Patent ID: 6737408
Filing Date: 2004-05-18
Classification: A61K,C07K,H01L

Abstract:
A therapeutic composition comprising:a therapeutically effective amount of a compound having the formula: â€ƒwherein: each R1 and R2, independently, is H, C1-C12 alkyl, C6-C18 aryl, C1-C18 acyl, C7-C18 aralkyl, C7-C18 alkaryl or a dihydrotrigonellinate group; A1 is a D or L-amino acid selected from the group consisting of Cys, Leu, Dap, Trp, Gln, a tethered amino acid with an indole ring, Phe, Hyp, a derivative of Trp selected from the group consisting of N-Me-Trp, nor Trp, beta Me-Trp, 2-Cl-Trp, and 5-X-Trp, where X is selected from the group consisting of CN, Br, NH2, COOH, CH2NH2 and CH2-CH2NH2; C&agr;Me-Trp, C&agr;Me-Gln, Des-amino-Trp, Pyr, Bth, Nal, Tcc, Asn, Nva, Abu, Tyr, Tic-OH, Tip, and Dip; A2 is a D or L-amino acid selected from the group consisting of Cys, Trp, Arg, N&agr;-Me-Arg, C&agr;Me-Arg, Orn, Cit, hArg(R)2, where R is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, and alkylaryl, Lys-&egr;-NH-R, where R is selected from the group consisting of alkyl, aryl, aralkyl, and alkylaryl; A3 is a D or L-amino acid selected from the group consisting of Glu, N-Me-Tyr, C&agr;Me-Tyr, Tic-OH, Tic, Dip, Trp, Phe, des-carboxylic-Tyr (tyramine), and Tyr-(R), where R is hydrogen or lipophilic group; W is OH, â€”Nâ€”R3R4, or OR5, where R3, R4 and R5, independently, is H, C1-C12 alkyl, C6-C18 aryl, C1-C12 acyl, C7-C18 aralkyl, or C7-C18 alkaryl, or a pharmaceutically acceptable salt thereof; and each bond between two amino acids or amino acid derivatives, represented by a dash (â€œâˆ’â€ ), can be either a peptide bond or a pseudopeptide bond; and a pharmaceutically acceptable carrier substance; wherein said therapeutically effective amount of said compound in said composition attenuates Neuropeptide Y (NPY) mediated physical responses.