Trp-Ala-Va.-BAla-His-Phe-Nle-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Ila-His-Leu-Nle-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-DAla-G I n-Trp-Ala-Va I-RAla- His- Phe-N le-N H 2 -Aepa-DPhe-GIn-Trp-Ala-Ala-RlAla-His-Phe-Nle-NH 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N

H

2

-(DOC)

2 -DPhe-Gin-Trp-Ala-VaIBAla-His-Leu-Nle-NH 2

-(DOC)

2 -D~he-Gln-Trp-Ala-VaI-GlIy-His-e-e-NH 2

-(DOC)

2 -DAha-Gln-Trp-Ala-Va-3Ala-H is-Phe-Nle-N H 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-AVal-GlA-His-e-Le-NH 2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-N

H

2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Aa-Va-RAla-His-Leu-Nle-NH 2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Va l-Gly-His-Leu-Leu-N H 2

-(DOC)

2 -Aepa-DAla-Gln-Trp-Ala-VaI-RlAla-His-Phe-Nle-NH 2 -133 (DoC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N

H

2 -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-QAla-H is-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-Gn-Trp-Ala-VaIBA~a-His-Ala-Nle-NH 2 (SEQ ID NO: 7) o DOC) 2 -Gln-Trp-Ala-Val-RIla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) c-i -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BlAia-His-Ala-Nle-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Val-BAla-His-Ala-N Ie-N H 2

DOC)

2 -DPhe-Gln-Trp-Ala-ValI-BAla-His-Ala-Nle-N

H

2 IND -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-3Ala-His-Ala-Nle-NH 2 (SEQ ID NO: 7) c-i -(Doc) 4 -Aepa-Gln-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7)

-(DOC)

4 -Gln-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) C) -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-flAla-His-Ala-N Ie-NH 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Val-RAla-His-Ala-N Ie-NH 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Va-BA~a-H is-Ala-N Ie-N H 2

-(DOC)

2 -Aepa-Gln-Trp-Ala-Val-RAla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7)

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 -Aepa-(DOC) 3 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 3 -Gln-Irp-Ala-Va-flAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-RAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 3 -Gln-Trp-Ala-Ala-rBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO:- 9) -Aepa-Doc-Gln-Trp-Ala-Va-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Doc-Gln-Irp-Ala-Ala- Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 3 -Gln-Trp-Ala-Vali3RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

3 -Gln-Trp-Ala-VaI-Ila-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

3 -Gln-Trp-Ala-VaI-IIAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

3 -Gln-Trp-Ala-Ala-fRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Val-lAla-His-Leu-Leu-NH 2

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Va-la-His-Leu-Nle-NH 2 -(Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 -134 -(DoC) 3 -DPhe-GIn-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2

-(DOC)

3 -DPhe-GIn-Trp-Ala-VaI-BlAla-His-Leu-Nle-N

H

2 -(DoC) 3 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-NH 2 0 -(DoC) 3 -DAla-Gln-Trp-Ala-ValIIAla-H is-Phe-Nle-NH 2 N- -(DOC) 3 -DPhe-GIn-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -Doc-GIn-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-GIn-Trp-Ala-VaI-t3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) c-i -Doc-Gln-Trp-Ala-VaI-BlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Doc-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Aepa-GIn-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -DcApcl-rilaVlRl-i-e-ieN2(E -Doc-Aepa-Gln-Trp-Ala-Va-BAl-His-Leu-Leu-NH 2 (SEQ ID NO: -Doc-Aepa-Gln-Trp-Ala-VaI-Gl~y-His-e-e-NH 2 (SEQ ID NO: 9) -Doc-Aepa-Gin-Trp-Ala-laItAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) TABLE F O OH 0 0 0

H

O0 OHO0 6HNH2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH2

-(DOC)

4 -DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N

H

2

-(DOC)

4 -D Phe-Gln-Trp-Ala-Va-RAla-H is-Leu-N Ie-.NH 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2

-(DOC)

4 DAla-Gln-Trp-Ala-VaI-BAa-His-Phe-Nle-N

H

2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 -(Doc) 4 -Aepa-Gln-Trp-Ala-ValISAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Ala-IRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

4 -Gln-Trp-Ala-VaI-RlAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) 135 -(Doc) 4 -Gln-Trp-Ala-VaI-BlAia-His-Leu-NIe-NH 2 (SEQ ID NO:

-(DOC)

4 -G In-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9)

-(DOC)

4 -Gln-Trp-Ala-VaI-PiAla-His-Phe-Nje-NH 2 (SEQ ID NO: 6) o -(DOC) 4 -G In-Trp-Ala-Ala-aAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -GIn-Trp-Ala-ValI-BAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(DOC) 4 -Gln-Trp-Ala-Val-IAla-His-Leu-Nle-NH2 (SEQ ID NO: -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) IND-Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-fBAla-His-Phe-N Ie-N H 2 (SEQ ID NO: 6) -Aepa-(DOC) 4 -Gln-Trp-Ala-Ala-PiAla-His-Phe-Nle-NH 2 (SEQ ID NO:- 1)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-P&Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Aepa-Gln-Trp-Ala-Va-IIAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va I-f3Aa-His-Leu-Leu-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-RlAla-His-Leu-Nle-NH 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Val-Gly-H is-Leu-Leu-N H 2 -Aepa-( Doc) 2 -DAla-G In-Trp-Ala-VaI-I.Ala-His-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -D Phe-Gln-Trp-Ala-Ala-BlAla-His-Phe-N Ie-NH 2 -Aepa-D Phe-Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-DAla-Gln-Trp-Ala-Val-BAla-H is-Phe-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-3AIa-His-Phe-Nle-N

H

2

-(DOC)

2 -DPhe-Gln-Trp-Ala-ValI-tAla-His-Leu-Leu-NH 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-Va-flAla-His-Leu-Nle-NH 2 -(DOC)2-DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 -(Doc) 2 -DAla-Gln-Trp-Ala-Va-BlAla-H is-Phe-N Ie-N H 2 -(DoC) 2 -DPhe-Gln-Trp-Ala-Ala-IlAla-His-Phe-NIe-N

H

2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 -(DOC)2-Aepa-DPhe-Gn-Trp-Aa-Va-JAla-His-Leu-Nle-NH 2

-(DOC)

2 -Aepa-DPhe-G In-Trp-Ala-Va I-Gly-H is-Leu-Leu-N H 2 -(Doc) 2 -Aepa-DAla-Gln-Trp-Ala-VaI-tla-His-Phe-Nle-NH 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-la-His-Ala-Nle-NH 2 (SEQ ID NO: 7) 136 -Aepa-Gln-Trp-Ala-Val-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(Doc) 2 -Gln-Trp-Ala-Val-flAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-ValI-BAla-H is-Ala-Nle-NH 2 o -Aepa-DPhe-Gln-Trp-Ala-Va-I3AIa-His-Ala-Nle-N

H

2 c-i -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-ala-His-Ala-N Ie-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-llAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7)

-(DOC)

4 -Aepa-Gn-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) IND -(DOC) 4 -Gln-Trp-Ala-VaI-aAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) c-i -Aepa-(DOC) 4 -DPhe-Gn-Trp-Ala-Va-2Ala-H is-Ala-N Ie-N H 2

-(DOC)

4 -Aepa-D Phe-Gln-Trp-Ala-Va I-flla-His-Ala-N Ie-N H 2

-(DOC)

4 -D Phe-Gln-Trp-Ala-ValI-BA~a-His-Ala-N Ie-N H 2 -(DoC) 2 -Aepa-Gln-Trp-Ala-Va-aAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7)

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-N Ie-N H 2 -Aepa-(Doc) 3 -Gln-Trp-Ala-Val-a3Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 3 -Gln-Trp-Ala-Val-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 3 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Va-RAla-His-Leu-NIe-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-Va-IRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Doc-Gn-Trp-Ala-Ala-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 1)

-(DOC)

3 -Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

3 -Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 3 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 3 -Gln-Trp-Ala-VaI-RlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

3 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2

-(DOC)

3 -Aepa-D Phe-Gln-Trp-Ala-VaI-RAla-H is-Leu-N Ie-N H 2

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-NH 2 -(Doc) 3 -DPhe-Gn-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2

-(DOC)

3 -DPhe-Gn-Trp-Ala-Val-RAla-His-Leu-Nle-N

H

2 -137-

-(DOC)

3 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 3 -DAla-Gln-Trp-Ala-Val-f.Ala-His-Phe-Nle-NH 2 -(Doc) 3 -DPhe-GIn-Trp-Ala-Ala-BIAla-His-Phe-N Ie-N H 2 -DcGnTpAaVl0~aHsLuLuN2(E DN:4 o -Doc-Gln-Trp-Ala-VaI-BAla-His-Leu-le-N H 2 (SEQ ID NO: 4) c-i -Doc-Gln-Trp-Ala-Va-GlAy-His-Leu-N e-N H 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-G~ly-His-e-Nleu-NH 2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-la-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Doc-epa-ln-Tp-Al-ValR~laHis-eu-LuNO: 1)QI N:4 -Doc-GA-p-AlnTa-Aa-VAl-a-Hse-N Ne-NH 2 (SEQ ID c-i -Doc-Aepa-Gln-Trp-Ala-VaI-BAl-His-Leu-Leu-NH 2 (SEQ ID NO: -Doc-Aepa-GIn-Trp-Ala-Va-IIla-His-Le-Nle-NH 2 (SEQ ID NO: -Doc-Aepa-Gln-Trp-Ala-Ala-&Ala-His-Phe-NIe-NH 2 (SEQ ID NO: 1) -AepaN pGlu-His-Trp-Ser-Tyr N 0~LuAgPr-~-H -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gy-NH 2 H i 0 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-NH El H 11 0 -(DoC) 2 -Aepa N

H

pG~u-His-Trp-Ser-Tyr -N Leu-Arg-Pro-N HEt

H

0 -138- -Aepa-(DoC) 2 H 4 pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-NHEt H 0 -Aepa N-

H

pGlu-His-Trp-Ser-Tyr -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -(Doc) 3 -Aepa N

H

N Leu-Arg-Pro-Gly-NH 2 H 0

K

Leu-Arg-Pro-Gly-NH 2 H0 pGiu-His-Trp-Ser-Tyr -(Doc) 4 -Aepa -N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 0 Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc N

H

K.

pGlu-H is-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

0 -Aepa-(Doc) 2

H

pGlu-His-Trp-Ser-Tyr NLeu-Arg-Pro-Gly-NH 2 H 0 139 -Aepa-(DOC) 3

N

H

pGiu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4

H

pGlu-His-Trp-Ser-Tyr N ,Leu-Arg-Pro-Gy-NH 2 H 0 -Aepa N-

H

Leu-Arg-Pro-Gly-N

H

2 pGlu-His-Trp-Ser-Tyr -Aepa-(DoC) 2

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H i 0 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 2

N-

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-NHEt H0

N

H0 Leu-Arg-Pro-NHEt -Aepa-(DoC) 4

N

H

pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H 0 140- -Aepa N

H

-N "Trp-Tyr-Pro-Gly-NH, H 0 pGlu-His-Trp-Ser-His -(DoC) 2 -Aepa N

H

pGlu-His-Trp-Ser-His -Aepa-(Doc) 2

N

H

H0 pGlu-His-Trp-Ser-His N ,ITrp-Tyr-Pro-Gly-NH 2 02 -Aepa N pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H i 0 -(Doc) 2 -Aepa N Hi pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 -Aepa N H I pGlu-His-Trp-Ser-Tyr- Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa N-1 pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

-Aepa-Doc N

H

pGlu-His-Trp-Ser-Tyr NLeu-Arg-Pro-Gly-NH 2 H 0 141 -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H H 0 __-Aepa-(DOC) 3 Nj pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 N4 c-H pGlu-His-Trp-Ser-Tyr N'>Leu-Arg-Pro-Gly-NH 2 c-I 0 -Aepa-(Doc) 4

N

H

pGlu-His-Trp-Ser-His Trp-Tyr-Pro-Gly-NH 2

H

0 -(O)-Aepa N

H

1 pGlu-His-Trp-Ser-His N rTrpTyrProGyNH 2 -(Doc)-Aepa) N* pGlu-His-Trp-Ser-His Ni Trp-Tyr-Pro-Gly-NH 2 0 142- -Doc-N

H

pGlu-His-Trp-Ser-Tyr -N -Leu-Arg-Pro-Gly-NH, H 0 -(DoC) 2 N

H

pGlu-His-Trp-Ser-Tyr N'F Leu-Arg-Pro-Gly-NH 2 02 -(DoC) 3

N

H

pG lu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 6 -(Doc) 4

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

0 -Doc N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0

N

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N H 2 H I 0

-(DOC)

4

N

H

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 143

H

-Aepa N OpGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2 o H0

H

-(DOC)

2 -Aepa N ~>Leu-Arg-Pro-GI -NH pGlu-His-Trp-Ser-Tyr -N g2 HO0

H

-(Doc) 3 -Aepa N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2

H

-(Dc),Aep N, pGlu-His-Trp-Ser-Tyr N--f Leu-Arg-Pro-Gly-NH 2 H 0

H

-Aepa-Doc l- pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N

H

2 H0

H

-Aepa-(Doc) 2

N.

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H0

H

-Aepa-(Doc) 3

N

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 144

H

-Aepa-(Doc) 4

N

OpGlu-His-Trp-Ser-Tyr N-r Leu-Arg-Pro-Gly-NH 2

H

-oc N pGlu-His-Trp-Ser-Tyr N' LeuArg-Pro-GlyNH 2 HO0

H

-(Doc) 2

N.

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

H

-(Doc) 3 pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 -Ap-His 4-e-l-Trp-Ser-Tyr N -HisLeu-ArgProGNHN -Aepa-(DoC) 4 -DPhe-Gln-Trp-Ala-Va-IAla-His-Leu-ie-N

H

2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Val-ly-His-Leu-N e-NH 2 -Aepa-(DOC) 4 -D~he-Gln-Trp-Ala-Val-G~ly-His-e-Nle-NH 2 -Aepa-(DOC) 4 -DAha-Gln-Trp-Aa-aIAla-H is-Phe-Nle-N H 2 -Aepa)-Doc)-DPhe-Gln-Trp-Ala-AVal-fAla-His-Peu-Neu-NH 2 -(Doc) 4 -Aepa-DPhe-GIn-Trp-Ala-Val-BAla-His-Leu-le-NH 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-GlAy-His-Leu-Le-N

H

2

-(DOC)

4 -Aepa-DAla-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 145- -(Doc) HS DG IFTDSYSRYR KQ MAVKKYLAAVL(RAa) KRYKQ RVKN K-N H 2 (SEQ ID NO: 23) -(Doc) HSDGI FTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQ RVKNK-N H 2 (SEQ ID 0 NO: 22) c-I-(Doc) HS DG IFTDSYS RYR KQ MAVKKYLAAVLG KRYKQ R(A 6 c)KN K- NH 2 (SEQ ID NO: 21) -(Doc) HSDG IFTDSYSRYRKQ MA(A 5 c)KKYLAAVLGKRYKQ RVKN K-N H 2 (SEQ ID NO: c-I -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(BAla)KRYKQRVKNK-NH 2 (SEQ ID r- NO:- 23) 0 -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 c)KNK-NH 2 (SEQ ID NO: 21) -(Aepa)HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO:

-(DOC)

6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Ih r-N H 2

-(DOC)

4 -D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Va I-Cys)-Ih r- N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Gys-3Tyr-DTrp-Lys-Va-Cys)-Thr-NH 2

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 O OH 0 0

N

II 'OH H 0 O 0 OHO0 ~NH2 OH 2 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(Doc) 4 -Aepa-Gaba-Gln-Trp-Aa-Va-lAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Gaba-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) 146 0 0 -Aepa-(DOC) 4 -Gaba-Gin-Trp-Ala-VaI-Gly-His-Leu-'v (C H 2 N H)-Leu-N H 2 (SEQ ID NO: 13) -(DoC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-His-Leu--P (CH 2 N H)-Leu-N H 2 (SEQ ID NO: 13)

-(DOC)

4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-T (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-,P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DoC) 4 -Aepa-Gln-Trp-Ala-Va-Gly-His-Leu-M (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

(CH

2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Doc N-

H

pGlu-His-Trp-Ser-Tyr -(Doc) 2 N4 pGlu-His-Trp-Ser-Tyr N--,Leu.-Arg-Pro-Gly-NH 2 0 N Leu-Arg-Pro-Gly-NH 2 H .1 0 -(Doc) 3

N

H

pGlu-His-Trp-Ser-Tyr -(DoC) 4

N

H

pG Iu-His-Trp-Ser-Tyr

N

H

0 Leu-Arg-Pro-Gly-NH 2

N

N

NH>

H

0 Leu-Arg-Pro-Gly-N

H

2 -Doc N

H

pG lu-H is-Trp-Ser-Tyr N H0 Leu-Arg-Pro-Gly-NH 2 147 -(Doc) 2

-N

pGlu-His-Trp-Ser-Tyr N- )Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 N -N

H

pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H i 0 -(Doc) 4

-N

H

pG Iu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0

H

-Aepa N pGlu-His-Trp-Ser-Tyr Le u-Arg-Pro-Gly-NH 2

H

0 6 Doc) 2 -Aepa

H

N

pGlu-His-Trp-Ser-Tyr N i HO6 Leu-Arg-Pro-Gly-NH 2 -(Doc) 3 -Aepa

H

N

pGlu-His-Trp-Ser-Tyr -N>I- HAIl Leu-Arg-Pro-Gly-NH 2 -(Doc) 4 -Aepa

H

pGlu-His-Trp-Ser-Tyr

N

Leu-Arg-Pro-Gly-NH 2 148-

H

-Aepa-Doc

N

OpGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H0

H

-Aepa-(Doc) 2

N

__pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

-Aepa-(Doc) 3

N

pGlu-His-Trp-Ser-Tyr N >Leu-Arg-Pro-Gly-NH 2 H 0

H

-Aepa-(DoC) 4 pGiu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0

HH

-Doc

N

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 HO6

H

-(Doc) 2 N.

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0

H

-(Doc) 3

N

pGlu-His-Trp-Ser-Tyr N L eu-Arg-Pro-Gly-N H H 12 0 149-

H

N

OpGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 -Aepa-(DOC) 4 -Gaba-GIn-Trp-Ala-Va-RAa-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-GIn-rp-Aa-Va-ViAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Gaba-GIn-Trp-Ala-Va-RAla-His-Leu-Nie-NH 2 (SEQ ID NO: 12) -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H

'I

0 -(Doc) 3 -Aepa N

H

1 pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 12 -(Doc) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H

!I

0 -Aepa-Doc N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H :1 0 -150 0 0 -Aepa-(DoC) 2

N

H1 pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 3

N.

H

pGlu-His-Trp-Ser-Tyr N ,Leu-Arg-Pro-Gly-NH 2 H 0 Leu-Arg-Pro-Gly-NH 2 H 11 0

H

pGlu-His-Trp-Ser-Tyr -Aepa

-N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 7 Leu-Arg-Pro-Gly-NH 2

N

0 o

H

Leu-Arg-Pro-Gly-NH 2

H

0 -Aepa N

H

pGiu-His-Trp-Ser-Tyr -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Le u-Arg-Pro-NHEt H6 N Leu-Arg-Pro-NHEI H 1 0 151 -Aepa-(DOC) 2

N

H

opGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt o H0 -Aepa N--

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H -2 0 -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 02 -(Doc) 3 -Aepa NI

HL

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 4 -Aepa N

H'

pGlu-His-Trp-Ser-Tyr N >Leu-Arg-Pro-Gly-NH 2 H 2 0 -Aepa-Doc N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -Aepa-(Doc) 2

N

pGlu-His-Trp-Ser-Tyr N ~-LuAgPoGyN 2 H Le-r-roGyN -Aepa-(Doc) 3 N -i

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H2 0 152 -Aepa-(DoC) 4

N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4

H

pGlu-His-Trp-Ser-His -Aepa N-

H

pGlu-His-Trp-Ser-His -(Doc) 2 -Aepa -N

H

pGlu-His-Trp-Ser-His N Leu-Arg-Pro-Gly-NH 2

H")

0 -N -'fTrp-Tyr-Pro-Gly-NH 2 H0 ~>Trp-Tyr-pro-Gly-NH 2 H0 NTrp-Tyr-Pro-Gly-NH 2 H2 0 -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2

H

0 -Doc-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -(Doc) 2 -DP he-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-3 ITyr-D~rp-Lys-Va I-Cys)-Th r-N H 2 -(Doc) 5 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Thr-NH 2

(DOC)

6 -D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-NH 2

-(DOC)

2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -(Doc)3-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va I-Cys)-Thr-N H 2

-(DOC)

5 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2

(DOC)

6 -Aepa-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-N H 2 -153 -(Aepa) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 TABLE G O OH 0o I I O

N

.'OH

0 0 OHO0 OH NH2 -Aepa -Doc)- DPh e-cyco(Cys-3 Iyr- DTrp- Lys-VaI-Cys)-Th r-N H 2 -Aepa-(DOC)4-DPhe-cyclo(Cys-3ITyr-Drp-Lys-Val-Cys)-Thr-N

H

2 Aepao)-DPhe-cyclo(Cys-3Tyr-D~rp-Lys-Va-Cys)-Th r-N H 2 -Aepa)-Doc)-DPhe-cyclo(Cys-3ITyr-D~rp-Lys-Va I-Cys)-Th r-N H 2 -(DOC)-Aepa-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC)5-Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)6-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(D-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(Doc)6p-DPhe-cyclo(Cys-3ITyr-D~rp-Lys-Th r-Cys)-Th r-N H 2 -(Aep) 2 -DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(DOC)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)4-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(Doc)a5-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Gys)-Thr-N H 2 -(Doc)6-D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)6-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC)4-D Ph e-cyclo (Cys-3 ITyr- DTrp- Lys-Th r-C ys)-Th r- N H 2 -(DocPhe-cyclo(C ys-3 I Tyr- DTrp-Lys-Th r-Cys)-Th r- N H -(Doc)-D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 -(Dc4eaDPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N 2 -A-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -()-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -154 -Doc-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2

-(DOC)

2 -Aepa-C aeg-cyclo(D Cys-3 Pa I- DTrp- Lys- DCys)-Th r(Bz)-Tyr- NH 2 3 -Aepa-C aeg-cyclo(D Cys-3 Pa I- DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(O)-ep-CagccoDCs aI 0p y-Dy)T (z)Tr o (Doc)5-Aepa-C aeg-cyclo( DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 ci-(Doc)6-Aepa-C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Ty r- N H 2 -(Doc)-Aea-eg-cyclo(DCys-3 Pa I-DTrp-Lys- DCys)-Thr(BzI)-Tyr- N H 2 -(Aea-Caeg-cyclo( DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(Doc)-Caeg-cyclo(DCys-3Pa-Drp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(DOC)3-C aeg -cycl o(D Cys-3 P aI-DTrp- Lys- DC ys)-Th r(Bz I)-Tyr- N H 2 -(o)-agccl(-s3ai~r-y-~s-hrBl-y-H Doc) 3 5-Caeg-cyclo(DCys-3Pa I-Drp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC)6-Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r(Bz)-Tyr-N H 2 -(Doc)-Caeg~r-y-cyclo(Cys-a -DTrp-Lys-uCys)-Th)Tr-N H 2 -(Doc)2-Caeg~r-y-cyclo(Cys- -DTrp-Lys-uCys)-Th)Tr-N H 2 -(Doc)-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)4-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 3 5-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)6- Lys- DTyr- DTyr-cyclIo (C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC)6- Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC)4-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Lys-) 6 -LysDTy r-ycycCys-Tyr-Drpy-Lysu-Ays)-Th r-N H -(Doc)-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -DCAp-Lys-DTyr-DTyr-cyclo(Cys-yr-DTrp-Lys-Abu-Cys)-Thr-N 2 -()-Aepa-DyrDey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Dochep-yyrDr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -()-Aepa-DPhe-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -DAe -Ly-Dyr yr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

DOC)

2 -Aepa-DP h e-cyc o (C ys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2

-(DOC)

4 -Aepa -C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys- D Cys)-T h r( Bz I)-Tyr- N H 2 -155 -(DoC) 4 -Aepa-Gaba N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4 -Gaba -N

H

pGlu-His-Trp-Ser-Tyr N e r -r y- H H Le-r-o-y-H 0 N- Le l- H H 1 e-rgPoG,-H 0

H

pGlu-.His-Trp-Ser-Tyr -(DoC) 4 -Aepa-Gaba 0 Leu-Arg-Pro-Gly-NH 2

H

N

pGlu-His-Trp-Ser-Tyr /',Leu-Arg-Pro-Gly-N H HO0 -Aepa-(Doc),-Gaba

H

N TpGlu-His-Trp-Ser-Tyr N1- Le rg-Pro-Gly-NH 2 HO0 -(DoC) 4 -Gaba

H

N

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2

HO

156 "OH

H

c-I0 0 0 0 OHO0 OH 2 -(Doc)6-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2

-(DOC)

4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Lys- DTyr- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-C ys) -Th r- N H 2 ci-Aepa- Lys- DTyr-DTyr-cycl o(C ys-Iyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 OC)4-Aepa- Lys- DTyr- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 c-i -(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-NH 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Ae pa -Lys- D~yr- DTy r-cycl o(C ys-Iyr- DTrp-Lys-Ab u-C ys)-Th r- N H 2 (DOC)4 -Aepa -Lys- DTy r- DTyr-cyclo (C ys-Ty r- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)Thr-N

H

2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)2-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2

-(DOC)

2 -Aepa-Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r(BzI)-Iyr-N H 2

-(DOC)

4 -Aepa.-Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r( BzI)-Iyr-N H 2 -Ae pa -Lys- DTyr- DTyr-cycl o(C ys-Tyr- DT rp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC)4-Aepa -Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2 -Aepa- Lys- DTyr- DTy r-cyclo (C ys-Tyr- DT rp- Lys-Ab u-C ys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

DOC)

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -(DOC)2-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr- NH 2 -(DOC)4-Ae pa-C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DC ys)-Th r(Bz I)-Ty r- N H 2 -Doc-Aepa-DPhe-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)2-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ihr-N

H

2 157- -(Doc)3-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

-(DOC)

5 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Ap)-0eccoCsTr-~pLsAuCs-h-H Doc -e D Ph e-cyclo(C ys-Tyr-DTrp-Lys-Ab u-C ys)-Th r-N H 2 -(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DoC)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

H

2 -(Doc)6-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 L-(Dc 6 Dhe-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -o-aLys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 DOC)-Aep a-Lys- DTyr-DTyr-cyclo(Cys-Tyr- DTrp-Lys-Ab u- Cys)-Th r-N H 2 DOC) -Aepa- Lys- DTy r- DTyr-cyc Io(C ys-Tyr- DTrp- Lys-.Ab u-Cys)-Th r-N H 2 -(DOC)4-Ae pa- Lys- DTy r- DTyr-cycl o(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 5-Aepa -Lys- DTy r- D~yr-cyclo (C ys-Tyr- DTrp- Lys-Ab u -Cys)-Th r- N H 2 -(DOC)6-Aepa -Lys- DTyr- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u- Cys)-Th r- N H 2 -(D6Aepa-Lys-DTyr-DTyr-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(ADpoc-Lys- DTyr-DTyr-cycl o(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 -(DOC)-Lys- DTyr-DTyr-cyco (Cys-Tyr- DTrp-Lys-Ab u- Cys)-Th r- N H 2 -(Doc)3- Lys- DTyr- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u -Cys)-Th r- N H 2 -(DOC)3- Lys- DTy r- DTy r-cycl o(C ys-Tyr- DTrp- Lys-A bu- Cys)-Th r-N H 2 Lys- DTyr- DTyr-cycto (C ys-Tyr- DTrp- Lys-Ab u- Cys)-Th r-N H 2 -(DOC)6- Lys- DTy r- DTy r-cycl o (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 Doc- Lys- DTyr-DTyr-cycl o(C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(DOC-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(DOC)3-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(Doc)4-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(Doc)-LysD~rey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(Doc)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(Doc)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(DOC)4-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc) 6 -Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 158 -(Doc)4-C aeg -cyclo (D Cys-3 P aI- DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 C aeg-cyclo(DC ys-3 Pa I-DTrp- Lys- D Cys)-Th r(Bz)-Tyr- NH 2 -Aepa-Caeg-cyclo(DCys-3Pal-DTrp-Lys-DCys).Thr(BzI)jyr.N

H

2 y-D s-hrB )Tr -(Doc)4-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2 -(o)eaCaeg-cyclo(DCDrLsysPakThrpBlys-cysr(BI)y2H -eCaeg-cyclo(DCys-3 l-DTrp-Lys-DCys) -ThThr(BzI)-yr... H 2 D-Aepa -Caeg -cyclo(DCys-3 PaI- DTrp- Lys )-Th r(Bz)-Ty r-N H 2 -DOC-Aepa-Caeg-cyclo( DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(DOC)2-Aepa-Caeg-cyclo(DCys-3Pal-DTrp-Lys-DCys)-Tr(Bz)-Tyr-N

H

2 -(DOC)3-Aepa-C aeg -cyclo(DC ys-3Pa I-DTrp-Lys- D Cys)-h r(Bz I)-Tyr- N H 2 -(Doc)4-Aepa-Caeg-cyclo(DCys-3Pak-DTrp-Lys-DCys)-hr(Bz)yr-NH 2 -(Doc)6-Aepa-C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys- D Cys) h r(Bz I)-yrN H 2 -(D-Aepa-Caeg-cyclo(DCys-3PaI-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -(Apa-Caeg-cyclo(DCys-3 Pa -DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2 -Doc-Caeg-cyclo(DCys-3 Pa-DTrp-Lys-DCys)-Th r(Bz)-Tyr-N H 2 -(DOC)3-Caeg-cyclo(DCys-3 Pal-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(DOC)4-Caeg-cyclo(DCys-3Pa i-D~rp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 Doc)5-Gaeg-cyclo(DCys-3 Pa I-D~rp-Lys-DCys)-Thr(BzI)-Tyr-N

H

2 -(Doc)5-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)Th r(Bz)Tyr-N H 2 -(eDoc-Caeg-cyclo( DCys-3Pa-DTrp-Lys-DCys)-Th r(Bz)-Tyr-N H 2 -Aepa-(DOC)-Caeg-cyclo(DCys-3Pa -TrpLysDCysTh r(Bz)..TyrN H 2 -Aepa-(DOC)3-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-N

H

2 -Aepa-(DOC)4-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Aepa-(yD)4-ae-cyclo(Cys-PaI-DTrp-Lys-ADuCys)ThrBIy-N 2 Lys- DTyr-DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -D)-Aepa Ly-Dr-hy-cyclo(Cys-TyrDTrp-LyAbu.Cys)Thr.N

H

2 -()-Aepa-D Phe-cyclo(Cys- 3 Tyr-DTrp-Lys- -Cys)-Thr-N H 2 -(DOC)2-Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DC ys)-h r(Bz).Tyr-NH 2 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-VaIAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO:. 12)

-(DOC)

4 -Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nie-NH 2 (SEQ ID NO: 12) -159- -(Doc) 4 -Aepa-Gaba N

H

o pGlu-His-Trp-Ser-Tyr N -)Leu-Arg-Pro-Gly-NH, o 06 -Aepa-(Doc) 4 -Gaba-

H

pGlu-His-Trp-Ser-Tyr N ,-LuAg-r-l-H 0 -(Doc) 4 -Gaba N pGlu-His-Trp-Ser-Tyr N' 11 Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 4 -Aepa-Gaba

W.

