Patent ID: 6770741
Filing Date: 2004-08-03
Classification: A61K,C07D,C07K

Abstract:
A peptide having the formula:N-A-B-C-D-E-F-G-H-I-J-Cn wherein N is hydrogen; A and B are independently selected from the group consisting of L-Arg, D-Arg, L-Gln, D-Gln, D-Asn, L-Asn, N-&egr;-acetyl-D-lysine, &egr;-acetyl-L-lysine, NG-p-tosyl-Arg, NG-nitro-Arg, Lysâ€”Lys, acetyl-D-Arg, L-Citrulline, L-Lys, Sar, and D-Lys; C and D are a direct bond or are independently selected from the group consisting of Pro, dehydroPro, 4Hyp, Tic, Aoc, Ala, L-azetidine-2-carboxylic acid, Eac, Gly, Thz, Oic, and Aib; E is a direct bond or is selected from the group consisting of Gly, Ala, Thr, and Ser; F is selected from the group consisting of Phe, Thi, Leu, Ile, Tic, Oic, homoPhe, phenylGly, &bgr;-cyclohexylalanine, Nal, and Val; G is a direct bond or is selected from the group consisting of Ser, Thr, 4Hyp, Gly, Val, and Ala; H is a compound of the D-configuration having the formula: â€ƒwherein R is selected from the group consisting of C1-C6 alkyl, substituted C1-C6 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl substituted C1-C6 alkyl, an aryl group, a substituted aryl group, an arylalkyl group, and a group of the formula R1NHC(o)â€” where R1 is C1-C6 alkyl or aryl, and where X is either, sulfur or oxygen; I is selected from the group consisting of Oic, Aoc, Thz, Tic, L-indoline-2-carboxylic acid, octahydro-1H-isoindole-1-carboxylic acid, pipecolinic acid, Pro, 4Hyp, azetidine-2-carboxylic acid, Aib, Leu, Ile, Val, Thi, Phe, and homoPhe, and compounds of the following formula: â€ƒwherein R is selected from the group consisting of C1-C6 alkyl, substituted C1-C6 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl substituted C1-C6 alkyl, an aryl group, a substituted aryl group, an arylalkyl group, and a group of the formula R1NHC(o)â€” where R1 is C1-C6 alkyl or aryl, and where X is either sulfur or oxygen; J is selected from the group consisting of Arg, Orn, Asn, Gln, N-&egr;-acetyl-Lys, N-&dgr;-acetyl-Orn, and Lys; Cn is a hydroxyl group or a C-terminal extension selected from the group consisting of amide, alkoxy group, an acidic, basic, or neutral aliphatic aromatic, cyclic amino acid residue of the D- or L-configuration, and a peptide extension composed of D- or L-amino acids; and pharmaceutically acceptable salts thereof.