US2005124548A1PendingUtilityA1
Peptide antiangiogenic drugs
Priority: May 22, 1998Filed: Jan 23, 2004Published: Jun 9, 2005
Est. expiryMay 22, 2018(expired)· nominal 20-yr term from priority
C07K 7/06
58
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Claims
Abstract
Peptides having the formula: A 0 -A 1 -A 2 -A 3 -A 4 -A 5 -A 6 -A 7 -A 8 -A 9 -A 10 wherein A 0 is selected from hydrogen or an acyl group; A 10 is a hydroxyl group or an amino acid amide; and A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , and A 9 are amino acyl residues as defined herein.
Claims
exact text as granted — not AI-modified1 . A compound of the formula:
A 0 -A 1 -A 2 -A 3 -A 4 -A 5 -A 6 -A 7 -A 8 -A 9 -A 10
or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein:
A 0 is hydrogen or an acyl group selected from:
(1) R—(CH 2 ) n —C(O)—; wherein n is an integer from 0 to 8 and R is selected from hydroxyl; methyl; N-acetylamino; methoxyl; carboxyl; cyclohexyl optionally containing a one or two double bonds and optionally substituted with one to three hydroxyl groups; and a 5- or 6-membered ring aromatic or nonaromatic ring optionally containing one or two heteroatoms selected from nitrogen, oxygen, and sulfur, wherein the ring is optionally substituted with a moiety selected from alkyl, alkoxy, and halogen; and
(2) R 1 —CH 2 CH 2 —(OCH 2 CH 2 O) p —CH 2 —C(O)—; wherein R 1 is selected from hydrogen, alkyl, and N-acetylamino, and p is an integer from 1 to 8;
A 1 is an aminoacyl residue selected from:
(1) alanyl,
(2) asparaginyl,
(3) citrullyl,
(4) glutaminyl,
(5) glutamyl,
(6) N-ethylglycyl,
(7) methionyl,
(8) N-methylalanyl,
(9) prolyl,
(10) pyro-glutamyl,
(11) sarcosyl,
(12) seryl,
(13) threonyl,
(14) —HN—(CH 2 ) q —C(O)—, wherein q is 1 to 8, and
(15) —HN—CH 2 CH 2 —(OCH 2 CH 2 O) r —CH 2 —C(O)—, wherein r is 1 to 8;
A 2 is an amino acyl residue selected from:
(1) alanyl,
(2) asparaginyl,
(3) aspartyl,
(4) glutaminyl,
(5) glutamyl,
(6) leucyl,
(7) methionyl,
(8) phenylalanyl,
(9) prolyl,
(10) seryl,
(11) —HN—(CH 2 ) q —C(O)—, wherein q is 1 to 8, and
(12) —HN—CH 2 CH 2 —(OCH 2 CH 2 O) n —CH 2 —C(O)—, wherein r is 1 to 8;
A 3 is an amino acyl residue selected from:
(1) alanyl,
(2) asparaginyl,
(3) citrullyl,
(4) cyclohexylalanyl,
(5) cyclohexylglycyl,
(6) glutaminyl,
(7) glutamyl,
(8) glycyl,
(9) isoleucyl,
(10) leucyl,
(11) methionyl,
(12) norvalyl,
(13) phenylalanyl,
(14) seryl,
(15) t-butylglycyl,
(16) threonyl,
(17) valyl,
(18) penicillaminyl, and
(19) cystyl;
A 4 is an amino acyl residue of L or D configuration selected from:
(1) allo-isoleucyl,
(2) glycyl,
(3) isoleucyl,
(4) prolyl,
(5) dehydroleucyl,
(6) D-alanyl,
(7) D-3-(naphth-1-yl)alanyl,
(8) D-3-(naphth-2-yl)alanyl,
(9) D-(3-pyridyl)-alanyl,
(10) D-2-aminobutyryl,
(11) D-allo-isoleucyl,
(12) D-allo-threonyl,
(13) D-allylglycyl,
(14) D-asparaginyl,
(15) D-aspartyl,
(16) D-benzothienyl,
(17) D-3-(4,4-biphenyl)alanyl,
(18) D-chlorophenylalanyl,
(19) D-3-(3-trifluoromethylphenyl)alanyl,
(20) D-3-(3-cyanophenyl)alanyl,
(21) D-3-(3,4-difluorophenyl)alanyl,
(22) D-citrullyl,
(23) D-cyclohexylalanyl,
(24) D-cyclohexylglycyl,
(25) D-cystyl,
(26) D-cystyl(S-t-butyl),
(27) D-glutaminyl,
(28) D-glutamyl,
(29) D-histidyl,
(30) D-homoisoleucyl,
(31) D-homophenylalanyl,
(32) D-homoseryl,
(33) D-isoleucyl,
(34) D-leucyl,
(35) D-lysyl(N-epsilon-nicotinyl),
(36) D-lysyl,
(37) D-methionyl,
(38) D-neopentylglycyl,
(39) D-norleucyl,
(40) D-norvalyl,
(41) D-omithyl,
(42) D-penicillaminyl,
(43) D-penicillaminyl(acetamidomethyl),
(44) D-penicillaminyl(S-benzyl),
(45) D-phenylalanyl,
(46) D-3-(4-aminophenyl)alanyl,
(47) D-3-(4-methylphenyl)alanyl,
(48) D-3-(4-nitrophenyl)alanyl,
(49) D-3-(3,4-dimethoxyphenyl)alanyl,
(50) D-3-(3,4,5-trifluorophenyl)alanyl,
(51) D-prolyl,
(52) D-seryl,
(53) D-seryl(O-benzyl),
(54) D-t-butylglycyl,
(55) D-thienylalanyl,
(56) D-threonyl,
(57) D-threonyl(O-benzyl),
(58) D-tryptyl,
(59) D-tyrosyl(O-benzyl),
(60) D-tyrosyl(O-ethyl),
(61) D-tyrosyl, and
(62) D-valyl;
A 5 is an amino acyl residue of L or D configuration selected from:
(1) alanyl,
(2) (3-pyridyl)alanyl,
(3) 3-(naphth-1-yl)alanyl,
(4) 3-(naphth-2-yl)alanyl,
(5) allo-threonyl,
(6) allylglycyl,
(7) glutaminyl,
(8) glycyl,
(9) histidyl,
(10) homoseryl,
(11) isoleucyl,
(12) lysyl(N-epsilon-acetyl),
(13) methionyl,
(14) norvalyl,
(15) octylglycyl,
(16) ornithyl,
(17) 3-(4-hydroxymethylphenyl)alanyl,
(18) prolyl,
(19) seryl,
(20) threonyl,
(21) tryptyl,
(22) tyrosyl,
(23) D-allo-threonyl,
(24) D-homoseryl,
(25) D-seryl,
(26) D-threonyl,
(27) penicillaminyl, and
(28) cystyl;
A 6 is an amino acyl residue of L or D configuration selected from:
(1) alanyl,
(2) 3-(naphth-1-yl)alanyl,
(3) 3-(naphth-2-yl)alanyl,
(4) (3-pyridyl)alanyl,
(5) 2-aminobutyryl,
(6) allylglycyl,
(7) arginyl,
(8) asparaginyl,
(9) aspartyl,
(10) citrullyl,
(11) cyclohexylalanyl,
(12) glutaminyl,
(13) glutamyl,
(14) glycyl,
(15) histidyl,
(16) homoalanyl,