Leu-Ar-r-yNH pGlu-His-Trp-Ser-Tyr N r-r-~-H HO0

H

-Aepa-(Doc) 4 -Gaba N pGlu-His-Trp-Ser-Tyr N ~'>Leu-Arg-Pro-Gly-NH 2 HO0

H

-(DoC) 4 -GabaN pGlu-His-Trp-Ser-Tyr N 1 Leu-Arg-Pro-Gly-NH 2 HO0 -(Doc)HSDAVFTDNYTRLRKQ(Nie)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -(Doc)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) -(Doc)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Doc)HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -(Aepa)HSDAVFTDNYTRLRKQ(NIe)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) 160 -(Aepa)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Aepa)HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-3Ala-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 N

H

Gip-His-Trp.-Ser-His -N r-yPoGyNH

DOC)

2 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 H~

OH

HO0 0 O HN-

II

0 H -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Va-RAia-His-Leu-Nie-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-VaIAla-His-Leu-Nie-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba N-

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4 -Gaba N

H

pGiu-His-Trp-Ser-Tyr N e H I I Le-Arg-Pro-Gly-NH 2 0 N- Leu-Arg-Pro-Gly-NH 2 H6 -(Doc) 4 -Gaba N

H

pGlu-His-Trp-Ser-Tyr -Leu-Arg-Pro-Gly-NH 2 H 0 161 -(DoC) 3 -Aepa-Gaba N-

H

pGlu-His-Trp-Ser-Tyr LeArPoGlNH 00 -Aepa-(Doc) 3 -Gaba N )3

H

pGlu-His-Trp-Ser-Tyr N e-rPoGlNH 0 -(DoC) 3 -Gaba -N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2

H

0

H

-(Doc) 4 -Aepa-Gaba N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 HO0

H

-Aepa-(Doc) 4 -Gaba N SLeu-ArgPoGyN pGlu-His-Trp-Ser-Tyr N 11 rgPoGN 2 HO0

H

-(Doc) 4 -Gaba

N,,

pGlu-His-Trp-Ser-Tyr N ~>Leu-Arg-Pro-Gly-NH 2 HO0

-(DOC)

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Val-Cys)-Th r-N H 2 -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RlAla-H is-Phe-Nle-N H 2 (S EQ ID NO: 6) -Aepa-(Doc) 2

N-

H

Glp-His-Trp-Ser-Tyr N'I- e-r-r-l-H H -AgPr-yNH 0 162 -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) C) -Aepa-(DOC) 2 -Gln-Trp-Ala-Val-IIAla-His-Leu-N Ie-NH 2 (SEQ ID NO: -Aepa-(DOC) 2 -GIn-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Ap-0-r-l-a-~aHsLuLuN2(E DN:4 o -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-le-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-VaI-QAla-His-Phe-Nle-NH 2 (SEQ ID NQ: 6) -(Aepa) 2

-(DOC)

2 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(Aepa) 2

-(DOC)

2 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: c-i-Doc- DPhe-G In-Trp-Ala-Va I-tRAla-H is-Leu-Leu-N H 2 -Doc- DPhe-G In-Trp-Ala-Va I-RAla-H is-Leu-N le-N H 2 C) -Doc-DPhe-GIn-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Doc-DA~a-Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 -Doc-DPhe-GIn-Trp-Ala-Ala-Rla-His-Phe-Nie-NH 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-BiAla-His-Leu-Leu-N

H

2 -Doc-Aepa-DPhe-GIn-Irp-Ala-Va-BlAIa-His-Leu-N Ie-NH 2 -Doc-Aepa-DPhe-GIn-Trp-Ala-VaI-G Iy-H is-Leu-Leu-N H 2 -Doc-Aepa-DAla-Gln-Trp-Ala-VaI-flAla-His-Phe-Nle-N

H

2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-Ila-His-Leu-Leu-NH 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(DoC) 3 -DAla-Gln-Trp-Ala-VaI-flAla-His-Phe-Nle-N

H

2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Ala-IRAla-His-Phe-Nie-N

H

2

-(DOC)

3 -Aepa-GIn-Trp-Ala-Val-R'Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

3 -Aepa-Gln-Trp-Ala-Val-RAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

3 -Aepa-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

3 -Aepa-Gln-Trp-Ala-Va-R!Aia-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

3 -Aepa-Gln-Trp-Ala-Ala-IRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Nle-N

H

2 -Aepa-Doc-DPhe-GIn-Trp-Ala-Val-Gly-His-Leu-Leu-N

H

2 -Aepa- Doc- DAla-GI n-Trp-Ala-Va I-Rla-H is- Phe- N le- N H 2 -Aepa- Doc- D Phe-G In-Trp-Ala-Ala- BAla-H is- Phe-N le- N H 2 -163- -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DoC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-IIAla-H is-Leu-Leu-NH 2 (SEQ ID NO: 14)

-(DOC)

4 -Gaba-GIn-Trp-Ala-ValIBAla-His-Leu-Leu-N H 2 (SEQ ID NO: 14) 0 -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'v (CH 2 NH)-Leu-N H 2 (SEQ ID NO: 13)

-(DOC)

4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-Tf (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13)

-(DOC)

4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'v (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BAla-H is-Leu-Nle-NH 2 (SEQ ID NO: 12) -(o)-eaGb(lNrpAaViIAaHsLu-l-H SQI O 2

-(DOC)

4 -A-Gaba-Gn-Trp-Aa-Va-BAIa-His-Leu-Ne-NH 2 (SEQ ID NO: 12) -(Doc)-Gaba)-Gln-Trp-Ala-VaI-RAl-His-Leu-N CHNee-NH 2 (SEQ ID NO: 2) -(O)-eaGnTpAl-a-l-i-e- (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2)

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-+ (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) 0 F 0 0 F N 0

N

0

H

-Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa N

H

Glp-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 0 0 6 0 164 -(DoC) 4 -Aepa-Gaba-Gn-Trp-Aa-Va-R1Ala-His-Leu-NIe-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gln-Trp-Ala-Va-BAla-H is-Leu-Nie-N H 2 (SEQ ID NO:

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Va-Ila-H is-Leu-N Ie-NH 2 00 0 00 00 OH 0\ 0

NH

HO 0 CI -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12)

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Gaba-GIn-Trp-Ala-Va-RAla-His-Leu-NIe-NH 2 (SEQ ID NO: )1 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Ala-Va-la-H is-Leu-N Ie-N H 2 TABLE H H OH 7 0 H l'

N

HO 0 0 0 -Suc-(DOC) 3 -Aepa-Gaba-Gn-Trp-Aa-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Suc-Aepa-(Doc) 3 -Gaba-Gn-Trp-Ala-Va-RAla-His-Leu-NIe-NH 2 (SEQ ID NO: 12) -Suc-Aepa-(DOC) 3 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: Suc-(DOC) 3 -Aepa-Gln-Trp-Ala-Val-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Suc-(DOC) 3 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Suc-Aepa-(DOC) 3 -DPhe-Gn-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 -Suc-(DOC) 3 -Aepa-DPhe-GIn-Trp-Ala-Va-RlAla-His-Leu-NIe-NH 2 165- Suc-Aepa-(Doc) 3

-NH

0 u-isTr-Sr -y N*'I Leu-Arg-Pro-Gly-NH 2 HO0 Suc-Aepa-(Doc) 5 s- NH Leu-Arg-Pro-Gly-NH 2 pGlu-His-Trp-Ser-Tyr N 1 HO0 Suc-(DoC) 3 -Aepa N pGlu-His-Trp-Ser-Tyr N 1, Leu-Arg-Pro-Gly-NH 2 HO0 Suc-(Doc) 5 -Aepa

NH

p~lu-is-Tp-SerTyr L eu-Arg-Pro-Gy-NH 2 0-N H 0H 020 H OHI 0 N 0O 0 -f 0 0 -Ap-Dc 2 G~-r-~-aIIAaHsLe-e-H SE0DN:4 -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-BAla-His-Leu-Le-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-G~ly-His-Leu-Le-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -Gln-Trp-Ala-ValIfAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) 166- -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-Gin-Trp-Ala-Va-RAla-His-Leu-N Ie-N H 2 (SEQ ID NO: o -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) c-i -Aepa-Gln-Trp-Ala-VaI-RIla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-Ala-Rla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 1) -(DoC) 2 -Gln-Trp-Ala-VaI-fRAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) IND -(Doc) 2 -Gln-Trp-Ala-Val-Ila-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC)2-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) C) -(DoC) 2 -Gln-Trp-Ala-Ala-RAla-His-Phe-NIe-NH 2 (SEQ ID NO: 1) -Ap-DC2Dh(GnTpAaVNi~l-i-e-e-H -Aepa-(Doc) 2 -DPhe-G In-Trp-Ala-Va I-RAla-H is-Leu-Lie-NH 2 -Aepa-(DOC) 2 -DPhe-G In-Trp-Ala-VaI-BAla-H is-Le-N Ie-N H 2 -Aepa-(Doc)-D en-Trp-Aa-V~a-H~i-H-e-NI-NH -Aepa-DPhe-Gln-Trp-Ala-Va-RAIa-His-Leu-le-NH 2 -Aepa-DPhe-Gln-Trp-Ala-VaI-aAla-His-Le-N Ie-N H 2 -(Aepa)2()-DPhe-Gln-Trp-AI-la-Vfa-His-Nee-NH 2 -(Aepa) 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Lie-NH 2 -(Aepa)-(Doc)-DPhe-Gn-Trp-Aa-Va-Aa-His-Leu-e-NH 2 -Aepa-(DOC) 4 -DPhe-Gn-Trp-Aa-Va-RAa-His-Leu.le.NH 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-RAl-His-Leu-Le-NH 2 -Aepa-(DOC) 4 -D~he-Gln-Trp-Ala-VaI-G~la-His-e-Nle-NH 2 -Aepa-(DOC) 4 -DAh-Gln-Trp-Ala-Va-4lAla-His-Phe-Nle-NH 2 -Aepa-(Doc)a-DPhe-Gln-Trp-Ala-AVal-Ala-His-heu-Ne-NH 2 -(Doc)4-Aepa-DPhe-Gln-Trp-Ala-Val-RAla-His-Leu-Le-N

H

2 -(DOC)4-Aepa-DPhe-Gln-Trp-Ala-Va-RAl-His-Leu-Leu-NH 2 -(Doc) 4 -Aepa-D~he-Gln-Trp-Ala-Vat-G~ly-His-e-e-NH 2

-(DOC)

4 -Aepa-DAha-Gln-Trp-Ala-a-flAla-His-Phe-Ne-NH 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-gAla-His-Phe-Nle-NH 2 -(Doc) 4 -AeDPhe-Gn-Trp-Aa--Ala-IAHis-Pe-NHe 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Va-fRAla-His-Leu-le-N

H

2

-(DOC)

4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N

H

2 167-

-(DOC)

4 -DAla-Gln-Trp-Ala-VaI-RlAla-His-Phe-Nle-N

H

2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Ala-IIla-H is-Phe-Nle-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) o -Aepa-(DoC) 4 -Gln-Trp-Ala-Va-BAla-His-Leu-Nle-N H 2 (SEQ ID NO: N- -Aepa-(Doc) 4 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 4 -Gin-Trp-Ala-Va-fRAla-His-Phe-Nle-N H 2 (SEQ ID NO: 6) -Aepa-(DOC) 4 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-N H 2 (SEQ ID NO:- 1) IND -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) c-i -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-RA~a-His-Leu-Nle-NH 2 (SEQ ID NO: -(DoC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

4 -Aepa-Gln-Trp-Ala-VaI-tla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 4 -Aepa-GIn-Trp-Ala-Ala-RIla-His-Phe-Nle-N H 2 (SEQ ID NO: 1) -(Doc) 4 -Gln-Trp-Ala-VaI-I2Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO:

-(DOC)

4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

4 -Gln-Trp-Ala-VaI-flAIa-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

4 Gln-Trp-Ala-Ala-h2Aa-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 2 -DPhe-Gn-Trp-Aa-Va-flAla-His-Leu-Leu-N

H

2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 -Aepa-(DOC) 2 -D Phe-G In-Trp-Ala-Val-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 2 -DAla-GIn-Trp-Ala-VaI-RAla-His-Phe-Nle-N

H

2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Aa-Ala-RAla-H is-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Aa-Va-R2Ala-His-Leu-Leu-N

H

2 -Aepa-D Phe-G In-Trp-Ala-Val-IAla-His-Leu-N Ie-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N

H

2 -Aepa-DAla-Gln-Trp-Ala-Va-IAla-His-Phe-Nle-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N

H

2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-N

H

2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Va-IIla-His-Leu-Nle-NH 2

-(DOC)

2 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2

-(DOC)

2 -DAla-Gln-Trp-Ala-VaI-I3AIa-His-Phe- Nle-N H 2 -(Doc) 2 -D Phe-Gln-Trp-Ala-Ala-BAla-His-Phe-N Ie-N H 2

-(DOC)

2 -Aepa-DPhe-Gln-Trp-Ala-Val-IRAla-His-Leu-Leu-N

H

2 168 r- -(DoC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-N H 2 C) -(DOC) 2 -Aepa-DPhe-GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DoC) 2 -Aepa-DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 C0 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-fla-His-Phe-Nle-N H 2 Cl -Aepa-(DOC) 2 -Gin-Trp-Ala-Va-BAla-His-Ala-NIe-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Val-fRAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7)

-(DOC)

2 -Gln-Trp-Ala-VaI-RAla-His-Ala-Nie-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 2 -DPhe-GIn-Trp-Ala-Va-Rla-His-Ala-Nle-NH 2 Nl -Aepa-DPhe-Gln-Trp-Ala-VaIla-His-Ala-N Ie-N H 2

-(DOC)

2 -DPhe-G In-Trp-Ala-Val-IAla-His-Ala-Nle-N H 2 -Aepa-(DoC) 4 -Gln-Trp-Ala-Va-BAla-His-Ala-NIe-N H 2 (SEQ ID NO: 7) -(O)-eaGnCrNl1a-~a-i-l-l-H2(E DN:7 -(Doc) 4 -A-Gn-Trp-Aa-Va-BAa-His-Aa-Ne-N H 2 (SEQ ID NO: 7) -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-RAla-His-Ala-Ne-NH 2

-(DOC)

4 -Aepa-DPhe-Gln-Trp-Aa-Va-QAla-His-Ala-N Ie-N H 2

-(DOC)

4 -DPhe-Gln-Trp-Ala-Va-BAla-His-Ala-Nle-N H 2 -(Doc) 2 -Aepa-Gln-Trp-Ala-Va-3Ala-His-Ala-Nle-NH 2 (SEQ ID NO: 7)

-(DOC)

2 -Aepa-DPhe-GIn-Trp-Aa-Va-RAla-His-Ala-Nle-N

H

2 -Aepa-(Doc) 3 -Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 3 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 3 -Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 3 -Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 3 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Va-IlAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-Va-RAla-His-Phe-Nle-NH 2 (SEQ ID NO:- 6) -Aepa-Doc-GIn-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1)

-(DOC)

3 -Gln-Trp-Ala-VaI-(lAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4)

-(DOC)

3 -Gln-Trp-Ala-VaI-BlAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC)3-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9)

-(DOC)

3 -GIn-Trp-Ala-VaI-I3Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 6)

-(DOC)

3 -Gln-Trp-Ala-Ala-(lAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) 169

-(DOC)

3 -Aepa-DPhe-Gln-Trp-Ala-Va-(Ila-His-Leu-Leu-NH 2 -(Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-N

H

2 -(Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-NH 2 o -(Doc) 3 -DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 Ni -(DOC) 3 -DPhe-Gln-Trp-Ala-VaI-IlAla-His-Leu-Nle-NH 2 -(DoC) 3 -DPhe-Gln-Trp-Ala-Va I-Gly-His-Leu-Leu-N H 2 -(Doc) 3 -DAla-Gln-Trp-Ala-Va-Ila-H is-Phe-NIe-N H 2

-(DOC)

3 -DPhe-Gln-Trp-Ala-Ala-IlAIa-His-Phe-Nle-N

H

2 -Doc-Gln-Trp-Ala-Val-Pila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-VaI-BAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -Doc-Gln-Trp-Ala-Ala-i2Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa

-NH

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 02 -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N -AgPr-lyN

-(DOC)

3 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N~ Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr NrgPoG~-H 0 170- -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 3

-N-

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4

N

H

pGlu-H is-Trp-Ser-Tyr H Leu-Arg-Pro-Gly-NH 2 02 Leu-Arg-Pro-Gly-NH 2 H 0 N e-r-rGlNH H Le-rPr-y-H 0 -Aepa. H pGlu-His-Trp-Ser-Tyr N'

H

Leu-Arg-Pro-Gly-N

H

2 -(DoC) 2 -Aepa N 1

H

pGlu-His-Trp-Ser-Tyr -(DoC) 3 -Aepa N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H0 N >Leu-Arg-Pro-Gly-NH 2 H6 -(DoC) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 2

N

N -r Leu-Arg-Pro-Gly-NH 2 0 pG Iu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2

H

171 -Aepa-(Doc) 3 -N

H

pGlu-His-Trp-Ser-Tyr N e-r-oGlNH H 0 -Aepa-(Doc) 4

-N

H

pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 0 -Doc

NH

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2

H

0 -(Doc) 3

N

H

pGlu-His-Trp-Ser-Tyr -(Doc) 4

-N

H

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 N Leu-Arg-Pro-Gly-NH 2 0 -(Doc) 2

N

H

pG~u-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 172- -(DoC) 3

-N

H

pGlu-His-Trp-Ser-Tyr H-NAgPr-~-H o) 0

H

pGiu-His-Trp-Ser-Tyr N 2 H ILeu-Arg-Pro-Gly-NH 2 No 0

H

CI-Aepa N cIpGlu-His-Trp-Ser-Tyr i- Leu-Arg-Pro-Gly-NH 2 02

H

-(Doc) 2 -AepaN pGlu-His-Trp-Ser-Tyr 7 L-Arg-Pro-Gly-NH 2 HO0 -(Doc) 3 -Aepa H N*,4 pGlu-His-Trp-Ser-Tyr*4 Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 4 -AepaN pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N

H

2

H

0

H

-Aepa-(Doc) 2 pGlu-His-Trp-Ser-Tyr N-r Leu-Arg-Pro-Gly-N

H

2 H 0 173-

H

-Aepa-(Doc) 3

N

0pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2

H

-Aepa-(DOC) 4

N

pGlu-His-Trp-Ser-Tyr N I Leu-Arg-Pro-Gly-NH 2 H0

H

-DocN pGlu-His-Trp-Ser-Tyr N 1 Leu-Arg-Pro-GlyNH 2 HO0

H

-(DoC) 2

N

pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N H 2

H

-(Doc) 3 0 pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0

H

-(DoC) 4

N

I I pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H0 -HSDGIFTDSYSRYRKQMAVKKYLAAVL(RAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22)

-HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A

6 C)KNK-NH 2 (SEQ ID NO: 21)

-HSDGIFTDSYSRYRKQMA(A

5

C)KKYLAAVLGKRYKQRVKNK-NH

2 (SEQ ID NO: -174- -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(IAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -(Aepa)HSDG IFTDSYSRYRKQ MAVKKYLAAVL(Ava) KRYKQRVKN K-NH 2 (SEQ ID o NO: 22) N- -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 c)KNK-NH 2 (SEQ ID NO: 21) -(Aepa)HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO: N- -(DOC) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2

N-

Doc) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 -Ap-DPh-yl( y- y-Dr-Ls-aICs-hr -()-Aepa-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va -Cys)-Th r-N 2 -DcAp-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-N H 2 -DeDPhe-cyclo(Cys-3 I Tyr- DTrp-Lys-Va I-Cys)-Th r-N H 2 -Aep-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Th r-N H 2 -(DOC)-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Th r-NH 2 -(Doc)3-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(DOC)4-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 -(Doc) 4 5-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Thr-N

H

2 -(Doc)6-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc) 6 ep-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 -(DOC)-Aepa-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 -(Doc)3-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-N H 2 -(DOC)5-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Thr-NH 2 -(Doc) 5 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-NH 2 -(D-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -(Aepa)oc-P he-cyclo (Cys-3 I Tyr- DTrp-Lys-VaI-Cys)-Th r-N H 2 -Aepa-(DOC)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va -Cys)-Thr-N H 2 -Aepa-(DOC)3-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Aepa-(DoC)4- D Phe-cyclo (Cys- 31Tyr- DTrp- Lys-Va I-C ys)-Th r- N H 2 Aepao)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-N

H

2 -(Doc)-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 175 -(DOC)3-Aepa -D Ph e-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2

-(DOC)

5 -Aepa- D Phe-cyclo (C ys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 __-(DOC)6-Aepa- D Phe-cyclo (Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 o -(Aepa) 2 -DPhe-cyclo(Gys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -Doc- D Phe-cyclo(C ys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r-N H 2

-(DOC)

2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -(DOC)3-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-.Thr-NH 2 IND ~-(Do00 4 D Phe-cycl o(C ys-3 I Tyr- DTrp-Lys-Th r-Cys)-Th r-N H 2

-(DOC)

5 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2

-(DOC)

6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2

-(DOC)

6 -D Phe-cyclo(C ys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2

-(DOC)

4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 0U 0 0 0~ 0 0 H%&J4H

L

HOH

0,I 0 -Aepa

N

H

p~lu-Hs-Trp-er/Ty Leu-Arg-Pro-Gly-NH 2 pGu-isTr-Sr-yrN 0

H

176 -Aepa-(DoC) 2 -N

H

pGlu-His-Trp-Ser-Tyr

N

H ILeu-Arg-Pro-Gly-NH2 0 -Aepa

H

pGlu-His-Trp-Ser-Tyr -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 2

N

H

pGlu-His-Trp-Ser-Tyr N F- Leu-Arg-Pro-NHEt H 0 Nl Leu-Arg-Pro-NHEt 0 HLeu-Arg-Pro-NHEt H0 -Aepa

N

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc)4 NpG lu-H is-Trp-Ser-Tyr />Leu-Arg-Pro-Gly-NH 2 NO0

H

N--,Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa N

H

pG Iu-His-Trp-Ser-Tyr N'hTLeu-Arg-Pro-NHEt HO0 177- -(DoC) 4 -Aepa N

H

pGlu-His-Trp-Ser-Tyr N-'-Leu-Arg-Pro-NHEt -Aepa-(Doc) 3

H

pGlu-His-Trp-Ser-Tyr -Aepa-(Doc) 4

N

H

pGlu-His-Trp-Ser-His Otepa

-N

H

pGlu-His-Trp-Ser-His N Leu-Arg-Pro-NHEt H 0 Trp-Tyr-pro-Gly-NH 2

H

Trp-Tyr-Pro-Gy-NH 2

H

0 -(Doc) 2 -Aepa N

H

pGlu-His-Trp-Ser-His Trp-Tyr-Pro-Gly-N

H

2 H I 0 -Aepa-(Doc) 2

H

pGlu-His-Trp-Ser-His Tr-yPoGlNH H Ip-y-r-~-H 0 -Aepa-(Doc) 4

N

H

pG Iu-His-Trp-Ser-His Trp-Tyr-Pro-Gly-N

H

2 0 -178- -Aepa

-N

H

pGlu-His-Trp-Ser-His r-y-r-l- H 0 -(DoC) 3 -Aepa N

H

pGlu-His-Trp-Ser-His -Aepa-(Doc) 3

N

pGlu-His-Trp-Ser-His Trp-Tyr-Pro-Gly-NH 2 02 N>'1 Trp-Tyr-Pro-Gly-NH 2 0 0 H 0 r ~.XH OH 0

H

0 0.

HO0 0 -Aepa

NH

pGlu-His-Trp-Ser-Tyr Ne-r-r-l-H H0 -(Doc),-Aepa

N

H

pGlu-His-Trp-Ser-Tyr N~--*LeuAgPoGyN H IF rgPo- yN 2 0 179 -Aepa-(Doc) 4

N

H

pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2 H 0

H

-(Doc) 4

-N

pGlu-His-Trp-Ser-Tyr

N

H0 Leu-Arg-Pro-Gy-NH 2 0 0.

