Novel compounds as GLP-1 agonists

31-12-2007 дата публикации
Номер:
AP0200704227A0
Принадлежит:
Контакты:
Номер заявки: 22-04-20077
Дата заявки: 04-05-2006

[1]

(19)AUSTRALIAN PATENT OFFICE (54) Title Novel compounds as GPL-I agonists (51)6 International Patent Classification(s) C07K 14/605 20060101AFI2007101 (2006.01) 8BHEP C07K 14/605 PCT/IN2006/000154 (21) Application No: 2006277557 (22) Application Date: 2006.05.04 (87) WIPONo: WO07/017892 (30) Priority Data (31) Number (32) Date (33) Country 645/MUM/2005 2005.05.31 IN 558/MUM/2005 2005.05.05 IN (43) Publication Date : 2007.02.15 (71) Applicant(s) Cadila Healthcare Limited (72) Inventor(s) Lohray, Braj Bhushan; Lohray, Vidya Bhushan; Bahekar, Rajesh H. (74) Agent/Attorney Lesicar Perrin, 49 Wright Street Adelaide, SA, 5000 (H) Application NoAU2006277557 A1(19)AUSTRALIAN PATENT OFFICE (54) Title Novel compounds as GPL-I agonists (51)6 International Patent Classification(s) C07K 14/605 20060101AFI2007101 (2006.01) 8BHEP C07K 14/605 PCT/IN2006/000154 (21) Application No: 2006277557 (22) Application Date: 2006.05.04 (87) WIPONo: WO07/017892 (30) Priority Data (31) Number (32) Date (33) Country 645/MUM/2005 2005.05.31 IN 558/MUM/2005 2005.05.05 IN (43) Publication Date : 2007.02.15 (71) Applicant(s) Cadila Healthcare Limited (72) Inventor(s) Lohray, Braj Bhushan; Lohray, Vidya Bhushan; Bahekar, Rajesh H.

[2]

(74) Agent/Attorney Lesicar Perrin, 49 Wright Street Adelaide, SA, 5000



[3]

The present invention describes a group of novel peptidomimetics useful for the treatment of diabetes. These compounds are defined by the general formula (I) as given below. A-X<SUB>1</SUB>- S<SUB>1</SUB>-Y-S<SUB>2</SUB>-X<SUB>2</SUB>-B (I)



JJO-CHO-^JOUU

We claim:

1. An isolated polypeptide having a sequence of Formula (I), including its tautomers, solvates and pharmaceutically acceptable salts

A-Xi- S1-Y-S2-X2-B (I) wherein,

A represents -NH-R1, wherein R1 represents hydrogen, groups selected from linear or branched (C1-C1S) alkyl chain, an amino acid or peptide containing one, two or three natural amino acid residues, R3-CO- group, RsO-C(O)- group, a sulfonyl group of formula Rs-SO2-, each of these groups may be substituted; R3 is selected from linear or branched (C1-C1O) alkyl, (C3-C6) cycloalkyl, aryl, heteroaryl, arylalkyl groups, each of these groups may be substituted;

B represents -COOR2, -CONHR2 or CH2OR2, R2 represents H, groups selected from linear or branched (Ci-C10) alkyl, aryl groups selected from phenyl, napthyl, indanyl, fluorenyl, biphenyl groups, aralkyl group, wherein the aryl groups are as defined earlier, each of these groups may be substituted; each of S1 and S2 may independently be a bond or independently represents a group '- NH-(CH2)n-C00-', where, n=l-9;

Y represents a bond or -CO-, -(CH2)m- (m = 1-3), '0',1S', -CO-NH-, -CO-NR4-, or represents a short peptide containing one or two or three amino acids selected from natural or non-natural amino acids; where R4 represents H, optionally substituted groups selected from linear or branched (C1-C1O) alkyl or aryl groups selected from phenyl, napthyl, indanyl, fluorenyl, biphenyl groups; with the proviso that when S1-Y- S2 represents a bond, X1 is selected from the following amino acid sequences HAEGTFTSD, HAEGTFTSDV, HAEGTFTSDVS, HAEGTFTSDVSS, HAEGTFTSDVSSY, HAEGTFTSDVSSYL, HAEGTFTSDVSSYLE,

HAEGTFTSDVSSYLEG, HAEGTFTSDVSSYLEGQ, HAEGTFTSDVSSYLEGQA, HAEGTFTSDVSSYLEGQAA, HAEGTFTSDVSSYLEGQAAK,

HAEGTFTSDVSSYLEGQAAICE, HAEGTFTSDVSSYLEGQAAKEF, HAEGTFTSDVSSYLEGQAAKEFI, with the further option that one or more of these amino acids may be replaced by unnatural amino acids, and X2 is selected from the following amino acid sequences GPSSGAPPPS or KELEKLL or GPPS or VKGR; and when S1-Y-S2 does not represent a bond X1 is selected from the following amino acid sequences HA, HAE, HAEG, HAEGT, HAEGTF, HAEGTFT, HAEGTFTS, HAEGTFTSD with the further option that one or more of these amino acids may be replaced by unnatural amino acids; X2 is selected from GPSSGAPPPS or KELEKLL or GPPS or VKGR or a dipeptide, selected from combination of two amino acids consisting of natural or unnatural amino acids, having a side chain containing an arylalkyl or heterorylalkyl moieties selected from benzyl, napthylmethyl, pyridylmethyl, thienylmethyl, furylmethyl, imidazolylmethyl, isooxazolylmethyl, quinolylmethyl, benzofuranylmethyl, benzothienylmethyl, indolinylmethyl, indolylmethyl, dibenzofuranylmethyl, dibenzothienylmethyl, benzodihydrofuranylmethyl, benzodihydrothienylmethyl, thienopyrimidylmethyl, benzimidazolylmethyl, phenanthrenylmethyl, dihydrophenanthrenylmethyl, fluorenylmethyl, dibenzofuranylmethyl, dibenzothiophenyl methyl groups, where each of these groups may be optionally substituted with (C1-C6)alkyl, (Q-C^alkoxy, cyano, halo, hydroxy or optionally substituted aryl or heteroaryl groups, with the further provision that such aryl or heteroaryl substituents may further be optionally substituted with (Cj-C6)alkyl, (Ci-C6)alkoxy, cyano, halo, hydroxy or aryl or heteroaryl groups.