(17) homoleucyl,
(18) homoseryl,
(19) isoleucyl,
(20) leucyl,
(21) lysyl(N-epsilon-acetyl),
(22) lysyl(N-epsilon-isopropyl),
(23) methionyl(sulfone),
(24) methionyl(sulfoxide),
(25) methionyl,
(26) norleucyl,
(27) norvalyl,
(28) octylglycyl,
(29) phenylalanyl,
(30) 3-(4-carboxyamidephenyl)alanyl,
(31) propargylglycyl,
(32) seryl,
(33) threonyl,
(34) tryptyl,
(35) tyrosyl,
(36) valyl,
(37) D-3-(naphth-1-yl)alanyl,
(38) D-3-(naphth-2-yl)alanyl,
(39) D-glutaminyl,
(40) D-homoseryl,
(41) D-leucyl,
(42) D-norvalyl,
(43) D-seryl,
(44) penicillaminyl, and
(45) cystyl;
A 7 is an amino acyl residue of L or D configuration selected from:
(1) alanyl,
(2) allylglycyl,
(3) aspartyl,
(4) citrullyl,
(5) cyclohexylglycyl,
(6) glutamyl,
(7) glycyl,
(8) homoseryl,
(9) isoleucyl,
(10) allo-isoleucyl
(11) leucyl,
(12) lysyl(N-epsilon-acetyl),
(13) methionyl,
(14) 3-(naphth-1-yl)alanyl,
(15) 3-(naphth-2-yl)alanyl,
(16) norvalyl,
(17) phenylalanyl,
(18) prolyl,
(19) seryl,
(20) t-butylglycyl,
(21) tryptyl,
(22) tyrosyl,
(23) valyl,
(24) D-allo-isoleucyl
(25) D-isoleucyl,
(26) penicillaminyl, and
(27) cystyl;
A 8 is an amino acyl residue selected from:
(1) 2-amino-4-[(2-amino)-pyrimidinyl]butanoyl,
(2) alanyl(3-guanidino),
(3) alanyl[3-pyrrolidinyl(2-N-amidino)],
(4) alanyl [4-piperidinyl(N-amidino)],
(5) arginyl,
(6) arginyl(N G N G′ diethyl),
(7) citrullyl,
(8) 3-(cyclohexyl)alanyl(4-N-isopropyl),
(9) glycyl[4-piperidinyl(N-amidino)],
(10) histidyl,
(11) homoarginyl,
(12) lysyl,
(13) lysyl(N-epsilon-isopropyl),
(14) lysyl(N-epsilon-nicotinyl),
(15) norarginyl,
(16) omithyl(N-delta-isopropyl),
(17) omithyl(N-delta-nicotinyl),
(18) omithyl[N-delta-(2-imidazolinyl)],
(19) [(4-amino(N-isopropyl)methyl)phenyl]alanyl,
(20) 3-(4-guanidinophenyl)alanyl, and
(21) 3-(4-amino-N-isopropylphenyl)alanyl;
A 9 is an amino acyl residue of L or D configuration selected from:
(1) 2-amino-butyryl,
(2) 2-amino-isobutyryl,
(3) homoprolyl,
(4) hydroxyprolyl,
(5) isoleucyl,
(6) leucyl,
(7) phenylalanyl,
(8) prolyl,
(9) seryl,
(10) t-butylglycyl,
(11) 1,2,3,4-tetrahydroisoquinoline-3-carbonyl,
(12) threonyl,
(13) valyl,
(14) D-alanyl, and
(15) D-prolyl; and
A 10 is a hydroxyl group or an amino acid amide is selected from:
(1) azaglycylamide,
(2) D-alanylamide,
(3) D-alanylethylamide,
(4) glycylamide,
(5) glycylethylamide,
(6) sarcosylamide,
(7) serylamide,
(8) D-serylamide,
(9) a group represented by the formula
and
(10) a group represented by the formula —NH—R 4 ;
wherein:
s is an integer selected from 0 to 8,
R 2 is selected from hydrogen, alkyl, and a 5- to 6-membered cycloalkyl ring;
R 3 is selected from hydrogen, hydroxy, alkyl, phenyl, alkoxy, and a 5- to 6-membered ring optionally containing from one to two heteroatoms selected from oxygen, nitrogen, and sulfur, provided that s is not zero when R 3 is hydroxy or alkoxy; and
R 4 is selected from hydrogen, hydroxy, and a 5- to 6-membered cycloalkyl ring.
2 . A compound according to claim 1 , wherein A 1 is sarcosyl, A 2 is glycyl, A 3 is valyl, A 7 is isoleucyl, A 8 is arginyl, A 9 is prolyl, and A 0 , A 4 , A 5 , A 6 , and A 10 are as defined in claim 1 .
3 . A compound according to claim 2 , wherein A 4 is an amino acyl residue having a D configuration selected from:
(1) D-alanyl, (2) D-3-(naphth-1-yl)alanyl, (3) D-3-(naphth-2-yl)alanyl, (4) D-(3-pyridyl)-alanyl, (5) D-2-aminobutyryl, (6) D-allo-isoleucyl, (7) D-allo-threonyl, (8) D-allylglycyl, (9) D-asparaginyl, (10) D-aspartyl, (11) D-chlorophenylalanyl, (12) D-3-(3-trifluoromethylphenyl)alanyl, (13) D-3-(3-cyanophenyl)alanyl, (14) D-3-(3,4-difluorophenyl)alanyl, (15) D-cyclohexylalanyl, (16) D-cyclohexylglycyl, (17) D-cystyl, (18) D-glutaminyl, (19) D-glutamyl, (20) D-histidyl, (21) D-homoisoleucyl, (22) D-homophenylalanyl, (23) D-homoseryl, (24) D-isoleucyl, (25) D-leucyl, (26) D-lysyl(N-epsilon-nicotinyl), (27) D-methionyl, (28) D-neopentylglycyl, (29) D-norleucyl, (30) D-norvalyl, (31) D-penicillaminyl, (32) D-penicillaminyl(acetamidomethyl), (33) D-penicillaminyl(S-benzyl), (34) D-phenylalanyl, (35) D-3-(4-aminophenyl)alanyl, (36) D-3-(4-methylphenyl)alanyl, (37) D-3-(4-nitrophenyl)alanyl, (38) D-3-(3,4-dimethoxyphenyl)alanyl, (39) D-3-(3,4,5-trifluorophenyl)alanyl, (40) D-prolyl, (41) D-seryl, (42) D-seryl(O-benzyl), (43) D-t-butylglycyl, (44) D-thienylalanyl, (45) D-threonyl, (46) D-threonyl(O-benzyl), (47) D-tyrosyl(O-ethyl), (48) D-tyrosyl, and (49) D-valyl.
4 . A compound according to claim 3 , wherein A 4 is an amino acyl residue having a D configuration selected from:
(1) D-allo-isoleucyl, (2) D-allylglycyl, (3) D-3-(3-cyanophenyl)alanyl, (4) D-cystyl, (5) D-isoleucyl, (6) D-leucyl, (7) D-penicillaminyl, (8) D-phenylalanyl, (9) D-3-(3,4,5-trifluorophenyl)alanyl, and (10) D-3-(4-aminophenyl)alanyl.
5 . A compound according to claim 2 , wherein A 5 is selected from:
(1) glycyl, (2) octylglycyl, (3) penicillaminyl, (4) seryl, (5) threonyl, and (6) tyrosyl.
