Patent ID: 6376489
Filing Date: 2002-04-23
Classification: A61K,A61P,C07D,Y02A

Abstract:
A compound having the formula: wherein R1 is lower alkyl, bridged alkyl, aryl, heteroaryl, aralkyl, cycloalkyl, a 5- or 6-membered saturated heterocycle, C1-4alkylenearyl, C1-4alkyleneoaryl, C1-4alkyleneheteroaryl, C1-4alkylene-Het, C2-4alkyleneoaryl, C1-4alkylene bridged alkyl, C1-3alkylenecycloalkyl, substituted or unsubstituted propargyl, substituted or unsubstituted allyl, or 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, halo-cycloalkyl, C1-3alkylenecycloalkyl, a 5- or 6-membered saturated heterocycle, aryl, heteroaryl, C1-3alkyleneC(&boxH;O)R7, C(&boxH;O)C(&boxH;O)NR8R9, C1-4alkyleneOR7, C1-3alkylenearyl, SO2heteroaryl, Het, 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, or aryl; R5 is hydrogen, lower alkyl, alkynyl, haloalkyl, cycloalkyl, or aryl; R6 and R12, independently, are hydrogen, lower alkyl, aralkyl, SO2R11, or C(&boxH;O)R7; R7 is selected from the group consisting of branched or unbranched lower alkyl, heteroaryl, a heterocycle, aralkyl, and aryl, and R7 can be optionally substituted wits one or more of RO8, 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 can be taken 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, a salt and a solvate thereof, CH2Oalkyl, CHO, CN, NO2, or SO2R11; R11 is alkyl, cycloalkyl, trifluoromethyl, aryl, aralkyl, or NR8R9; salt and solvate thereof.