2. A compound as claimed in claim 1 wherein the non-natural amino acids are represented by the general formula (Ha)

wherein R5 is selected from H, F, (C1-Cs) alkyl, the stereochemical configuration at the carbon bearing R5 may be (R) or (S); R6 is selected from H or (C1-C3) alkyl; each of R7 and R$ is independently selected from H, (C1-C2) alkyl or halogen atom, preferably fluorine atom; R9 represents groups, selected from (C1-Cs) alkyl, aryl or heteroryl moieties selected from phenyl, napthyl, pyridyl, thienyl, furyl, imidazolyl, isooxazolyl, quinolyl, benzofuranyl, benzothienyl, indolinyl, indolyl, dibenzofuranyl, dibenzothienyl, benzodihydrofuranyl, benzodihydrothienyl, thienopyrimidyl, benzimidazolyl, phenanthrenyl, dihydrophenanthrenyl, fluorenyl, dibenzofuranyl, dibenzothiophenyl groups, where each of these groups may be optionally substituted with (C1-C6) alkyl, (C1-C6) alkoxy, cyano, halo, hydroxy or optionally substituted aryl or heteroaryl groups, with the further provision that such aryl or heteroaryl substituents may further be optionally substituted with (C1- C6)alkyl, (d-C6)alkoxy, cyano, halo, hydroxy or aryl or heteroaryl groups.

3. The isolated peptide as claimed in claim 1, wherein the dipeptide representing X2 is preferably selected from Bip, Bip(2-Me), Biρ(2-Et), Bip(2-Ipr), Bip(2-CN), Bip(2'- Et-4'-OMe), Bip(4'-fluoro), Bip(4'-Phenyl), 2-(9,10-Dihydro-phenanthrenyl]-Ala, 2-(Phenanthrenyl)-Ala, 4-(2-Naphthyl)-Phe, 4-(l-Naphthyl)-Phe, 2-Fluorenyl-Ala, 4-dibenzofuran-Phe, 4-dibenzothiophene-Phe, 4-(2'-methylρhenyl)-3-pyridylalanine groups.

4. The isolated peptide as claimed in claim 1, wherein the substituents are selected from hydroxyl, oxo, halo, thio, nitro, amino, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, cycloalkyl, aryl, aryloxy, aralkyl, aralkoxy, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, carboxylic acid and its derivatives selected from esters and amides.

5. The isolated polypeptide of claim 1, wherein the isolated polypeptide is a compound selected from HGEGTFTSD-(CH2)3-GPSSGAPPPS

HGEGTFTSD-(CH2)4-GPSSGAPPPS HGEGTFTSD-(CH2)s-GPSSGAPPPS HGEGTFTSD-(CH2)6-GPSSGAPPPS HGEGTFTSD-(CH2)7-GPSSGAPPPS HGEGTFTSD-(CH2)10-GPSSGAPPPS

HGEGTFTSD-(CH2)n-GPSSGAPPPS

HGEGTFTSDLSKQM-(CH2)3-GPSS

HGEGTFTSDLSKQM-(CH2)4-GPSS HGEGTFTSDLSKQM-(CH2)5-GPSS

HGEGTFTSDLSKQM-(CH2)6-GPSS

HGEGTFTSDLSKQM-(CH2)7-GPSS

HGEGTFTSDLSKQM-(CH2)IO-GPSS

HGEGTFTSDLSKQM-(CH2)Π-GPSS HGEGTFTSDLSKQME-G-GPSSGAPPP1S

HGEGTFTSDLSKQME-(CH2)2-GPSSGAPPPS

HGEGTFTSDLSKQME-(CH2)3-GPSSGAPPPS

HGEGTFTSDLSKQME-(CH2)4-GPSSGAPPPS

HGEGTFTSDLSKQME-(CH2)5-GPSSGAPPPS HGEGTFTSDLSKQME-(CH2)6-GPSSGAPPPS

HGEGTFTSDLSKQME-(CH2)7-GPSSGAPPPS

HGEGTFTSDLSKQME-(CH2)1o-GPSSGAPPPS

HGEGTFTSDLSKQME-(CH2)π-GPSSGAPPPS

HAEGTFTSD-(CH2)2-VKGR HAEGTFTSD-(CH2)3-VKGR

HAEGTFTSD-(CH2)4-VKGR

HAEGTFTSD-(CH2)5-VKGR

HAEGTFTSD-(CH2)6-VKGR

HAEGTFTSD-(CH2)IO-VKGR HAibEGTFTSD-(CH2)2-VKGR

HAibEGTFTSD-(CH2)3-VKGR

HAibEGTFTSD-(CH2)4-VKGR

HAibEGTFTSD-(CH2)s-VKGR

HAibEGTFTSD-(CH2)6-VKGR HAibEGTFTSD-(CH2)10-VKGR

HGEGTFTSDLSKQMKELEKLL

HAEGTFTSDKELEKLL

HGEGTFTSDKELEKLL

HAibEGTFTSDGKELEKLL HGEGTFTSDGKELEKLL HGEGTFTSDVSKELEKLL HAEGTFTSDVSKELEKLL HAEGTFTSDVSEKELEKLL HAEGTFTSDVSGKELEKLL

HAEGTFTSDVSSYLEKELEKLL HAEGTFTSDVSSYLEGKELEKLL HGEGTFTSDVSSYLEGKELEKLL HaEGTFTSDVSSYLEGKELEKLL HAibEGTFTSDVSSYLEGKELEKLL

HAEGTFTSDVSSYLEGKELEKLLVKG HAEGTFTSDVSSYLEPKELEKLL HAEGTFTSDVSSYLEGQAAKELEKLL HAEGTFTSDVSSYLEGQAAKEFIKELEKLL HAIBEGTFTSDVSSYLEGQAAKEFIKELEKLL