6 . A compound according to claim 2 , wherein A 6 is selected from:
(1) glutaminyl, (2) leucyl, (3) norvalyl, and (4) seryl.
7 . A compound according to claim 3 , wherein A 0 is selected from:
(1) acetyl, (2) butyryl, (3) caproyl, (4) (4-N-acetylamino)butyryl, (5) N-acetyl-beta-alanyl, (6) (6-N-acetylamino)caproyl, (7) chloronicotinyl, (8) cyclohexylacetyl, (9) furoyl, (10) gamma-aminobutyryl, (11) 2-methoxyacetyl, (12) methylnicotinyl, (13) nicotinyl, (14) (8-N-acetylamino)-3,6-dioxo-octanoyl, (15) phenylacetyl, (16) propionyl, (17) shikimyl, (18) succinyl, and (19) tetrahydrofuroyl.
8 . A compound according to claim 3 , wherein A 10 is selected from:
(1) D-alanylamide, (2) azaglycylamide, (3) serylamide, (4) ethylamide, (5) hydroxylamide, (6) isopropylamide, (7) propylamide, (8) 2-(cyclohexyl)ethylamide, (9) 2-(1-pyrrolidine)ethylamide, (10) 1-(cyclohexyl)ethylamide, (11) 2-(methoxy)ethylamide, (12) 2-(hydroxy)ethylamide, (13) 2-(2-pyridine)ethylamide, (14) (2-pyridine)methylamide, (15) 2-(3-pyridine)ethylamide, (16) 2-(2-(1-methyl)pyrrolidine)ethylamide, (17) 2-(N-morpholine)ethylamide, and (18) cyclopropylmethylamide.
9 . A compound according to claim 1 , wherein A 4 is an amino acyl residue having a D configuration selected from:
(1) D-allo-isoleucyl, (2) D-allylglycyl, (3) D-3-(3-cyanophenyl)alanyl, (4) D-cystyl, (5) D-isoleucyl, (6) D-leucyl, (7) D-penicillaminyl, (8) D-phenylalanyl, (9) D-3-(3,4,5-trifluorophenyl)alanyl, and (10) D-3-(4-aminophenyl)alanyl; A 5 is an amino acyl residue selected from: (1) octylglycyl, (2) glycyl, (3) penicillaminyl, (4) seryl, (5) threonyl, and (6) tyrosyl; and A 6 is an amino acyl residue selected from: (1) glutaminyl, (2) leucyl, (3) norvalyl, and (4) seryl.
10 . A compound according to claim 9 , wherein A 0 is selected from:
(1) acetyl, (2) butyryl, (3) caproyl, (4) (4-N-acetylamino)butyryl, (5) N-acetyl-beta-alanyl, (6) (6-N-acetylamino)caproyl, (7) chloronicotinyl, (8) cyclohexylacetyl, (9) furoyl, (10) gamma-aminobutyryl, (11) 2-methoxyacetyl, (12) methylnicotinyl, (13) nicotinyl, (14) (8-N-acetylamino)-3,6-dioxo-octanoyl, (15) phenylacetyl, (16) propionyl, (17) shikimyl, (18) succinyl, and (19) tetrahydrofuroyl.
11 . A compound according to claim 9 , wherein A 10 is selected from:
(1) D-alanylamide, (2) azaglycylamide, (3) serylamide (4) ethylamide, (5) hydroxylamide, (6) isopropylamide, (7) propylamide, (8) 2-(cyclohexyl)ethylamide, (9) 2-(1-pyrrolidine)ethylamide, (10) 1-(cyclohexyl)ethylamide, (11) 2-(methoxy)ethylamide, (12) 2-(hydroxy)ethylamide, (13) 2-(2-pyridine)ethylamide, (14) (2-pyridine)methylamide, (15) 2-(3-pyridine)ethylamide, (16) 2-(2-(1-methyl)pyrrolidine)ethylamide, (17) 2-(N-morpholine)ethylamide, and (18) cyclopropylmethylamide.
12 . A compound, or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, selected from:
(1) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (2) pyroGlu-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (3) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 3 , (4) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (5) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 2 -(1-pyrrolidine), (6) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHethylpiperidine, (7) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHmethylcyclopropyl, (8) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH(ethyl-1-(R)-cyclohexyl), (9) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH 2 , (10) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (11) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 2 cyclohexyl, (12) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (13) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (14) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (15) N-Ac-Sar-Gly-Val-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (16) N-Ac-Sar-Gly-Val-Gly-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (17) N-Ac-Sar-Gly-Val-D-Val-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (18) N-Ac-Sar-Gly-Val-D-Ala-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (19) N-Ac-Sar-Gly-Val-D-Met-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (20) N-Ac-Sar-Gly-Val-D-Nle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (21) N-Ac-Sar-Gly-Val-D-Phe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (22) N-Ac-Sar-Gly-Val-D-Tyr-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (23) N-Ac-Sar-Gly-Val-D-4,4-Biphenylala-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (24) N-Ac-Sar-Gly-Val-D-Cha-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (25) N-Ac-Sar-Gly-Val-D-Chg-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (26) N-Ac-Sar-Gly-Val-D-4-ClPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (27) N-Ac-Sar-Gly-Val-D-Hphe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (28) N-Ac-Sar-Gly-Val-Dehydroleu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (29) N-Ac-Sar-Gly-Val-D-3-CF 3 Phe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (30) N-Ac-Sar-Gly-Val-D-pentaFPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (31) N-Ac-Sar-Gly-Val-D-3,4-diClPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (32) N-Ac-Sar-Gly-Val-D-3-ClPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (33) N-Ac-Sar-Gly-Val-D-2-Thienylala-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (34) N-Ac-Sar-Gly-Val-D-3-CNPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (35) N-Ac-Sar-Gly-Val-D-Ile-Thr-DNva-Ile-Arg-ProNHCH 2 CH 3 , (36) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (37) N-Ac-Sar-Gly-Val-D-Ile-Thr-Cha-Ile-Arg-ProNHCH 2 CH 3 , (38) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gly-Ile-Arg-ProNHCH 2 CH 3 , (39) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ala-Ile-Arg-ProNHCH 2 CH 3 , (40) N-Ac-Sar-Gly-Val-D-Ile-Thr-Val-Ile-Arg-ProNHCH 2 CH 3 , (41) N-Ac-Sar-Gly-Val-D-Ile-Thr-Abu-Ile-Arg-ProNHCH 2 CH 3 , (42) N-Ac-Sar-Gly-Val-D-Ile-Thr-Allylgly-Ile-Arg-ProNHCH 2 CH 3 , (43) N-Ac-Sar-Gly-Val-D-Ile-Thr-Octylgly-Ile-Arg-ProNHCH 2 CH 3 , (44) N-Ac-Sar-Gly-Val-D-Ile-Thr-Met-Ile-Arg-ProNHCH 2 CH 3 , (45) N-Cyclohexylacetyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (46) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (47) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (48) N-Nicotinyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (49) N-Propionyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (50) N-(MeO)acetyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (51) N-(Shikimyl)-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (52) N-(2-Furoyl)-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (53) N-Butyryl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (54) N[2-THFcarbonyl]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (55) N—[CH 3 C(O)NH—(CH 2 ) 2 —O—(CH 2 ) 2 —O—CH 2 —C(O)]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (56) N[6-N-acetyl-(CH 2 ) 5 C(O)]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (57) N-Hexanoyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (58) N-[4-N-Acetylaminobutyryl]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (59) H-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (60) N-Ac-Sar-Gly-Asn-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (61) N—[CH 3 C(O)NH—(CH 2 ) 2 —O—(CH 2 ) 2 —O—CH 2 —C(O)]-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (62) N-Ac-Pro-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (63) N-Ac-Gly-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (64) N-Ac-Ala-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (65) N-Ac-NEtGly-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (66) N-Ac-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (67) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ser-Ile-Arg-ProNHCH 2 CH 3 , (68) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-D-AlaNH 2 , (69) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-D-ProNHCH 2 CH 3 , (70) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-AbuNHCH 2 CH 3 , (71) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Phe-NHCH 2 CH 3 , (72) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Tic-NHCH 2 CH 3 , (73) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Hyp-NHCH 2 CH 3 , (74) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Aib-NHCH 