-Aepa-(Doc) 4

NH

pGlu-His-Trp-Ser-Tyr -N I Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa NH pGlu-His-Trp-Ser-Tyr N HO0 Leu-Arg-Pro-Gly-NH 2 -180

-(DOC)

4

-NH

0pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 HO0 TABLE I 0 O HN o P o o -H OH 0 .0 N HO 00 0 0 0 0 -Aep a -Lys DTy r- DTy r- cycIo(C ys-Ty r- DTrp -L y s-A bu Cys)-T hr-N H 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa -Lys- DTyr- DTyr-cyc lo(Cys-Ty r- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 (Do0C) 2 -Aep a -C aeg -cyclIo (D Cys 3Pa I -DT rp- Lys- D Cys) -T h r(Bz1) -Ty r- N H 2

-(DOC)

4 -Aepa-Caeg-cyclo(DC ys-.3Pa I- DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2 0 01 0 HN 0 Po -H OH 0

H

0 N HO /0 0 00 0 -Ae pa- Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Doc-Aepa-DP he-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Th r-NH 2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 181

-(DOC)

3 -Aepa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 5 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 CI-(DoC) 6 -Ae pa- D Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 O -(Aepa) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Dc0 e c c o C s 3 I y p y b u C s h r -(DOC)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

-(DOC)

2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DoC)4-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)5-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)6- D Phe-cyclo(C ys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2

-(DOC)

6 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)4-D Phe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -()-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -A-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -()-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Dc 4 p-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -A-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Th r-NH 2 -Aepa- ys y-D~h -cyclo(Cys- Tyr-DTrp- Lys-Ab u-Cys)-Th r-NH2 -(D004 Lys- DTyr- DTy r-cyclo(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -()-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Ae-Lys- DTyr- DTy r-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th -N H 2 -()-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2

-(DOC)

4 -Aepa--D yrhy-cycio(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-NH -DcAp-D Phe-cyc f o(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -A-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

-Aepa--D~ye y-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -()-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 (D)-Aepa-Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys) -Th r-N H 2 -AepaL-D~yrey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -()-Aepa-DPhe-cyclo(Cys- 3 Tyr-DTrp-Lys- -Cys)-Thr-N H 2 -(Doc) 2 -Aepa-De-cyclo(Cys-3Pay-DTrp-Lys-VaICys)-ThrB-

H

2

N

(DOC)

2 -Ae pa-C aeg -cyc lo(D Cys-3 Pa I-DTrp- Lys- DCys)-Ih r( BzI)-Tyr-N H 2 182 -Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DOC)2-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc)3-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 o -(Doc) 5 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2

-(DOC)

6 -Aepa-D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Doc- DPh e-cyclo(C ys-Tyr- DTrp-Lys-Abu -C ys)-Th r- N H 2 'No -(DoC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2

-(DOC)

3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(DoC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(Doc) 5 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(Doc) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 Lys- DTyr- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 Doc-Aep a -Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-C ys) -Th r-N H 2 (DoC) 2 -Ae pa- Lys- DTy r- DTyr-cycl o(C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 3-Ae pa- Lys- DTyr- DTyr-cycl o(C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC)4-Aep a- Lys- DTyr- DTyr-cycl o(C ys-Tyr-DTrp- Lys-A bu-C ys)-Th r- N H 2 Doc 5 -Ae pa- Lys- DTy r- D~yr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 6 -Aepa -Lys- DTyr- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(Aepa)2-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 Doc- Lys- DTyr- DTyr-cyc lo(C ys-Tyr- DTrp- Lys-Ab u -Cys)-Th r- N H 2 -(Doc)2-Lys-.DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)3-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 oc) 4 Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-A b u-Cys)-T hr- N H 2 -(DOC) 5 Lys- DTy r- DTy r-cyclo (C ys-Tyr- DTrp- Lys-A bu-C ys)-Th r- N H 2 (Do006- Lys- DTy r- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-T hr- N H 2 -Ae pa -Doc- Lys- DTyr- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u- Cys)-Th r- N H 2 -Aepa-(Doc)2-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(DOC) 3 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(DOC) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-.Doc-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(Doc) 2 -D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 183 -Aepa-(DoC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Tr-NH 2 -(Doc)6-C aeg-cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 -(Doc)4-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Ce-yl(0s3a-~pLy-~s-h(z)TrNH o p-Caeg-cycDys-3PoI(D p-Las-Dc-ys-TDChr(BzIz)Tyr-N

H

2 ci-Aepa)-Ceaeg -cyclo(DCys-3 Pa -ysr-Dys-mr(Bz)-Ty (z Tr-N H 2

H

-(DOC)4-Ae pa-C aeg -cycl o(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- NH 2 IND -(Dogc4-Ae(D Caeg3 -cyloD~y-3P~ ys- D s)-D ys)-Tr)-T-Ty-

H

2

H

-A-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 Aepa-Caeg-cyclo(DCys-3Pal-DTrp-Lys-DCys)-hr(Bzl)-Tyr-N

H

2 -(O)-eaC g-cc DCy- aI--p y-DCy)Th(zI-yr -(DOC)-Aepa-C aeg -cyclo(D Cys-3 PaI-DTrp- Lys- DCys)-Th r(BzI)-Tyr-N H 2 -(Doc)2-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DC ys)-Th r(Bz)-Tyr- N H 2 -(Doc)6-Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(D5Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-Dcys)-Thr(BzI)-Tyr-N

H

2 -(Doc)6p-Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -(Aep) 2 -Caeg-cyclo( DCys-3Pa-DTrp-Lys-DCys)-Th r(Bz)-Tyr-NH 2 -(DOC)-Caeg-cyclo(DCys-3Pa -DTrp-Lys-DCys)-Thr(Bz)-Tyr-N

H

2 -(Doc)4-Caeg-cyclo(DCys-3 Pal-DTrp-Lys-DCys)-Th r(BzI)-Tyr-NH 2 -(DOC)5-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2 -(Doc)6-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2 -(e-Doc)-Caeg-cyclo(DCys-3 PaI-DTrp- Lys- DCys)-Thr(Bz)TyrN H 2 (DOC)2-Caeg-cyclo(DCys-3 Pal-DTrp-Lys-DCys)-ThBz)-TN

H

-Aepa-(Doc)-Caeg-cyclo( DCys-3Pa-DTrp-Lys-DCys)-hr( Bz)-yr-N H 2 -Aepa-(Doc)4-Caeg-cyclo(DCys-3PaI-Drp-Lys-DCys)-Tr(Bz)-Tyr-NH 2 HSDAVFTDNYTRLRKQ(Nle)AVKKYLNSILN-NH 2 (SEQ ID NO: 19)

-HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH

2 (SEQ ID NO: 18)

-HSDAVFTDNYTRLRKQMAVKKALNSILN-NH

2 (SEQ ID NO: 16)

-HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH

2 (SEQ ID NO: -(Aepa)HSDAVFTDNYTRLRKQ(Nle)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) -(Aepa)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) 184 -(Aepa)HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 4 -Aepa- Lys- DTyr- DTyr-cyclo(Gys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 o -Aepa-DPhe-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Th r-N H 2 ci-(DOC) 2 -Ae pa-D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-Va I-C ys)-Th r- N H 2 0 0 0~ 0 Nk O H 0 0 N HO 0/ 0 0 00l 0 -(Doc) 4 -Aepa-DP he-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 6 -D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2

-(DOC)

4 Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-C ys)-Th r- N H 2

-(DOC)

6 Lys- DTyr- DTy r-cyclo(C ys-Iyr- DTrp- Lys-Ab u-G ys)-T hr- N H 2

DOC)

4 -Aepa-D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2

DOC)

4 -D Phe-cyclo(C ys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp- Lys-Th r-Cys)-Th r- N H 2

-(DOC)

4 -Aepa-Lys-DTyr- DTyr-cyclo(Cys-3 ITyr-DTrp- Lys-Th r-Cys)-Ih r- N H 2

-(DOC)

4 Lys- DTyr- DTyr-cycl o(C ys-3 ITy r- DTrp- Lys-Th r-C ys)-Th r- N H 2 -(Doc) 6 -Lys- DTyr-DTyr-cyc lo(C ys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2

-(DOC)

4 -Aepa-Caeg-cyclo(DCys-3Pal-Drp-Lys-DCys)-Th r( BzI)-Tyr-N H 2

-(DOC)

4 -Caeg-cyclo(DCys-3 PaI-DTrp-Lys-DCys)-Th r( BzI)-Tyr-N H 2 -(DOC)6-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2 -185- SH- OH o.0

N

HO 0 0

-(DOC)

4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ihr-N

H

2 c-i -(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 -(Doc) 6 -DPhe.-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Thr-N H 2 c- (DOC) 4 -Aepa- Lys- DTy r- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2

-(DOC)

4 Lys- DTyr- DTyr-cycl o(C ys-Tyr- DTrp-Lys-Ab u-C ys)-Th r- N H 2

(DOC)

6 Lys- DTyr- DTyr-cyclIo (C ys-Tyr- DT rp- Lys-Ab u-C ys)-Th r-N H 2

-(DOC)

4 -Aepa--DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N

H

2

-(DOC)

4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2

-(DOC)

6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 (Doc) 4 -Ae pa- Lys- DTyr- DTyr-cyclo(C ys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2

-(DOC)

4 -Lys-DTyr-DTyr-cycio(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2

-(DOC)

6 -Lys-DTyr-DTyr-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2

-(DOC)

4 -Aepa-C aeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2 (D oc) 4 -Ca eg -cycl o(D Cys-3 Pa I- DTrp- Lys- D Cys)-Th r(BzI)-Tyr- N H 2 -(DOC)6-Caeg-cyclo(DCys-3Pa I-DTrp-Lys-DCys)-Th r(Bzl)-Tyr-N H 2 0H 0 0

H,,

.H

O

HO 0,0 0 0 -S uc-(DOC) 3 -Aepa-D Phe-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -S uc-(DOC) 3 -D Phe-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Suc-(Doc) 5 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -186- -Suc-(DOC) 3 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Suc-(DOC) 3 -Lys- DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Suc-(DOC) 5 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N

H

2 C.)(o)-eaDh-ccoCs3~rDr-LsTrCs-h-H o ~-Suc-(DOC) 3 -A-DPhe-cyclo(Cys-3 lTyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 ci-S uc-(Doc) 3 DPh e-cycl o(Cys-3 IlTyr- DTrp- Lys-Th r-Cys)-Th r-N H 2 -S uc-(DOC)3-DAe-yDrDr-cyclo(Cys-3lTyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 IND~-s Su c-(DOC) 3 -AeLys- DTyr- DTyr-cyclo (Cys- 3 lTyr-D~rp-Lys-Th r-Cys)-Thr-N H 2 -S uc-(DOC)5-Lys- DTyr- DTyr-cyclo (Cys- 3 1lTyr- D~rp- Lys-Th r-Cys) -Th r- N H 2 c-i -S uc-(DOC)3-Lys-CyrDe-cyclo(Cys-3Ply-DTrp-Lys-ThCys)-Thz r-N H 2 -Suc-(DOC) 3 -A-Caeg-cyclo(DCys-3Pal-D~rp-Lys-DCys)-Th r(Bzl)-Tyr-N H 2 -Suc-(DOC)5-Caeg-cyclo(DCys-3Pal-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 c-i -Suc-(DOC)4-Caeg-cyclo(DCys-3Pa l-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-N H 2 -Suc-(DOC)5-e-Caeg-cyclo(D~ys-3Pa l-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-N H -Suc-(Doc)4-Aepa-Caeg-cyclo(DCys-3 Pal-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 Biological Assays Somatostatin Receptor-Radioligand Binding Assays [0222] Membranes for in vitro receptor binding assays were obtained by homogenizing (Polytron setting 6, 15 sec) the CHO-Ki cells, expressing the human somatostatin receptor subtypes (hSSTR-1, hSSTR-2, hSSTR-3, hSSTR-4, or in ice-cold 50 mM Tris-HCI and centrifuging twice at 39,000 g (10 min), with an intermediate resuspension in fresh buffer. The final pellets were resuspended in 10 mM Tris-HCI for assay. For the hSSIR-1, hSSTR-3, and hSSTR-4 assays, aliquots of the membrane preparations were incubated 0 C with 0.05 nM 125 -Tyrll]SRIF-14 in 50 mM HEPES (pH 7.4) containing BSA M90I 2 (5 mM). The final assay volume was 0.3 ml. For the hSSTR-2 and hSSTR-5 assays, 25 l]-[4-(2-hydroxyethyl)]-1 -piperazinylacetyl-DPhe-cyclo(Cys- Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (0.05 nM) and [1 25 1I]-D Phe-cyclo(Cys-Tyr-DTrp-Lys- VaI-Cys)-Thr-NH 2 were employed as the radioligands, respectively, and the incubation times were 90 min/25*C. The incubations were terminated by rapid -187filtration through GF/C filters (pre-soaked in 0.3% polyethylenimine) using a Brandel O filtration manifold. Each tube and filter were then washed three times with S aliquots of ice-cold buffer. Specific binding was defined as the total radioligand o bound minus that bound in the presence of 1000 nM SRIF-14 (for hSSTR-1, hSSTR- S3, hSSTR-4, or hSSTR-5), or 1000 nM DPhe-c(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 for hSSTR-2.

In Vitro Growth Assays S[0223] For the in vitro proliferation assays, cultured CHO-K1 cells or CHO-K1 cells expressing the hSSTR-2 receptor were seeded into plastic 24-well plates in RPMI 01640 Medium (DMEM) containing 10% fetal bovine serum (FBS) at a density of approximately 104 cells/well/1.0 ml. The test peptides were added at the desired concentration and maintained in culture CO2, 37°C, humidified air) for one to three days. The cells were rinsed with serum-free RPMI media, trypsinized, resuspended RPMI 1640 FBS), and counted using a Coulter Counter at 1:20 dilution.

LHRH Radioligand Binding [0224] Membranes were prepared for radioligand binding studies by homogenization of CHO-K1 cells expressing the rat recombinant LHRH receptor in ml of ice-cold 50 mM Tris-HCI with a Brinkman Polytron (Westbury, NY; setting 6, sec). The homogenates were washed twice by centrifugation (39,000 g 10 min), and the final pellets were resuspended in 50 mM Tris-HCI, containing 5 mM MgCI 2 and 0.1% BSA (bovine serum albumin). For the assay, aliquots (0.4 ml) were incubated with 0.05 nM 125 1]D-Trp6 LHRH (2200 Ci/mmol) with and without 0.05 ml of unlabeled competing test peptides. After a 60 min incubation the bound 125 1]D-Trp6 LHRH was separated from the free by rapid filtration through GF/B filters (Brandel, Gaithersburg, MD), which had been previously soaked in polyethyleneimine/0.1% BSA. The filters were then washed three times with aliquots of ice-cold 50 mM Tris-HCI, and the bound radioactivity trapped on the filters was counted by gamma spectrometry (Wallac LKB, Gaithersburg, MD). Specific binding was defined as the total 125 1]D-Trp6 LHRH bound minus that bound in the presence of 1000 nM D-Trp6 LHRH (Bachem, Torrence, CA).

188- Bombesin/GRP Radioligand Binding

O

S[0225] Membranes were prepared for radioligand binding studies by homogenization of AR42J rat pancreas cells expressing the native bombesin/GRP O receptor, in 20 ml of ice-cold 50 mM Tris-HCI with a Brinkman Polytron (Westbury, CI NY; setting 6, 15 sec). The homogenates were washed twice by centrifugation (39,000 g 10 min), and the final pellets were resuspended in 50 mM Tris-HCI, Scontaining 2.5 mM MgCI 2 and 0.1% BSA. For the assay, aliquots (0.4 ml) were incubated with 0.05 nM 1 25 1-Tyr4]bombesin (2200 Ci/mmol, New England Nuclear, CNl Boston, MA), with and without 0.05 ml of unlabeled competing test peptides. After a 30 min incubation the bound 125 1-Tyr4]bombesin was separated from the free O by rapid filtration through GF/B filters (Brandel, Gaithersburg, MD), which had been previously soaked in 0.3% polyethyleneimine. The filters were then washed three times with 5-ml aliquots of ice-cold 50 mM Tris-HCI, and the bound radioactivity trapped on the filters was counted by gamma spectrometry (Wallac LKB, Gaithersburg, MD). Specific binding was defined as the total 1 25 1-Tyr4]bombesin bound minus that bound in the presence of 1000 nM bombesin (Bachem, Torrence,

CA).

[0226] Some of the compounds of the instant invention have at least one asymmetric center. Additional asymmetric centers may be present in the molecule depending upon the nature of the various substituents of the molecule. Each such asymmetric center will produce two optical isomers and it is intended that all such optical isomers, as separated, pure or partially purified optical isomers, racemic mixtures or diastereomeric mixtures thereof, are included within the scope of the instant invention.

[0227] The compounds of the instant invention generally can be provided in the form of their pharmaceutically acceptable acid addition salts, such as the salts derived from using inorganic and organic acids. Examples of such acids are hydrochloric, nitric, sulfuric, phosphoric, formic, acetic, trifluoroacetic, propionic, maleic, succinic, D-tartaric, L-tartaric, malonic, methane sulfonic and the like. In addition, certain compounds containing an acidic function such as a carboxy can be isolated in the form of their inorganic salt in which the counter-ion can be selected from sodium, potassium, lithium, calcium, magnesium and the like, as well as from organic bases.

189- [0228] The pharmaceutically acceptable salts can be formed by taking about 1 O equivalent of a compound of the invention and contacting it with about 1 equivalent or more of the appropriate corresponding acid of the salt which is desired. Work-up

C.)

o and isolation of the resulting salt is well-known to those of ordinary skill in the art.

N [0229] The compounds of this invention can be administered by oral, parenteral intramuscular, intraperitoneal, intravenous or subcutaneous injection, or implant), nasal, vaginal, rectal, sublingual or topical routes of administration and can Ibe formulated with pharmaceutically acceptable carriers to provide dosage forms C appropriate for each route of administration. Accordingly, the present invention features pharmaceutical compositions comprising, as an active ingredient, at least one compound of the invention in association with a pharmaceutically acceptable carrier.

[0230] Solid dosage forms for oral administration include capsules, tablets, pills, powders and granules. In such solid dosage forms, the active compound is admixed with at least one inert pharmaceutically acceptable carrier such as sucrose, lactose, or starch. Such dosage forms can also comprise, as is normal practice, additional substances other than such inert diluents, lubricating agents such as magnesium stearate. In the case of capsules, tablets and pills, the dosage forms may also comprise buffering agents. Tablets and pills can additionally be prepared with enteric coatings.

[0231] Liquid dosage forms for oral administration include pharmaceutically acceptable emulsions, solutions, suspensions, syrups, the elixirs containing inert diluents commonly used in the art, such as water. Besides such inert diluents, compositions can also include adjuvants, such as wetting agents, emulsifying and suspending agents, and sweetening, flavoring and perfuming agents.

[0232] Preparations according to this invention for parenteral administration include sterile aqueous or non-aqueous solutions, suspensions, or emulsions.

Examples of non-aqueous solvents or vehicles are propylene glycol, polyethylene glycol, vegetable oils, such as olive oil and corn oil, gelatin, and injectable organic esters such as ethyl oleate. Such dosage forms may also contain adjuvants such as preserving, wetting, emulsifying, and dispersing agents. They may be sterilized by, for example, filtration through a bacteria-retaining filter, by incorporating sterilizing agents into the compositions, by irradiating the compositions, or by heating the -190compositions. They can also be manufactured in the form of sterile solid 0 compositions which can be dissolved in sterile water, or some other sterile injectable N medium immediately before use.

O [0233] Compositions for rectal or vaginal administration are preferably Nsuppositories which may contain, in addition to the active substance, excipients such as coca butter or a suppository wax.

[0234] Compositions for nasal or sublingual administration are also prepared with standard excipients well known in the art.

[0235] In general, an effective dose of an active ingredient in the compositions of this invention may be varied; however, it is necessary that the amount of the active ingredient be such that a suitable dosage form is obtained. The selected dosage depends upon the desired therapeutic effect, on the route of administration, and on the duration of the treatment, all of which are within the realm of knowledge of one of ordinary skill in the art. Generally, dosage levels of between 0.0001 to 100 mg/kg of body weight daily are administered to humans and other animals, mammals.

[0236] Preferred dosage ranges are from 0.01 to 10.0 mg/kg of body weight.

Such dosages may be administered, for example, daily as a single dose or divided into multiple doses.

OTHER EMBODIMENTS [0237] Various modifications and variations of the described method and system of the invention will be apparent to those skilled in the art without departing from the scope and spirit of the invention. Although the invention has been described in connection with specific desired embodiments, it should be understood that the invention as claimed should not be unduly limited to such specific embodiments.

Indeed, various modifications of the described modes for carrying out the invention that are obvious to those skilled in the fields of medicine, immunology, pharmacology, endocrinology, or related fields are intended to be within the scope of the invention.

[0238] All publications mentioned in this specification are herein incorporated by reference to the same extent as if the disclosure of each independent publication was explicitly provided herein.

-191

Claims (10)

