Patent ID: 6649593
Filing Date: 2003-11-18
Classification: A61K,A61P,C07K

Abstract:
A compound of the formula:R1â€”C(&boxH;O)-Aa1-Aa2-Aa3-R2 whereinR1 is a member selected from the group consisting of (C1-C6)alkyl, aryl(C1-C6)alkyl, aryl, (C1-C6)alkylamino, aryl(C1-C6)alkylamino, (C1-C6)alkoxy, and aryl(C1-C6)alkoxy; Aa1 is an amino acid selected from the group consisting of 3-(amidino)phenylglycine, 4-(amidino)phenylglycine, 3-(amidino)phenylalanine, 4-(amidino)phenylalanine, R and K; Aa2 is an amino acid selected from the group consisting of S, R and N; Aa3 is an amino acid selected from the group consisting of M, V and L; R2 is a radical selected from the group consisting of whereinX is a member selected from the group consisting of O, NH and Nâ€”(C1-C4)alkyl; the subscript nâ€² is an integer of from 0 to 4; R11 and R12 are members independently selected from the group consisting of H, (C1-C8)alkyl, aryl, and aryl(C1-C6)alkyl; or taken together R11 and R12 form a five- to seven-membered ring; R13 is a member selected from the group consisting of H, CF3, CH2Y, heteroaryl, CONHR16 and CO2R16; wherein Y is a leaving group and R16 is selected from the group consisting of H and (C1-C4)alkyl; and R14 and R15 are members independently selected from the group consisting of H, (C1-C6)alkyl, aryl, and aryl(C1-C6)alkyl.