2 CH 3 , (75) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-D-Ala-NHCH 2 CH 3 , (76) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pip-NHCH 2 CH 3 , (77) N-Ac-Sar-Gly-Val-D-Tyr(Et)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (78) N-Ac-Sar-Gly-Val-D-Cys(tBu)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (79) N-Ac-Sar-Gly-Val-D-Cys-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (80) N-Ac-Sar-Gly-Val-D-Tyr(Bzl)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (81) N-Ac-Sar-Gly-Val-D-Ser(Bzl)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (82) N-Ac-Sar-Gly-Val-D-1 Nal-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (83) N-Ac-Sar-Gly-Val-D-tButylgly-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (84) N-Ac-Sar-Gly-Val-D-Orn-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (85) N-Ac-Sar-Gly-Val-D-Thr(Bzl)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (86) N-Ac-Sar-Gly-Val-D-2Nal-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (87) N-Ac-Sar-Gly-Val-D-Phe(4-Me)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (88) N-Ac-Sar-Gly-Val-D-Phe(3,4-diMeO)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (89) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (90) N-Ac-Sar-Gly-Val-D-Phe(4-NO 2 )-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (91) N-Ac-Sar-Gly-Val-D-Pen-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (92) N-Ac-Sar-Gly-Val-D-Pen(Acm)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (93) N-Ac-Sar-Gly-Val-D-Abu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (94) N-Ac-Sar-Gly-Val-D-Phe(4-NH 2 )-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (95) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Ala-Arg-ProNHCH 2 CH 3 , (96) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Met-Arg-ProNHCH 2 CH 3 , (97) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Phe-Arg-ProNHCH 2 CH 3 , (98) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Tyr-Arg-ProNHCH 2 CH 3 , (99) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Nva-Arg-ProNHCH 2 CH 3 , (100) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Asp-Arg-ProNHCH 2 CH 3 , (101) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Gly-Arg-ProNHCH 2 CH 3 , (102) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Lys(Ac)-Arg-ProNHCH 2 CH 3 , (103) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Leu-Arg-ProNHCH 2 CH 3 , (104) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-2Nal-Arg-ProNHCH 2 CH 3 , (105) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-1 Nal-Arg-ProNHCH 2 CH 3 , (106) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Allylgly-Arg-ProNHCH 2 CH 3 , (107) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Cit-Arg-ProNHCH 2 CH 3 , (108) N-Ac-Sar-Gly-Val-D-Leu-Ala-Nva-Ile-Arg-ProNHCH 2 CH 3 , (109) N-Ac-Sar-Gly-Val-D-Leu-Pro-Nva-Ile-Arg-ProNHCH 2 CH 3 , (110) N-Ac-Sar-Gly-Val-D-Leu-Trp-Nva-Ile-Arg-ProNHCH 2 CH 3 , (111) N-Ac-Sar-Gly-Val-D-Leu-Tyr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (112) N-Ac-Sar-Gly-Val-D-Leu-Nva-Nva-Ile-Arg-ProNHCH 2 CH 3 , (113) N-Ac-Sar-Gly-Val-D-Leu-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (114) N-Ac-Sar-Gly-Val-D-Leu-Lys(Ac)-Nva-Ile-Arg-ProNHCH 2 CH 3 , (115) N-Ac-Sar-Gly-Val-D-Leu-2Nal-Nva-Ile-Arg-ProNHCH 2 CH 3 , (116) N-Ac-Sar-Gly-Val-D-Leu-1Nal-Nva-Ile-Arg-ProNHCH 2 CH 3 , (117) N-Ac-Sar-Gly-Val-D-Leu-Octylgly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (118) N-Ac-Sar-Gly-Val-D-Leu-Gln-Nva-Ile-Arg-ProNHCH 2 CH 3 , (119) N-Ac-Sar-Gly-Val-D-Leu-Met-Nva-Ile-Arg-ProNHCH 2 CH 3 , (120) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (121) N-Ac-Sar-Gly-Val-D-Leu-Allylgly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (122) N-Ac-Sar-Gly-Val-D-Leu-Ile-Nva-Ile-Arg-ProNHCH 2 CH 3 , (123) N-Ac-Sar-Gly-Val-D-Leu-D-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (124) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ile-Ile-Arg-ProNHCH 2 CH 3 , (125) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nle-Ile-Arg-ProNHCH 2 CH 3 , (126) N-Ac-Sar-Gly-Val-D-Ile-Thr-Cit-Ile-Arg-ProNHCH 2 CH 3 , (127) N-Ac-Sar-Gly-Val-D-Ile-Thr-Met(O 2 )-Ile-Arg-ProNHCH 2 CH 3 , (128) N-Ac-Sar-Gly-Val-D-Ile-Thr-Arg-Ile-Arg-ProNHCH 2 CH 3 , (129) N-Ac-Sar-Gly-Val-D-Ile-Thr-Tyr-Ile-Arg-ProNHCH 2 CH 3 , (130) N-Ac-Sar-Gly-Val-D-Ile-Thr-Glu-Ile-Arg-ProNHCH 2 CH 3 , (131) N-Ac-Sar-Gly-Val-D-Ile-Thr-Lys(Ac)-Ile-Arg-ProNHCH 2 CH 3 , (132) N-Ac-Sar-Gly-Val-D-Ile-Thr-Propargylgly-Ile-Arg-ProNHCH 2 CH 3 , (133) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (134) N-Ac-Sar-Gly-Val-D-Leu-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (135) N-Ac-Bala-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (136) N-Phenylacetyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (137) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-AzaglyNH 2 , (138) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Sar-NHCH 2 CH 3 , (139) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-SerNH 2 , (140) N-Succinyl-Sar-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (141) N-Ac-Sar-Ala-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (142) N-Ac-Sar-Leu-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (143) N-Ac-Sar-Phe-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (144) N-Ac-Sar-Glu-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (145) N-Ac-Sar-Pro-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (146) N-Ac-Sar-Asn-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (147) N-Ac-Sar-Asp-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (148) N-Ac-Asn-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (149) N-Ac-Gln-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (150) N-Ac-Ser-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (151) N-Ac-Cit-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (152) N-Ac-Glu-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (153) N-Ac-Gaba-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (154) N-Ac-Bala-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (155) N-Ac-Gln-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (156) N-Ac-Sar-Gly-Gly-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (157) N-Ac-Sar-Gly-Glu-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (158) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (159) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (160) N-Succinyl-Sar-Gly-Val-D-Leu-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (161) N-Succinyl-Sar-Gly-Val-D-Leu-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (162) N-Ac-Sar-Gly-Val-D-Leu-Thr-Asp-Ile-Arg-ProNHCH 2 CH 3 , (163) N-Ac-Sar-Gly-Val-D-Ile-Thr-Asp-Ile-Arg-ProNHCH 2 CH 3 , (164) N-Ac-Sar-Gly-Val-D-Ile-Thr-Asn-Ile-Arg-ProNHCH 2 CH 3 , (165) N-Ac-Sar-Gly-Val-D-Ile-Thr-Met(O)-Ile-Arg-ProNHCH 2 CH 3 , (166) N-Ac-Sar-Gly-Val-D-Leu-Thr-Asn-Ile-Arg-ProNHCH 2 CH 3 , (167) N-Ac-Sar-Gly-Val-D-Thr-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (168) N-Ac-Sar-Gly-Val-D-Ser-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (169) N-Ac-Sar-Gly-Val-D-Hser-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (170) N-Ac-Sar-Gly-Val-D-Gln-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (171) N-Ac-Sar-Gly-Val-D-Asn-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (172) N-Ac-Sar-Gly-Val-D-Cit-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (173) N-Ac-Sar-Gly-Val-D-Hcit-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (174) N-Ac-Sar-Gly-Val-D-Hle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (175) N-Ac-Sar-Gly-Val-D-Neopentylgly-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (176) N-Ac-Sar-Gly-Val-D-Ile-Thr-Phe(4-CONH 2 )-Ile-Arg-ProNHCH 2 CH 3 , (177) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-His-ProNHCH 2 CH 3 , (178) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Lys(Isp)-ProNHCH 2 CH 3 , (179) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Lys(Nic)-ProNHCH 2 CH 3 , (180) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Orn(Nic)-ProNHCH 2 CH 3 , (181) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Orn(Isp)-ProNHCH 2 CH 3 , (182) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Phe(4-NIsp)-ProNHCH 2 CH 3 , (183) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Cha(4-NIsp)-ProNHCH 