HAibEGT-(α-Me)Phe(2-F)-TSDVSSYLEGQAAKEFIKELEKLL

Des-amino-HAibEGT-(α-Me)Phe(2-F)-TSDVSSYLEGQAAKEFIKELEKLL

HAEGTFTSD-(CH2)3-KELEKLL

HAEGTFTSD-(CH2)4-KELEKLL HAEGTFTSD-(CH2)S-KELEKLL

HAEGTFTSD-(CH2)6-KELEKLL

HA-(CH2)3-DVSSYLEGQAAKEFIKELEKLL

HAib-(CH2)3-DVSSYLEGQAAKEFIKELEKLL

HAibEGTFTSDVSSYLEGQ-(CH2)2-KELEKLL HAibEGTFTSDVSSYLEGQ-(CH2)3-KELEKLL

HAibEGTFTSDVSSYLE-(CH2)2-FIKELEKLL

HGEGTFTSD-(CH2)3-Bip-Bip

HAibEGTFTSD-(CH2)3-Bip-Bip

HAibEGT-(α-Me)-Phe(2-F)-TSD-(CH2)3-Bip-Bip HAEGTFTSD-G-Bip(2-Me)-Bip(2-Me)

HAibEGTFTSD-G-Bip(2-Me)-Bip(2-Me)

HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Biρ(2-Me)-Bip(2-Me)

HAEGTFTS-G-Bip(2-Me)-Bip(2-Me)

HAibEGTFTS-G-Bip(2-Me)-Bip(2-Me) HAibEGT-(α-Me)-Phe(2-F)-TS-G-Bip(2-Me)-Bip(2-Me)

HAEGTFTS-(CH2)2-Biρ(2-Me)-Bip(2-Me)

HAibEGTFTS-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGT-(α-Me)-Phe(2-F)-TS-(CH2)2-Bip(2-Me)-Bip(2-Me) HAEGTFT-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGTFT-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGT-(α-Me)-Phe(2-F)-T-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAEGTF-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGTF-(CH2)2-Bip(2-Me)-Bip(2-Me) HAibEGT-(α-Me)-Phe(2-F)-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAEGT-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGT-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAEG-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEG-(CH2)2-Bip(2-Me)-Bip(2-Me) HAEGTFTSD-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGTFTSD-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAibEGT-(α-Me)-Phe(2-F)-TSD-(CH2)2-Bip(2-Me)-Bip(2-Me)

HAEGTFTSD-G-Bip-Bip(2-Me)

HAibEGTFTSD-G-Bip-Bip(2-Me) HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip-Bip(2-Me)

HAEGTFTSD-G-Bip(2-Me)-Bip

HAibEGTFTSD-G-Bip(2-Me)-Bip

HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Me)-Bip

HAEGTFTSD-G-Bip-Bip HAibEGTFTSD-G-Bip-Bip HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Biρ-Bip

HAEGTFTSD-G-Bip-Bip(2-Et)

HAibEGTFTSD-G-Bip-Bip(2-Et)

HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip-Bip(2-Et)

HAEGTFTSD-G-Bip(2-Et)-Bip(2-Et) HAibEGTFTSD-G-Bip(2-Et)-Biρ(2-Et)

HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Et)-Bip(2-Et)

HAEGTFTSD-G-Bip(2-Et)-Bip

HAibEGTFTSD-G-Bip(2-Et)-Bip HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Et)-Bip HAEGTFTSD-G-Bip(2-Et)-Bip(2-Me) HAibEGTFTSD-G-Bip(2-Et)-Bip(2-Me) HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Et)-Bip(2-Me) HAEGTFTSD-G-Bip(2-Me)-Bip(2-Et)

HAibEGTFTSD-G-Bip(2-Me)-Bip(2-Et) HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Me)-Bip(2-Et) HGEGTFTSD-G-Bip(2-Me)-Bip(2-Me) HGEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Me)-Bϊp(2-Me) HGEGTFTSD-G-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-Et)-Bip(2-Et) HGEGTFTSD-(CH2)3-Bip(2-Me)-Bip(2-Me) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)3-Bip(2-Me)-Bip(2-Me) HGEGTFTSD-(CH2)4-Bip(2-Me)-Bip(2-Me) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)4-Bip(2-Me)-Bip(2-Me)

HGEGTFTSD-(CH2)5-Bip(2-Me)-Bip(2-Me) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)5-Bip(2-Me)-Bip(2-Me) HGEGTFTSD-(CH2)6-Bip(2-Me)-Bip(2-Me) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)6-Bip(2-Me)-Bip(2-Me) HGEGTFTSD-(CH2)10-Bip(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)10-Bip(2-Me)-Bip(2rMe) HGRCτTFTSD-(CH2)3-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)3-Bip(2-Et)-Bip(2-Et) HGEGTFTSD-(CH2)4-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)4-Bip(2-Et)-Bip(2-Et)

HGEGTFTSD-(CH2)5-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)5-Bip(2-Et)-Bip(2-Et) HGEGTFTSD-(CH2)6-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)6-Bip(2-Et)-Bip(2-Et) HGEGTFTSD-(CH2)10-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)io-Bip(2-Et)-Bip(2-Et) HGEGTFTSD-(CH2)! i-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)π-Bip(2-Et)-Bip(2-Et) HGEGTFTS-(CH2)3-Bip(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)3-Bip(2-Me)-Bip(2-Me)

