Patent ID: 6534495
Filing Date: 2003-03-18
Classification: A61K,A61P,C07K

Abstract:
A compound having the formula IR1SO2â€”Bâ€”Xâ€”Zâ€”C(O)â€”Yâ€ƒâ€ƒ(I) whereinR1 is R2OOCâ€”(CHR2)mâ€” or R2NHâ€”COâ€”(CHR2)mâ€” or is selected from (1-12C)alkyl, (2-12C)alkenyl, which groups may optionally be substituted with (3-8C)cycloalkyl, (1-6C)alkoxy, OH, COOR2, CF3 or halogen, and from (6-14C)aryl, (7-15C)aralkyl and (8-16C)aralkenyl, the aryl groups of which may optionally be substituted with (1-6C)alkyl, (3-8C)cycloalkyl, (1-6C)alkoxy, OH, COOH, CF3 or halogen; m is 1, 2 or 3; each group R2 is independently H, (1-12C)alkyl, (3-8C)cycloalkyl, (6-14C)aryl or (7-15C)aralkyl, the aryl groups of which may be substituted with (1-6C)alkyl, (1-6C)alkoxy or halogen; B is a bond, an amino-acid of the formula â€”NHâ€”CH[(CH2)pC(O)OH]â€”C(O)â€” or an ester derivative thereof wherein p is 1, 2 or 3, Gly, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an L-amino acid with a hydrophobic side chain, serine, threonine, a cyclic amino acid optionally having an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, â€”NR2â€”CH2â€”C(O)â€” or the fragment wherein n is 2, 3, or 4, W is CH or N and R3 is H or (1-6C)alkyl; Z is lysine or 4-aminocyclohexylglycine; Y is â€”NH-(1-6C)alkylene-C6H5, the phenyl group of which may be substituted with (1-6C)alkyl, (1-6C)alkoxy or halogen, or Y is â€”OR4 or â€”NR5R6, wherein R4 is H, (2-6C)alkyl or benzyl, and R5 and R6 are independently H or (1-6C)alkyl or R5 and R6 together are (3-6C)alkylene; or a prodrug thereof, which after administration are metabolized into the active compounds, or a pharmaceutically acceptable salt thereof.