2 CH 3 , (184) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Harg-ProNHCH 2 CH 3 , (185) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Norarg-ProNHCH 2 CH 3 , (186) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Cit-ProNHCH 2 CH 3 , (187) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Lys-ProNHCH 2 CH 3 , (188) N-Ac-Sar-Gly-Val-D-Ile-Phe(4-CH 2 OH)-Nva-Ile-Arg-ProNHCH 2 CH 3 , (189) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Phe(4-guanidino)-ProNHCH 2 CH 3 , (190) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Aminopyrimidinylbutanoyl-Pro-NHCH 2 CH 3 , (191) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Phe(4-CH 2 NHIsp)-ProNHCH 2 CH 3 , (192) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Gly [4-Pip(N-amidino)]-Pro-NHCH 2 CH 3 , (193) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Ala[4-Pip(N-amidino)]-Pro-NHCH 2 CH 3 , (194) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Ala(3-guanidino)-ProNHCH 2 CH 3 , (195) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Ala(3-pyrrolidinylamidino)-Pro-NHCH 2 CH 3 , (196) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Orn(2-imidazo)-ProNHCH 2 CH 3 , (197) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (198) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (199) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (200) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (201) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (202) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (203) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (204) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-Pro-D-AlaNH 2 , (205) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (206) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (207) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (208) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (209) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (210) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-SarNH 2 , (211) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-Pro-SarNH 2 , (212) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-SarNH 2 , (213) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-SarNH 2 , (214) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Ser-Ile-Arg-Pro-D-AlaNH 2 , (215) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Ser-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (216) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Ser-Ile-Arg-ProNHCH 2 CH 3 , (217) N-Ac-Sar-Gly-Val-D-Ile-Thr-Orn(Ac)-Ile-Arg-ProNHCH 2 CH 3 , (218) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-AzaglyNH 2 , (219) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-Pro-AzaglyNH 2 , (220) N-Ac-Sar-Gly-Val-D-allo le-Thr-Gln-Ile-Arg-Pro-AzaglyNH 2 , (221) N-(2-THFcarbonyl)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-Pro-NHCH 2 CH 3 , (222) N-(2-THFcarbonyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (223) N-(2-THFcarbonyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-NHCH 2 CH 3 , (224) N-(2-THFcarbonyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (225) N-(2-THFcarbonyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (226) N-(2-THFcarbonyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-NHCH 2 (CH 3 ) 2 , (227) N-(6-Ac-Aca)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (228) N-(6-Ac-Aca)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (229) N-(6-Ac-Aca)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (230) N-(6-Ac-Aca)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (231) N-(6-Ac-Aca)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (232) N-(6-Ac-Aca)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (233) N-(4-Ac-Gaba)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (234) N-(4-Ac-Gaba)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (235) N-(4-Ac-Gaba)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (236) N-(4-Ac-Gaba)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (237) N-(4-Ac-Gaba)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (238) N-(4-Ac-Gaba)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-NHCH 2 (CH 3 ) 2 , (239) N-(2-Furoyl)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (240) N-(2-Furoyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (241) N-(2-Furoyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (242) N-(2-Furoyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (243) N-(2-Furoyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (244) N-(2-Furoyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (245) N-(Shikimyl)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (246) N-(Shikimyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (247) N-(Shikimyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (248) N-(Shikimyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (249) N-(Shikimyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (250) N-(Shikimyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (251) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-Pro-NHCH 2 CH 3 , (252) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (253) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-NHCH 2 CH 3 , (254) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (255) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-D-AlaNH 2 , (256) N-(2-Me-Nicotinyl)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-NHCH 2 (CH 3 ) 2 , (257) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Leu-Ile-Arg-Pro-D-AlaNH 2 , (258) N-Ac-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (259) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (260) N-Ac-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-Pro-D-AlaNH 2 , (261) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-Pro-D-AlaNH 2 , (262) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (263) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (264) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (265) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Leu-Ile-Arg-Pro-D-AlaNH 2 , (266) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-Pro-AzaglyNH 2 , (267) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHethyl-(1-pyrrolidine), (268) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNH(ethyl-1-cyclohexyl), (269) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHethyl-(1-pyrrolidine), (270) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNH(ethyl-1-cyclohexyl), (271) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNH(ethyl-1-cyclohexyl), (272) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (273) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (274) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ser-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (275) N-Ac-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (276) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (277) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (278) N-Succinyl-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (279) N-Ac-Sar-Gly-Val-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (280) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 2 OCH 3 , (281) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Allygly-Ile-Arg-ProNHCH 2 CH 3 , (282) N-Ac-Sar-Gly-Val-D-Ile-Thr-Allygly-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (283) N-Ac-Sar-Gly-Val-D-Ile-Thr-Allygly-Ile-Arg-Pro-D-AlaNH 2 , (284) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Allygly-Ile-Arg-Pro-D-AlaNH 2 , (285) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Allygly-Ile-Arg-Pro-D-AlaNH 2 , (286) N-Ac-Sar-Gly-Val-D-Ile-Ser-Allygly-Ile-Arg-Pro-ProNHCH 2 CH 3 , (287) N-Ac-Sar-Gly-Val-D-Leu-Ser-Allygly-Ile-Arg-Pro-ProNHCH 2 CH 3 , (288) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-SarNH 2 , (289) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHOH, (290) N-Ac-Sar-Gly-Val-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (291) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (292) N-Ac-Sar-Gly-Val-D-Leu-Hser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (293) N-Ac-Sar-Gly-Gln-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (294) N-Ac-Sar-Gly-Nva-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (295) N-Ac-Sar-Gly-Ile-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (296) N-Ac-Sar-Gly-Phe-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (297) N-Ac-Sar-Gly-Leu-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (298) N-Ac-Sar-Gly-Ser-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (299) N-Ac-Thr-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (300) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Ala-Ile-Arg-ProNHCH 2 CH 3 , (301) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ala-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (302) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ala-Ile-Arg-Pro-D-AlaNH 2 , (303) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Ala-Ile-Arg-Pro-D-AlaNH 2 , (304) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Ala-Ile-Arg-Pro-D-AlaNH 2 , (305) N-Ac-Sar-Gly-Val-D-Ile-Ser-Ala-Ile-Arg-ProNHCH 2 CH 3 , (306) N-Ac-Sar-Gly-Val-D-Leu-Ser-Ala-Ile-Arg-ProNHCH 2 CH 3 , (307) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Val-Ile-Arg-ProNHCH 2 CH 3 , (308) N-Ac-Sar-Gly-Val-D-Ile-Thr-Val-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (309) N-Ac-Sar-Gly-Val-D-Ile-Thr-Val-Ile-Arg-Pro-D-AlaNH 2 , (310) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Val-Ile-Arg-Pro-D-AlaNH 2 , (311) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Val-Ile-Arg-Pro-D-AlaNH 2 , (312) N-Ac-Sar-Gly-Val-D-Ile-Ser-Val-Ile-Arg-ProNHCH 2 CH 3 , (313) N-Ac-Sar-Gly-Val-D-Leu-Ser-Val-Ile-Arg-ProNHCH 2 CH 3 , (314) N-Ac-Sar-Gly-Val-D-alloIle-Thr-D-Nva-Ile-Arg-ProNHCH 2 CH 3 , (315) N-Ac-Sar-Gly-Val-D-Ile-Thr-D-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (316) N-Ac-Sar-Gly-Val-D-Ile-Thr-D-Nva-Ile-Arg-Pro-D-AlaNH 2 , (317) N-Ac-Sar-Gly-Val-D-alloIle-Thr-D-Nva-Ile-Arg-Pro-D-AlaNH 2 , (318) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-D-Nva-Ile-Arg-Pro-D-AlaNH 2 , (319) N-Ac-Sar-Gly-Val-D-Ile-Ser-D-Nva-Ile-Arg-ProNHCH 2 CH 3 , (320) N-Ac-Sar-Gly-Val-D-Leu-Ser-D-Nva-Ile-Arg-ProNHCH 2 CH 3 , (321) N-Ac-Sar-Gly-Val-D-Ile-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (322) N-Ac-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (323) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-Pro-D-AlaNH 2 , (324) N-Ac-Sar-Gly-Val-D-Ile-Ser-Nva-Ile-Arg-Pro-D-AlaNH 2 , (325) N-Succinyl-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (326) N-Succinyl-Sar-Gly-Val-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (327) N-Succinyl-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (328) N-Succinyl-Sar-Gly-Val-D-Ile-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (329) N-Ac-Sar-Gly-Val-D-Ile-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (330) N-Ac-Sar-Gly-Val-D-Leu-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (331) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (332) N-Ac-Sar-Gly-Val-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (333) N-Ac-Sar-Gly-Val-D-Leu-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (334) N-Ac-Sar-Gly-Val-D-Ile-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (335) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (336) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (337) N-Succinyl-Sar-Gly-Val-D-alloIle-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (338) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Nva-Ile-Arg-ProNHCH 2 (C 1 H 3 ) 2 , (339) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Nva-Ile-Arg-Pro-D-AlaNH 2 , (340) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (341) N-Ac-Sar-Gly-Val-D-alloIle-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (342) N-Ac-Sar-Gly-Val-D-Ile-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (343) N-Ac-Sar-Gly-Val-D-alloIle-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (344) N-Ac-Sar-Gly-Val-D-Leu-Gly-Gln-Ile-Arg-ProNHCH 2 CH 3 , (345) N-Ac-Sar-Gly-Val-D-Ile-Gly-Gln-Ile-Arg-ProNHCH 2 CH 3 , (346) N-Ac-Sar-Gly-Val-D-alloIle-Gly-Gln-Ile-Arg-ProNHCH 2 CH 3 , (347) N-Ac-Sar-Gly-Val-D-Ile-Tyr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (348) N-Ac-Sar-Gly-Val-D-alloIle-Tyr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (349) N-Ac-Sar-Gly-Val-D-Leu-Tyr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (350) N-Ac-Sar-Gly-Val-D-Ile-Tyr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (351) N-Ac-Sar-Gly-Val-D-alloIle-Tyr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (352) N-Ac-Sar-Gly-Val-D-Ser-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (353) N-Ac-Sar-Gly-Val-D-Thr-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (354) N-Ac-Sar-Gly-Val-D-Gln-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (355) N-Ac-Sar-Gly-Val-D-Asn-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (356) N-Ac-Sar-Gly-Val-D-Arg-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (357) N-Ac-Sar-Gly-Val-D-3-Pal-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (358) N-Ac-Sar-Gly-Val-D-Glu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (359) N-Ac-Sar-Gly-Val-D-Asp-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (360) N-Ac-Sar-Gly-Val-D-His-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (361) N-Ac-Sar-Gly-Val-D-Hser-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (362) N-Ac-Sar-Gly-Val-D-alloThr-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (363) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-D-Ile-Arg-ProNHCH 2 CH 3 , (364) N-Ac-Sar-Gly-Val-D-Ser-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (365) N-Ac-Sar-Gly-Val-D-Thr-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (366) N-Ac-Sar-Gly-Val-D-alloThr-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (367) N-Ac-Sar-Gly-Val-D-Ser-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (368) N-Ac-Sar-Gly-Val-D-Thr-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (369) N-Ac-Sar-Gly-Val-D-alloThr-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (370) N-Ac-Sar-Gly-Val-D-alloThr-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (371) N-Ac-Sar-Gly-Val-D-Thr-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (372) N-(6-Ac-Aca)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (373) N-(6-Ac-Aca)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (374) N-(4-Ac-Gaba)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (375) N-(4-Ac-Gaba)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (376) N-(2-Furoyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (377) N-(2-Furoyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (378) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (379) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (380) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (381) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (382) N-(2-Me-nicotinyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (383) N-(2-Me-nicotinyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (384) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHethyl-1-(R)-cyclohexyl, (385) N-Ac-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHethyl-1-(R)-cyclohexyl, (386) N-Ac-Sar-Gly-Val-DIle-Thr-Ser-Ile-Arg-ProNHethyl-1-(R)-cyclohexyl, (387) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHethyl-1-(R)-cyclohexyl, (388) N-Ac-Sar-Gly-Val-D-Leu-Ser-Ser-Ile-Arg-ProNHethyl-1-(R)-cyclohexyl, (389) N-Ac-Sar-Gly-Val-DIle-Thr-Nva-Ile-Arg-ProNHethyl-1-(S)-cyclohexyl, (390) N-Ac-Sar-Gly-Val-D-Pen-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (391) N-Ac-Sar-Gly-Val-D-Pen-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (392) N-Ac-Sar-Gly-Val-D-Pen-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (393) N-Ac-Sar-Gly-Val-D-Pen-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (394) N-Succinyl-Sar-Gly-Val-D-Pen-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (395) N-Ac-Sar-Gly-Val-D-Pen-Ser-Nva-Ile-Arg-Pro-D-AlaNH 2 , (396) N-Ac-Sar-Gly-Val-D-Pen-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (397) N-Ac-Sar-Gly-Val-D-Pen-Gly-Gln-Ile-Arg-ProNHCH 2 CH 3 , (398) N-Ac-Sar-Gly-Val-D-Pen-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (399) N-Ac-Sar-Gly-Val-D-Pen-Thr-Ser-Ile-Arg-ProNHCH 2 CH 3 , (400) N-Ac-Sar-Gly-Val-D-Pen-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (401) N-Ac-Sar-Gly-Val-D-Pen-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (402) N-Succinyl-Sar-Gly-Val-D-Pen-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (403) N-Succinyl-Sar-Gly-Val-D-Pen-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (404) N-Succinyl-Sar-Gly-Val-D-Pen-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (405) N-Ac-Sar-Gly-Val-D-Cys-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (406) N-Ac-Sar-Gly-Val-D-Cys-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (407) N-Ac-Sar-Gly-Val-D-Cys-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (408) N-Ac-Sar-Gly-Val-D-Cys-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (409) N-Ac-Sar-Gly-Val-D-Cys-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (410) N-Succinyl-Sar-Gly-Val-D-Cys-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (411) N-Ac-Sar-Gly-Val-D-Cys-Ser-Nva-Ile-Arg-Pro-D-AlaNH 2 , (412) N-Ac-Sar-Gly-Val-D-Cys-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (413) N-Ac-Sar-Gly-Val-D-Cys-Gly-Gln-Ile-Arg-ProNHCH 2 CH 3 , (414) N-Ac-Sar-Gly-Val-D-Cys-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (415) N-Ac-Sar-Gly-Val-D-Cys-Thr-Ser-Ile-Arg-ProNHCH 2 CH 3 , (416) N-Ac-Sar-Gly-Val-D-Cys-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (417) N-Ac-Sar-Gly-Val-D-Cys-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (418) N-Succinyl-Sar-Gly-Val-D-Cys-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (419) N-Succinyl-Sar-Gly-Val-D-Cys-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (420) N-Ac-Sar-Gly-Pen-DIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (421) N-Ac-Sar-Gly-Cys-DIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (422) N-Ac-Sar-Gly-Pen-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (423) N-Ac-Sar-Gly-Pen-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (424) N-Ac-Sar-Gly-Pen-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (425) N-Ac-Sar-Gly-Pen-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (426) N-Ac-Sar-Gly-Pen-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (427) N-Ac-Sar-Gly-Pen-D-Ile-Thr-Nva-Ile-Arg-Pro-D-AlaNH 2 , (428) N-Succinyl-Gly-Pen-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (429) N-Succinyl-Sar-Gly-Pen-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (430) N-Succinyl-Sar-Gly-Pen-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (431) N-Ac-Sar-Gly-Val-D-Leu-Pen-Nva-Ile-Arg-ProNHCH 2 CH 3 , (432) N-Ac-Sar-Gly-Val-D-Ile-Pen-Nva-Ile-Arg-ProNHCH 2 CH 3 , (433) N-Ac-Sar-Gly-Val-D-alloIle-Pen-Nva-Ile-Arg-ProNHCH 2 CH 3 , (434) N-Ac-Sar-Gly-Val-D-Ile-Pen-Gln-Ile-Arg-ProNHCH 2 CH 3 , (435) N-Ac-Sar-Gly-Val-D-Ile-Pen-Ser-Ile-Arg-ProNHCH 2 CH 3 , (436) N-Ac-Sar-Gly-Val-D-Ile-Pen-Leu-Ile-Arg-ProNHCH 2 CH 3 , (437) N-Ac-Sar-Gly-Val-D-Ile-Pen-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (438) N-Ac-Sar-Gly-Val-D-Ile-Pen-Nva-Ile-Arg-Pro-D-AlaNH 2 , (439) N-Succinyl-Sar-Gly-Val-D-Ile-Pen-Nva-Ile-Arg-ProNHCH 2 CH 3 , (440) N-Succinyl-Sar-Gly-Val-D-Ile-Pen-Gln-Ile-Arg-ProNHCH 2 CH 3 , (441) N-Succinyl-Sar-Gly-Val-D-Ile-Pen-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (442) N-Ac-Sar-Gly-Val-D-Ile-Thr-Pen-Ile-Arg-ProNHCH 2 CH 3 , (443) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Pen-Ile-Arg-ProNHCH 2 CH 3 , (444) N-Ac-Sar-Gly-Val-D-Leu-Thr-Pen-Ile-Arg-ProNHCH 2 CH 3 , (445) N-Ac-Sar-Gly-Val-D-Ile-Thr-Pen-Ile-Arg-Pro-D-AlaNH 2 , (446) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Pen-Ile-Arg-ProNHCH 2 CH 3 , (447) N-Ac-Sar-Gly-Val-D-Ile-Thr-Pen-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (448) N-Ac-Sar-Gly-Val-D-Leu-Ser-Pen-Ile-Arg-ProNHCH 2 CH 3 , (449) N-Ac-Sar-Gly-Val-D-Leu-Gly-Pen-Ile-Arg-ProNHCH 2 CH 3 , (450) N-Succinyl-Sar-Gly-Val-D-Leu-Ser-Pen-Ile-Arg-ProNHCH 2 CH 3 , (451) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (452) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (453) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (454) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Ser-Leu-Ile-Arg-ProNHCH 2 CH 3 , (455) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Ser-Nva-Ile-Arg-Pro-D-AlaNH 2 , (456) N-Succinyl-Sar-Gly-Val-D-Phe(3,4,5-triF)-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (457) N-Succinyl-Sar-Gly-Val-D-Phe(3,4,5-triF)-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (458) N-Succinyl-Sar-Gly-Val-D-Phe(3,4,5-triF)-Thr-Gln-Ile-Arg-ProNH—CH 2 (CH 3 ) 2 , (459) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (460) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Ser-Ser-Ile-Arg-ProNHCH 2 CH 3 , (461) N-Ac-Sar-Ala-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (462) N-Ac-Sar-Ala-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (463) N-Ac-Sar-Ala-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (464) N-Ac-Sar-Ala-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (465) N-Ac-Sar-Ala-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (466) N-Succinyl-Sar-Ala-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (467) N-Succinyl-Sar-Ala-Val-D-Ile-Thr-Gln-Nva-Ile-Arg-ProNHCH 2 CH 3 , (468) N-Succinyl-Sar-Ala-Val-D-Ile-Thr-Gln-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (469) N-Succinyl-Sar-Ala-Val-D-Ile-Thr-Gln-Nva-Ile-Arg-Pro-D-AlaNH 2 , (470) N-(3-Ac-Bala)-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (471) N-(3-Ac-Bala)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (472) N-(3-Ac-Bala)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (473) N-(3-Ac-Bala)-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-DAlaNH 2 , (474) N-(3-Ac-Bala)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-Pro-DAlaNH 2 , (475) N-(3-Ac-Bala)-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (476) N-(3-Ac-Bala)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (477) N-(3-Ac-Bala)-Sar-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (478) N-(3-Ac-Bala)-Sar-Gly-Val-D-Pen-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (479) N-(3-Ac-Bala)-Sar-Gly-Val-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (480) N-(3-Ac-Bala)-Sar-Ala-Val-D-alloIle-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (481) N-(3-Ac-Bala)-Sar-Ala-Val-D-Ile-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (482) N-(3-Ac-Bala)-Sar-Ala-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (483) N-(3-Ac-Bala)-Sar-Ala-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 CH 3 , (484) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-OH, (485) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-Pro-OH, (486) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Ile-Arg-Pro-OH, (487) N-Ac-Sar-Gly-Val-D-Pen-Thr-Nva-Ile-Arg-Pro-OH, (488) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Thr-Nva-Ile-Arg-Pro-OH, (489) N-Ac-Sar-Gly-Val-D-Ile-Thr-Gln-Ile-Arg-Pro-OH, (490) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-Pro-OH, (491) N-Ac-Sar-Ala-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-OH, (492) N-Ac-Sar-Gly-Val-D-Ile-Ser-Gln-Ile-Arg-Pro-OH, (493) N-Succinyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-OH, (494) N-Succinyl-Sar-Gly-Val-D-Leu-Thr-Gln-Ile-Arg-Pro-OH, (495) N-Ac-Sar-Gly-Asp-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (496) N-Ac-Sar-Gly-Ala-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (497) N-Ac-Sar-Gly-Cha-D-Leu-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (498) N-Ac-Sar-Gly-Met-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (499) N-Ac-Cit-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 ,N-Ac-Sar-Gly-Val-D-Ile-Thr-Hser-Ile-Arg-ProNHCH 2 CH 3 , (501) N-Ac-Sar-Gly-Val-DalloIle-His-Nva-Ile-Arg-ProNHCH 2 CH 3 , (502) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-n-Butyl, (503) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-iso-Butyl, (504) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-iso-Amyl, (505) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-n-hexyl, (506) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-(3,3-dimethyl)butyl, (507) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-(2-ethoxy)ethyl, (508) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-(2-isopropoxy)ethyl, (509) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-(3-methoxy)propyl, (510) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-(cyclopentyl)methyl, and (511) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH-cyclohexyl.
