Patent ID: 6500856
Filing Date: 2002-12-31
Classification: A61P,C07D

Abstract:
A method of inhibiting activation of human T-lymphocytes in a mammal comprising administering to said mammal a therapeutically effective amount of a compound having a formula: wherein Y is OR5 or NR5R6; R1 is lower alkyl, bridged alkyl, aralkyl, cycloalkyl, a 5- or 6-membered saturated heterocycle, C1-3alkylenecycloalkyl, aryl- or heteroaryl-substituted propargyl, aryl- or heteroaryl-substituted allyl, or halocycloalkyl; R2 is hydrogen, methyl, or halo-substituted methyl; R3 is C(&boxH;O)OR7, C(&boxH;O)R7, C(&boxH;NH)NR8R9, C(&boxH;O)â€”NR8R9, aryl, or heteroaryl; R4 is hydrogen, lower alkyl, haloalkyl, cycloalkyl, or aryl; R5 and R6, independently, are hydrogen, lower alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, or alkaryl; R7 is branched or unbranched lower alkyl or aryl, and R7 can be optionally substituted with one or more of OR8, NR8R9, or SR8; and R8 and R9, same or different, are selected from the group consisting of hydrogen, lower alkyl, cycloalkyl, aryl, heteroaryl, and aralkyl, or R8 and R9 are taken together with the nitrogen to which they are attached to form a 5-membered or 6-membered nonaromatic ring; R10 is hydrogen, alkyl, haloalkyl, cycloalkyl, aryl, C(&boxH;O)alkyl, C(&boxH;O)cycloalkyl, C(&boxH;O)aryl, CH2OH, CH2Oalkyl, CHO, CN, NO2, or SO2R11; and R11 is alkyl, cycloalkyl, trifluoromethyl, aryl, aralkyl, or NR8R9.