1. 2. A compound according to claim 1, wherein X is doxorubicin, or a doxorubicin derivative; or a pharmaceutically acceptable salt thereof.
2. 3. A compound according to claim 1, wherein X is camptothecin, a camptothecin derivative, paclitaxel, or a paclitaxel derivative.
3. 4. A compound according to claim 3, wherein said camptothecin derivative is: -193- 00 N NN N ONN N F- N. F N 00 ~0-1 or a pharmaceutically acceptable salt thereof. A compound according to claim 3, wherein X is paclitaxel or a paclitaxel derivative, wherein said paclitaxel derivative is: -194 00 HI 3 C 1 HC CH OH SCH 3 H O CH 3 O. HO H 0 0 >0 or a pharmaceutically acceptable salt thereof.
4. 6. A compound according to claim 2, wherein X is doxorubicin or a doxorubicin Sderivative, wherein said doxorubicin derivative is: H '-OH ,O 0 OH 9 H C H3C NH 2 or a pharmaceutically acceptable salt thereof.
5. 7. A compound according to any one of claims 1 to 6, wherein Z is a somatostatin analog according to the formula: -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -DPhe-cyclo(Cys-31Tyr-DTrp-Lys-Val-Cys)-Thr-NH 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 or a pharmaceutically acceptable salt thereof.
6. 8. A compound according to any one of claims 1 to 6, wherein Z is a bombesin analog according to the formula: -GIn-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4); -DPhe-Gln-Trp-Ala-Val-pAla-His-Leu-Leu-NH 2 or a pharmaceutically acceptable salt thereof. -195-
7. 9. A compound according to claim 1, wherein at least one of m and n is not 0; or a pharmaceutically acceptable salt thereof. A compound according to claim 1, wherein said compound comprises the formula according to: F N 0 Fl N 0 Doc)-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 F )a -N F I (Doc),-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 N NN I I 0 0 F NN Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 H 0 IN 0 j- (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 >-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-PAla-His-Leu-Leu-NH 2 196 (SEQ ID NO: 4) fN_ 0 Aepa-(Doc) 2 -Gln-Trp-Ala-Va-3Ala-His-Leu-Leu-NH 2 N0 H 0 (SEQ ID NO: 4) NN N 0 N Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Leu-NH 2 CN 0 H 0 j-Aepa-(Doc-Gaba-Gn-Trp-Aa-Va-Aa-His-Leu-Nle-NH 2 (SEQ ID NO: 14) 197
8. 41--Aepa-Lys-DTyr-DTyr-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 Aepa-(Doc) 4 N H 0 o pGI u-His-Trp-Ser-Tyr- Leu-Arg-Pro-Gly-N H 0 ,0 0 0H ,C OHNH, 0 Y- H 4 -Aepa-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Val-Cys)-Thr-N H 2 H, (SEQ ID NO: 6) 198 0=1 0 HN-"--Aepa-(Doc) 4 H H OH0 HC H OH C H1pluHsTp-e-y- Leu-Arg-Pro-Gy-NH, 0O 3 H C- H, 0 GI-i-r-e-y- 0 c)-Aepa- N-\ pGu- isTp-e-Trl -Le-rgPo---N 00 F N ~~ply-s-TySr-Tyr-yclo(Cys-yr-r-Glys-b-Cs-T HH 00 N 0 N~ 0H 0 Lys- DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 I j- Doc)-Dyhe~-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H (Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -199 uljI I DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 N0 0 F 0 0 0 F N F~a 0 (Doc-Aepa~y-D~he-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 F 0 O~r H (Dc,Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 0 FN N N' 0 (Doc) 4 ep-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 200 00 (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys 0 H 3 C~~ o OH I (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 0 OH 9 H(NiHCH 0 OH 2 NN N 0 I0 I o Aepa-(DoC) 4 H 0 pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 0 H, Doc-Aepa-(Do -N-j PQ 0 0 OH H,C y HO" H IuHi-r-e-y- Leu-Arg-Pro-Gly-NH 2 y CH, J 0 H, ~Aepa-(D)oc) 4 -N N OH OJ Q -o H O HC 3 C3 0 p u H s T p e y r L e u -A rg -P ro -G ly -N H 0 CH,- isTr-S r0y 0 ZHH NSC-Aepa-(Doc) 3 '-NH OH H 0H pGlu-His-Trp-Ser-Tyr-N 72 201 H pGlu-His-Trp-Ser-Tyr-~> Leu-Arg-Pro-Gly-NH 2 0 (SEQ ID NO: 12); 0 (SEQ ID NO: 12) .(DOC) 4 -Aepa-Gaba-Gln-Trp-Aa-Va-P3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) 202 (SEQ ID NO: 12) (SEQ ID NO: 12) H2 91 ll f-"N (Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-PAla-His-Leu-Nle-NH2 ,0 0 0H H,C j rNH, (SEQ ID NO: 12) O OH HC 0 CNH (SEQ ID NO: 12); .rp-Lys-Abu-Cys)-Thr-NH 2 203 OH (Doc)-Aepa-D Phe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H OHH OHH HO3 OH, 0 H C H,0 0 PH, rA "-C(DOC)3-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-NH 2 :pl I-t(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 0O 0 0H H 3 HC OH NH 204 00 a pharmaceutically acceptable salt thereof. 11. A compound according to claim 1, wherein the formula comprises: (DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 205 (SEQ ID NO: 12) -N (Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-3Ala-His-Leu-Nle-NH 2 0 (SEQ ID NO: 12) or (DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-3Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) or a pharmaceutically acceptable salt thereof. 12. The compound according to claim 1, wherein said compound comprises the formula: a pharmaceutically acceptable salt thereof. 206 00 13. The compound according to claim 1, wherein said compound comprises the formula: N_ 1' 0 (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 C N 0OH 00 or a pharmaceutically acceptable salt thereof. 14. A compound according to claim 1, wherein said compound comprises the formula according to: I- Na N 0 0 IN 0 0 -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Val-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-RAla-H is-Leu-N le-N H 2 (SEQ ID NO: 12) -Aepa-(DOC) 2 -Gln-Trp-Ala-Val-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gln-Trp-Ala-Val-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-Val-RiAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-Ala-flAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-Val-2lAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Val-BAla-His-Leu-Ne-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DoC) 4 -Aepa-Gaba-N- pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH- 2 H 0 -Aepa-(Doc) 4 -Gaba pGlu-His-Trp-Ser-Ty -WN> Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Gaba pGlu-His-Trp-Ser-Ty N'>-Leu-Arg-Pro-Gly-NH- 2 H 0 207 00 H -(Doc) 4 -Aepa-Gaba -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 o H -Aepa-(DOC) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 -Doc-DPhe-Gln-Trp-Ala-Va-BlAla-His-Leu-Leu-NH 2 -Doc-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-N Ie-N H 2 -Doc-DPhe-GIn-Trp-Ala-Val-Gly-H is-Leu--Leu-N H 2 -Doc-DAla-Gln-Trp-Ala-Va-IIla-H is-Phe-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Ala-3Ala-H is-Phe-N Ie-NH 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-VaIBAla-H is-Leu-N Ie-NH 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-Aepa-DAla-Gln-Trp-Ala-Va-IlAla-H is-Phe-N Ie-N H 2 -Doc-Aepa-DPhe-GIn-Trp-Ala-Ala-IlAla-His-Phe-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va- Ala-His-Leu-Leu-NH 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(Doc) 3 -DAla-Gln-Trp-Ala-VaI-IlAla-His-Phe-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-GIn-Trp-Ala-Ala-BiAla-H is-Phe-N Ie-N H 2 -(DOC) 3 -Aepa-GIn-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 3 -Aepa-Gln-Trp-Ala-Val-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 3 -Aepa-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DOC) 3 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 3 -Aepa-GIn-Trp-Ala-VaI-BiAla-His-Leu-Leu-NH 2 (SEQ ID NO:. 4) -Aepa-Doc-DPhe-Gln-Trp-Ala-Ala-BIAla-H is-Phe-N Ie-N H 2 -Aepa-Doc-DAla-Gln-Trp-Ala-ValI-IAla-H is-Phe-N Ie-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Aia-Va-RAla-H is-Leu-Leu-N H 2 208 00 -Doc-DPhe-Gln-Trp-Ala-Ala-la-H is-Phe-N Ie-N H 2 -Doc-DAla-Gln-Trp-Ala-VaI-BAla-His-Phe-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 o -Doc-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 -Doc-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 -(DOC) 2 -Gln-Trp-Ala-Ala-fRAla-His-Phe-NIe-NH 2 (SEQ ID NO: 1) -(DoC) 2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) (N -(Doc) 2 -GIn-Trp-Ala-Val-fla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 2 -Gln-Trp-Ala-VaI-fla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-BiAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Y(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-Gly-His-Leu-YP(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(DOC) 4 -GIn-Trp-Ala-Va-Gly-His-Leu--(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Gaba-GIn-Trp-Ala-VaI-Gly-His-Leu-T(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-TP(C H 2 N H)-Leu-N H 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-TP(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BiAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(Doc) 4 -Gaba-GIn-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Gaba-Gln-Trp-Ala-Va-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 2 -Gln-Trp-Ala-Ala-B Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 2 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DoC) 2 -GIn-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DoC) 2 -Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) 209 00 -Aepa-Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-Va.-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 O aDh0l-r-l-a-I l- i-e l- H 0 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Val-RAla-H is-Leu-N eu-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BIAla-H is-Phe-Nle-N H 2 -Aepa-(DOC) 4 -DAla-Gln-Trp-Ala-VaI-IIla-His-Phe-N Ie-N H 2 C \-Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 c-I -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-VaIIla-H is-Leu-N Ie-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-VaI-aAla-H is-Leu-Leu-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Ala-ViAla-H is-Phe-N Ie-N H 2 -(Doc) 4 -DAla-Gln-Trp-Ala-Va-RAla-H is-Phe-N Ie-N H 2 -(DOC) 4 -DPhe-Gln-Irp-Ala-Va-Gly-His-Leu-Leu-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-BlAla-His-Leu-N Ie-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Val-Vla-His-Leu-Leu-NH 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-Ila-H is-Phe-N Ie-N H 2 -(Doc) 4 -Aepa-DAla-Gln-Trp-Ala-Va-RAla-H is-Phe-N Ie-N H 2 -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 4 -GIn-Trp-Ala-Ala-BlAIa-H is-Phe-N Ie-N H 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-.Ala-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Ila-His-Leu-N le-N H 2 (SEQ ID NO: -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-BAla-.His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 4 -Gln-Trp-Ala-VaI-rBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Gln-Irp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Gln-Trp-Ala-ValI-BAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -(DOC) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -Aepa-Gln-Trp-Ala-Ala-IlAIa-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DoC) 4 -Aepa-Gln-Trp-Ala-Va-IlAla-H is-Phe-N le-N H 2 (SEQ ID NO: 6) -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-N H 2 210 00 -Aepa-DPhe-Gln-Trp-Ala-VaH-IAla-H is-Leu-Leu-NH 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -DAla-Gln-Trp-Ala-VaI-llAla-H is-Phe-Nle-N H 2 -Ap-DC2DhCGnTpAaVlG)-i-e-e-H o -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Val-Iy~-His-Leu-le-NH 2 -Aepa-(DOC) 2 -DPhe-GIn-Trp-Ala-Val-iAla-H is-Leu-N eu-N H 2 -Ap-(DOC) 2 -DPhe-Gln-Trp-AAa-VaIAla-His-e-leu-N 2 IND)-~eGn-r-~-l-Aa-i-h-l-H -(DOC) 2 -DAla-Gln-Trp-Ala-VaI-BiAla-H is-Phe-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Val-Gly-H is-Leu-Leu-NH 2 -(Doc) 2 -DPhe-Gn-Trp-Ala-Va-fla-His-Leu-N le-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-IIla-His-Leu-Leu-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-Pila-H is-Phe-N Ie-NH 2 -Aepa-DAla-Gln-Trp-Ala-VaI-IlAla-His-Phe-Nle-N H 2 -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-Ila-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-llAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-DPhe-Gln-Trp-Ala-VaIAla-H is-Ala-N Ie-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Irp-Ala-Val-BlAIa-H is-Ala-Nle-N H 2 -(DOC) 2 -Gln-Trp-Ala-VaI-RAla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -Aepa-Gn-Trp-Ala-VaI-f3Ala-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 2 -Gln-Trp-Ala-ValI-aAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-VaI-flAla-His-Ala-N Ie-N H 2 -(DOC) 2 -Aepa-Gln-Trp-Ala-Val-RAla-H is-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 4 -DPhe-Gln-Trp-Ala-Val-RAla-His-Ala-N Ie-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-IIla-H is-Ala-Nle-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-la-His-Ala-N le-N H 2 -(DOC) 4 -Gln-Trp-Ala-Val-llAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DOC) 4 -Aepa-Gln-Trp-Ala-Val-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-PBAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -Aepa-(DoC) 2 -DPhe-Gln-Trp-Ala-Va-RAla-H is-Ala-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-ilAla-H is-Ala-N le-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Val-flAla-H is-Ala-N le-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-PIAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -211- 00 -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-Rla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) C) -(DOC) 4 -Gln-Trp-Ala-Val-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-IlAla-H is-Ala-Nle-N H 2 o e a Dh0l- r l- a-i l- i- l- l- H 0 ~-(DOC) 4 -A-DPhe-Gn-Trp-Aa-Val-Aa-His-Ala-N Ie-N H 2 -(DOC) 2 -Aepa-Gln-Trp-Ala-Val-RAla-H is-Ala-N Ie-N H 2 (SEQ ID NO: 7) -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Val-BIAla-H is-Ala-Nle-N H 2 -Aepa-(DOC) 3 -Gln-Trp-Ala-Va-P.Ala-H is-Leu-Leu-N H 2 (S EQ ID NO: 4) (Ni -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-RAla-His-Leu-N le-N H 2 (SEQ ID NO: -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO:- 9) -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-RlAla-His-P he-NIe-N H 2 (SEQ ID NO: 6) -Aepa-(DOC) 3 -Gln-Trp-Ala-Ala-IlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-Val-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Va-IIla-His-Leu-NIe-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-Va-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Doc-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 3 -Gln-Trp-Ala-VaI-Rfla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(Doc) 3 -Gln-Trp-Ala-Va-IRAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 3 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 3 -Gln-Trp-Ala-Ala-RAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 1) -(DOC) 3 -DPhe-Gln-Trp-Ala-Ala-IlAIa-His-Phe-Nie-N H 2 -(DOC) 3 -DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-N Ie-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-VaIRAla-His-Leu-Nle-N H 2 -(Doc) 3 -DPhe-Gln-Trp-Ala-ValI-fla-His-Leu-Leu-NH 2 -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Ala-3Ala-H is-Phe-N Ie-N H 2 -(DOC) 3 -Aepa-DAla-Gln-Trp-Ala-Va-RAla-H is-Phe-N le-N H 2 -(Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 3 -Aepa-DPhe-Gln-Irp-Ala-Val-BAla-His-Leu-Nie-N H 2 -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-B3AIa-His-Leu-Leu-N H 2 -Doc-Gln-Trp-Ala-Va-f3lAla--His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N H 2 (SEQ ID NO: 1) 212 00 -Doc-Aepa-Gln-Trp-Ala-ValI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) 0 -Doc-Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -DcAp(lNrilaVlRl-i-e-ieN2(E -Doc-Aepa-GIn-Trp-Ala-Va-Rla-H is-Leu-NLe-N H 2 (SEQ ID NO: 4) o ~-Doc-AeGln-Trp-Aa-a-I la-His-e-le-NH 2 (SEQ ID NO: 4) -Doc-Gln-Trp-Ala-AVal-Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-VaI-IIla-His-Leu-Nle-NH 2 (SEQ ID NO: N -Doc-Gln-Trp-Ala-VaI-IlAIa-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 4 -Ae pa- Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Aepa-N pGlu-His-Trp-Ser-Tyr -N%-Leu-Arg-Pro-Gly-NH 2 H 0 -(DOC) 2 -Aepa-N- pGlu-His-Trp-Ser-Tyr-N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 -Aepa-N-) pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa -N- -pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc- N pGlu-His-Trp-Ser-Tyr- Leu-Arg-Pro-Gly-NH 2 H 0 -213- 00 -Aepa-(DoC) 2 -N- H pGlu-His-Trp-Ser-Tyr- N Thr- Leu-Arg-Pro-Gly-NH 2 H 0 __-Aepa-(DoC)-N-) pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 H pGlu-His-Trp-Ser-Tyr N-hI- Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-N pGlu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0 (Doc) 2 Aepa-W K pGlu-His-Trp-Ser-Tyr-N> Leu-Arg-Pro-Gly-NH 2 H 0 (Doc) 3 Aepa-W K pGlu-His-Trp-Ser-Tyr--N- Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc Nt pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-N H 2 H 0 -(Doc) 4 -Aepa -N pGlu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DOc) 2 -N pGlu-His-Trp-Ser-Tyr- N- Leu-Arg-Pro-Gly-NH 2 H 0 -214- 00 -Aepa-(Doc) 3 -N-1, pGlu-His-Trp-Ser-Tyr- Leu-Arg-Pro-Gly-NH 2 0 Aepa(DOC) 4 N-K, pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Doc -N H pGlu-His-Trp-Ser-Tyr- N- ,r Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 pGlu-His-Trp-Ser-Tyr '>-Leu-Arg-Pro-Gy-NH 2 H 0 -(Doc) 3 -N\ pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -N\ pGlu-His-Trp-Ser-Tyr- N>"--Leu-Arg-Pro-Gy-NH 2 H 0 -Doc NL H 0 pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 (Doc)-NK pGlu-His-Trp-Ser-Tyr- N>-rLeu-Arg-Pro-Gy-NH 2 H 0 215 00 (DOC)4N-1K C1 pGlu-His-Trp-Ser-Tyr -N> 1 F- Leu-Arg-Pro-Gly-N H 2 o H -Aepa pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 2 -Aepa -N pGlu-His-Trp-Ser-Tyr Le-rPoGlNH H 0 H -(DoC) 3 -Aepa- pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 4 -Aepa -N pGlu-His-Trp-Ser-Tyr- N- Leu-Arg-Pro-Gly-NH 2 H 0 2 H -Aepa-Doc- pGlu-His-Trp-Ser-Tyr- Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 2 -N pG Iu- H is-Trp- Ser-Ty r Leu-Arg- Pro- G y- N H 2 H 0 -Aepa-(Doc) 3 N pGlu-His-Trp-Ser-Tyr N> 1 -Leu-Arg-Pro-Giy-NH 2 H 0 -216- 00 H -Aepa-(DoC) 4 N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-GIy-N H 2 o H 0 0 F 0Q -0 NN 0_ H -(DOC) 2 -Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 2 -Gln-Trp-Ala-VaI-lAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 2 -Gln-Irp-Ala-ValI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 2 -Gln-Trp-Ala-ValIIAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-IlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-ValIRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -GIn-Trp-Ala-Ala- Ala-H is-Phe-N Ie-N H 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Leu-N Ie-N H 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-ValI.-Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BlAla-His-Phe-Nle-N H 2 -(DOC) 4 -DAla-Gln-Trp-Ala-VaI-IlAla-H is-Phe-NIe-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-BAla-H is-Leu-Nle-N H 2 -(DoC) 4 -DPhe-Gln-Trp-Ala-ValIBAla-His-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-BlAIa-His-Phe-N Ie-N H 2 -(DOC) 4 -Aepa-DAla-Gln-Trp-Ala-VaI-rlAla-His-Phe-N le-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-N Ie-N H 2 217 00 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BlAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-Va-la-H is-Phe-N Ie-N H 2 o -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-IIla-His-Leu-Nle-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Val-41Ala-H is-Leu-Leu-N H 2 -(Doc) 4 -Gln-Trp-Ala-Ala-Rla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) C -(DOC) 4 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) r- -(DOC) 4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: C) -(DOC) 4 -Gln-Trp-Ala-VaI-BiAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -Aepa-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 1) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-BAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Aepa-Gln-Trp-Ala-ValI-rla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-Pila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -Gln-Trp-Ala-Ala-rBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-RAla-H is-Phe-N le-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 4 -Gln-Trp-Ala-ValIrA~a-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 2 -DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -(Doc) 2 -DAla-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-Va-IlAla-His-Leu-Nle-NH 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -Aepa-DAla-Gln-Trp-Ala-Va-IlAla-H is-Phe-NIe-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Val-BIAla-His-Leu-Leu-N H 2 -Aepa.-(DoC) 2 -DPhe-Gln-Trp-Ala-Ala-BlAla-His-Phe-Nle-N H 2 -Aepa-(DoC) 2 -DAla-Gln-Trp-Ala-Va-RAla-H is-Phe-N Ie-N H 2 -Aepa-(DoC) 2 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -218- 00 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Val-BAla-H is-Leu-N le-N H 2 -Aepa-(DOC) 2 -DPhe-Gn-Trp-Ala-Val-PiAla-H is-Leu-Leu-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-gAla-H is-Phe-N Ie-N H 2 o -(DOC) 2 -Aepa-DAla-Gln-Trp-Ala-Val-RIAla-H is-Phe-N Ie-N H 2 -(DoC) 2 -Aepa-DPhe-Gln-Trp-Ala-Val-Gly-H is-Leu-Leu-N H 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BiAla-His-Leu-Leu-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Val-'Ala-H is-Ala-Nle-N H 2 -(DOC) 2 -Aepa-Gln-Trp-Ala-Va-BlAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(Doc) 4 -DPhe-Gln-Trp-Ala-VaIRAla-His-Ala-Nle-N H 2 -(DOC) 4 -Aepa-DPhe-Gn-Trp-Ala-Va-Ila-His-Ala-N Ie-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-N le-N H 2 -(Doc) 4 -Gln-Trp-Ala-VaI-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 4 -Aepa-Gln-Irp-Ala-Va-BllAa-H is-Ala-N Ie-N H 2 (SEQ ID NO: 7) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-BllAa-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DOC) 2 -DPhe-GIn-Trp-Ala-VaI-aAla-H is-Ala-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-la-His-Ala-N Ie-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-N le-N H 2 -(DOC) 2 -Gln-Trp-Ala-Va-3Ala-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Val-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 2 -GIn-Trp-Ala-Val-BllAa-His-Ala-Nle-N H 2 (SEQ ID NO: 7) -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 2 -Aepa -N- pGlu-His-Trp-Ser-Tyr N>j-Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa -N- pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -219- 00 -Aepa-(DoC) 4 -NA H pGlu-His-Trp-Ser-Tyr 44')rh--Leu-Arg-Pro-Gly-NH, H0 -Aepa -N pGlu-His-Trp-Ser-Tyr -N r- Leu-Arg-Pro-NHEt H 0 -(DoC) 2 -Aepa -N- pGlu-His-Trp-Ser-Tyr N> 1 Leu-Arg-Pro-N HEt H 0 -(DoC) 4 -Aepa -N- pGlu-His-Trp-Ser-Tyr-N- LeuArg.Pro-NHEt H 0 -Aepa-(Doc) 2 pGlu-His-Trp-Ser-Tyr N>-Leu-Arg-Pro-NHEt H 0 *(Doc) 2 -N- pGlu-His-Trp-Ser-Tyr -NNF- Leu-Arg-Pro-N HEt H 0 -Aepa-(Doc) 4 -N pGlu-His-Trp-Ser-His N---Trp-Tyr-Pro-Gy-NH 2 H 0 -Aepa pGlu-His-Trp-Ser-His N>-'Trp-Tyr-Pro-Gy-NH 2 H 0 -(DoC) 2 -Aepa -N- pGlu-His-Trp-Ser-His N>j-Trp-Tyr-Pro-Gy-NH 2 H 0 220 00 -(Doc) 4 -Aepa -N pGlu-His-Trp-Ser-His N%--Trp-Tyr-Pro-Gly-N H, H H 0 -Aepa-(DoC)2- pGlu-His-Trp-Ser-His N-'-Trp-Tyr-Pro-Gly-N H 2 H 0 INN0 NN 0 H0 H H 0 -Aepa-(Doc)-Gaba -N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -A -(Doc) 4 -Gaba -N pGu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gy-N H 2 H 0 -(Doc) 4 A-Gaba pGu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gy-NH 2 H 0 221 00H -Aepa-(Doc) 4 -Gaba- o pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 o 0 S N_ 0 0 N N0 aN N 0 -Aepa-(DOC) 4 -Gaba-GIn-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba-Gn-Trp-Aa-Va-.Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DoC) 4 -Aepa-Gaba -N-N pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -Gaba -N- pGlu-His-Trp-Ser-Tyr '-Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 -Aepa-Gaba- pGlu-His-Trp-Ser-Tyr -N n- Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -Gaba- pGlu-His-Trp-Ser-Tyr rLeu-Arg-Pro-Gly-NH 2 H 0 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 222 00 0 Nz N 0 C) N 0 -(DOC) 4 Lys- DTy r- DTy r-cyclo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 cIN c-I 0 F N N I 0 0 F-I N- 0 0 N HH Doc-N pGlu-His-Trp-Ser-Tyr N"'FLeu-Arg-Pro-Gly-NH 2 H 0 (Doc) 2 N pGlu-His-Trp-Ser-Tyr -N >"-Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 3 rl pG Iu- His-Trp- Ser-Ty r Leu-Arg -P ro-G ly- N H 2 H 0 -(DoC) 4 pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa- Lys- DTy r- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 223 00 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(o)-0eccoCs3Iy-~pLsVICs-hrNH 0 -(Doc) 5 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(o)-0eccoCs3~r-~pLsVlCs-h-H o-(DOC) 4 DPh e-cyclo(Cys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -(DOC) 3 DPh e-cyc lo(C ys-3I Tyr- Drp-Lys-Va I-Cys)-Th r- N H 2 -(DOC) 2 DPh e-cyc lo(C ys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -Doc- D Phe-cyclo(C ys- 3Tyr-DTrp- Lys-Va I-C ys)-Th r- N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(Doc) 6 -Aepa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(Doc) 5-Aep a- D Phe-cyc lo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(Doc) 3 -Ae pa- D Phe-cycl o(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 Doc-Aepa- DP he-cyclo (C ys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- NH 2 -Ae pa -(Doc) 4 D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Aepa-(DOC) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -Aepa-Doc-.DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc)5-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 4 DPh e-cycl o(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 -(Doc) 3 DP he-cycl o(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 -(DOC) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -Doc-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Aepa) 2 -DPhe-cyclo(Gys-3Tyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC) 6 -Ae pa- D Phe-cyc lo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Thr-N H 2 -(Doc) 5-Aep a- D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DoC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC) 3 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 2 -Aep a- DP he-cyc lo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -Ae pa-(Doc) 4 D Phe-cycl o(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -Aepa-(Doc) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Aepa-(DOC) 2 DP he-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 224 00 ~-Aepa- Doc- DP he-cycl o(C ys-3 [Tyr- DTrp- Lys-Th r-Cys)-Th r- NH 2 -Aepa-DPhe-cyclo(Cys-3Iyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 o -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc) 6 -D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 5 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Doc-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (DOC) 5 -Ae pa- DPh e-cyclo(Cys-3 ITyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc) 2 -DPhe-cyclo(Cys-3Iyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa- Doc- D Phe-cyclo (C ys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys) -Th r- N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(DOC) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 5 DP he-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -(Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DoC) 6 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 5 -Ae pa- D Phe-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 225 00 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -Aepa- Lys- DTy r- DTyr-cyclo (Cys-Tyr- DT rp-Lys-Ab u-Cys)-Th r- N H 2 -Ls 0r ~rccoCysTr ~pLsA s-hr o-(DOC)4-Ae pa- Lys- DTyr- DTyr-cycl o(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 -(DOC) 3-Ae pa- Lys- DTy r-DTy r-cycl o(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC)2-Ae pa -Lys- DTy r- DTyr-cyclo (Cys-Ty r- DTrp- Lys-Ab u-Cys)-Th r- N H 2 'No)-eaLsDy-Dy-yl(y-y-~p-y-b-y)TrNH -Doc-Ae pa- Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 r- -Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 2 Lys- DTy r- DTy r-cyclo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 3 Lys- DTy r- DTy r-cyclo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 4 Lys- DTy r- DTyr-cyc lo(Cys-Ty r-DTrp- Lys-Ab u-Cys)-Th r- N H 2 (Doc) 5 Lys- DTy r- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 6 Lys- DTyr- DTyr-cyclIo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa- Doc- D Phe-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa-(Doc) 4 Lys- DTy r- DTy r-cyclo (Cys-Ty r-DT rp- Lys-Ab u-C ys)-Th r- N H 2 -Aepa -(DOC) 3 Lys- DTy r- DTyr-cyc lo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -Ae pa- (DOC) 2 Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -Ae pa- Doc- Lys- DTyr-DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(DOC) 4 -Aepa- DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Aepa) 2 -C aeg-cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(DOC) 6 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 5 -Ae pa-C aeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 (DOC) 4 -Aepa-C aeg-cyc lo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Ty r- N H 2 -(DOC) 3 -Aepa-Caeg-cyclo(DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Tyr- N H 2 -(Doc) 2 -Aepa-C aeg -cycl o(D Cys- 3Pa I-DTrp- Lys- D Cys)-Th r(BzI)-Tyr- N H 2 Doc-Aep a-C aeg-cycl o(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(DOC) 6 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 226 00 ~-(DOC) 5 -Caeg-cyclo(D Cys-3 P aI- DTrp-Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(Doc) 4 -C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(Doc) 3 -Caeg-cyclo(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(Bz) -Ty r- N H 2 e-ylo( y- -D0p y-DCs-hrBl Tr o(Doc)-C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Doc-a- cyClo(Dcys-3PoD~p-Las-Dr- ys-Thr(BzIT zl)-y H 2 -Ae pa-(DOC-Caeg-cyclo(DCys-3 Pa I-DTrp-Lys- DCys)-Th r(Bz)-Tyr-N H 2 -Ae pa-(Doc)3-C aeg-cyclo(DC ys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -Aepa-(DOC)4-C aeg-cycl o(D Cys-3 Pa I-DTrp- Lys- DC ys)-Th r(Bz)-Tyr- N H 2 Ls-Caeg y -cycl(Cys-- DTrp- Lys- -Cys)-Th Tr- N H 2 -(Doc)4-Ae pa- Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -()-Aepa-Lysc)-D~yrey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-()-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -()-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(D-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(D2Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)8-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)HS-Aep-Ve-yl(sTrDNYRrp-AVKLySI-A -H2 r-Q NO -(Aepa)HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -(Aepa)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Aepa)HSDAVFTDNYIRLRKQMAVKKFLNSILN-NH 2 (SEQ ID NO: 17) -(Aepa)HSDAVFTDNYTRLRKQMNAVKKYLNSILN-NH 2 (SEQ ID NO: 1) (aHSDAVFTDNYTRLRKQ (eAVKK YLNSILN-NH 2 (SEQ ID NO: 1 9) -HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -HSDAVFTDNYTRLRKQMAVKKFLNSILN-NH 2 (SEQ ID NO: 17) -HSDAVFTDNYTRLRKQMNAVKKYLNSILN-NH 2 (SEQ ID NO: 1) -HSAVFTDNag -yTlRKD (Ns-eaVKI-D Lys-N-h 2 r(SEQ IDy NO 19) A-C aeg-cyclo(DC ys-3 P aI-DTrp- Lys-h y)-TB-yr-N H 2 (D OC) 4 -Ae pa-C aeg-cyc lo(DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Ty r- N H 2 227 00 0 CIF N 0 I0 o FNN 0 H 2 (SEQ ID NO: -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 c)KNK-NH 2 NI (SEQ ID NO: 21) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 CI (SEQ ID NO: 22) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(IIAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) 2 (SEQ ID NO: -HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 C)KNK-NH 2 (SEQ ID NO: 21) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(gAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -Aep a- Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r- N H 2 Lys- DTyr- DTy r-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Ih r- NH 2 -(DOC) 4 Lys- DTy r- DTyr-cyclo(Cys-Ty r- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC) 4 DPh e-cyclo (Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 6 -D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys) -Th r- N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -D Phe-cyclo(C ys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r-N H 2 -(DOC) 4 D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC) 6 D Phe-cycl o(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r-N H 2 228 00 -(Aepa) 2 Lys- DTyr- D~yr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 o-(DOC) 4 DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 6 DP he-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Aepa) 2 Lys- DTyr- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 6 -Ae pa- Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 IND)-eaLsDy-Dy-yl(y-y-~p-y-b-y)TrNH -(DOC)4-Aepa- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 N -(C)-Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 Lys- DTyr- D rcyc o Cys-Tyr-D~p-Lys-Abu-Cys)-Th r-N 2 -ALps-Doc 6 -y-Dyr-D(Cy-cyTyr-yrDrpys-s-Au-Cys)-ThrrN H 2 H -Ae pa- (DOC)6- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Docpa- OLys- rDTy r r-cycl o(Cys-Tyr- rp-Ly-buys) Th r- H 2 -Aepa)-CLs-aeg Dy-cycCys-3PaI- DTrp-D ys-hrBzI N H 2 -A-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H -Ce-Dc 4 caeog(C yo( a-D~ys- Ls- Dr-y-ys s)-Th rB)-Ty-Ty- H 2 H -(DOC)4-C aeg -cyclo(DCys-3 P aI- DTrp- Lys-D Cys)-Th r(Bz) -Tyr- N H 2 N- a N N 0 00 0 N H 0 -Doc-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Gln-Trp-Ala-ValIRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Doc-Gln.