Patent ID: 6329365
Filing Date: 2001-12-11
Classification: A61K,A61P,C07K,Y02A

Abstract:
A compound represented by formula (III): ##STR102##wherein: ##STR103##provided that if R.sup.5 is --OH, then Y may also be: ##STR104##C is benzo, wherein any hydrogen bound to any ring atom is optionally replaced by --R.sup.4 ;R.sup.1 is -aryl, -heteroaryl, -alkylaryl, -alkylheteroaryl, or -cycloalkyl, wherein each aryl or heteroaryl is optionally singly or multiply substituted with R.sup.17 ;R.sup.2 is a bond, --C(O)--, --C(O)C(O)--, --S(O).sub.2 --, --OC(O)--, --N(H)C(O)--, --N(H)S(O).sub.2 --, --N(H)C(O)C(O)--, --CH.dbd.CHC(O)--, --OCH.sub.2 C(O)--, --N(H)CH.sub.2 C(O)--, --N(R.sup.19)C(O)--, --N(R.sup.19)S(O).sub.2 --, --N(R.sup.19)C(O)C(O)--, --N(R.sup.19)CH.sub.2 C(O)--, or --C(O)C(.dbd.NOR.sup.11)--, provided that when R.sup.2 is not a bond, R.sup.2 is bonded to the NH attached to the 7-membered ring through carbonyl or sulfonyl;R.sup.3 is -aryl, -heteroaryl, -cycloalkyl, -alkyl, --N(alkyl).sub.2, ##STR105##R.sup.4 is --OH, --F, --Cl, --Br, --I, --NO.sub.2, --CN, --NH.sub.2, --CO.sub.2 H, --C(O)NH.sub.2, --N(H)C(O)H, --N(H)C(O)NH.sub.2, -alkyl, -cycloalkyl, -perfluoroalkyl, --O-alkyl, --N(H)(alkyl), --N(alkyl).sub.2, --C(O)N(H)alkyl, --C(O)N(alkyl).sub.2, --N(H)C(O)alkyl, --N(H)C(O)N(H)alkyl, --N(H)C(O)N(alkyl).sub.2, --S-alkyl, --S(O.sub.2)alkyl, --C(O)alkyl, --CH.sub.2 NH.sub.2, --CH.sub.2 N(H)alkyl, or CH.sub.2 N(alkyl).sub.2 ;R.sup.5 is --OH, --OR.sup.8, or --N(H)OH;R.sup.6 is --H, --CH.sub.2 OR.sup.9, --CH.sub.2 SR.sup.10, --CH.sub.2 NHR.sup.9, --CH.sub.2 N(R.sup.9)R.sup.12, --CHN.sub.2, --CH.sub.2 F, --CH.sub.2 Cl, --C(O)N(R.sup.11)R.sup.12, --R.sup.13, or --R.sup.14 ;R.sup.8 is -alkyl, -cycloalkyl, -aryl, -heteroaryl, -alkylaryl, -alkylheteroaryl, or alkylheterocycle;R.sup.9 is --H, --C(O)aryl, --C(O)heteroaryl, --C(O)alkylaryl, --C(O)alkylheteroaryl, -alkylaryl, -alkylheteroaryl, -aryl, -heteroaryl, or --P(O)R.sup.15 R.sup.16 ;R.sup.10 is -alkylaryl, -aryl, -heteroaryl, or -alkylheteroaryl;each R.sup.11 and R.sup.12 is independently --H, -alkyl, -aryl, -heteroaryl, -cycloalkyl, -alkylaryl, or -alkylheteroaryl;R.sup.13 is -alkylaryl, -alkenylaryl, -alkynylaryl, or -alkylheteroaryl;R.sup.14 is ##STR106##wherein any hydrogen bound to (i) is optionally replaced with R.sup.17 and any hydrogen bound to (ii) is optionally replaced with R.sup.17, R.sup.18 or R.sup.20 ;each R.sup.15 and R.sup.16 is independently --H, --OH, -alkyl, -aryl, -heteroaryl, -cycloalkyl, -alkylaryl, -alkylheteroaryl, --Oalkyl, --Oaryl, --Oheteroaryl, --Oalkylaryl, or --Oalkylheteroaryl;R.sup.17 is --OH, --F, --Cl, --Br, --I, --NO.sub.2, --CN, --NH.sub.2, --CO.sub.2 H, --C(O)NH.sub.2, --N(H)C(O)H, --N(H)C(O)NH.sub.2, --S(O).sub.2 NH.sub.2, --C(O)H, -alkyl, -cycloalkyl, -perfluoroalkyl, --O-alkyl, --N(H)alkyl, --N(alkyl).sub.2, --CO.sub.2 alkyl, --C(O)N(H)alkyl, --C(O)N(alkyl).sub.2, --N(H)C(O)alkyl, --N(H)C(O)N(H)alkyl, --N(H)C(O)N(alkyl).sub.2, --S(O).sub.2 N(H)alkyl, --S(O).sub.2 N(alkyl).sub.2, --S-alkyl, --S(O.sub.2)alkyl, or --C(O)alkyl;R.sup.18 is -aryl, -heteroaryl, -alkylaryl, -alkylheteroaryl, --O-aryl, --O-heteroaryl, --O-alkylaryl, --O-alkylheteroaryl, --N(H)aryl, --N(aryl).sub.2, --N(H)heteroaryl, --N(heteroaryl).sub.2, --N(H)alkylaryl, --N(alkylaryl).sub.2, --N(H)alkylheteroaryl, --N(alkylheteroaryl).sub.2, --S-aryl, --S-heteroaryl, --S-alkylaryl, --S-alkylheteroaryl, --C(O)aryl, --C(O)heteroaryl, --C(O)alkylaryl, --C(O)alkyheteroaryl, --CO.sub.2 aryl, --CO.sub.2 heteroaryl, --CO.sub.2 alkylaryl, --CO.sub.2 alkylheteroaryl, --C(O)N(H)aryl, --C(O)N(aryl).sub.2, --C(O)N(H)heteroaryl, --C(O)N(heteroaryl).sub.2, --C(O)N(H)alkylaryl, --C(O)N(alkylaryl).sub.2, --C(O)N(H)alkylheteroaryl, --C(O)N(alkylheteroaryl).sub.2, --S(O).sub.2 -aryl, --S(O).sub.2 -heteroaryl, --S(O).sub.2 -alkylaryl, --S(O).sub.2 alkylheteroaryl, --S(O).sub.2 N(H)aryl, --S(O.sub.2)N(H)heteroaryl, --S(O.sub.2)N(H)alkylaryl, --SO).sub.2 N(H)alkylheteroaryl, --S(O).sub.2 N(aryl).sub.2, --S(O).sub.2 N(H)(heteroaryl).sub.2, --S(O).sub.2 N(alkylaryl).sub.2, --S(O).sub.2 N(alkylheteroaryl).sub.2, --N(H)C(O)N(H)aryl, --N(H)C(O)N(H)heteroaryl, --N(H)C(O)N(H)alkylaryl, --N(H)C(O)N(H)alkylheteroaryl, --N(H)C(O)N(aryl).sub.2, --N(H)C(O)N(heteroaryl).sub.2, --N(H)C(O)N(alkylaryl).sub.2, --N(H)C(O)N(alkylheteroaryl).sub.2 ;R.sup.19 is --H, -alkyl, -cycloalkyl, -aryl, -heteroaryl, -alkylaryl, -alkylheteroaryl, or -alkylheterocycle;R.sup.20 is -alkyl-R.sup.18 ;m is 0 or 1; andX is O or S.