HGEGTFTS-(CH2)4-Bip(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)4-Bip(2-Me)-Bip(2-Me) HGEGTFTS-(CH2)5-Bip(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)5-Bip(2-Me)-Bip(2-Me)

HGEGTFTS-(CH2)6-Bip(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)6-Bip(2-Me)-Bip(2-Me)

HGEGTFTS-(CH2)io-Bip(2-Me)-Bip(2-Me) HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)io-Bip(2-Me)-Bip(2-Me)

HGEGTFTS-(CH2)π-Biρ(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)n-Bip(2-Me)-Bip(2-Me)

HGEGTFTS-(CH2)3-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)3-Bip(2-Et)-Biρ(2-Et) HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)4-Bip(2-Et)-Bip(2-Et)

HGEG1TTS-(CH2)4-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)4-Bip(2-Et)-Bip(2-Et)

HGEGTFTS-(CH2)5-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)5-Bip(2-Et)-Bip(2-Et) HGEGTFTS-(CH2)6-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)6-Bip(2-Et)-Bip(2-Et)

I-IGEGTFTS-(CII2)-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)10-Bip(2-Et)-Bip(2-Et)

HGEGTFTS-(CH2)π-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)jrBip(2-Et)-Bip(2-Et)

HGEGTFTS-(CH2)2-Bip(2-Me)-Bip(2-Me)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)2-Bip(2-Me)-Bip(2-Me)

HGEGTFTS-(CH2)2-Bip(2-Et)-Bip(2-Et)

HGEGT-(α-Me)-Phe(2-F)-TS-(CH2)2-Bip(2-Et)-Biρ(2-Et) HAEGTFTS-(CH2)2-Bip(2-Et)-Bip(2-Et)

HAibEGTFTS-(CH2)2-Bip(2-Et)-Bip(2-Et)

HAibEGT-(α-Me)-Phe(2-F)-TS-(CH2)2-Bip(2-Et)-Bip(2-Et)

HGEGTFTSD-(CH2)2-Bip(2-Et)-Bip(2-Et) HGEGT-(α-Me)-Phe(2-F)-TSD-(CH2)2-Bip(2-Et)-Bip(2-Et)

HAEGTFTSD-(CH2)2-Bip(2-Et)-Bip(2-Et)

HAibEGTFTSD-(CH2)2-Bip(2-Et)-Bip(2-Et)

HAibEGT-(α-Me)-Phe(2-F)-TSD-(CH2)2-Bip(2-Et)-Bip(2-Et) HAEGTF-(CH2)2-Biρ(2-Me)-Bip(2-Et)

HAibEGTF-(CH2)2-Bip(2-Me)-Bip(2-Et)

HAibEGT-(α-Me)-Phe(2-F)-(CH2)2-Bip(2-Me)-Bip(2-Et)

HAEGTFTSD-G-TrPh-TrPh

HAibEGTFTSD-G-TrPh-TrPh HAibEGT-(α-Me)-Phe(2-F)-TSD-G-TrPh-TrPh

HAibEGT-(α-Me)-Phe(2-F)-(CH2)2-TrPh-TrPh

HAibEG-(CH2)2-TrPh-TrPh

HAibE-(CH2)2-TrPh-TrPh

HAib-(CH2)3-TrPh-TrPh HAEGTFTSD-G-Nap-Nap

HAibEGTFTSD-G-Naρ-Nap

HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Nap-Nap

HAEGTFTSD-G-Bip(2-F)-Bip(2-F)

HAibEGTFTSD-G-Bip(2-F)-Bip(2-F) AibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2-F)-Bip(2-F)

HAEGTFTSD-G-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGTFTSD-G-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGT-(α-Me)-Phe(2-F)-TSD-G-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAEGTFTSD-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala HAibEGTFTSD-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGT-(α-Me)-Phe(2-F)-TSD-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa

HAEGTFTS-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGTFTS-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala HAibEGT-(α-Me)-Phe(2-F)-TS-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

Ala HAEGTFT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGTFT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala HAibEGT-(α-Me)-Phe(2-F)-T-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAEGTF-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGTF-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGT-(α-Me)-Phe(2-F)-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala HAEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAibEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAEG-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala HAibEG-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala

HAEGT-(CH2)2-Bip(2-Me)-Bip(2-Me)

HGEGT-(CH2)3-Bip(2-Me)-Bip(2-Me)

HGEGT-(CH2)4-Bip(2-Me)-Bip(2-Me)

HGEGT-(CH2)5-Bip(2-Me)-Bip(2-Me) HGEGT-(CH2)6-Bip(2-Me)-Bip(2-Me)

HAEGT-(CH2)2-Bip(2-Me)-DBiρ(2-Me)

HAEGT-(CH2)2-DBip(2-Me)-Bip(2-Me)

HaEGT-(CH2)2-Bip(2-Me)-Bip(2-Me)

HGEG-(CH2)3-Bip(2-Me)-Bip(2-Me) HAEG-(CH2)3-Bip(2-Me)-Bip(2-Me)

HGEG-(CH2)4-Bip(2-Me)-Bip(2-Me)

HGEG-(CH2)5-Bip(2-Me)-Bip(2-Me)

HGEG-(CH2)0-Biρ(2-Me)-Bip(2-Me)

HAEG-(CH2)3-Bip(2-Et)-Biρ(2-Me) HAEG-(CH2)3-Bip(2-Me)-DBip(2-Me)

HAEG-(CH2)4-Bip(2-Me)-DBip(2-Me)