-Trp-Ala-VaI-IIla-His-Leu-Nle-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-Val-IAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2 -Doc-DPhe-Gln-Trp-Ala-ValI-BAla-H is-Leu-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-DAla-Gln-Trp-Ala-VaI-PIla-H is-Phe-Nle-N H 2 229 00 -Doc-DPhe-Gln-Trp-Ala-Ala-B Ala-His-Phe-Nle-NH 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 -Doc-Aepa-DAla-Gln-Trp-Ala-VaI-gAla-His-Phe-Nle-NH 2 o -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-BlAla-H is-Leu-N Ie-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-ValAla-H is-Leu-Leu-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-N H 2 -Aepa-(Doc) 3 -DAla-Gln-Trp-Ala-VaI-IlAla-His-Phe-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Val-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 3 -DPhe-GIn-Trp-Ala-Va-RAla-H is-Leu-N Ie-N H 2 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-Va-I la-H is-Leu-Leu-N H 2 -(DOC) 3 -Aepa-Gin-Trp-Ala-Ala-RlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 3 -Aepa-Gln-Trp-Ala-ValI-RAia-H is-Phe-Nle-N H 2 (SEQ ID NO: 6) -(Doc) 3 -Aepa-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -(Doc) 3 -Aepa-Gln-Trp-Ala-VaI-RlAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 3 -Aepa-Gln-Trp-Ala-ValIrla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-DPhe-Gln-Trp-Ala-Ala-QAla-His-Phe-N Ie-N H 2 -Aepa-Doc-DAla-Gln-Trp-Ala-VaI-RAla-H is-Phe-N Ie-N H 2 -Aepa-Doc- DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-la-H is-Leu-N Ie-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-RlAla-H is-Leu-Leu-N H 2 -(DOC) 4 -GIn-Trp-Ala-VaI-Gly-His-Leu- T I- (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Y (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-T (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-T (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-H is-Leu-'f (CH 2 N H)-Leu-N H 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-I (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Gaba-Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 14) 230 00 -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-Vila-H is-Leu-Leu-N H 2 (SEQ ID NO: 14) C) -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Va-V3Ala-H is-Leu-Leu-N H 2 (SEQ ID NO: 14) -(DOC) 4 -Gaba-Gln-Trp-Ala-Va-IlAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) SQI O 2 0 -(Doc)-Aepa)-Gaba-Gln-Trp-Ala-Va-Rla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Aepa(c-ba-Gn-Trp-Aa-Va I-fGAy-His-Leu-Lee-NH 2 (SEQ ID NO: 12) -Aepa-Gln-Trp-Ala-VaI-G~ly-His-Leu-le-NH 2 (SEQ ID NO: 9) 2 (E -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-BAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-alAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-BAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -Aepa-(DOC) 2 -GIn-Irp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 2 -Gln-Trp-Ala-Ala-IRAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 2 -GIn-Trp-Ala-VaI-PiAa-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 2 -Gln-Trp-Ala-VaI-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-ValIBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-fBAla-H is-Leu-N le-N H 2 -(DOC) 4 -Aepa-DPhe-GIn-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gn-Trp-Aa-Aa-2Ala-H is-Phe-N Ie-NH 2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-VaI-IIla-His-Phe-N le-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-NH 2 -Aepa-(Doc) 4 -DPhe-Gn-Trp-Aa-Va-.Ala-H is-Leu-N le-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-f Ala-H is-Leu-Leu-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Ala-aAla-H is-Phe-N Ie-N H 2 -(DOC) 4 -DAla-Gln-Trp-Ala-VaI-IlAla-His-Phe-N Ie-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-BlAla-H is-Leu-N le-N H 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-ValI-fla-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-BiAla-His-Phe-Nle-NH 2 231 00 -(DOC) 4 -Aepa-DAla-Gln-Trp-Ala-VaIBAIa-His-Phe-Nle-N H 2 -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -(Doc) 4 -Aepa-Gln-Trp-Ala-Va-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: o -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-BlAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -GIn-Trp-Ala-Ala-aAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Rla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) IND-Dc 4 Gn-r-~-a-Aa-i-e-~-H 2 (E C-i -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Ila-His-Leu-le-NH 2 (SEQ ID NO: 4) -Ap-DC4GnTpAl-a-il-i-e-LuN2(E DN:4 -(DOC) 4 -Gln-Trp-Ala-Ala-faAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) C) -(Doc) 4 -Gln-Trp-Ala-ValIfla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Gln-Trp-Ala-ValIBAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 4 -Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -(Doc) 4 -Aepa-Gln-Trp-Ala-Ala-aAla-His-Phe-N le-N H 2 (SEQ ID NO: 1) -(DOC) 4 -Aepa-Gln-Trp-Ala-ValIaAla-His-Phe-N le-N H 2 (SEQ ID NO: 6) -Aepa-DAla-Gln-Trp-Ala-VaIIAla-H is-Phe-N le-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-1la-H is-Phe-N le-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -(DOC) 2 -DAla-Gln-Irp-Ala-VaI-Ila-His-Phe-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-N Ie-N H 2 0 0 0 N CH 0 -(Doc) 2 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -(DOC) 2 -DAla-GIn-Trp-Ala-VaI-BAla-His-Phe-N Ie-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-PiAla-H is-Leu-NIe-N H 2 232 00 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-IIAla-H is-Leu-Leu-NH 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -Aepa-DAla-Gln-Trp-Ala-VaI-PiAla-H is-Phe-Nle-N H 2 o -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-aIAla-H is-Phe-N Ie-N H 2 -(DOC) 2 -Aepa-DAla-Gln-Irp-Ala-VaIBAla-H is-Phe-N Ie-N H 2 -(DOC) 2 -Aepa-DPhe-Gin-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RlAla-His-Leu-Nle-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-VaIBAla-H is-Leu-Leu-N H 2 -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Va-IAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 2 -GIn-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-ValI-BAla-H is-Ala-N Ie-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-ValI-RAla-His-Ala-Nle-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-BAla-His-Ala-Nle-N H 2 (SEQ ID NO: 7) -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-Nle-N H 2 -(Doc) 2 -Aepa-Gln-Trp-Ala-Va-IIAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(Doc) 4 -DPhe-Gln-Trp-Ala-Va-RllAa-H is-Ala-Nle-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Val-BIAla-H is-Ala-Nle-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Val-lAla-H is-Ala-Nle-N H 2 -(Doc) 4 -Gln-Trp-Ala-Val-IIla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 4 -Aepa-Gln-Trp-Ala-Val-PIAla-His-Ala-Nle-NH2 (SEQ ID NO: 7) -Aepa-Doc-Gln-Trp-Ala-Val-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-Va-BAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Val-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 3 -Gin-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc)-Gln-Trp-Ala-Va-IIAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DoC) 3 -Gln-Trp-Ala-Val-Ila-His-Leu-Nle-NH2 (SEQ ID NO: -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-IIAla-His-Leu-Leu-NH2 (SEQ ID NO: 4) -(DOC) 3 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N H 2 (SEQ ID NO: 1) -(DOC) 3 -Gln-Trp-Ala-VaI-IIla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 3 -Gln-Trp-Ala-Val-IlAia-H is-Leu-N Ie-N H 2 (SEQ ID NO: 233 00 -(DOC) 3 -Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-GIn-Trp-Ala-Va-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) 0 -(Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 3 -Aepa-DPhe-GIn-Trp-Ala-ValI-BAla-His-Leu-N Ie-N H 2 (Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Ila-H is-Leu-Leu-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -(DOC) 3 -DAla-Gln-Trp-Ala-ValIBAla-His-Phe-N Ie-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Va-BlAla-His-Leu-Nle-NH 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-ValI-RAla-H is-Leu-Leu-N H 2 -DcGnTpAl(l-NaHs-hil-H (E DN:1 -Doc-Gln-Trp-Ala-AVal-Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-GIn-Trp-Ala-VaI-BAl-His-Pe-Ne-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-G~ly-His-Leu-e-NH 2 (SEQ ID NO: 9) -Doc-.Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: -Doc-GepGn-Trp-Aa-Ala-is~-eu-e-NH 2 (SEQ ID NO: -Doc-Aepa-GIn-Trp-Ala-AVa-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Doc-Aepa-Gln-Trp-Ala-VaI-lAy-His-e-Ne-NH 2 (SEQ ID NO: -Doc-Aepa-Gln-Trp-Ala-VaI-G~ly-His-Leu-Le-NH 2 (SEQ ID NO: 9) -Doc-Aepa-Gln-Trp-Ala-Va-BAla-H is-Leu-NLeu-N H 2 (SEQ ID NO: -Aepa -N H pGlu-His-Trp-Ser-Tyr- N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 -Aepa -N H pGlu-His-Trp-Ser-Tyr N -)Leu-Arg-Pro-Gly-NH 2 H 0 234 00 -(Doc) 3 -Aepa -N H o pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 M ~-(DoC) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc- N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2 H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 3 N H pGlu-His-Trp-Ser-Tyr N Le-rPoGyNH H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-Tyr N Le-rPoGy-H H 0 -Aepa N H pGlu-His-Trp-Ser-Tyr N--jLeu-Arg-Pro-Gly-NH 2 H 0 235 00 -(DOC) 2 -Aepa-N H pGlu-His-Trp-.Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 -Aepa N H pGlu-His-Trp-Ser-Tyr N Le-r-oGyNH -(Doc) 4 -Aepa-N H pGlu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 c-iH 0 -Aepa-Doc -N H pGlu-His-Trp-Ser-Tyr )Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Le-rPoGy-H H 0 -Aepa-(Doc) 3 N H pGlu-His-Trp-Ser-Tyr N---Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-G ly-NH 2 H 0 -Doc -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 236 00 -(DoC) 2 -N H opGlu-His-Trp-Ser-Tyr N _--Leu-Arg-Pro-Gly-NH 2 H 0 -(DOC) 3 -N H pGlu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -(DOC) 4 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 2 -Doc-N H pGlu-His-Trp-Ser-Tyr N Le-r-rGy-H H 0 -(Doc) 2 1N pGlu-His-Trp-Ser-Tyr N _-Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc)3 -N 3 H pGlu-His-Trp-Ser-Tyr -Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 N H pGlu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 H -Aepa -N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-G ly-N H 2 H 0 237 00 H -(DOC) 2 -Aepa-N opGlu-His-Trp-Ser-Tyr /--Leu-Arg-Pro-GyNH 2 HO0 H -(DoC) 3 -Aepa-N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 2 H 8 -(Doc) 4 -Aepa N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-Doc -N pGlu-His-Trp-Ser-Tyr -N--'--Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(DoC) 2 -N pGlu-His-Trp-Ser-Tyr N *-Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(DoC) 3 -N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 4 N pGlu-His-Trp-Ser-Tyr -Leu-Arg-Pro-Gly-NH 2 H 0 -238- 00 H -Doc- N opGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 HO0 H -(DOC) 2 -N pGlu-His-Trp-Ser-Tyr N ~~~-Leu-Arg-Pro-Gly-NH 2 H 0 H pGlu-His-Trp-Ser-Tyr N 'Leu-Arg-Pro-Gly-NH 2 H 0 H -(DoC) 4 -N pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys) -Th r- N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Val-Cys)-Thr-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 Doc-Aepa- D Phe-cycl o(Cys-3I yr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -(Doc) 2 -Aepa- DP he-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC) 3 -Aepa- DPh e-cyclo (Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC) 5 -Aepa- D Phe-cycl o(Cys-3 I Tyr- DTrp- Lys-Va I-Cys) -Th r- N H 2 -(Doc) 6 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 239 00 -Doc-DPhe-cyclo(Cys-3 I~yr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 2 D Phe-cycl o(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC) 3 DPh e-cyclo(Cys- 3I1Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(O)-DPh-yloCy- y-Dr-LsV -y)T oA -(Doc) Phe-cyclo(Cys-3 I r-DTrp-Lys-Vays-Th-hr H 2 -Aepa-(Doc)3-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-NH2 -Aepa-(Doc)2-D Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- NH 2 -Ae pa-(Doc)- DP he-cyc lo (Cys-3 ITy r-DTrp- Lys-Va I-Cys)-Th r-N H 2 -AeDoc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VI-Cys)-Thr-N H 2 -(Doc) 6 DPh e-cyclo(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-T hr- N H 2 -(DOC)4-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(DOC)3- D Phe-cycl o(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC)2- DPh e-cyclo(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 DP he-cyclo(C ys-3 ITyr-DTrp- Lys-Th r-Cys)-Th r- N H 2 -Do D Ph e-cycl o(Cys-3 ITyr- DTrp-Lys-Thr-Cys)-Th r- NH 2 DP he-cycl o(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2 -(Doc) 6 5-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC)3-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC)2-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc)-Aepa-DPhe-cyco(Cys-3 Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Ae pa-D -Ph e-cyc lo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2 -Aepa-(DOC)3-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Ae pa- (DOC)2- D Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Th r-Cys) -Th r-N H 2 -Aepa-(Doc)-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Aepa--DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -AeD Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r-N H 2 -(DoCh-e-y aC-3he-y-Dlrp-ys-ITyr-CDr ys-Th r- y)T H-N 2 -()-Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -A-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -()-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 oc)6- DP he-cyclo(Cys-3 I Tyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 -(DOC) 6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc)5-DPhe-cyclo(Cys-31Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (DOC)4- DPh e-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 240 00 -(Doc) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc- D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 o -(Aepa) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 5 -Aepa-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 3 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa-(DOC) 4 DP he-cyc lo(Cys-3 ITyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 -Aep a-(DOC) 3 -D Ph e-cycl o(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(Doc) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-Doc-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-D~rp-.Lys-Abu-Cys)-Thr-N H 2 D Phe-cyc lo(C ys-3 ITyr- DTrp- Lys-Abu-Cys)-Th r- N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DoC) 4 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 5 DPhe-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys) -Th r-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 Doc- D Phe-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 5 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyco(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Aepa) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -Aepa- Lys- DTy r- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 241 00 -(Doc) 5 -Aepa- Lys- DTy r- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -Ae pa- Lys- DTy r- DTyr-cycl o(Cys-Tyr- DT rp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 3 -Ae pa- Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 y-Dyr 0rcc CsTr ~p y-buCs-hr o (Doc)-Aepa- Lys- DTyr- DTyr-cyclo(Cys-Ty r- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Do-aLys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys)-Thrr-N H 2 -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-IIla-His-Phe-N Ie-N H 2 (SEQ ID NO: 6) C \-(DOC) 4 -Aepa-GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) ci -(DOC) 4 -Aepa-Gln-Trp-Ala-VaIaAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-N H 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-BiAla-His-Phe-Nle-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Ila-His-Leu-N Ie-N H 2 (SEQ ID NO: -Aepa-(Doc) 4 -GIn-Trp-Ala-Va-f Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -Gln-Trp-Ala-Ala-RAla-His-Phe-N Ie-N H 2 (SEQ ID NO: 1) -(Doc) 4 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Gln-Trp-Ala-VaI-BiAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Gln-Trp-Ala-VaI-PiAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -(DOC) 4 -Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 6 Lys- DTy r- DTy r-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Ih r- N H 2 DOC) 5 Lys- DTy r- DTyr-cyc lo(Cys-Ty r- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 3 Lys- DTy r-DTyr-cyc lo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 2 Lys- DTyr- DTyr-cyclIo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 Doc- Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r- NH 2 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-Iyr-Drp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc) 2 -DPhe-cyclo(Cys-Tyr-Drp-Lys-Abu-Cys)-Thr-N H 2 -Aepa- Doc- D Phe-cyclo (C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(Doc) 4 Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa- (DOC) 3 Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(DOC) 2 Lys- DTy r- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 242 00 -Ae pa- Doc- Lys- DTyr- DTyr-cyclo(Cys-Ty r- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 6 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH2 -(Doc) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH2 -Ap-agccoDy-PlDrpLsDy)TrBl0y-H o -Ap-Caeg-cyclo(DCys-3PaI-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -()-Caeg -cyclo(D s-3Pa PaDIp-ys-ys-T r(Bz)-Ty (zl Tr-N 2 H -(Doc)6-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -(Doc)-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(AO)ep -C aeg -cycl o(DCys-3 PaI- DTrp- L ys-ThCB)-TrBTyr- NH 2 aeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- NH 2 -(Doc)4-Aep a-C aeg-cyclo (DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- NH 2 -(DOC)3-Aepa-Caeg-cycl o(DC ys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(DOC)2-Ae pa-C aeg -cyclo (DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(Doc)-Aepa-Caeg -cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 DO e-C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 -(Doc) 5-C aeg -cyclo(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(Doc)4-G aeg -cyc lo(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 (Doc) 4 -C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2 -(DOC)2-C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(Doc)-C aeg -cyco(DCys-3 P a-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Doc-(Caeg-yl(C -y-3PaID~r-LyPa-D~r- ys-hr(B)-Ty r(-N H -Ae pa- (DoC)3-Caeg-cycl o(DC ys-3 PaI- DTrp- Lys- DC ys)-Th r(Bz I)-Ty r- N H 2 -Aepa-(DoC)2-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -Aepa-(Doc)-C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 0 F~ N N 1 00 N 0 0of' N 0 H -Aepa-(Doc) 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(BzI)-Tyr-N H 2 -Ae p a-C a eg-cyc Io (D Cys- 3Pa I -DT rp -Lys -D Cys) -T hr(Bz) -Ty r- N H 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-N H 2 -Ae pa-(Doc) 2 DP he-cyclo(Cys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 243 00 -(Doc) 4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 N. N0 0 0 -o N H c-I 0 -Aep a- Lys- DTyr- DTy r-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Lys- DTyr- DTyr-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- NH 2 DoC) 4 Lys- DTyr-DTyr-cyclo(Cys-Ty r- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(Doc) 6 Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 0 S N 0 N~ 0 0 -Aepa-(DOC) 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -Aepa-Caeg-cyclo(DCys-3 Pa I-DTrp-Lys-DCys)-Th r(Bz)-Tyr-N H 2 -C aeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Iyr- N H 2 -Aepa-(DOC) 2 -D Phe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc) 4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 0 N 00 a'NNN 0 0 -(DOC) 2 -Gln-Trp-Ala-Ala-I3Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) 244 00 -(Doc) 2 -Gln-Trp-Ala-VaI-f Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 2 -GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DoC) 2 -Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: o -(Doc) 2 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-Ala-BIAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) 2 (E -Aepa-Gln-Irp-Ala-Va-BAla-His-Leu-le-NH 2 (SEQ ID NO: 4) -Aepa-(Doc)-G-Tr-a-Aa-Bi-Hs-e--NH 2 (SEQ ID NO: 1) r- -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -GIn-Trp-Ala-Va-G3I-H is-e-NLe-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-ly-H is-Leu-N e-N H 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-RAla-H is-Leu-ie-N H 2 (SEQ ID NO: 4) -(Doc)-GDOCn-rp-ra-Aa-VAI~as-Phe-Nee-NH 2 (SEQ ID NO: -(DOC) 2 -Gln-Trp-Ala-VlaIAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -(Doc) 2 -Gln-Trp-Ala-VaI-G~ly-His-e-Nle-NH 2 (SEQ ID NO: 9) -(Doc) 2 -Gln-Trp-Ala-VaI-IlAy-His-Leu-Le-N H 2 (SEQ ID NO: -(DOC) 2 -Gln-Trp-Ala-VaI-IRAla-His-Leu-le-NH 2 (SEQ ID NO: 4) -Aepa)-Gln-rp-Aa-Va-AIa-His-he-e-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-Vla-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-VaI-Iy~-His-e-Nleu-NH 2 (SEQ ID NO: 9) -Aepa-Gln-Trp-Ala-VaI-GAl-His-Leu-Le-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-gAla-His-Leu-le-NH 2 (SEQ ID NO: 4) -Aepa-(Doc)-G-Tr-a-Aa-BAi-Hi-e--NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -Gln-Trp-Ala-la-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -GIn-Trp-Ala-Va-GIyl-H is-e-Nle-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-BAl-His-Leu-Le-NH 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-Ila-His-Leu-le-N H 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gln-Trp-Ala-ValIIAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BIAla-His-Phe-Nle-NH 2 -(DOC) 4 -DAla-Gln-Trp-Ala-Va-3Ala-H is-Phe-Nie-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-N H 2 245 00 -(Doc) 4 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-IIla-His-Phe-N Ie-N H 2 -(Doc) 4 -Aepa-DAla-Gln-Trp-Ala-VaI-BiAla-His-Phe-Nie-N H 2 O aDh0l-r-l-a- l- i-e -e H o -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-G~ly-H is-Leu-le-N H 2 -(DOC) 4 -Aepa-DPhe-Gn-Trp-Aa-Va-RAla-His-Leu-N eu-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 4 -DAla-Gln-Trp-Ala-Va-BiAla-H is-Phe-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-RAla-H is-Leu-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-BlAla-His-Leu-Leu-N H 2 -(Doc) 4 -Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 1) -(DOC) 4 -Gln-Trp-Ala-VaI-4la-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Gln-Trp-Ala-Va-B Ala-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -(Doc) 4 -Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-RAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 4 -Aepa-Gln-Trp-Ala-VaIRAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-Ala-Ila-His-Phe-NIe-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -GIn-Trp-Ala-ValIIAla-H is-Leu-N Ie-NH 2 (SEQ ID NO: -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-fla-His-Leu-Nie-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(Doc) 2 -DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Ala-RAla-H is-Phe-N le-N H 2 -Aepa-DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-Leu-NH 2 -Aepa-DPhe-Gln-Trp-Ala-VaIQAla-H is-Leu-N le-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 246 00 -Aepa-DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BiAla-His-Phe-N Ie-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 o -(DOC) 2 -DPhe-Gln-Trp-Ala-ValI-fla-H is-Leu-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DoC) 2 -DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-Ala-IIAla-H is-Phe-N Ie-N H 2 IND)-eaD~eGnTpAa-a-1~-isLuLuNH Ci\ -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-N eu-NH 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-GIyl-H is-Leu-le-N H 2 -(Doc) 2 -Aepa-D~la-Gn-Trp-Aa-Va-GlAy-H is-Pe-Ne-N H 2 -(DOC) 2 -Aepa-DPhe-GIn-Trp-Ala-Ala-IIAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -GIn-Trp-Ala-Va-BAla-H is-Ala-N Ie-N H 2 (S EQ ID NO: 7) -Aepa-Gln-Trp-Ala-VaI-BAla-H is-Ala-N Ie-N H 2 (SEQ ID NO: 7) -(DOC) 2 -Gln-Trp-Ala-Va-BAla-H is-Ala-N Ie-N H 2 (SEQ ID NO: 7) -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-His-Ala-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Ala-N Ie-N H 2 -(DOC) 2 -DPhe-Gn-Trp-Ala-Va-RAla-H is-Ala-N Ie-N H 2 -Aepa-(DoC) 4 -Gln-Trp-Ala-Va-IIla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-BlAla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DOC) 4 -Gln-Trp-Ala-Val-IlAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-BiAla-H is-Ala-N Ie-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Val-lAla-H is-Ala-Nle-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Val-IlAla-H is-Ala-N Ie-N H 2 -(DOC) 2 -Aepa-Gln-Trp-Ala-Va-llAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Val-BiAla-H is-Ala-Nle-N H 2 -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Val-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Val-Gly-His-Leu-P(CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Gaba-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-Y (CH 2 N H)-Leu-N H 2 (SEQ ID NO: 13) 247 00 -(Doc) 4 -Gaba-Gln-Trp-Ala-Va-Gly-His-Leu-V (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 0 13) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Y (CH 2 NH)-Leu-NH 2 (SEQ ID NO: o 2) -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-T (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Gln-Irp-Ala-VaI-Gly-His-Leu-P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Gaba-Gln-Trp-Ala-Va-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Aepa- N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 2 -(DoC) 2 -Aepa N H pGlu-His-Trp-Ser-Tyr -N -ILeu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 -Aepa N H pGlu-His-Trp-Ser-Tyr -N---Leu-Arg-Pro-Gly-N H 2 H 0 -(DoC) 4 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Le-rPrGy-H H 0 -Aepa-Doc N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 248 00 -Aepa-(Doc) N o pGlu-His-Trp-Ser-Tyr N -rLeu-Arg-Pro-Gly-NH 2 -Aepa-(DOC) 3 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -Aepa N H pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 2 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 -Aepa -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 -Aepa -N H pGlu-His-Trp-Ser-Tyr -N -tLeu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 249 00 -Aepa-(Doc) 2 N H pGlu-H is-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 o 0 -Aepa-(Doc) 3 -N H pGl u-H is-Trp-Ser-Tyr N Leu-Arg- Pro-Gly-N H 2 H 0 -Aepa-(Doc) 4 -N H pG lu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 -Doc -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 -N H pG Iu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -(Doc) 4 N H pGlu-His-Trp-Ser-Tyr N _-Leu-Arg-Pro-Gly-NH 2 H 0 -Doc -N H pGlu-His-Trp-Ser-Tyr N _-Leu-Arg-Pro-Gly-NH 2 H 0 250 00 -(DOC) 2 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H H 0 -(DOC) 3 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa N pGlu-His-Trp-Ser-Tyr N- ,Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 2 -Aepa -N pGlu-His-Trp-Ser-Tyr 'N LeuArgProGy-NH 2 HO0 H -(Doc) 3 -Aepa -N pGlu-His-Trp-Ser-Tyr -N 'trLeu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 4 -Aepa -N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 H 0 251 00 H -Aepa-Doc N O pGlu-His-Trp-Ser-Tyr -N-->.Leu-Arg-Pro-Gy-NH 2 H0 H -Aepa-(Doc)N 7N p G Iu- H is-Trp-Ser-Ty r N Leu-Arg -Pro- G y- NH 2 H 0 C-0 H -Aepa-(Doc) 3 N pGlu-His-Trp-Ser-Tyr N--'Nr Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 4 N pGlu-His-Trp-Ser-Tyr N _-Leu-Arg-Pro-Gly-NH 2 H 0 H -Doc N pGlu-His-Trp-Ser-Tyr N"jt Leu-Arg-Pro-Gly-N H 2 H 0 H -(Doc) 2 N pGlu-His-Trp-Ser-Tyr N rLeu-Arg-Pro-Gly-NH 2 H 0 H -(DoC) 3 -N pGlu-His-Trp-Ser-Tyr -WN Leu-Arg-Pro-Gly-NH 2 H 0 252 H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 -HSDGIFTDSYSRYRKQMAVKKYLAAVL(RAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) 110 -HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(Arc)KNK-NH 2 (SEQ ID NO: 21) c-I -HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO: -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(RlAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(Ac)KNK-NH2 (SEQ ID NO: 21) -(Aepa)HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK- NH 2 (SEQ ID NO: -Aepa-Doc-C aeg -cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Ae pa-(Doc) 2 -C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DC ys)-Th r(BzI)-Tyr- N H 2 -Aepa-(DOC) 3 -C aeg-cyc lo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Tyr- N H 2 -Aepa-(DOC) 4 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Doc)r 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(DOC) 4 D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-NH 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 -(Doc) 4 -Aepa- D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-NH 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 2 -Ae pa- D Phe-cyclo (Cys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 253 00 -(DOC) 3 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 5 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 6 -Ae pa- D Phe-cycl o(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 o -(Aepa) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Doc- DP he-cyclo(C ys-3 ITyr-DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 3 DPhe-cycl o(Cys-3 I Tyr-DTrp- Lys-Va I- Cys)-Th r- N H 2 C \-(Doc) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(Doc) 5 DPhe-cyclo (Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 Doc) 6 DPh e-cycl o(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Ae pa- Doc- DP he-cycl o(Cys-3 ITyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -Aepa-(Doc) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aep a-(DOC) 3 D Phe-cyclo (Cys- 31Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 (Doc) 2 -Ae pa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r-N H 2 -(DOC) 3 -Aepa- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 5 -Aepa- DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 -Ae pa- DPh e-cyclo(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Ae pa) 2 D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC) 2 DPh e-cyclo (Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 3 DPh e-cyc lo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 4 D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 5 D Phe-cyclo(C ys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Aepa-Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Aepa-(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Aepa-(Doc) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -Aep a-(Doc) 4 D Phe-cycl o(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 DPh e-cyclo(C ys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 4 D Phe-cyclo (C ys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 254 00 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3I~yr-DTrp-Lys-Thr-Cys)-Th r-NH 2 -Aepa- D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-NH 2 -DcAp-0eccoCs3~y-~pLsAuCs-h-H o -(DOC)-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)3-Aepa- D Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc)5-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)r,-Aepa- DP he-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Do)-AeD P he-cycl o(Cys-3 ITyr-DTrp- Lys-Ab u-Cys)-Thr-N H 2 -(Aea-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)3- D Phe-cyclo(Cys-3 I Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC)4-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)5-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)r 5 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Doc- D Phe-cyclo (Cys-3 I Tyr-DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Aep a-(DOC- DPhe-cyclo(Cys-3 ITyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 -Aepa-(DOC)3-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa-(Doc)4-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ap-(Doc) 4 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC)4-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -()-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -A-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H -Aepa)-Depa-hhe-cyclo(Cys-3 Tr-ys-bysbuy)-Th r-N 2 (DcAp-DPhe-cyclo(Cys-3 I~yr-D~rp-Lys-Abu-Cy S)-Thr-N H 2 -A-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Thr-N 2 -A-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -A-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)6-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)4-p-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cy)-Thr-N H 2 -(Doc)-Aepa)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Aepa)-Doc) 2 ep-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -AeacAepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-C YS)-Thr-N H 2 255 00 -(DOC) 2 -DPhe-cyclo(Cys-Iyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(ea 2 (o)-0eccoCsTy-~pLsAuCs-hrNH -(Aepa-(DOC)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ap-Dc0Dh-yl(y-y-~pLsAuCs-h-H o -(Doc) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 6 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ih r-N H 2 N -(DOC) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 5 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Ih r-N H 2 -(Doc) 6 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Doc- D Phe-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 5 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 Lys- DTyr- DTy r-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r-N H 2 Doc-Aepa- Lys- DTyr- DTyr-cyclo(Cys-Ty r- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 2 -Aepa- Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Ih r- N H 2 -(DOC) 3 -Ae pa- Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 4 -Ae pa- Lys- DTyr-DTyr-cycl o(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 (Doc) 5 -Aepa- Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 6 -Aepa- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Aepa) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 Lys- DTy r- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 3 Lys- DTyr- DTy r-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 (Do00 4 Lys- DTy r- DTy r-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-T h r- N H 2 -(Doc) 5 Lys- DTyr- DTyr-cyclIo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa- Doc- Lys-- DTyr- DTyr-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 256 00 ~-Ae pa-(DOC) 2 Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r-N H 2 -Aepa-(Doc) 3 Lys- DTy r- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r-N H 2 -Ae pa-(Doc) 4 Lys- DTy r-DTyr-cycl o(Cys-Tyr- DTrp- Lys-Abu -Cys)-Th r- N H 2 -A a o-DPh-ylo(y-yr 0p y-bu-y)-hrNH o -Aepa-(DOC-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc)4-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 c-i 0 N 00 N- 0 0 N 0 H -Aepa -N H pG Iu- H is-Trp-S er-Ty r N Le u-Arg Pro-G Iy- NH 2 H 0 -(Doc) 2 -Aepa -N H p GI u -H is-T rp- Se r-Ty r N Le u-A rg -Pro- G y- NH 2 H 0 -(Doc) 4 -Aepa -N H p G Iu- H is-T rp- S er-Ty r N Le u-Arg -P ro-G Iy- NH 2 H 0 257 00 -Aepa- N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt o H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -(DoC) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -Aepa-(DOC) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 (DoC) 2 N H Glp-His-Trp-Ser-Tyr N Leu-Arg-Pro-N HEt H 0 -Aepa- N H pGlu-His-Trp-Ser-Tyr -N -"Leu-Arg-Pro-Gly-NH 2 H 0 258 00 -(DOC) 2 -Aepa -N H o ~~pGlu-His-Trp-Ser-Tyr N Le-rPoGyNH o H 0 -(Doc) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DoC) 4 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -Aepa- N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -(DoC) 3 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -(Doc) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N LuAgPoNHE H 0 -Aepa-(Doc) 4 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 259 00 -(Doc) 4 N H oGlp-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt o H 0 -Aepa-(DoC) 4 N H pGlu-His-Trp-Ser-His -N Tr-yPoGyNH H2 -Aepa- N H pGlu-His-Trp-Ser-His N Tr-yPoGyNH H 0 -(DoC) 2 -Aepa -N H pGlu-His-Trp-Ser-His N Tr-yPoGyNH H 0 -(Doc) 4 -Aepa N H pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-His N Tr-rPoGy-H H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-His -N -TpyrPoGyN 102 260 00 -Aepa-(Doc) 3 N H 2 pGlu-His-Trp-Ser-His N H 0 -Aepa -N H pGlu-His-Trp-Ser-His -N -rTrp-Tyr-Pro-G ly-N H 2 H 0 -(Doc) 3 -Aepa -N H pGlu-His-Trp-Ser-His N Tr-yPoGy-H H 0 -(Doc) 4 -Aepa -N H pGlu-His-Trp-Ser-His -N--TTrp-Tyr-Pro-Gly-NH 2 H 0 -Lys- DTyr- DTy r-cycl o(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r-N H 2 -Lys- Lys- Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa- Lys- DTyr- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa-(DOC) 4 Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(DOC) 2 Lys- DTyr- DTy r-cyclo(Cys-Tyr-Drp- Lys-Ab u-C ys)-Th r- NH 2 Doc) 4 Lys- DTyr- DTyr-cyc lo(Cys-Ty r-DT rp- Lys-Ab u-C ys)-Th r- N H 2 -(Doc) 6 Lys- DTyr- DTyr-cyclIo (C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- NH 2 -(Doc) 8 Lys- DTyr- DTy r-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- NH 2 -Ae pa-(DOC) 2 Lys- DTy r- DTy r-cyclo (Cys-Tyr- DT rp- Lys-Ab u-Cys)-Th r- N H 2 -(Aep a) 2 Lys- DTyr- DTyr-cyc lo(Cys-Ty r- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 2 -Ae pa- Lys- DTyr- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 (DOC) 4 -Ae pa- Lys- DTy r- DTyr-cyclo (Cys-Tyr-DTrp- Lys-Ab u-Cys)-T h r- N H 2 -(DOC) 6 -Aepa- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(DOC) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa -(DOC) 4 Lys- DTy r- DTyr-cyclo(C ys-Ty r- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa-(DOC) 6 Lys- DTy r- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 261 00 ~~Lys-Aepa- Lys- D~yr- DTyr-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 0 0 -Dh-yl(ysTrDr-y-ANCs-h- H 2 0 -Ae-(Do)-eaLsy-~r(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Dopa -Ays-y- DTyr- r-(Cys-Tyr-D rpy-Lysu-Abys s)-Thrr N H 2 H -Doc-Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 0 SN_ 0 N 0 0 -(Doc) 4 Lys- DTy r- DTyr-cyclIo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 Doc-Aepa- Lys- DTyr- DTyr-(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 2 -Aepa-Lys-DTyr-DTyr-(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -Aepa-Lys-DTyr-DTyr-(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 4 -Ae pa- Lys- D~yr-DTyr- (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa- Doc-Ae pa- Lys- DTyr- DTyr-(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 2 Lys- DTyr- DTy r-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Doc- Lys- DTyr- DTy r-cyclo(C ys-Tyr- DT rp- Lys-Ab u-Cys)-Th r- NH 2 0 N 00 N 0A 0 N0 0 -(DOC) 4 Lys- DTy r- DTyr-cyc lo(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 262 00 ~~Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 00 oN 00 N N H N, r* N 0- 0 -(DOC) 6 -C aeg-cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(DOC) 4 -C aeg-cyc o (D Cys-3 Pa I-DTrp- Lys-D Cys)-Th r(Bzi) -Tyr- N H 2 -C aeg-cyclo (DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 CI-Ae pa-C aeg-cyclo(DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2 -(DOC) 4 -Ae pa-C aeg -cyclo (D Cys-3 Pa I-DTrp- Lys- DC ys)-Th r(BzI)-Tyr- N H 2 -(DOC) 6 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -Aep a-C aeg -cyclo(D Cys-3 Pa- DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2 -Doc-Aepa-Caeg -cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 (Doc) 2 -Aep a-C aeg-cyclo(DC ys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(DOC) 3 -Aepa-Caeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(DOC) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -(Doc) 5 -Aepa-Caeg-cyclo(DCys-3 PaI-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -(DOC) 6 -Ae pa-C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(Aepa) 2 -C aeg-cyclo(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Doc-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 2 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Doc) 3 -C aeg -cyclo (D Cys-3 Pa I-DTrp- Lys-D Cys)-Th r(Bz) -Tyr- N H 2 -(Doc) 4 -C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys-D Cys)-Th r(Bz) -Tyr- N H 2 -(Doc) 5 -Caeg -cyclo(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(BzI) -Tyr- N H 2 (DOC) 6 -Caeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI) -Tyr- N H 2 (Ae pa) 2 -(DOC) 2 -D P he-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Aepa-Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (DOC) 2 -D Ph e-cyclo (C ys-Ty r- DTrp- Lys-Ab u-C ys) -Th r- N H 2 263 00 -(Aepa) 2 -(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (Doc) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 o -Ap-(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc)2-(Aepa)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -HSDAVFTDNYTRLRKQ(Nle)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) Cl -HSDAVFTDNYIRLRKQMAVKKFLNSILN-NH 2 (SEQ ID NO: 17) r--SAFDYTLKMVKLNINN2(EQI O 6 -HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(eHSDAVFTDNYTRLRKQ eAVKK LNSILN-NH 2 (SEQ ID NO: 1 -(eaHDVTNTRRQAKYNINNH SQI O 8 -(Aepa)HSDAVFTDNYTRLRKQNeAVKKLNSILN-NH 2 (SEQ ID NO: 1) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) -(Aepa)HSDAVFTDNYTRLRKQMAVKKFLNSILN-NH 2 (SEQ ID NO: 17) 0 -'XN 0 H4 0 -Aep a-(Doc) 4 Lys- DTy r- DTyr-cyclo (Cys-Ty r-DT rp- Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -(DOC) 6 Lys- DTyr- DTy r-cyclo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- NH 2 -(DOC) 8 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Ae pa-(DoC) 2 Lys- DTy r- DTyr-cyclo(C ys-Tyr- Drp- Lys-Ab u-Cys)-Th r- N H 2 -(Ae pa) 2 Lys- DTyr- DTyr-cycl o(C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 2 -Aepa- Lys- DTy r- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -Ae pa- Lys- D~yr- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 6 -Ae pa- Lys- DTyr- DTyr-cyclo (Cys-Tyr- D~rp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa -(Doc) 2 Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-T hr- N H 2 -Aep a-(Doc) 4 Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 264 00 -Aepa-(DOC) 6 -Lys-DTyr-D~yr-cyco(CYs-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 -Lys-Aepa- Lys- DTyr-DTyr-cycl o(Cys-Tyr- DTrp- Lys-Abu-Cys)-Th r- N H 2 0 No 0 oN 0 NH 0~ N -Ae pa- Lys- D~yr- DTyr-cycle (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 2 -Ae pa- Lys- DTy r- D~yr-cyc le(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- NH 2 -Aepa-(Doc) 2 -Aepa-Lys-DTyr-DTyr-cycle(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr- NH 2 _(DOC) 6 -Aep a- Lys- DTy r- DTyr-cycle(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 0 N N 0 0 -(o)-Ap-y-Dy-~r-yl(ysTrD~pLsAb-y)Th0NH -(DOC)-Aepa- Lys- DTyr-DTyr-cycle(C ys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 -(Doc)-Ae pa- Lys- DTyr-DTyr-cycle (Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(DOC)3-Aep a- Lys- DTy r- DTyr-cycle (Cys-Tyr-DT rp-Lys-Ab u-Cys)-Th r- N H 2 -Aepa-Doc-Aepa-Lys-DTyr-DTyr-cycle(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 O OH 0 0 "OH N /0 0 OHO0 01 H -Doc-DPhe-Gin-Trp-Ala-Val-BAla-H is-Leu-Leu-N H 2 -Doc-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-DAla-Gln-Trp-Ala-ValIBAla-His-Phe-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 265 00 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-IIla-His-Leu-Leu-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-ala-H is-Leu-N Ie-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N H 2 o -Doc-Aepa-DAla-Gln-Trp-Ala-ValI-IAla-H is-Phe-N Ie-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Ala-BIAla-His-Phe-N Ie-N H 2 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-NH 2 -Aepa.-(Doc) 3 -DPhe-GIn-Trp-Ala-Va-B Ala-H is-Leu-N Ie-N H 2 C \-Aepa-(DoC) 3 -DPhe-GIn-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 ci -Aepa-(Doc) 3 -DAla-Gln-Trp-Ala-Va-.Ala-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Ala-3Ala-His-Phe-Nie-NH 2 -(DOC) 3 -Aepa-Gln-Trp-Ala-VaI-IIla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 3 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 3 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DOC) 3 -Aepa-Gln-Trp-Ala-VaI-IIla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) -(Doc) 3 -Aepa-GIn-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-DPhe-Gln-Trp-Ala-VaIRAla-His-Leu-Leu-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-N Ie-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N H 2 -Aepa- Doc- DAla-G In-Trp-Ala-VaI-RAla-H is-Phe-N Ie-N H 2 -Aepa-Doc-DPhe-GIn-Trp-Ala-Ala-VBAla-His-Phe-NIe-N H 2 -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-IIla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-gAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-fla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-VaI-IlAla-His-Leu-Nle-NH2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH2 (SEQ ID NO: 9) -Aepa-GIn-Trp-Ala-VaIBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -Gln-Trp-Ala-ValIBAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaIIAla-H is-Leu-Nle-N H 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-aAla-H is-Phe-N le-N H 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-BAla-His-Phe-Nie-NH2 (SEQ ID NO: 1) 266 00 -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Ap-0-r-~-a-l~-isLuNeN 2 (E -Aepa-GIn-Trp-Ala-VaI-Iy~-His-Leu-le-NH 2 (SEQ ID NO: 9) -Ap0l-r-l-a-l-isLuLuN2(E DN:9 0 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-Ala-Rla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(Doc) 2 -Gln-Trp-Ala-VaI-IgAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(Doc) 2 -Gln-Trp-Ala-VaI-f Ala-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 2 -GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) N -(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 2 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-NH 2 (SEQ ID NO: 14) -(O)-eaGb(lNrpAaVli~aHsLu-e-H SQI O 4 -(Doc) 4 -A-Gaba-Gn-Trp-Aa-Va-lAa-H is-Leu-Leu-NH 2 (SEQ ID NO: 14) 4 -Gaba-Glrp-Ala-VaAla-His-Leu- C2H-Leu-N H 2 (SEQ O 4 ID NO: 13) -(DoC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-H is-Leu-T1 (C H 2 N H)-Leu-N H 2 (SEQ ID NO: 13) -(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-+ (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-Gly-H is-Leu-TV (C H 2 N H)-Leu-N H 2 (SEQ ID NO: 2) -(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-'P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Aepa-(DOC) 4 -Gaba-GIn-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BA~a-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Gaba-Gln-Trp-Ala-ValIIAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) 267 00 0 OH 0 00 0_ 0 -N2 OH 2 -Doc-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -Doc-DPhe-Gln-Trp-Ala-Va-BlAla-His-Leu-N Ie-N H 2 c-i -Doc-DPhe-Gln-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 -Doc-DAla-Gin-Trp-Ala-Val-Ila-H is-Phe-N Ie-N H 2 -Doc-DPhe-Gln-Trp-Ala-Ala-BiAla-His-Phe-Nle-NH 2 -Aepa-Gln-Trp-Ala-Ala-IlAIa-His-Phe-NIe-NH 2 (SEQ ID NO: 1) -(DOC) 2 -GIn-Trp-Ala-VaI-RAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -(Doc) 2 -Gin-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 2 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-VaI-IIla-His-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-ila-H is-Leu-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DAla-Gln-Trp-Ala-VaI-BAla-His-Phe-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-IIla-His-Phe-Nle-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-BiAla-His-Leu-Nle-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-N Ie-N H 2 -(Doc) 4 -Aepa-DPhe-GIn-Trp-Ala-Ala-Ila-H is-Phe-N Ie-N H 2 -(DOC) 4 -DPhe-GIn-Trp-Ala-VaI-BiAla-His-Leu-Leu-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Nle-NH 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 4 -DAla-GIn-Trp-Ala-VaI-Ila-H is-Phe-N Ie-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BiAla-H is-Phe-Nle-N H 2 -Aepa-(DoC) 4 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-N Ie-N H 2 (SEQ ID NO: 268 00 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nie-N H 2 (SEQ ID NO: 6) -Aepa-(Doc) 4 -Gln-Trp-Ala-Ala-RAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 1) -(O)-eaGnTpAaVl0~aHsLuLuN2(E DN:4 o -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-le-NH 2 (SEQ ID NO: 4) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-ly~-His-Leu-Le-NH 2 (SEQ ID NO: -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-RlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 4 -Aepa-Gln-Trp-Ala-Ala-RAla-His-Phe-NIe-NH 2 (SEQ ID NO: 1) (N -(Doc) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) r- -(DOC) 4 -GIn-Trp-Ala-Va-fRAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(O)(lNrpAaVlil-HsPeNeN2(E DN:6 -(Doc) 4 -Gln-Trp-Ala-Vla-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc)-GDc2DeGn-Trp-Aa-isPh-Ie~-NH S-EQ ID NO: 1 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-VaIBAla-H is-Leu-Lie-N H 2 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAl-His-Leu-Le-N H 2 -Aepa-(DOC) 2 -D~he-Gln-Trp-Ala-VaI-G~ly-H is-Le-Nle-N H 2 -Aepa-(Doc) 2 -DAha-GIn-Trp-Aa-a4BAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -DG Gn-Trp-Aa-Aa-Hi3A-H-he-Ne H -Aepa-DPhe-Gln-Trp-Ala-Val-BlAla-H is-Leu-Le-N H 2 -Aepa-DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 -Aepa-DAla-Gln-Trp-Ala-VaI-IIla-His-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-BiAla-His-Leu-Leu-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-VaIBAla-H is-Leu-NIe-N H 2 -(DoC) 2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 -(Doc) 2 -DAla-Gln-Trp-Ala-Va-IlAla-H is-Phe-N Ie-NH 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Ala-BlAla-His-Phe-N le-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-VaIBAla-H is-Leu-Leu-N H 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Ila-H is-Leu-N Ie-N H 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 -(Doc) 2 -Aepa-DAla-Gln-Trp-Ala-ValIIAla-H is-Phe-Nle-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-NIe-N H 2 -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-Pila-His-Ala-Nle-N H 2 (SEQ ID NO: 7) 269 00 -Aepa-Gln-Trp-Ala-Va-aAla-His-Ala-Ne-NH 2 (SEQ ID NO: 7) C) -(DOC) 2 -Gln-Trp-Ala-Va-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-aAla-H is-Ala-Nle-N H 2 C0 -Aepa-DPhe-Gln-Trp-Ala-Va-3Ala-H is-Ala-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-ala-H is-Ala-N Ie-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-BiAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 4 -Aepa-Gln-Trp-Ala-Val-BIAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 4 -Gln-Trp-Ala-Val-RIAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-lAla-His-Ala-N Ie-N H 2 r- -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Val-VBAla-His-Ala-N Ie-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-BAla-His-Ala-Nle-N H 2 -(DOC) 2 -Aepa-Gln-Trp-Ala-Va-aAla-His-Ala-N Ie-N H 2 (SEQ ID NO: 7) -(DoC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-aAla-H is-Ala-N le-N H 2 -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-IlAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(Doc) 3 -Gln-Trp-Ala-Val-BiAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 3 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DOC) 3 -Gln-Trp-Ala-Val-flAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 3 -GIn-Trp-Ala-Ala-IlAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-Val-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Val-BIAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gn-Trp-Ala-Va-IlAla-H is-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Doc-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 3 -GIn-Trp-Ala-ValIBAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 3 -Gln-Trp-Ala-VaI-aIla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 3 -Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 3 -Gln-Trp-Ala-Val-BlAIa-His-Phe-Nle-N H 2 (SEQ ID NO: 6) -(Doc) 3 -GIn-Trp-Ala-Ala-BiAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 1) -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Val-BiAla-H is-Leu-Leu-N H 2 -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-IIla-His-Leu-N Ie-N H 2 -(Doc) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 3 -DPhe-Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-VaIAla-H is-Leu-Nie-N H 2 -(DOC) 3 -DPhe-Gln-Irp-Ala-Va-Gly-H is-Leu-Leu-N H 2 270 00 -(Doc) 3 -DAla-Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-N H 2 -(Doc) 3 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N Ie-N H 2 -Doc-Gln-Trp-Ala-ValIBAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -DcGnTpAaVl0l-isLuNeN2(E o -Doc-Gln-Trp-Ala-VaI-BAl-His-Leu-NLe-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-G~ly-His-e-Nleu-NH 2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-Vla-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) INDGnTpAaAa-l~-i-h-~-N 2 (E DN:1 -Doc-Aepa-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) N -Doc-Aepa-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: r- -Doc-Aepa-Gin-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Doc-Aepa-Gln-Trp-Ala-VaI-BiAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Doc-Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) O OH 0 0 'OH N /0 H OH 01 NH, OH2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-IIAla-H is-Phe-N le-N H 2 -(DOC) 4 -DPhe-GIn-Trp-Ala-ValIBAla-H is-Leu-Leu-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 4 -DAla-Gln-Trp-Ala-Va-IIla-H is-Phe-Nle-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-IIla-H is-Phe-N le-N H 2 -(Doc) 4 -Aepa-Gln-Trp-Ala-Val-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 4 -Aepa-Gln-Trp-Ala-Ala-RAla-H is-Phe-N Ie-NH 2 (SEQ ID NO: 1) -(Doc) 4 -Gln-Trp-Ala-VaI-l Ala-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DoC) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(DOC) 4 -Gln-Trp-Ala-Va-B Ala-H is-Phe-N le-N H 2 (SEQ ID NO: 6) -(DOC) 4 -Gln-Trp-Ala-Ala-fIl~Aa-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 4 -GIn-Trp-Ala-VaI-Pila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) 271 00 -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Ap-Dc4Gn(r-N-a-ia-i-h-l-H2(E DN:6 -Aepa-(Doc) 4 -Gln-Trp-Ala-a-BAla-H is-Phe-Nle-N H 2 (SEQ ID NO: 6) o -p-(Doc) 4 p-GIn-Trp-Ala-AVal-I3Aa-His-eu-NLe-NH 2 (SEQ ID NO: 1) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-BAla-H is-Leu-le-N H 2 (SEQ ID NO: 4) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-BAl-His-Leu-Le-NH 2 (SEQ ID NO: IND)-eaGnTpA~-a-~-i-e-euN 2 (E DN:9 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-VaIBAla-H is-Leu-Leu-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Nle-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(Doc) 2 -DAla-GIn-Trp-Ala-Va-RAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -DPhe-GIn-Trp-Ala-Ala-fIla-H is-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-VaI-BllAa-His-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-N H 2 -Aepa-DAla-Gln-Trp-Ala-Val-GAla-H is-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-BAIa-His-Phe-N Ie-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-VaI-Rla-His-Leu-Leu-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-N Ie-NH 2 -(DOC) 2 -DPhe-GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 -(DOC) 2 -DAla-Gln-Trp-Ala-VaI-IIla-H is-Phe-Nle-N H 2 -(DoC) 2 -DPhe-Gin-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 -(Doc) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 2 -Aepa-DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-N Ie-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-IBAla-His-Phe-Nle-N H 2 -Aepa-(DoC) 2 -Gln-Trp-Ala-Va-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-VaI-RAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 2 -Gln-Trp-Ala-VaI-BiAla-H is-Ala-N Ie-N H 2 (SEQ ID NO: 7) -Aepa-(DoC) 2 -DPhe-GIn-Trp-Ala-VaI-RAla-H is-Ala-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Ala-N Ie-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-ValI-BAla-His-Ala-Nle-N H 2 -Aepa-(DOC) 4 -Gln-Trp-Ala-ValI-BAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) 