Patent ID: 6313156
Filing Date: 2001-11-06
Classification: A61P,C07D

Abstract:
A compound having the formula: ##STR12##wherein R.sup.1 is lower alkyl, bridged alkyl, aralkyl, cycloalkyl, a 5- or 6-membered saturated heterocycle, C.sub.1-3 alkylenecycloalkyl, aryl- or heteroaryl-substituted propargyl, aryl- or heteroaryl-substituted allyl, or halocycloalkyl;R.sup.2 is hydrogen, methyl, or halo-substituted methyl;R.sup.3 is selected from the group consisting of C(.dbd.O)OR.sup.7, C(.dbd.O)R.sup.7, C(.dbd.NH)NR.sup.8 R.sup.9, C(.dbd.O)NR.sup.8 R.sup.9, lower alkyl, bridged alkyl, cycloalkyl, haloalkyl, halo-cycloalkyl, C.sub.1-3 alkylenecycloalkyl, a substituted or unsubstituted 5- or 6-membered saturated heterocycle, aryl, heteroaryl, heteroarylSO.sub.2, aralkyl, alkaryl, heteroaralkyl, heteroalkaryl, C.sub.1-3 alkylene-C(.dbd.O)OR', C(.dbd.O)C.sub.1-3 alkyleneC(.dbd.O)OR.sup.7, C.sub.1-3 alkyleneheteroaryl, C(.dbd.O)C(.dbd.O)OR.sup.7, C(.dbd.O)C.sub.1-3 alkyleneC(.dbd.O)OR.sup.7, C(.dbd.O)C.sub.1-3 alkyleneNHC(.dbd.O)OR.sup.7, C(.dbd.O)C.sub.1-3 alkyleneNH.sub.2, and NHC(.dbd.O) OR.sup.7 ;R.sup.4 is hydrogen, lower alkyl, haloalkyl, cycloalkyl, aryl, C(.dbd.O)R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, or SR.sup.8 ;R.sup.5 is hydrogen, lower alkyl, haloalkyl, cycloalkyl, or aryl;R.sup.7 is selected from the group consisting of cycloalkyl, branched or unbranched lower alkyl, heteroaryl, aryl, a substituted or unsubstituted heterocycle, and substituted or unsubstituted aralkyl, and R.sup.7 is optionally substituted with one or more of RO.sup.8, NR.sup.8 R.sup.9, or SR.sup.8 ; andR.sup.8 and R.sup.9, same or different, are selected from the group consisting of hydrogen, lower alkyl, cycloalkyl, aryl, heteroaryl, alkaryl, heteroaralkyl, heteroalkaryl, and aralkyl, or R.sup.8 and R.sup.9 are taken together form a 4-membered to 7-membered ring;R.sup.10 is hydrogen, alkyl, haloalkyl, cycloalkyl, aryl, C(.dbd.O)alkyl, C(.dbd.O)cycloalkyl, C(.dbd.O)aryl, C(.dbd.O)Oalkyl, C(.dbd.O)Ocycloalkyl, C(.dbd.O)aryl, CH.sub.2 OH, CH.sub.2 Oalkyl, CHO, CN, NO.sub.2, or SO.sub.2 R.sup.11 ; andR.sup.11 is alkyl, cycloalkyl, trifluoromethyl, aryl, aralkyl, or NR.sup.8 R.sup.9.