13 . A compound according to claim 12 , selected from:
(1) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (2) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 2 -(1-pyrrolidine), (3) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH(ethyl-1-(R)-cyclohexyl), (4) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNH 2 , (5) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (6) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (7) N-Ac-Sar-Gly-Val-D-Val-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (8) N-Ac-Sar-Gly-Val-D-Nle-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (9) N-Ac-Sar-Gly-Val-D-Phe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (10) N-Ac-Sar-Gly-Val-D-Cha-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (11) N-Ac-Sar-Gly-Val-D-3,4-diClPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (12) N-Ac-Sar-Gly-Val-D-3-ClPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (13) N-Ac-Sar-Gly-Val-D-2-Thienylala-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (14) N-Ac-Sar-Gly-Val-D-3-CNPhe-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (15) N-Ac-Sar-Gly-Val-D-Ile-Thr-Cha-Ile-Arg-ProNHCH 2 CH 3 , (16) N[2-THF-C(O)]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (17) N[6-N-acetyl-(CH 2 ) 5 C(O)]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (18) N-Hexanoyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (19) N-[4-N-Acetylaminobutyryl]-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (20) N—[CH 3 C(O)NH—(CH 2 ) 2 —O—(CH 2 ) 2 —O—CH 2 —C(O)]-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (21) N-Ac-Pro-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (22) N-Ac-NEtGly-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (23) N-Ac-Sar-Gly-Val-D-Ile-Thr-Leu-Ile-Arg-ProNHCH 2 CH 3 , (24) N-Ac-Sar-Gly-Val-D-Ile-Thr-Ser-Ile-Arg-ProNHCH 2 CH 3 , (25) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-D-AlaNH 2 , (26) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Lys(Ac)-Arg-ProNHCH 2 CH 3 , (27) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Leu-Arg-ProNHCH 2 CH 3 , (28) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-1Nal-Arg-ProNHCH 2 CH 3 , (29) N-Ac-Sar-Gly-Val-D-Leu-Thr-Nva-Allylgly-Arg-ProNHCH 2 CH 3 , (30) N-Ac-Sar-Gly-Val-D-Leu-Ala-Nva-Ile-Arg-ProNHCH 2 CH 3 , (31) N-Ac-Sar-Gly-Val-D-Leu-Trp-Nva-Ile-Arg-ProNHCH 2 CH 3 , (32) N-Ac-Sar-Gly-Val-D-Leu-Tyr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (33) N-Ac-Sar-Gly-Val-D-Leu-Gly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (34) N-Ac-Sar-Gly-Val-D-Leu-2Nal-Nva-Ile-Arg-ProNHCH 2 CH 3 , (35) N-Ac-Sar-Gly-Val-D-Leu-1Nal-Nva-Ile-Arg-ProNHCH 2 CH 3 , (36) N-Ac-Sar-Gly-Val-D-Leu-Octylgly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (37) N-Ac-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 CH 3 , (38) N-Ac-Sar-Gly-Val-D-Leu-Allylgly-Nva-Ile-Arg-ProNHCH 2 CH 3 , (39) N-Ac-Sar-Gly-Val-D-Leu-D-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (40) N-Ac-Sar-Gly-Val-D-Ile-Thr-Tyr-Ile-Arg-ProNHCH 2 CH 3 , (41) N-Ac-Sar-Gly-Val-D-Ile-Thr-Glu-Ile-Arg-ProNHCH 2 CH 3 , (42) N-Ac-Sar-Gly-Val-D-Ile-Thr-Propargylgly-Ile-Arg-ProNHCH 2 CH 3 , (43) N-Ac-Sar-Gly-Val-D-alloIle-Thr-Gln-Ile-Arg-ProNHCH 2 CH 3 , (44) N-Ac-Bala-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (45) N-Phenylacetyl-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (46) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-AzaglyNH 2 , (47) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-SerNH 2 , (48) N-(6-Ac-Aca)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (49) N-(6-Ac-Aca)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (50) N-(4-Ac-Gaba)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (51) N-(4-Ac-Gaba)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (52) N-(2-Furoyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (53) N-(2-Furoyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (54) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (55) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (56) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (57) N-(Shikimyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (58) N-(2-Me-nicotinyl)-Sar-Gly-Val-D-Leu-Ser-Gln-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (59) N-(2-Me-nicotinyl)-Sar-Gly-Val-D-Leu-Ser-Nva-Ile-Arg-ProNHCH 2 (CH 3 ) 2 , (60) N-Ac-Sar-Gly-Val-D-Ile-Thr-Nva-Ile-Arg-Pro-OH, (61) N-Ac-Sar-Ala-Val-D-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (62) N-Ac-Sar-Gly-Val-D-Pen-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , (63) N-Ac-Sar-Gly-Val-D-Phe(3,4,5-triF)-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 , and (64) N-Ac-Sar-Gly-Val-D-Phe(4-NH 2 )-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3 .
14 . A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
15 . A method of treating a patient in need of anti-angiogenesis therapy comprising administering to the patient in need a therapeutically effective amount of a compound in claim 1 .
16 . A composition for the treatment of a disease selected from cancer, arthritis, psoriasis, angiogenesis of the eye associated with infection or surgical intervention, macular degeneration and diabetic retinopathy comprising a peptide as defined in claim 1 in combination with a pharmaceutically acceptable carrier.
17 . A method of isolating a receptor from an endothelial cell comprising binding a peptide as defined in claim 1 to the receptor to form a peptide receptor complex; isolating the peptide receptor complex; and purifying the receptor.Join the waitlist — get patent alerts
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