272 00 -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-gAla-His-Ala-N Ie-N H 2 (SEQ ID NO: 7) -(DOC) 4 -Gln-Trp-Ala-Va-gAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-BiAla-H is-Ala-N Ie-N H 2 O a Dh0l- r l- a-I l- i- l- l- H 0 ~-(Doc) 4 -A-DPhe-Gn-Trp-Ala-Val-Aa-H is-Ala-Ne-N 2 -(Doc) 2 -Aepa-Gln-Trp-Ala-Va-RAla-His-Ala-N Ie-N H 2 (SEQ ID NO: 7) -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-BlAla-H is-Ala-Nle-N H 2 C -Aepa-(DOC) 3 -Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) (Ni -Aepa-(DOC) 3 -Gln-Trp-Ala-Va-Rla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -Aepa-(Doc) 3 -Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(DoC) 3 -Gln-Trp-Ala-Va-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 3 -Gln-Trp-Ala-Ala-Vila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-Va-BAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Va-IlAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Doc-Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Doc-Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 3 -GIn-Trp-Ala-Val-!IAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 3 -Gln-Trp-Ala-VaI-B Ala-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 3 -Gln-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DOC) 3 -Gln-Trp-Ala-VaI-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DOC) 3 -Gln-Trp-Ala-Ala-BIAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 3 -Aepa-DPhe-GIn-Trp-Ala-VaIBAla-H is-Leu-Leu-N H 2 -(DOC) 3 -Aepa-DPhe-Gln-rp-Ala-Va-la-His-Leu-Nle-NH 2 -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-VaI-RAla-H is-Leu-N Ie-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 -(DOC) 3 -DAla-Gln-Trp-Ala-Va-Ila-H is-Phe-N Ie-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N H 2 -Doc-Gln-Trp-Ala-ValIBAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-Gln-Trp-Ala-VaI-Ila-His-Leu-Nle-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH2 (SEQ ID NO: 9) -Doc-Gln-Trp-Ala-ValIfla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) 273 00 -Doc-Gln-Trp-Ala-Ala-BiAla-His-Phe-Nle-NH2 (SEQ ID NO: 1) -DcAp-0-r-~-a-AaHsLuLuN 2 (E DN:4 0 -Doc-Aepa-Gln-Trp-Ala-Va-Rla-His-Leu-NLe-NH 2 (SEQ ID NO: N 0 -Doc-Aepa-Gln-Trp-Ala-Va-G~ly-His-Leu-Le-NH 2 (SEQ ID NO: 9) -Doc-Aepa-Gln-Trp-Ala-VaI-ly-His-Pe-Ne-NH 2 (SEQ ID NO: -Doc-Aepa-Gln-Trp-Ala-AVal-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa -N H >Leu-Arg-Pro-Gly-NH 2 pGlu-His-Trp-Ser-Tyr-N 0 H c-I -Aepa-(Doc) 2 -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa -N H pGlu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-N H Et H 0 -(DoC) 2 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-N H Et H 0 -Aepa-(Doc) 2 N H pGlu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -Aepa -N H pGlu-His-Trp-Ser-Tyr N ,Leu-Arg-Pro-GlyNH 2 H 0 274 00 -(Doc) 2 -Aepa N H 2pGiu-His-Trp-Ser-Tyr N re-r-r-l-H H 0 -(Doc) 3 -Aepa-N H pGlu-His-Trp-Ser-Tyr N ,Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N ,Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -Aepa-(Doc) 2 N H pGl u-H is-Trp-Se r-Tyr N Leu-Arg-Pro-G ly-N H 2 H 0 -Aepa-(Doc) 3 N H pGlu-His-Trp-Ser-Tyr N -TLeu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 N H pG Iu-H is-Trp-Se r-Tyr N Le u-Arg-Pro-Gly- NH 2 H 0 275 H SLeu-Arg-Pro-Gly-N H, pGlu-His-Trp-Ser-Tyr-N o -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa N H pGlu-His-Trp-Ser-Tyr N -)Leu-Arg-Pro-NHEt H 0 -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-N HEt H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-N H 2 H 0 -Aepa N H pGlu-His-Trp-Ser-His -N ITrp-Tyr-Pro-Gly-NH 2 H 0 -(DoC) 2 -Aepa N H pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H 0 276 00 -Aepa-(DoC) 2 -N H opGlu-His-Trp-Ser-His N -'-Trp-Tyr-Pro-Gly-NH 2 o H 0 2 -Aepa -N H pGlu-His-Trp-Ser-Tyr N LeAr-oGyNH -(Doc) 2 -Aepa- N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 H 0 -(DoC) 3 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -(Doc) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -Aepa-Doc -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2 -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 0 -Aepa-(Doc) 3 14N- pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 277 00 -Aepa-(DoC) 4 -N __pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 -Aepa -N H pGlu-His-Trp-Ser-His -N Trp-Tyr-Pro-Gly-NH 2 H 0 -(Doc) 2 -Aepa N H pGlu-His-Trp-Ser-His N _'-Trp-Tyr-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-His N -_)Trp-Tyr-Pro-Gly-NH 2 H 0 -Doc -N H pGlu-His-Trp-Ser-Tyr N -_-Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 Hl 0 2 278 00 -N H opGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 o H 0 -(Doc) 4 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 Cl -Doc-N H C1 pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 2 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 3 -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc)4 N pGlu-His-Trp-Ser-Tyr N Le-rPoGy-H H 0 H -Aepa -N pGlu- H is-Trp-Se r-Tyr N TLe u-Arg-Pro-G ly-NH 2 H 0 H -(Doc) 2 -Aepa -N pGlu-His-Trp-Sear-Tyr -N Leu-Arg-Pro Gly NH 2 HO0 -279- 00 H 00 -(Doc) 3 -Aepa -N O nGlu-His-Trn-Ser-Tyr N--Leu-Arg-Pro-Gly-NH 2 o H 0 H -(Doc) 4 -Aepa -N pGlu-His-Trp-Ser-Tyr N--Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-Doc-N pGlu-His-Trp-Ser-Tyr -Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 2 -N pGlu-His-Trp-Ser-Tyr N--Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 3 -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 4 N pGlu-His-Trp-Ser-Tyr N--Leu-Arg-Pro-Gly-NH 2 H 0 H -Doc N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-G Iy-NH 2 HO0 280 H 00 -(Doc) 2 -N pGlu-His-Trp-Ser-Tyr N _-Leu-Arg-Pro-Gly-NH 2 H pGlu-His-Trp-Ser-Tyr N _'~Leu-Arg-Pro-Gly-N H 2 H 0 H -(oC4 pGlu-His-Trp-Ser-Tyr N--Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-lAla-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Aepa-(DOC) 4 -DAla-Gln-Trp-Ala-Val-RAla-H is-Phe-N Ie-N H 2 -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BIAla-His-Phe-Nle-NH 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Rla-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DPhe-GIn-Trp-Ala-Va-RAla-H is-Leu-N Ie-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 4 -Aepa-DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-N Ie-N H 2 -(Doc) H SDG I FTDSYS RYRKQ MAVKKYLAAVL(RAla) KRYKQ RVKN K-N H 2 (SEQ ID NO: 23) -(Doc) H SDGI FTDSYS RYRKQ MAVKKYLAAVL(Ava) KRYKQ RVKN K-N H 2 (SEQ ID NO: 22) -(Doc) H SDGI FTDSYS RYR KQ MAVKKYLAAVLG KRYKQ R(A 6 c) KN K-N H 2 (SEQ ID NO: 21) -(Doc) HSDGI FTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQ RVKN K-N H 2 (SEQ ID NO: -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(RAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) 281 -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 c)KNK-NH 2 (SEQ ID NO: 21) -(Aepa)HSDG IFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQ RVKN K-NH 2 (SEQ ID NO: -(DOC) 6 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DoC) 4 DPh e-cyclo(C ys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-NH 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 O OH 0 0 0 N 'OH N /0 0 OHO0 0 OH 2 -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-Va-BiAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-aAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-BiAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(Doc) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-Gly-H is-Leu--f (CH 2 N H)-Leu-N H 2 (SEQ ID NO: 13) -(DOC) 4 -Gaba-Gln-Trp-Ala-Val-Gly-His-Leu-'f (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gln-Trp-Ala-Va-Gly-His-Leu-TP (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) _(DOC) 4 -Aepa-Gln-Trp-Ala-Va-Gly-His-Leu-Tf (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) 282 00 -(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-'P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -Doc- N H 00 -(DoC) 2 N H pGlu-His-Trp-Ser-Tyr N Le-rPrGyNH -(Doc) 3 N H A pG Iu-H is-T rp-Ser-Tyr N Leu-Arg- Pro-G ly- NH 2 H 0 -(Doc) 4 -N H pGlu-His-Trp-Ser-Tyr N Le-rPoGyNH H 0 -Doc-N H pGlu-His-Trp-Ser-Tyr N ,Leu-Arg-Pro-Gly-NH 2 H 0 D o C 2 pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 N4 pGlu-His-Trp-Ser-Tyr -N .,Leu-Arg-Pro-Gly-NH 2 H 0 283 00 -(DoC)-N H H 0 H -Aepa -N pG lu-H is-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 0 c-i H -(DoC) 2 -Aepa-N pGlu-His-Trp-Ser-Tyr-NNf -Leu-Arg-Pro-Gly-NH 2 HO0 H -(Doc) 3 -Aepa-N pGlu-His-Trp-Ser-Tyr -N N- Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 4 -Aepa-N pGlu-His-Trp-Ser-Tyr N -,NrLeu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-Doc -N pGlu-His-Trp-Ser-Tyr N- ,Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) N N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -284- 00 H -Aepa-(Doc) 3 -N o oGlu-His-Trp-Ser-Tvr N Leu-Arg-Pro-Gly-N H 2 o H 0 H -Aepa-(DOC) 4 -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 Ho C-0 H -Doc -N ni pGlu-His-Trp-Ser-Tyr Ni> Leu-Arg-Pro-Gly-NH 2 HH -(DoC) 2 -N pGlu-His-Trp-Ser-Tyr N- Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 3 -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-GIy-NH 2 H 0 H pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-N Ie-N H 2 (SEQ ID NO: 12) -(DOC) 4 -Gaba-Gln-Trp-Ala-Va-IIla-H is-Leu-NIe-N H 2 (SEQ ID NO: 12) 285 -Aepa- N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -(DoC) 2 -Aepa -N H pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(Doc) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N--TLeu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc -N H pGlu-His-Trp-Ser-Tyr -N----Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DOC) 2 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 3 -N H pGlu-His-Trp-Ser-Tyr N---Leu-Arg-Pro-Gly-NH 2 H 0 286 00 -Aepa-(Doc) 4 -N H O nGlu-His-Trn-Ser-Tvr N Leu-Arg-Pro-Gly-NH 2 o H 0 -Aepa-N H />-Leu-Arg-Pro-Gly-NH 2 pGlu-His-Trp-Ser-Tyr -N0 c-i H 0 -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -(Doc) 2 -Aepa N H pGlu-His-Trp-Ser-Tyr N--Leu-Arg-Pro-NHEt H 0 -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-N HEt H 0 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 287 00 -(DOC) 2 -Aepa -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H0 -(Doc) 3 -Aepa -N H ~zJ-pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H -(DoC) 4 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-Doc -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 2 -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH2 H 0 -Aepa-(Doc) 3 -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DoC) 4 N pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H 0 288 00 -Aepa- N H o pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH, o) H 0 M -(DoC) 2 -Aepa- N H pGlu-His-Trp-Ser-His N Tr-rPoGyNH -Aepa-(DoC) 2 N H pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-N H 2 H 0 -DcD~ecyl(Cs3 ~rD~pLy-aICs)T rNH -(Doc)-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 (DoC)2- D Phe-cyclo(C ys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(Doc)3- DP he-cycl o(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC)4-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(Doc)5-DPhe-cyclo(Cys-3ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC-A-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc)-Aepa- D Phe-cyclo (C ys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -(DOC)2-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(DOC)3-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC)5-Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(D6Aepa-DPhe-cyclo(Cys-3 Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 0 OH 289 00 -Ae pa- Doc- D Phe-cyclo (C ys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Aepa -(DOC) 2 DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Aepa-(DOC) 3 -D Ph e-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 o-Aep a-(DOC) 4 D Phe-cycl o(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 -Doc-Aep a- D Phe-cycl o(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC) 3 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC) 5 -Aep a- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 6 -Aepa- DPh e-cyc lo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-NH 2 -Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-NH 2 -(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc) 3 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 4 D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 5 D Phe-cyclo(C ys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 D Phe-cyclo(C ys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -Ae pa- DP he-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -Doc-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 2 -Ae pa-C aeg -cyclo(DCys-3 Pa I- DTrp- Lys- D Cys)-Th r(Bz)-Ty r- N H 2 -(DOC) 3 -Ae pa-C aeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 OC) 4 -Ae pa-C aeg-cyc lo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Ty r- N H 2 -(DOC) 5 -Aepa-C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(Doc) 6 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Ae pa) 2 -C aeg-cyclo (D Cys-3 Pa I-DTrp- Lys- D Cys)-Th r(BzI) -Tyr- N H 2 -Doc-Caeg-cyclo(D Cys-3 Pa I -DTrp- Lys- D Cys)-Th r(BzI)-Tyr- N H 2 -(Doc) 2 -C aeg -cycl o(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(DOC) 3 -C aeg -cyclo(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(BzI) -Tyr- N H 2 (Doc) 4 -C aeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 290 00 5 -C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys-D Cys)-T hr(Bz)-Tyr- N H 2 -(DOC) 6 -Caeg-cycl o(D Cys- 3Pa I-DT rp-Lys- DCys)-Th r(Bz) -Ty r- N H 2 Doc- Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 D02 y-Dyr 0 -yl(y-y-Dr-y-bu-y)T -NH o-(DOC)3- Lys- DTy r- DTyr-cyc lo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc)4-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 5-Lys- DTy r- DTy r-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 IND)-y-~r-~rccoCs-y-~pLsAb-y)TrNH Doc) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 -(Doc)r 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa- Lys- DTyr- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa- Lys- DTyr- DTy r-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Doc) 4 -Aepa-Gaba N H pGiu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -Gaba -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 -Gaba N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 291 H -(Doc) 4 -Aepa-Gaba -N pGlu-His-Trp-Ser-Tyr -N N/--rLeu-ArgPo-Gly H 2 HO0 H -Aepa-(Doc) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr -N /-,LeuArgProGlyNH 2 HO0 H -(DOC) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr 'W Leu-Arg-Pro-Gy-N H 2 HO0 O OH 0 0 l'OH- N l 00 H 0 H0 /0 0 OHO0 01 F NH, OH 2 -(DOC) 6 Lys- DTy r-DTyr-cyc lo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Lys- DTyr- DTy r-cycl o(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Ih r- N H 2 -Aepa- Lys- DTy r- DTy r-cyclo (C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa -Lys- DTyr- DTy r-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -(DOC) 4 -Aep a- Lys- DTy r- DTyr-cycl o(C ys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -Ae pa- Lys- DTyr- DTy r-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 292 00 ~-(DoC) 2 -Aepa- DPh e-cycl o(Cys-3 I Tyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -(DOC) 2 -Aepa-DPhe-cyclo(Cys-3 I Tyr- DTrp- Lys-VaI-Cys)-Th r-N H 2 Doc) 2 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 o -(Doc) 4 -Aepa-Caeg-cyclo( DCys-3 PaI-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Aepa- Lys- DTyr- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-T hr- N H 2 -(DOC) 4 -Aepa- Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- NH 2 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(Doc) 2 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 4 -Ae pa-C aeg -cyclo(DCys-3 Pa I-DTrp- Lys- D Cys)-T h r(BzI)-Tyr- N H 2 -Doc-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 3 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 5 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 6 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -Aepa) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 5 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Doc-Ae pa -Lys- DTyr- DTyr-cyclo(Cys-Ty r- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 2 -Ae pa- Lys- DTyr- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 3 -Aep a- Lys- DTy r- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 4 -Ae pa- Lys- DTy r- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 5 -Aepa- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 6 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Aep a) 2 Lys- DTyr- DTyr-cyclo (Cys-Ty r- DTrp- Lys-Ab u-Cys)-Th r- N H 2 Doc- Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 2 Lys- DTy r-DTyr-cyclo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 293 00 3 Lys- DTyr- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 4 Lys- DTyr-DTyr-cyc lo(Cys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- NH 2 5 Lys- DTyr- DTy r-cycl o(C ys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(O)-y-0rDy-yl(y-y-~pLsAuCs-h-H o Doc- Lys- DTyr-DTyr-cyclo (Cys-Tyr-Drp- Lys-Ab u-Cys)-Thr- N H 2 -Ae pa-(DOC-Lys- DTyr- DTyr-cycl o(Cys-Tyr-DTrp-Lys-Ab u-Cys)-Th r-N H 2 -Ae pa-(DOC) 3-Lys- DTy r- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ap-Dc 3 LsDy-Dy-yl(y-y-Np-y-b-y)TrNH -Aep a-(Doc) 4 Lys- D~yr- D~yr-cyc lo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Ih r-N H 2 ci-Aepa- Doc- DP he-cyclo (C ys-Tyr-DTrp- Lys-Abu -Cys) -Th r- N H 2 -Ap-DC2Dh-ycoCsTrDr-ysAuCs-h-H -Aepa-(Doc)3-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC)4-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ap-(Doc)-D-cyclo(Cys-Tyrl-DTrp-Lys-AuCys)-h()-Tr-N H 2 -(DOC)4-C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys-D Cys)-Th r(Bz) -Tyr- N H 2 (DC) 4 -a-cyclo(DCys -3~PaILy- Dr-ys-DTys)-Tr()-Ty-Ty- H 2 2 -eCaeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -()-Aepa-C aeg-cyclo(DCys-3P -ys-ys-Thr(Bz)-T r- y H 2 H -(Doc) 4 -Aepa-Caeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(o)eaCaeg-cyco( P -D~y-3P LysDys -Dys)-Tr)-T-Tyr- HH 2 Caeg-cyclo(D-cys-3PaD p-Lya- Drys-Thr(Bz)-Iyr(z Tr-N 2 H D-Ae pa-Caeg-cycIo (DCys-3 P aI-DTrp- L ys-Thr(B)-TB Tyr- N H 2 -DoC-Aepa-C aeg-cyclo(DC ys-3 P aI-DTrp- Lys)-Th r(Bz I)-Tyr- N H 2 -(DoC) 2 -Aepa-Caeg-cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(DOC)4-Aepa-C aeg -cyclo (D Cys-3 Pa I-DTrp- Lys- D Cys)-Th r(Bz)-Tyr- N H 2 -(Doc) 5-Ae pa-C aeg-cyclo(DCys-3 Pa I-Drp- Lys- DCys)-Th r(BzI)-Ty r- N H 2 -(Doc) 5 -Aep a-C aeg-cycl o(DC ys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(Do)e-C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Tyr- N H 2 -(Apa-Caeg-cyclo( DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -DOC-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC)3-C aeg-cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(BzI)-Iyr- N H 2 -(DOC)4-C aeg -cyc lo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys) -Th r(Bz)-Tyr- N H 2 -(Doc)r 5 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(e-Doc-Caeg-cyc lo(D Cys- 3PaI-DTrp- Lys- DCys)-Thr(Bz)-Tyr- N H 2 294 00 -Aep a-(Doc) 2 -C aeg-cyclo (DC ys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Aepa-(Doc) 3 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Aep a-(DOC) 4 -Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -Ap-Ls 0r ~rccoCsTr-Dr-LsA Cs-hr o -Aepa-y Tyr-Dyc o(Cys-Tyr- p-Ly-buysbuy)-Th H -N 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 2 -Aepa- DP he-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- NH 2 -(DOC) 2 -Aep a-Caeg -cyclo (D Cys- 3Pa I-DTrp- Lys- DC ys)-T h r(BzI)-Tyr- N H 2 (Ni -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-VaIAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-aAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Aepa-Gaba N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 -Gaba N H pGlu-His-Trp-Ser-Tyr N Le-rPrGyNH H 0 -(Doc) 4 -Gaba -N H pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 4 -Aepa-Gaba -N pGlu-His-Tr-Ser-Tyr Leu-Arg-Pro-Gly-N H 2 HO0 H -Aepa-(Doc) 4 -Gaba -N pGlu-His-Trp-Ser-Tyr N'ThF Leu-Arg-Pro-Gly-NH 2 HO0 295 00 H -(Doc) 4 -Gaba N pGlu-His-Trp-Ser-Tyr -N -rLeu-Arg-Pro-Gly-NH 2 -(o)HDVFDYTLKQNe)VKYNIH-H (SQ0 O 9 -(Doc) H SDAVFTD NYTRLRKQM( AVKKYLN S ILN-NH 2 (SEQ ID NO: 1) -(Doc)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Doc) HSDAVFTDNYTRLRKQMAVKKLLN S ILN-N H 2 (SEQ ID NO: -(o)HSDVT YRLK AKLNSIL-NH SQI O -(Aepa)HSDAVFTDNYTRLRKQ(Nle)AVKKYLNSILN-NH 2 (SEQ ID NO: 19) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) c-I -(Aepa)HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Aepa)HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -Aepa-(Doc) 2 -Gln-Trp-Ala-Va-fiAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 H Glp-His-Trp-Ser-His -N Tr-yPoGlNH H0 -(DOC) 2 -Aepa-C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- D Cys)-Th r(BzI)-Tyr- N H 2 O 0 OH Q H 0 0 NH HO 0 0 0 0 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-gAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gaba-Gin-Trp-Ala-Va-Ila-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -296- 00 -(Doc) 4 -Aepa-Gaba- N H o pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 o H 0 -Aepa-(DoC) 4 -Gaba -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H -(Doc) 4 -Gaba N H pGlu-His-Trp-Ser-Tyr N -Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 -Aepa-Gaba N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 3 -Gaba N H pGlu-His-Trp-Ser-Tyr- N -rLeu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 -Gaba -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 H -(Doc) 4 -Aepa-Gaba -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 HO0 297 00 H -Aepa-(DoC) 4 -Gaba -N Q pGlu-His-Trp-Ser-Tyr. Leu-Arg-Pro-Gly-N H, H -(DoC) 4 -Gaba-N pGlu-His-Trp-Ser-Tyr e-r-r-~-H -(DOC) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(Doc) 2 N H Glp-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H 0 -Aepa-(DoC) 2 -Gln-Trp-Ala-Va.-RAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-(Doc) 2 -GIn-Trp-Ala-VaI-ViAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-VaI-RAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-.Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Aepa) 2 -(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -(Aepa) 2 -(DOC) 2 -Gln-Trp-Ala-Va-RAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -Doc- D Phe-G In-Trp-Ala-Va I- Rla-H is-Leu-Leu-N H 2 -Doc-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Nle-NH 2 -Doc-DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 -Doc-DAla-Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-N H 2 -Doc-DPhe-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-VaIRAla-His-Leu-Nle-N H 2 -Doc-Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -Doc-Aepa-DAla-Gln-Trp-Ala-VaI-IlAIa-His-Phe-N Ie-N H 2 -Doc-Aepa-DPhe-Gln-rp-Aa-Ala- Ala-H is-Phe-N le-N H 2 298 00 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Va-Ila-H is-Leu-N Ie-N H 2 -Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 o -Aepa-(DOC) 3 -DAla-Gin-Trp-Ala-Va-BAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 3 -DPhe-Gln-Trp-Ala-Ala-IlAla-H is-Phe-Nle-N H 2 -(DOC) 3 -Aepa-Gln-Trp-Ala-Val-la-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -(DOC) 3 -Aepa-Gln-Trp-Ala-Va-BAla-H is-Leu-Nle-N H 2 (SEQ ID NO: -(DOC) 3 -Aepa-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) (Ni -(Doc) 3 -Aepa-Gln-Trp-Ala-VaI-BAla-His-Phe-NIe-NH 2 (SEQ ID NO: 6) r- -(Doc) 3 -Aepa-Gin-Trp-Ala-Ala-ViAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Va-BAla-H is-Leu-NIe-N H 2 -Aepa-Doc-DPhe-GIn-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-Doc-DAla-Gln-Trp-Ala-Va-BAla-H is-Phe-Nle-N H 2 -Aepa-Doc-DPhe-Gln-Trp-Ala-Ala-la-H is-Phe-N Ie-N H 2 -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-VaIIAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-aAla-His-Leu-Leu-NH 2 (SEQ ID NO: 14) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-T (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -(DOC) 4 -Gaba-Gln-Trp-Ala-VaI-Gly-His-Leu-'P (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 13) -Aepa-(DOC) 4 -Gaba-Gln-Trp-Ala-Va-RAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gaba-GIn-Trp-Ala-Va-IlAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(Doc) 4 -Gaba-Gln-Trp-Ala-Va-IlAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Aepa-(Doc) 4 -Gln-Trp-Ala-Va-Gly-His-Leu-T~ (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) -(DOC) 4 -Aepa-Gln-Trp-Ala-Va-Gly-His-Leu-T~ (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) _(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Y (CH 2 NH)-Leu-NH 2 (SEQ ID NO: 2) 299 00 F N 0 0 0 N 0 -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-RAla-His-Leu-Leu-NH 2 (SEQ ID NO. 4) -Aepa -N H G Ip- H is-T rp- S er-Ty r N Le u-A rg -Pro- G y- NH 2 H 0 K-0 HO /N- 0 -(Doc) 4 -Aepa-Gaba-Gln-Trp-Ala-VaIIAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-GIn-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Val-RAla-H is-Leu-N Ie-N H 2 0 -(DOC) 4 -Aepa-Gaba-Gln-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-Gln-Irp-Ala-Va-BAla-H is-Leu-Nle-N H 2 (SEQ ID NO: -(Doc) 4 -Gaba-Gln-Trp-Ala-Va-BiAla-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-N H 2 300 00 "0 N H HO 0 0 0 IND 0 -Suc-(DoC) 3 -Aepa-Gaba-Gln-Trp-Ala-Va-Rla-H is-Leu-N Ie-N H 2 (S EQ ID NO: 12) -Suc-Aepa-(DOC) 3 -Gaba-Gn-Trp-Aa-Va-f&Ala-His-Leu-Nle-NH 2 (SEQ ID NO: 12) -Suc-Aepa-(DOC) 3 -Gln-Trp-Ala-Va-BAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -Suc-(DOC) 3 -Aepa-Gln-Trp-Ala-VaI-FiAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Suc-(DOC) 3 -Gln-Trp-Ala-VaI-fBAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Suc-Aepa-(DOC) 3 -DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-NIe-N H 2 -Suc-(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-N Ie-N H 2 Suc-Aepa-(Doc) 3 -NH pGlu-His-Trp-Ser-Tyr -N11, Leu-Arg-Pro-Gly-N H 2 HO0 Suc-Aepa-(DoC) 5 -NH pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 HO0 Suc-(Doc) 3 -Aepa 'NH pGlu-His-Trp-Ser-Tyr-Ni Leu-Arg-Pro-Gly-NH 2 HO0 301 00 Suc-(DoC) 5 -Aepa NH pGlu-His-Trp-Ser-Tyr 'N -7H 0 oS~ 1 O0 N O HO 07 0 0 "r 0 -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-l Ala-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(DOC) 2 -Gln-Trp-Ala-Va-IlAla-H is-Leu-Nle-N H 2 (SEQ ID NO: -Aepa-(DOC) 2 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 2 -Gln-Trp-Ala-VaI-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-(DOC) 2 -Gln-Trp-Ala-Ala-fiAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Aepa-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-Gin-Trp-Ala-ValIfla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Aepa-Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 2 -Gin-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(Doc) 2 -Gln-Trp-Ala-VaIaAla-His-Leu-NIe-NH 2 (SEQ ID NO: -(Doc) 2 -Gln-Trp-Ala-VaI-Gly-H is-Leu-Leu-N H 2 (SEQ ID NO: 9) -(DOC) 2 -Gln-Trp-Ala-VaI-PBAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 2 -Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-ValI-BAla-His-Leu-Leu-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-N Ie-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-VaI-BAla-His-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-IIla-H is-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Leu-Nle-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-H is-Phe-N Ie-N H 2 302 00 -(Aepa) 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-fla-H is-Leu-Leu-N H 2 -(Aepa) 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-IlAla-H is-Leu-N Ie-N H 2 -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-BAla-His-Leu-Leu-N H 2 -A p -D C4Dh0l-r-l-a-i l-i-e -l-H o -Aepa-(Doc) 4 -DPhe-Gln-Trp-Ala-Va-BAl-His-Leu-N e-N H 2 -Aepa-(DOC) 4 -D~he-GIn-Trp-Ala-VaI-G~ly-His-Le-NLe-N H 2 -Aepa-(Doc) 4 -DAha-Gln-Trp-Ala-a-Ala-H is-Phe-N Ie-N H 2 IND-Dc 4 Dh-GnTpAaAaB~aHsPeNeNH -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-BlAla-His-Leu-Leu-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-3Ala-His-Leu-Nle-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DoC) 4 -Aepa-DAla-Gln-Trp-Ala-ValI-BAla-H is-Phe-NIe-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-ViAla-H is-Phe-Nle-N H 2 -(DOC) 4 -Aepa-DPhe-Gln-Trp-Ala-Ala-RAla-H is-Phe-N Ie-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-ValI-rAla-His-Leu-Leu-NH 2 -(Doc) 4 -DPhe-Gln-Trp-Ala-Va-aAla-His-Leu-Nle-NH 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 4 -DAla-Gln-Trp-Ala-ValIBAla-His-Phe-Nle-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-ala-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Aepa-(DOC) 4 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-N H 2 (SEQ ID NO: 9) -Aepa-(Doc) 4 -Gln-Trp-Ala-VaIfAla-H is-Phe-N Ie-N H 2 (SEQ ID NO: 6) -Aepa-(DOC) 4 -Gln-Trp-Ala-Ala-aAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DoC) 4 -Aepa-GIn-Trp-Ala-VaI-BAla-His-Leu-Leu-N H 2 (SEQ ID NO: 4) -(Doc) 4 -Aepa-Gln-Trp-Ala-ValI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DOC) 4 -Aepa-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 4 -Aepa-Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DoC) 4 -Aepa-Gln-Trp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DoC) 4 -Gln-Trp-Ala-VaI-Ila-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -(DOC) 4 -GIn-Trp-Ala-Va-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -(DoC) 4 -Gln-Irp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 4 -Gln-Trp-Ala-VaI-lAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(DoC) 4 -Gln-Trp-Ala-Ala-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-RiAla-His-Leu-Leu-N H 2 303 00 -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Val-IlAia-H is-Leu-N Ie-N H 2 -Aepa-(Doc) 2 -DPhe-Gln-Trp-Ala-Va-Gly-His-Leu-Leu-NH 2 -Aepa-(DOC) 2 -DAla-Gln-Trp-Ala-Va-Ila-H is-Phe-N Ie-N H 2 o -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-Ala-BIAla-H is-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Va-PBAla-His-Leu-Leu-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Val-BIAla-H is-Leu-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-N H 2 -Aepa-DAla-GIn-Trp-Ala-VaI-llAla-His-Phe-N Ie-N H 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-flAla-His-Phe-N Ie-N H 2 -(Doc) 2 -DPhe-Gln-Trp-Ala-Val-IlAla-H is-Leu-Leu-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Val-BIAla-H is-Leu-N Ie-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 -(Doc) 2 -DAla-Gln-Trp-Ala-VaI-IlAla-His-Phe-N Ie-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Ala-fIla-H is-Phe-N le-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Val-IlAla-His-Leu-N Ie-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(DOC) 2 -Aepa-DAla-Gln-Trp-Ala-VaI-RllAa-His-Phe-N Ie-N H 2 -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Ala-lAla-H is-Phe-N Ie-N H 2 -Aepa-(Doc) 2 -Gln-Trp-Ala-ValI-RAla-H is-Ala-N Ie-N H 2 (SEQ ID NO: 7) -Aepa-Gln-Trp-Ala-Va-BAla-His-Ala-N Ie-N H 2 (SEQ ID NO: 7) -(DOC) 2 -Gln-Trp-Ala-VaI-BAla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -Aepa-(DOC) 2 -DPhe-Gln-Trp-Ala-ValI-RAla-H is-Ala-Nle-N H 2 -Aepa-DPhe-Gn-Trp-Ala-Val-VBAla-H is-Ala-Nle-N H 2 -(DOC) 2 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-Nle-N H 2 -Aepa-(Doc) 4 -Gln-Trp-Ala-VaIAla-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DoC) 4 -Aepa-Gln-Trp-Ala-Va-RlAla-His-Ala-Nle-NH 2 (SEQ ID NO: 7) -(DOC) 4 -Gln-Trp-Ala-Val-BAla-His-Ala-Nie-NH 2 (SEQ ID NO: 7) -Aepa-(DOC) 4 -DPhe-Gln-Trp-Ala-Va-aAla-H is-Ala-Nle-N H 2 -(Doc) 4 -Aepa-DPhe-Gln-Trp-Ala-VaIBAla-His-Ala-N le-N H 2 -(DOC) 4 -DPhe-Gln-Trp-Ala-Va-BAla-H is-Ala-Nle-N H 2 -(Doc) 2 -Aepa-Gln-Trp-Ala-Val-allAa-H is-Ala-Nle-N H 2 (SEQ ID NO: 7) -(DOC) 2 -Aepa-DPhe-Gln-Trp-Ala-Val-IIAla-His-Ala-N Ie-N H 2 -Aepa-(DOC) 3 -Gln-Trp-Ala-Va-RAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) 304 00 -Aepa-(Doc) 3 -Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: C) -Aepa-(DOC) 3 -Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Aepa-(Doc) 3 -Gln-Trp-Ala-Va-fgAla-His-Phe-Nle-NH 2 (SEQ ID NO: 6) 0 -Aepa-(DOC) 3 -Gln-Trp-Ala-Ala-r Ala-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa-Doc-Gln-Trp-Ala-ValI-BAla-H is-Leu-Leu-N H 2 (SEQ ID NO: 4) -Aepa-Doc-Gln-Trp-Ala-Va-BiAla-H is-Leu-N Ie-N H 2 (SEQ ID NO: -Aepa-Doc-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) IND-o-~-r-~aVI~~-i-h-~eN 2 (E DN:6 (Ni -Aepa-Doc-Gln-Trp-Ala-AVa-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(eDoc-Gln-Trp-Ala-la-BAa-His-e-e-NH 2 (SEQ ID NO: -(Doc) 3 -Gln-Trp-Ala-VaI-aiAla-His-Leu-Le-NH 2 (SEQ ID NO: C)-DC3GnTr(lNai~a-i-e-l-H2(E -(DOC) 3 -GIn-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -(Doc) 3 -Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -(Doc) 3 -Gln-Trp-Ala-Ala-RAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-RAla-His-Leu-Leu-N H 2 -(DOC) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-ila-H is-Leu-Nle-N H 2 -(DoC) 3 -Aepa-DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 3 -DPhe-Gln-Trp-Ala-VaI4Ala-H is-Leu-Leu-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Va-Rla-His-Leu-N Ie-NH 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Va-Gly-H is-Leu-Leu-N H 2 -(Doc) 3 DAla-Gln-Trp-Ala-VaIIAla-H is.