HAEG-(CH2)5-Biρ(2-Me)-DBip(2-Me)

HGEG-(CH2)5-DBip(2-Me)-Bip(2-Me)

HAE-(CH2)3-Bip(2-Me)-Bip(2-Me) HAE-(CH2)3-Bip(2-Me)-DBiρ(2-Me)

HAE-(CH2)2-D-Biρ(2-Me)-Bip(2-Me)

HAE-(CH2)3-D-Bip(2-Me)-Bip(2-Me)

HAE-(CH2)4-D-Biρ(2-Me)-Bip(2-Me)

HAE-(CH2)4-Biρ(2-Me)-DBiρ(2-Me) HAE-(CH2)5-D-Bip(2-Me)-Bip(2-Me)

HAE-(CH2)3-Biρ(2-Et)-Bip(2-Me)

HAE-(CH2)2-Bip(2-Me)-Bip(2-Me)

H-(CH2)3-Bip(2-Me)-Bip(2-Me) H-(CH2)4-Bip(2-Me)-Bip(2-Me)

H-(CH2)5-Bip(2-Me)-Bip(2-Me)

H-(CH2)3-Bip(2-Et)-Bip(2-Me)

H-(CH2)4-Bip(2-Et)-Bip(2-Me)

H-(CH2)5-Bip(2-Et)-Bip(2-Me) H-(CH2)6-Bip(2-Et)-Biρ(2-Me)

H-(CH2)10-Bip(2-Et)-Bip(2-Me)

H-(CH2)5-Bip(2-Me)-DBip(2-Me)

H-(CH2)5-DBip(2-Me)-Bip(2-Me)

H-(CH2)5-DBip(2-Me)-DBip(2-Me) HG-(CH2)3-Bip(2-Me)-Bip(2-Me)

HG-(CH2)4-Bip(2-Me)-Bip(2-Me)

HG-(CH2)3-Bip(2-Et)-Bip(2-Me)

HG-(CH2)4-Bip(2-Et)-Bip(2-Me)

HG-(CH2)3-Bip(2-Et)-DBip(2-Me) HG-(CH2)3-Bip(2-Me)-DBip(2-Me)

FA-(CH2)3-DBip(2-Me)-Bip(2-Et)

FA-(CH2)3-DBip-Dbip

Ha-(CH2)3-Bip(2-Me)-Bip(2-Me)

Ha-(CH2)4-Bip(2-Me)-Bip(2-Me) Ha-(CH2)5-Bip(2-Me)-Bip(2-Me)

Ha-(CH2)3-Bip(2-Et)-Bip(2-Me)

Ha-(CH2)3-Bip(2-Et)-DBiρ(2-Me)

Ha-(CH2)3-Bip(2-Me)-DBip(2-Me)

Ha-(CH2)3-Blp(2-Et)-DBip(2-Et) Ha-(CH2)3-Bip(2-Me)-Bip

Ha-(CH2)3-(N(Me))-DBip(2-Me)-Bip(2-Et)

Ha-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)

Ha-(CH2)3-(N(Me))-DBip-Bip(2-Et)

Ha-(CH2)3-DBip(2-Me)-Bip(2-Et) HA-(CH2)3-Bip(2-Me)-Bip(2-Me)

HA-(CH2)4-Bip(2-Me)-Bip(2-Me)

HA-(CH2)5-Bip(2-Me)-Biρ(2-Me)

HA-(CH2)6-Bip(2-Me)-Bip(2-Me) HA-(CH2)i0-Bip(2-Me)-Bip(2-Me)

HA-(CH2)!1-Bip(2-Me)-Bip(2-Me)

HA-(CH2)3-Bip(2-Et)-Bip(2-Me)

HA-(CH2)3-Bip(2-Et)-DBip(2-Et)

HA-(CH2)3-DBip(2-Me)-DBip(2-Me) HA-(CH2)3-DBip(2-Me)-Bip(2-Me)

HA-(CH2)3-Bip(2-Me)-DBip(2-Me)

HA-(CH2)3-Bip(2-Ipr)-Bip(2-Ipr)

HA-(CH2)3-Bip(2-Ipr)-Bip(2-Me)

HA-(CH2)3-Bip(2-Me)-Bip(2-Ipr) HA-(CH2)4-Bip(2-Et)-Bip(2-Me)

HA-(CH2)3-Bip(2-Me)-DBip(2-Et)

HA-(CH2)2-Bip(2-Et)-Bip(2-Me)

HA-(CH2)5-Bip(2-Et)-Bip(2-Me)

HA-(CH2)6-Bip(2-Et)-Bip(2-Me) HA-(CH2)2-Bip(2-Me)-Bip(2-Me)

HA-(CH2)3-DBip(2-Et)-DBip(2-Me)

HA-(CH2)3-DBip(2-Et)-Biρ(2-Me)

HA-(CH2)2-Bip(2-Me)-DBip(2-Me)

HA-(CH2)3-Bip(2-Et)-Bip(2-Et) HA-(CH2)3-DBip(2-Et)-DBiρ(2-Et)

HA-(CH2)3-DBip(2-Et)-Biρ(2-Et)

HA-(CH2)3-DBip(2-Me)-DBip(2-Et)

HA-(CH2)3-Bip(2-Me)-Bip(2-Et)

HA-(CH2)3-DBip(2-Me)-Bip(2-Et) HA-(CH2)3-Bip-Bip

HA-(CH2)3-Bip-D-Bip

HA-(CH2)3-DBip-D-Bip

HA-(CH2)3-DBip-Bip

HA-(CH2)3-Bip-Bip(2-Me) HA-(CH2)3-Bip(2-Me)-Bip

HA-(CH2)3-Bip(2-Et)-Bip

HA-(CH2)3-Bip-Bip(2-Et)

