Patent ID: 6455562
Filing Date: 2002-09-24
Classification: A61P,C07D

Abstract:
A method of inhibiting IL-1&bgr; release by monocytes in a mammal comprising administering to said mammal a therapeutically effective amount of a compound having a formula: wherein Y is O or NR4; R1 is selected from the group consisting of 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, and halocycloalkyl; R2 is hydrogen, methyl, or halo-substituted methyl; R3 is selected from the group consisting of C(&boxH;O)OR7, C(&boxH;O)R7, C(&boxH;NH)NR8R9, C(&boxH;O)NR8R9, lower alkyl, bridged alkyl, cycloalkyl, haloalkyl, halocycloalkyl, C1-3alkylenecycloalkyl, a 5- or 6-membered saturated heterocycle, aryl, heteroaryl, heteroarlySO2, aralkyl, alkaryl, heteroaralkyl, heteroalkaryl, C1-3alkyleneC(&boxH;O)OR7, C(&boxH;O)C1-3alkyleneC(&boxH;O)OR7, C1-3alkyleneheteroaryl, C(&boxH;O)C(&boxH;O)OR7, C(&boxH;O)C1-3alkyleneC(&boxH;O)OR7, C(&boxH;O)C1-3alkyleneNH(C&boxH;O)OR7, C(&boxH;O)C1-3alkyleneNH2, and NHC(&boxH;O)OR7; R4 is hydrogen, lower alkyl, haloalkyl, cycloalkyl, aryl, or heteroaryl; R7 is selected from the group consisting of cycloalkyl, branched or unbranched lower alkyl, heteroaryl, a heterocycle, aralkyl, and aryl, and R7 can be optionally substituted with one or more of OR8, NR8R9, or SR8; R8 and R9, same or different, are selected from the group consisting of hydrogen, lower alkyl, cycloalkyl, aryl, heteroaryl, alkaryl, heteroaralkyl, heteroalkaryl, and aralkyl, or R8 and R9 together form a 4-membered to 7-membered ring; R10 is hydrogen, alkyl, haloalkyl, cycloalkyl, aryl, C(&boxH;O)alkyl, C(&boxH;O)cycloalkyl, C(&boxH;O)aryl, C(&boxH;O)Oalkyl, C(&boxH;O)Ocycloalkyl, C(&boxH;O)aryl, CH2OH, CH2Oalkyl, CHO, CN, NO2, or SO2R11; and R11 is alkyl, cycloalkyl, trifluoromethyl, aryl, aralkyl, or NR8R9.