-Phe-N Ie-N H 2 -(DOC) 3 -DPhe-Gln-Trp-Ala-Ala-BAla-H is-Phe-N le-N H 2 -Doc-Gln-Trp-Ala-VaI-BAla-His-Leu-Leu-NH 2 (SEQ ID NO: 4) -Doc-Gln-Trp-Ala-VaI-BAla-His-Leu-Nle-NH 2 (SEQ ID NO: -Doc-Gln-Trp-Ala-VaI-Gly-His-Leu-Leu-NH 2 (SEQ ID NO: 9) -Doc-.Gln-Trp-Ala-VaI-Ila-His-Phe-Nle-NH 2 (SEQ ID NO: 6) -Doc-Gln-Irp-Ala-Ala-BAla-His-Phe-Nle-NH 2 (SEQ ID NO: 1) -Aepa -NH pGlu-His-Trp-Ser-Tyr N _)_Leu-Arg-Pro-Gly-NH 2 H 0 305 00 -(Doc) 2 Aepa -N H o ~~pGlu-His-Trp-Ser-Tyr N LuAgPoG- o H 0 -(DoC) 3 -Aepa- N H pGlu-His-Trp-Ser-Tyr N LuAgPoGyNH -(Doc) 4 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(DoC) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 Hl 0 -Aepa-(DoC) 3 N H pG Iu- His-Trp- Ser-Tyr N Leu-Arg -Pro-G ly-N H 2 H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -AepaH pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 306 00 -(DoC) 2 -Aepa -N H pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 3 -Aepa -N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -(DoC) 4 -Aepa-N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H CIH 02 -Aepa-(DoC)2 N pGl u- His-Trp-Ser-Ty r N ~-Leu-Arg -P ro-G ly- NH 2 H -Aepa-(Doc) 3 -N H p GI u- His-Trp-Ser-Ty r N Leu-Arg- Pro-G ly-N H 2 H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-Tyr -N Le-rPoGyNH H 0 -Doc NH pGlu-His-Trp-Ser-Tyr Le-rPoGyNH -(Doc) 2 N H pGlu-His-Trp-Ser-Tyr NLeu-Arg-Pro-Gly-NH 2 H 0 307 00 -(DOC) 3 -N H 2 pGlu-His-Trp-Ser-Tyr N H 0 -(DOC) 4 -N H pGlu-His-Trp-Ser-Tyr N Le-rPoGyNH H o)~uAgPr-l-H -(Doc) 2 -N H pGlu-His-Trp-Ser-Tyr N FLeu-Arg-Pro-Gly-N H 2 H 0 -(Doc)3 N pG lu-His-Trp-Ser-Tyr N Le-rPoGy-H H 0 -(Doc) 4 N H pGlu-His-Trp-Ser-Tyr N -)-Leu-Arg-Pro-Gly-N H 2 H 0 H -Aepa N pGlu-His-Trp-Ser-Tyr -W N Leu-Arg-Pro-Gly-NH 2 H 0 2 H -(Doc) 2 -Aepa-N pGlu-His-Trp-Ser-Tyr N 'Leu-Arg-Pro-Gly-NH 2 HO0 308 00 -(Doc) 3 -Aepa H] c--N o pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH, H 0 H -(Doc) 4 -Aepa N pGlu-His-Trp-Ser-Tyr N--Leu-Arg-Pro-Gly-NH, H 0 C-0 H -Aepa-(DOC) 2 -N pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 H -Aepa-(Doc) 3 -N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gy-NH, H 0 H -Aepa-(Doc) 4 N pGlu-His-Trp-Ser-Tyr )Leu-Arg-Pro-Gly-NH 2 H 0 H -Doc-N pGlu-His-Trp-Ser-Tyr -N /-Leu-Arg-Pro-Gly-NH 2 HO0 H J pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH 2 H 0 309 00 H -(Doc) 3 -N pGiu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H 2 H -(Doc) 4 -N pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -HSDGIFTDSYSRYRKQMAVKKYLAAVL(aAla)KRYKQRVKNK-NH 2 (SEQ ID NO: 23) -HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 c)KNK-NH 2 (SEQ ID NO: 21) -HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO: -(Aepa)H SDG IFTDSYSRYRKQMAVKKYLAAVL(RAla) KRYKQ RVKN K-NH 2 (SEQ ID NO: 23) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVL(Ava)KRYKQRVKNK-NH 2 (SEQ ID NO: 22) -(Aepa)HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQR(A 6 C)KNK-NH 2 (SEQ ID NO: 21) -(Aepa)HSDGIFTDSYSRYRKQMA(A 5 c)KKYLAAVLGKRYKQRVKNK-NH 2 (SEQ ID NO: -(Doc) 6 D Phe-cycl o(C ys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- N H 2 (DOC) 4 DPh e-cyclo(Cys-3 I Tyr- DTrp- Lys-Va I-C ys)-Th r- N H 2 -DPhe-cyclo(Cys-3 lTyr-DTrp-Lys-VaI-Cys)-Thr-NH 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Ihr-N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Val-Cys)-Thr-NH 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-N H 2 -Doc-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 310 00 -(Doc) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(DOC) 3 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -(o)-DPh-ylo( s3ITy-Dr-LsV -y)T -NH o -(DOC)6-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 (Doc)-D P he-cycl o(Cys-3 I Tyr-DTrp-Lys-Va I-Cys)-Th r-N H 2 -(DOC)-Aep a- DPhe-cyclo(Cys-3 I Tyr- DTrp-Lys-VaI-Cys)-Th r-N H 2 'No)-eaDh-ycoCs3~rDr-LsVICs-h-H -(DoC) 3 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Th r-NH 2 N -(DOC) 5 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Va-Cys)-Thr-NH 2 -(DOC) 6 -Aep a- DPh e-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- NH 2 -(Aepa) 2 -D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-T hr- N H 2 -Aep a- Doc- DP he-cyclo (C ys-3 I Tyr- DTrp-Lys-Va I-Cys)-Th r- N H 2 -Ae pa-(Doc) 2 DP he-cyclo(Cys-3 ITyr- DTrp- Lys-Va I-Cys)-Th r- NH 2 -Ae pa-(Doc) 3 DPh e-cyclo(Cys-3 I Tyr- DTrp- Lys-Va I-Cys)-Th r- NH 2 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-VaI-Cys)-Thr-N H 2 -Doc-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(Doc) 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 3 -Ae pa- D Phe-cyclo (Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 5 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -(DOC) 6 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Aepa) 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-NH 2 -Doc-DPhe-cyclo(Cys-3lTyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -(DOC) 2 DP he-cyclo(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 3 DP he-cycl o(Cys-3 ITyr-DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 4 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 5 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 (DoC) 6 DPh e-cycl o(Cys-3I[Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -(DOC) 4 D Phe-cycl o(Cys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Th r-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Th r-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Th r-Cys)-Th r-N H 2 -311 00 0 0 OH 0 H N -Ir HO0 0 0 0 -Aepa H Leu-Arg-Pro-Gly-N H 2 pGlu-His-Trp-Ser-Tyr -N o H -Aepa-(Doc) 2 N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa N H pGtu-His-Trp-Ser-Tyr N 'rLeu-ArgPro-NHEt HO0 -(DOC) 2 -Aepa N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-NHEt H 0 -Aepa-(DoC) 2 N H pGlu-His-Trp-Ser-Tyr N -,FLeu-Arg-Pro-NHEt Hl 0
9. 312- 00 -Aepa XN H O f> Leu-Arg-Pro-Gly-NH 2 o pGlu-His-Trp-Ser-Tyr-N H -Aepa-(Doc) 4 N H pG Iu-H is-Trp- Se r-Tyr N Leu-Arg-Pro-G ly-N H H2 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -(Doc) 4 -Aepa N H pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-NHEt H 0 -Aepa-(Doc) 3 H pG Iu- H is-Trp-Ser-Tyr N Leu-Arg -P ro- N HEt H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-His N Tr-yPrGy-H H 0 -Aepa-N H pGlu-His-Trp-Ser-His N -7Trp-Tyr-Pro-Gly-NH 2 H 0
10. 313- -(Doc) 2 -Aepa N H pGlu-His-Trp-Ser-His N Tr-rPoGyNH H 0 -Aepa-(Doc) 2 -N pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H 0 2 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-His N -)Trp-Tyr-Pro-Gly-NH 2 H 0 2 -Aepa -N H pGlu-His-Trp-Ser-His -N Tr-rPrGy-H H 0 -(Doc) 3 -Aepa -N H pGlu-His-Trp-Ser-His N Tr-yPoGy-H H 0 -Aepa-(Doc) 3 -H pGlu-His-Trp-Ser-His N Trp-Tyr-Pro-Gly-NH 2 H 0 -314- 00 0 0 N o 0P 0 o H: OH7 "0 N No 00 0 IND 0 CI -Aepa\ NH pGlu-His-Trp-Ser-Tyr N Leu-Arg-Pro-Gly-N H H 0 2 -(Doc) 4 -Aepa -N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 -Aepa-(Doc) 4 N H pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH 2 H 0 2 H -(DoC) 4 N pGlu-His-Trp-Ser-Tyr -W N Leu-Arg-Pro-Gly-NH 2 H 0 315 00 0 CKI0=4. 0 0 00 Yo 'H OHH 0 H HO 0 7 0 -Aepa-(Doc) 4 -N pGlu-His-Trp-Ser-Tyr Leu-Arg-Pro-Gly-NH, -(Doc) 4 -Aepa -NH pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-NH, HO0 -(Doc) 4 -NH pGlu-His-Trp-Ser-Tyr -N Leu-Arg-Pro-Gly-N H 2 HO0 7 0 0 0 0 0 H: OH 0 0 H 0 7 0 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -316- 00 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Ae pa- Lys- DTyr- DTy r-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 o -(DOC)4-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -Y 0 H N 0- 0 00 H: -OH qH "0 N H 0 00 0 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 Doc-Aepa- DP he-cyc lo (Cys- 31Tyr- DTrp- Lys-Abu-Cys)-Th r- N H 2 -(DOC) 2 -Aepa- DPh e-cycl o(Cys-3 I Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -(DOC) 3 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 5 -Aep a- D Phe-cyclo(Cys-3 ITyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -(Doc) 6 -Ae pa-D Ph e-cycl o(Cys-3 I Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(Aepa) 2 D Phe-cyclo(Cys-3 I Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Doc-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 3 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 4 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(DOC) 5 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 6 D Phe-cyclo(Cys-3 ITyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 6 DP he-cyclo(C ys-3 ITyr- DT rp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Ihr-N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -317- 00 ~-(DOC) 6 Lys- DTyr- DTyr-cycl10(CYs-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 4 Lys- DTyr- DTyr-cyclo(Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 -Lys- DTyr- DTyr-cyclo(Cys-Ty r-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Apa y-Dy-Dy-yl CsTy-Dr-LsA Cs-hr oD )-Aep a-Lys- DTy r-DTyr-cyclo(C ys-Tyr- DTrp- Lys-Abu-Cys)-Th r-N H 2 -(Doc) 4 -Aepa--D~yrey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 (DcAp-DPhe-cyclo(Cys-Tyr-DTrp-Lys.-Abu-Cys)-Thr-N H 2 -A-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H -Aepa--D~ye~ y-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 ci-Aepa)-ys-y- yr- Dyc o(Cys-Tyr- p-Ly-buysbuy)-Th H 2 N -Ap-Ls cr -rcyl CsTr ip ysA -y)T -NH -()-Aepa -Ly-Dr-ey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa--D~yrey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa)-ePaDPhe-cyclys- 3 ITyr- p-Ly -u a -Cys)-Th H -N 2 pa- -cyclo(DCys-I-DTrp- Lys-DCys)-Th B -y -N H 2 -(DOC)4-Aepa-DCe-cycl o (Cys-3 aIy- DTrp- Lys-VaICys)-Th rI-H r-N 2 -(Doc)-Aepa-Che-cyclo(Cys-3P-DTrp-Lys-DuCys)-Thr(I-TrN H -(DOC)2-Aepa-Ce-cyclo(DCys-3Pa-DTrp-Lys-DbuCys)-ThrBIy-N H 2 -(DOC)-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 5-Ae pa- DPh e-cyclo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-T hr- N H 2 -(DOC)6-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(D-Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc)-AP ep-DclCyclo(y- Tr-Dp-Lyu-bys s)-Thrr- NHH -(Aep) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (DOC)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC)6-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 (D) 5 -Dhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 oc)-Dep-y-(y- Ty r-DrpLo(ys-Abur-Crpys-h u-s-hr-N H 2 Lys-D2yr-DayrLys-clo(Cr-Tyr-Dr-loCys-Ab-Crp ysThr-N H 2 -NH -(Doc) -Aepa- Lys- DTyr-DTyr-cycl o(C ys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 (DOC)4-Ae pa- Lys- DTy r- DTyr-cyclo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-T h r-N H 2 -(Doc) 5-Aepa- Lys- DTyr- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 318 00 -(Doc) 6 -Ae pa- Lys- DTy r- DTyr-cyc lo(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Aepa) 2 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Doc-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(O)-y-0rDy-yl(y-y-~pLsAuCs-h-H o-(DOC)3- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- N H 2 -(DOC)4- Lys- DTy r- DTyr-cyc lo(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 Lys- DTyr- DTy r-cyc lo (Cys-Tyr- DTrp- Lys-Ab u-C ys)-Th r- N H 2 'No)-y-~r-~rccoCs-y-~pLsAb-y)TrNH Lys- DTy r- DTy r-cyclIo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Ae pa- Doc-Lys- DTyr- DTyr-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys) -Th r- NH 2 -Aepa-(Doc) 2 Lys- DTy r- DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-(DOC) 3 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 -Aepa-(DOC) 4 Lys- DTyr- DTyr-cycl o(C ys-Tyr-DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Aepa-Doc-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(Doc) 2 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Aepa-(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 6 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 DOC) 4 -C aeg -cycl o(D Cys-3 Pa I-DT rp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -C aeg-cyclo(DC ys-3 P aI-DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 oc) 4 -Aep a-C aeg-cycl o(DCys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(DOC) 4 -Aepa-C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- D Cys)-Th r(BzI)-Ty r-N H 2 -C aeg-cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- NH 2 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -Doc-Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 2 -Ae pa-C aeg-cyclo(DCys-3 Pa I-DTrp- Lys- D Cys)-Th r(BzI)-Tyr-N H 2 -(Doc) 3 -Ae pa-C aeg-cyc o (DC ys-3 P aI- DTrp- Lys- DCys)-Th r(Bz)-Tyr-N H 2 -(Doc) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Th r(BzI)-Tyr-N H 2 -(Doc) 5 -Ae pa-C aeg-cyc lo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Ty r- N H 2 -(Doc) 6 -Aep a-C aeg-cycl o(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -(Ae pa) 2 -C aeg-cyclo( DCys-3 Pa I-DTrp- Lys- DCys) -Th r(BzI) -Tyr- N H 2 -Doc-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(DOC) 2 -Caeg -cyclo(D Cys-3 P aI-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(DOC) 3 -Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 319 00 -(DOC) 4 -C aeg-cycl o(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -(DOC) 5 -Caeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz) -Tyr- N H 2 -(DoC) 6 -C aeg -cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 o-Aepa- Doc-C aeg -cyclo (D Cys-3 Pa- DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Ae pa-(DOC) 2 -Caeg -cyclo (D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Ty r- N H 2 -Ae pa-(DOC) 3 -Caeg-cyclo(DCys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Ty r- N H 2 ~-Ae pa-(DOC) 4 -Caeg-cyc lo(DCys-3 P aI- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 INDVTNTLK(NeAKYNINNH SQI O 9 ci-HSDAVFTDNYTRLRKQMNAVKKYLNSILN-NH 2 (SEQ ID NO: 1) (N -SAFDYRRQAKYNSL-H QI O 8 -HSDAVFTDNYTRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -HSDAVFTDNYTRLRKQMAVKKLLNSILN-NH 2 (SEQ ID NO: -(eaHDVTNTLRQNeAKYNIN-H SQI O 9 -(Aepa)HSDAVFTDNYTRLRKQNeAVKKYLNSILN-NH 2 (SEQ ID NO: 1) -(Aepa)HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH 2 (SEQ ID NO: 18) -(Aepa)HSDAVFTDNYRLRKQMAVKKALNSILN-NH 2 (SEQ ID NO: 16) -(Aepa)Hys-rDATNyr-yl(-yTRLKMAKLLL-NH 2 (ySEQ Lys- DTy r-DTyr-cyclo (Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r-N H 2 -()-Aepa-Ly-Dr-ey-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 -()-Aepa-DPhe-cyclo(Cys-3Tyr-DTrp-Lys- -Cys)-Thr-N 2 7 0 0 Poo 0 N H~ OH 0 HI a N Ho 0 0 H 0 7~ 0 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(DOC) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -Aepa-Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 -(DOC) 4 Lys- DTy r- DTy r-cyc lo(Cys-Ty r-DT rp- Lys-Ab u-C ys)-T h r- N H 2 -(DoC) 6 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 320 00 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(Doc) 4 -D Phe-cyclo(C ys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r-N H 2 -(Doc) 6 -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 y-0 -Dy-yl( s- y-Dr-LsT -y)-hrNH o -(Doc) 4 -A-Lys-DTyr-DTyr-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC)6- Lys- DTy r-DTyr-cyclo(Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC)4-Lysp-CyrDe-cyclo(Cys-3I a-DTrp- Lys-ThCys)-Th zIyr- N H 2 -(Doc) 4 -A-Caeg-cyclo(DCys-3PaI-DTrp-Lys-DCys)-Thr(BzI)-Tyr-N H 2 -(DOC)6-C aeg -cyclo(DCys-3 Pa I-DTrp- Lys-D Cys)-Th r(Bz) -Tyr- N H 2 090 0 0 H: OH 00 0 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Th r-N H 2 -(Doc) 6 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -(Doc) 4 -Aepa- Lys- DTy r- DTyr-cyclo(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 Lys- DTy r- DTy r-cyclIo (C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -(Doc) 6 Lys- DTyr- DTy r-cycl o(Cys-Tyr- DTrp-Lys-Ab u-Cys)-Th r- N H 2 -(DOC) 4 -Aepa-DPhe-cyclo(Cys-3 ITyr-DTrp-Lys-Thr-Cys)-Thr-N H 2 -(DOC) 4 DP he-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 DP he-cyclo(C ys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(DOC) 4 -Aepa- Lys- DTy r- DTyr-cyclo(C ys-3 ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 4 Lys- DTy r- DTy r-cyclo (Cys-3 I Tyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -(Doc) 6 Lys- DTy r-DTy r-cyclo(Cys-3 ITyr- DTrp- Lys-Ih r-Cys)-Th r- N H 2 -(DOC) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 -(Doc) 4 -Caeg -cyclo(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz1) -Tyr- N H 2 -(DOC) 6 -Caeg -cycl o(D Cys-3 P aI- DTrp- Lys- DCys)-Th r(BzI) -Tyr- N H 2 321 00 o= 000 o H: OH 0 "0 N H 0 07 0 IND 0 -S uc- (DOC) 3 -Ae pa-D Phe-cycl o(C ys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -Suc-(DOC) 3 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -Suc-(Doc) 5 -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-N H 2 -S uc-(Doc) 3 -Aepa- Lys- DTyr- DTy r-cyc lo(Cys-Tyr- D~rp- Lys-Ab u-Cys)-Th r- N H 2 -S uc-(DOC) 3 Lys- DTyr- DTyr-cyclo(Cys-Iyr- DTrp- Lys-Abu -Cys)-Ih r- N H 2 -S uc-(Doc) 5 Lys- DTy r- DTyr-cycl o(Cys-Tyr- DTrp- Lys-Ab u-Cys)-Th r- N H 2 -S uc-(Doc) 3 -Aep a- D Phe-cyc lo(Cys-3 IlTyr- DTrp-Lys-Th r-C ys)-Th r- N H 2 -S uc-(DOC) 3 D Phe-cyclo(Cys-3ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -S uc-(Doc) 5 DP he-cyclo(Cys-3ITyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -S uc-(DoC) 3 -Ae pa- Lys- DTyr- DTyr-cyclo (C ys-3lITyr-DTrp-Lys-Th r-Cys)-Th r- NH 2 _S uc-(DOC) 3 Lys- DTyr- DTyr-cyclo(Cys-3 ITyr- DTrp-Lys-Th r-Cys) -Th r- N H 2 -S uc-(DOC) 5 Lys- DTyr-DTyr-cycl o(Cys-3 IlTyr- DTrp- Lys-Th r-Cys)-Th r- N H 2 -Suc-(Doc) 3 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-NH 2 -Suc-(Doc) 3 -C aeg-cyclo (DCys-3 Pal- DTrp- Lys- DCys)-Th r(Bz I)-Ty r- N H 2 -S uc- (Doc) 5 -Caeg -cyclo(DCys-3 P aI- DTrp- Lys- D Cys)-T h r(Bzl)-Tyr- N H 2 -S uc-(DOC) 4 -C aeg -cyclo(DCys-3 Pa I- DTrp- Lys- DCys)-Th r(Bzl)-Iy r- N H 2 -Su c-(Doc) 5 -Ae pa-C aeg-cycl o(D Cys-3 Pa I-DTrp- Lys- DCys)-Th r(Bz)-Tyr- N H 2 -Suc-(DOC) 4 -Aepa-Caeg-cyclo(DCys-3Pa-DTrp-Lys-DCys)-Thr(Bz)-Tyr-N H 2 A compound according to claim 1, wherein said compound comprises the formula according to: F 0 I 1 0 F N (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 322 (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 or a pharmaceutically acceptable salt thereof. 16. A compound according to claim 1, wherein said compound comprises the formula according to: F N 0 Fi N- (Doc) 4 -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 O 0 or a pharmaceutically acceptable salt thereof. 17. A compound according to claim 1, wherein said compound comprises the formula according to: I N I (Doc) 4 -Aepa-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 0 0 or a pharmaceutically acceptable salt thereof. 18. A compound according to claim 1, wherein said compound comprises the formula according to: or a pharmaceutically acceptable salt thereof. -323- 00 O O C©) 19. A pharmaceutical composition comprising an effective amount of a compound according to any one of claims 1-18 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a compound according to any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein said disease is selected from the group consisting of fibrosis, benign prostatic hyperplasia, atherosclerosis, restenosis, breast cancer, colon cancer, pancreas cancer, prostate cancer, lung cancer, small cell, lung cancer, ovarian cancer, epidermal cancer, and hematopoietic cancer. 21. A method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a compound according to any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein said disease is selected from the group consisting of benign prostatic hyperplasia, restenosis, breast cancer, colon cancer, pancreas cancer, prostate cancer, lung cancer, small cell lung carcinoma, ovarian cancer, epidermal cancer, and hematopoietic cancer. 22. A method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a compound according to any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein said disease is characterized by undesired proliferation of cells that express one or more somatostatin-type receptors. 23. A method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a compound according to any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein said disease is characterized by undesired proliferation of cells that express one or more of bombesin-type receptors. 24. A method of treating a disease in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a compound according to any one of claims 1-18, or a pharmaceutically -324- 00 acceptable salt thereof, wherein said disease is characterized by undesired 0 proliferation of cells that express one or more LHRH-type receptors. N 0 -325- 119PPCT2 Sequence Listing.txt SEQUENCE LISTING <110> SOCIETE DE CONSEILS DE RECHECHES ET D'APPLICATIONS C1 SCIENTIFIQUES S.A.S. o <120> SOMATOSTATIN VECTORS <130> 119P-PCT2 <140> PCT/US04/012200 <141> 2004-04-21 S <150> 60/464,528 <151> 2003-04-22 <160> 23 S <170> PatentIn Ver. 3.3 <210> 1 <211> 8 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MOD_RES <222> <223> Beta-alanine <220> <221> MODRES <222> (8) <223> Norleucine <400> 1 Gin Trp Ala Ala Xaa His Phe xaa 1 <210> 2 <211> 8 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> SITE <222> <223> Psi(CH2-NH) linker between residues 7-8 <400> 2 Gin Trp Ala val Gly His Leu Leu 1 <210> 3 <211> 8 <212> PRT <213> Artificial Sequence Page 1 119PPCT2 Sequence Listing.txt <220> <223> Description of Artificial Sequence: Synthetic C peptide <220> <221> SITE o <222> O <223> Psi(CH2-NH) linker between residues 7-8 <400> 3 Gin Trp Ala Val Gly His Leu Phe 1 <210> 4 I <211> 8 <212> PRT <213> Artificial Sequence <220> S <223> Description of Artificial Sequence: Synthetic O peptide C <220> <221> MOD_RES <222> <223> Beta-alanine <400> 4 Gin Trp Ala val Xaa His Leu Leu 1 <210> <211> 8 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MOD_RES <222> <223> Beta-alanine <220> <221> MOD_RES <222> (8) <223> Norleucine <400> Gin Trp Ala val Xaa His Leu Xaa 1 <210> 6 <211> 8 <212> PRT <213> Artificial Sequence <220> -<223> Description of Artificial Sequence: Synthetic peptide <220> <221> MOD_RES Page 2 119PPCT2 Sequence Listing.txt <222> <223> Beta-alanine <220> S <221> MOD_RES <222> (8) <223> Norleucine 0 <400> 6 S Gin Trp Ala Val Xaa His Phe xaa 1 <210> 7 S <211> 8 0 <212> PRT S <213> Artificial Sequence C1 <220> C <223> Description of Artificial Sequence: Synthetic Speptide <220> 1 <221> MOD_RES <222> <223> Beta-alanine <220> <221> MOD_RES <222> (8) <223> Norleucine <400> 7 Gin Trp Ala Val Xaa His Ala Xaa 1 <210> 8 <211> 8 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MODRES <222> <223> Beta-alanine <220> <221> MOD_RES <222> (8) <223> Norleucine <400> 8 Gln Trp Ala val Xaa Ala Phe xaa 1 <210> 9 <211> 8 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic Page 3 119PPCT2 Sequence Listing.txt peptide <400> 9 Gln Trp Ala Val Gly His Leu Leu C- 1 0 <210> <211> 8 C-i <212> PRT <213> Artificial sequence <220> <223> Description of Artificial Sequence: Synthetic peptide S <400> Gin Trp Ala Val Gly His Leu Met c 1 <210> 11 <211> 8 C- <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <400> 11 Gin Trp Ala Val Gly His Phe Met 1 <210> 12 <211> 9 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MOD_RES <222> (1) <223> 4-Aminobutyric acid <220> <221> MOD_RES <222> (6) <223> Beta-alanine <220> <221> MODRES <222> (9) <223> Norleucine <400> 12 xaa Gin Trp Ala val Xaa His Leu Xaa 1 <210> 13 <211> 9 <212> PRT <213> Artificial Sequence Page 4 119PPCT2 Sequence Listing.txt <220> S <223> Description of Artificial Sequence: Synthetic Speptide <220> o <221> MOD_RES O <222> (1) <223> 4-Aminobutyric acid <220> <221> SITE <222> <223> Psi(CH2-NH) linker between residues 8-9 <400> 13 S Xaa Gln Trp Ala val Gly His Leu Leu 1 <210> 14 <211> 9 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MODRES <222> (1) <223> 4-Aminobutyric acid <220> <221> MODRES <222> (6) <223> Beta-alanine <400> 14 Xaa Gin Trp Ala Val Xaa His Leu Leu 1 <210> <211> 28 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial sequence: Synthetic peptide <400> His Ser Asp Ala val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gln 1 5 10 Met Ala val Lys Lys Leu Leu Asn Ser Ile Leu Asn <210> 16 <211> 28 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: synthetic Page 119PPCT2 Sequence Listing.txt peptide S <400> 16 His Ser Asp Ala Val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gin 1 5 10 O Met Ala val Lys Lys Ala Leu Asn Ser Ile Leu Asn 0 20 S <210> 17 <211> 28 <212> PRT S <213> Artificial Sequence <220> S <223> Description of Artificial Sequence: Synthetic peptide tC <400> 17 S His Ser Asp Ala val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gin 1 5 10 c-I Met Ala val Lys Lys Phe Leu Asn Ser Ile Leu Asn <210> 18 <211> 28 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <400> 18 His Ser Asp Ala Val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gin 1 5 10 Met Ala val Lys Lys Tyr Leu Asn Ser Ile Leu Asn <210> 19 <211> 28 <212> PRT <213> Artificial sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MOD_RES <222> (17) <223> Norleucine <400> 19 His Ser Asp Ala val Phe Thr Asp Asn Tyr Thr Arg Leu Arg Lys Gin 1 5 10 Xaa Ala val Lys Lys Tyr Leu Asn Ser Ile Leu Asn <210> <211> 38 Page 6 119PPCT2 Sequence Listing.txt <212> PRT <213> Artificial Sequence S <220> C. <223> Description of Artificial Sequence: Synthetic peptide O <220> <221> MOD_RES <222> (19) <223> 1-Amino-l-cyclopentanecarboxylic acid <400> His Ser Asp Gly Ile Phe Thr Asp Ser Tyr Ser Arg Tyr Arg Lys Gin S 1 5 10 \O S Met Ala Xaa Lys Lys Tyr Leu Ala Ala Val Leu Gly Lys Arg Tyr Lys 25 C Gin Arg val Lys Asn Lys 035 C1 <210> 21 <211> 38 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MOD_RES <222> <223> 1-Amino-l-cyclohexanecarboxylic acid <400> 21 His Ser Asp Gly Ile Phe Thr Asp Ser Tyr Ser Arg Tyr Arg Lys Gin 1 5 10 Met Ala val Lys Lys Tyr Leu Ala Ala val Leu Gly Lys Arg Tyr Lys 25 Gin Arg xaa Lys Asn Lys <210> 22 <211> 38 <212> PRT <213> Artificial Sequence <220> <223> Description of Artificial Sequence: Synthetic peptide <220> <221> MODRES <222> (28) <223> 5-Aminovaleric acid <400> 22 His Ser Asp Gly Ile Phe Thr Asp Ser Tyr Ser Arg Tyr Arg Lys Gin 1 5 10 Met Ala val Lys Lys Tyr Leu Ala Ala val Leu Xaa Lys Arg Tyr Lys 25 Page 7 119PPcT2 Sequence Listing.txt Gin Arg val LYS Asn Lys <210> 23 <211> 38 0 <212> PRT O <213> Artificial sequence <220> <223> Description of Artificial sequence: Synthetic pepti de <220> IC <221> MOD-RES <222> (28) <223> Beta-alanine (i <400> 23 His Ser ASP Gly Ilie Phe Thr Asp Ser Tyr Ser Arg Tyr Arg Lys Gin 1 5 10 (i met Ala val LYS Lys Tyr LeU Ala Ala val Leu xaa Lys Arg Tyr Lys 25 Gin Arg 'ial Lys Asn Lys Page 8