HA-(CH2)3-Bip(2-Ipr)-DBip(2-Iρr) HA-(CH2)3-DBip(2-Ipr)-Bip(2-Ipr)

HA-(CH2)3-DBip(2-Ipr)-DBip(2-Ipr)

HA-(CH2)3-Bip(2-Me)-Bip(2-CN)

HA-(CH2)3-Bip-Bip(2-CN)

HA-(CH2)3-Bip(2-Et)-Bip(2-CN) HA-(CH2)3-Bip(2-Ipr)-Biρ(2-CN)

HA-(CH2)3-Bip(2-CN)-Bip(2-Me)

HA-(CH2)3-Bip(2-CN)-Bip

HA-(CH2)3-Bip(2-CN)-Bip(2-Et)

HA-(CH2)3-Bip(2-CN)-Bip(2-Ipr) HA-(CH2)3-Bip(2-CJN)-Biρ(2-CN)

HA-(CH2)2-F-(CH2)2-Bip(2-Et)-DBip(2-Et)

HA-(CH2)2-F-(CH2)2-Bip(2-Et)-DBip(2-Me)

HA-(CH2)5-Bip(2-Me)-DBiρ

HA-(CH2)3-Bip(2-Me)-DBip-R HA-(CH2)3-DBip(2-Me)-DBip

HA-(CH2)5-Bip(2-Me)-DBip(2-Me)

HA-(CH2)5-DBip(2-Me)-Bip(2-Me)

HA-(CH2)4-D(Bip)-Bip(2-Et)

HA-(CH2)5-D(Bip)-Bip(2-Et) HA-(CH2)4-Bip(2-Me)-DBip(2-Me)

HA-(CH2)5-Bip(2-Me)-DBip(2-Me)

HA-(CH2)3-(N(Me))-DBip-Bip(2-Et)

HA-(CH2)4-DBip(2-Me)-Bip(2-Et)

HA-(CH2)5-DBip(2-Me)-Bip(2-Et) HA-(CH2)3-(N(Me))-DBip(2-Me)-Bip(2-Et)

HA-(CH2)4-Bip(2-Me)-DBip

HA-(CH2)5-Bip(2-Me)-DBip

HA-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)

HA-(N(Me))-(CH2)3-DBip(2-Me)-Bip(2-Et) HA-(N(Me))-(CH2)3-DBip-Bip(2-Et) HA-(N(Me))-(CH2)3-Bip(2-Et)-Bip(2-Me) HA-(N(Me))-(CH2)3-Bip(2-Me)-DBip HAE-(CH2)2-F-(CH2)2-Bip(2-Et)-DBip(2-Et) HAE-(CH2)2-F-(CH2)2-Bip(2-Et)-DBip(2-Me)

HAib-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)

6. The isolated polypeptide of claim 1 wherein the isolated polypeptide is a compound selected from HA-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-Aib-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

Ha-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 H-(N(Me))Aib-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-NH2

H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-NH2 H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH2

H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4- (2'-Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me»-

4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH-(CH2)6-CH3 H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH-(CH2)10-CH3 H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)i0-CH3

CH3-(CH2)6-NH-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 CH3-(CH2)6-NH-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NΗ-(CH2)6-CH3

CH3-(CH2)1o-NH-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

HA-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-Aib-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

Ha-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 H-(N(Me))A-(N(Me))-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-(N(Me))-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-NH2

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr- AIa-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH2

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH2 Des-amino-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-

(2'-Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)- 3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH-(CH2)10-CH3 H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)i0-CH3

CH3-(CH2)6-NH-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)io-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

HA-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-Aib-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-a-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NΗ2

H-(N(Me))A-(CH2)4-Biρ(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 H-(N(Me))A-(N(Me))-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-(N(Me))-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-NH2

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr- AIa-NH2

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH2

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH2 Des-amino-H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-

(2'-Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)- 3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-NH-(CH2)10-CH3 H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)10-CH3

CH3-(CH2)6-NH-H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)io-NH-H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)10-NH-H-N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

HAE-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-Aib-E-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

HaE-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))AE-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 H-(N(Me))AE-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-E-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-

NH2

H-(N(Me))AE^(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-NH2 H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-NH2

H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)io-CH3

H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)10-CH3 CH3-(CH2)6-NH-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)6-NH-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)io-NH-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

HAEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-Aib-EG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 HaEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))AEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))AEG-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-EG-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-

NH2 H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-NH2

H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-NH2

H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 Des-amino-H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)io-CH3 H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-NH-(CH2)io-CH3

CH3-(CH2)6-NH-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)6-NH-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)io-NH-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)1o-NH-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 HAEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-Aib-EGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

HaEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))AEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

H-(N(Me))AEGT-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala- NH2

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-

NH2

H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-NH2 H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-NH2

H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH2

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'- Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH2

Des-amino-H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH2 H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-NH-(CH2)io-CH3

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-NH-(CH2)io-CH3

CH3-(CH2)6-NH-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)6-NH-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

CH3-(CH2)io-NH-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3 CH3-(CH2)io-NH-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-NH-(CH2)6-CH3

HA-(CH2)3-Bip(2-Me)-Bip(2-Me)-NH2 H-Aib-(CH2)3-Bip(2-Me)-Bip(2-Me)-NH2 Ha-(CH2)3-Bip(2-Me)-Bip(2-Me)-NH2 H-(N(Me))A-(CH2)3-Bip(2-Me)-Bip(2-Me)-NH2

H-(N(Me))A-(N(Me))-(CH2)3-Bip(2-Me)-Bip(2-Me)-NH2 H-(N(Me))Aib-(N(Me))-(CH2)3-Bip(2-Me)-Bip(2-Me)-NH2 H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Biρ(2-Me)-Biρ(2-Me)-NH2 H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-Bip(2-Me)-NH2 H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-NH2

