Patent ID: 6797710
Filing Date: 2004-09-28
Classification: A61K,A61P,C07D,C07K

Abstract:
A serine protease inhibitor of formula (XL), wherein(Râ€³â€²)1 and (Râ€³â€²)2 are independently H, lower alkyl, aryl, heteroaryl, cycloalkyl or lower alkyl substituted by one or more substituents selected from CONH2, COO-(lower alkyl), aryl, as heteroaryl and cycloalkyl; or (Râ€³â€²)2 is lower alkanoyl;(Râ€³â€²)3 is H, COOH, CONH2, COO-(lower alkyl), CONH-(lower alkyl) or CON(lower alkyl)2; (Râ€³â€²)4, (Râ€³â€²)5 and (Râ€³â€²)6 are independently H, lower alkyl, aryl, aralkyl or cycloalkyl; or (Râ€³â€²)4 and/or one of (Râ€³â€²)5 and (Râ€³â€²)6 is heteroaryl or lower alkyl substituted with OH, SO2H, SO3H, guanidino, aryl-(lower alkoxy), lower alkoxy or lower alkylthio;or (Râ€³â€²)2 together with (Râ€³â€²)4 forms a tri- or tetramethylene group, in which (a) a methylene group may be replaced by S, SO or SO2 or may be substituted with OH, lower alkyl, lower alkenyl or carboxy-(lower alkyl) or (b) one of the methylene groups may be substituted with lower alkenyl and the other with (lower alkyl)-COOH;and at least one of (Râ€³â€²)1, (Râ€³â€²)2, (Râ€³â€²)4, (Râ€³â€²)5 and (Râ€³â€²)6 is the group of formula Q,wherein Q is represented by formula wherein the substructure is a structure selected from wherein X is O or S;Xâ€² being independently CH or N; andm is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an unsubstituted or substituted nitrogen or carbon atom.