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-NH2 Des-amino-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)- NH2

Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2- Me)-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Biρ(2-Me)-(N(Me))-Bip(2-Me)-NH- (CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-NH- (CH2)6-CH3 H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-NH-

(CH2)10-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-NH-

(CH2)I0-CH3 CH3-(CH2)6-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-NH-(CH2)6-CH3

CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-NH-(CH2)6-CH3

CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))- Bip(2-Me)-NH-(CH2)6-CH3

CH3-(CH2)10-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-NH-(CH2)6-CH3

HA-(CH2)3-Bip(2-Et)-Bip(2-Me)-NH2

H-Aib-(CH2)3-Bip(2-Et)-Bip(2-Me)-NH2 Ha-(CH2)3-Bip(2-Et)-Bip(2-Me)-NH2

H-(N(Me))A-(CH2)3-Bip(2-Et)-Bip(2-Me)-NH2

H-(N(Me))A-(N(Me))-(CH2)3-Bip(2-Et)-Bip(2-Me)-NH2

H-(N(Me))Aib-(N(Me))-(CH2)3-Bip(2-Et)-Bip(2-Me)-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)-NH2 H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-NH2

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-NH2

Des-amino-H-(N(Me))A-(N(Me))-(CΗ?)r(N(Me))-Bi'p(2-F,t)-(N(Me))-Bip(2-Me)-

NH2 Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-

Me)-NH2

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-NH-(CH2)6-

CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-NH- (CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-NH-(CH2)io-

CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-NH-

(CH2)I0-CH3 CH3-(CH2)6-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-

Me)-NH-(CH2)6-CH3

CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-

Bip(2-Me)-NH-(CH2)6-CH3 CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-

Me)-NΗ-(CH2)6-CH3

CH3-(CH2)10-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-

Bip(2-Me)-NH-(CH2)6-CH3

HA-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-Aib-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

Ha-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

Η-(N(Me))A-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))Aib-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)- 3-Pyr-Ala-OH

H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-OH .

Des-amino-H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-

(2'-Me-Ph)-3-Pyr-Ala-OH Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-COO-(CH2)io-CH3

H-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)io-CH3 CH3-(CH2)6-NH-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)6-NH-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 CH3-(CH2)io-NH-(N(Me))A-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)io-NH-(N(Me))Aib-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

HA-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-Aib-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

Ha-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(N(Me))-(CH2)3-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-Biρ(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)- 3-Pyr-Ala-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-

(2'-Me-Ph)-3-Pyr-Ala-OH Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-COO-(CH2)10-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2),o-CH3 CH3-(CH2)6-NH-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Biρ(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)jo-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

HA-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-Aib-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

Ha-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(N(Me))-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))Aib-(N(Me))-(CH2)4-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)- 3-Pyr-Ala-OH

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-

(2'-Me-Ph)-3-Pyr-Ala-OH Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-Ph)-

3-Pyr-Ala-COO-(CH2)io-CH3

H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)jo-CH3 CH3-(CH2)6-NH-H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)io-NH-H-N(Me))Aib-(N(Me))-(CH2)4-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

HAE-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-Aib-E-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

HaE-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AE-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AE-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)^3-Pyr-Ala-OH

H-(N(Me))Aib-E-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-OH

H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-OH

H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-

4-(2'-Me-Ph)-3-Pyr-Ala-OH Des-amino-H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me- Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)10-CH3 H-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)10-CH3 CH3-(CH2)6-NH-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)6-NH-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 CH3-(CH2)io-NH-(N(Me))AE-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))Aib-E-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

HAEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-Aib-EG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

HaEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AEG-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AEG-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))Aib-EG-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala- OH

H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Biρ(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-

AIa-OH

H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-OH H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-OH

H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)10-CH3 H-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-COO-(CH2)10-CH3

CH3-(CH2)6-NH-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 CH3-(CH2)6-NH-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))AEG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))Aib-EG-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

HAEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-Aib-EGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

HaEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AEGT-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-OH H-(N(Me))AEGT-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-

OH

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-Pyr-Ala-

OH

H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3- Pyr-Ala-OH

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-4-(2'-Me-Ph)-3-

Pyr-Ala-OH

H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-OH H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-OH

Des-amino-H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-OH

H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3 H-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-Me-

Ph)-3-Pyr-Ala-COO-(CH2)io-CH3

H-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-(N(Me))-4-(2'-

Me-Ph)-3-Pyr-Ala-COO-(CH2)10-CH3 CH3-(CH2)6-NH-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)6-NH-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))AEGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)- (N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

CH3-(CH2)10-NH-(N(Me))Aib-EGT-(N(Me))-(CH2)2-(N(Me))-Bip(2'-Et-4'-OMe)-

(N(Me))-4-(2'-Me-Ph)-3-Pyr-Ala-COO-(CH2)6-CH3

HA-(CH2)3-Bip(2-Me)-Biρ(2-Me)-OH

H-Aib-(CH2)3-Bip(2-Me)-Bip(2-Me)-OH Ha-(CH2)3-Bip(2-Me)-Bip(2-Me)-OH

H-(N(Me))A-(CH2)3-Bip(2-Me)-Bip(2-Me)-OH

H-(N(Me))A-(N(Me))-(CH2)3-Bip(2-Me)-Bip(2-Me)-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-Bip(2-Me)-Bip(2-Me)-OH

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Biρ(2-Me)-Bip(2-Me)-OH H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-Bip(2-Me)-OH

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-OH

Des-amino-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-

OH Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-

Me)-OH

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-COO-

(CH2)6-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-COO- (CHz)6-CH3

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-COO-

(CH2)10-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-Bip(2-Me)-COO-

(CHz)1O-CH3 CH3-(CH2)6-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-COO-(CH2)6-CH3

CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-COO-(CH2)6-CH3 CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-COO-(CH2)6-CH3

CH3-(CH2)10-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Me)-(N(Me))-

Bip(2-Me)-COO-(CH2)6-CH3

HA-(CH2)3-Bip(2-Et)-Bip(2-Me)-OH H-Aib-(CH2)3-Bip(2-Et)-Bip(2-Me)-OH

Ha-(CH2)3-Bip(2-Et)-Bip(2-Me)-OH

H-(N(Me))A-(CH2)3-Bip(2-Et)-Bip(2-Me)-OH

H-(N(Me))A-(N(Me))-(CH2)3-Bip(2-Et)-Bip(2-Me)-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-Bip(2-Et)-Bip(2-Me)-OH H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-Bip(2-Me)-OH

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-OH

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-OH

Des-amino-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)- OH

Des-amino-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Biρ(2-Et)-(N(Me))-Bip(2-

Me)-OH

H-(N(Me))A-(N(Mc))-(CH2)3-(N(Mc))-Bip(2-Et)-(N(Mc))-Bip(2-Mc)-COO-

(CHa)6-CH3 H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-COO-

(CH2)6-CH3

H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-COO-

(CHa)10-CH3

H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-Me)-COO- (CH2)IO-CH3

CH3-(CH2)6-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-

Me)-COO-(CH2)6-CH3

CH3-(CH2)6-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-

Bip(2-Me)-COO-(CH2)6-CH3 CH3-(CH2)10-NH-H-(N(Me))A-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-Bip(2-

Me)-COO-(CH2)6-CH3

CH3-(CH2)10-NH-H-(N(Me))Aib-(N(Me))-(CH2)3-(N(Me))-Bip(2-Et)-(N(Me))-

Bip(2-Me)-COO-(CH2)6-CH3 HA-(CH2)3-DVSSYLEGQAAKEFIKELEKLL

HAib-(CH2)3-DVSSYLEGQAAKEFIKELEKLL

HAibEGTFTSDVSSYLEGQ-(CH2)2-KELEKLL

HAibEGTFTSDVSSYLEGQ-(CH2)3-KELEKLL

HAibEGTFTSDVSSYLE-(CH2)2-FIKELEKLL HAibEGT-(α-Me)Phe(2-F)-TSDVSSYLE-(CH2)2-FIKELEKLL

HAib-(CH2)3-VSSYLE-(CH2)2-FIKELEKLL

HAib-(CH2)3-VSSYLE-(CH2)3-FIKELEKLL

HAib-(CH2)3-YLE-(CH2)3-FIKELEKLL

HAib-(CH2)4-YLE-(CH2)3-FIKELEKLL HAib-(CH2)4-YL-(CH2)3-FIKELEKLL

HAib-(CH2)4-Y-(CH2)3-FIKELEKLL

HAib-(CH2)4-FIKELEKLL

HAib-(CH2)5-FIKELEKLL

HAib-(CH2)6-FIKELEKLL HAib-(CH2)8-FIKELEKLL

HAib-(CH2)3-VSSYLEGQ-(CH2)3-KELEKLL

HAib-(CH2)3-VSSYLEG-(CH2)3-KELEKLL

HAib-(CH2)3-VSSYLE-(CH2)4-KELEKLL

HAib-(CH2)3-SSYLE-(CH2)4-KELEKLL HAib-(CH2)3-SYLE-(CH2)4-KELEKLL

HAib-(CH2)3-YLE-(CH2)4-KELEKLL

HAib-(CH2)3-YL-(CH2)4-KELEKLL

HAib-(CH2)3-Y-(CH2)4-KELEKLL

HAib-(CH2)5-KELEKLL HAib-(CH2)6-KELEKLL

HAib-(CH2)8-KELEKLL

7. A pharmaceutical composition comprising compounds as claimed in claims 1-6 prepared according to the processes described herein and a suitable pharmaceutically acceptable carrier(s).

8. The compounds or their pharmaceutical compositions as claimed in claims 1-7, which possess the ability to mimic the biological activity of GLP-I, more preferably mimic the GLP-IR agonist activity.

9. The compounds or their pharmaceutical compositions as claimed in any of the claims 1-7, useful for the treatment or prevention of diseases wherein GLP-IR peptide plays a patho-physiological function. 10. A method of preventing or treating diseases caused by hyperlipidaemia, hypercholesteremia, hyperglycemia, hyperinsulinemia, elevated blood levels of free fatty acids or glycerol, hypertriglyceridemia, wound healing, obesity, impaired glucose tolerance, leptin resistance, insulin resistance, diabetic complications, such as nephropathy, retinopathy, neuropathy and cataracts, comprising administering an effective, non-toxic amount of compound of formula (I) as defined in any preceding claims to a patient in need thereof.

11. The method according to any preceding claims, wherein the disease is type 2 diabetes, impaired glucose tolerance, dyslipidaemia, hypertension, obesity, atherosclerosis, hyperlipidaemia, coronary artery disease, cardiovascular disorders and other diseases wherein insulin resistance is the underlying pathophysiological mechanism.

12. A medicine for treating/reducing any of the disease conditions described in any preceding claims which comprises administering a compound of formula (I), as defined in claims 1-7 and a pharmaceutically acceptable carrier, diluent, excipients or solvate to a patient in need thereof.

13. A medicine for treating/reducing any of the disease conditions described in any preceding claims which comprises administering a compound of formula (I), as defined in claims 1-7 in combination with a suitable DPP IV inhibitor, to a patient in need thereof. 14. Use of compounds of formula (I), alone or in combination with suitable DPP IV inhibitors, their pharmaceutical compositions and medicines containing them as defined in any previous claims as a medicament suitable for the treatment of diseases mentioned in any of the aforesaid claims.