Patent ID: 6258793
Filing Date: 2001-07-10
Classification: A61P,C07H

Abstract:
A compound having the formula: ##STR85##wherein X.sup.1.dbd.O, S, NR.sup.6 ; Y.dbd.O, S, N--CN, N--OR.sup.7 ; Z.dbd.O, S, NR.sup.8 ;R.sup.1 is a monocyclic group containing from 3 to 15 carbon atoms wherein one carbon atom is substituted with an atom or molecule selected from the group consisting of N, O, and S--(O).sub.0-2 and wherein R.sup.1 does not contain an epoxide group;R.sup.2 is selected from the group consisting of hydrogen, halo, CF.sub.3, and cyano;R.sup.3 and R.sup.4 are each independently selected from the group consisting of hydrogen, and --(CO)--R' and --(CO)--R"" wherein R', and R"" are independently selected from the group consisting of C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, which alkyl, alkenyl, alkynyl, aryl, heterocyclyl, and heteroaryl are optionally substituted with 1 to 3 substituents independently selected from the group consisting of halo, NO.sub.2, heterocyclyl, aryl, heteroaryl, CF.sub.3, CN, OR.sup.20, SR.sup.20, N(R.sup.20).sub.2, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, SO.sub.2 NR.sup.20 COR.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 COR.sup.22, NR.sup.20 CO.sub.2 R.sup.22, NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 C(NR.sup.20)NHR.sup.23, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, CONR.sup.20 SO.sub.2 R.sup.22, NR.sup.20 SO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, OCONR.sup.20 SO.sub.2 R.sup.22, OC(O)R.sup.20, C(O)OCH.sub.2 OC(O)R.sup.20, and OCON(R.sup.20).sub.2 and each optional heteroaryl, aryl, and heterocyclyl substituent is further optionally substituted with halo, NO.sub.2, alkyl, CF.sub.3, amino, mono- or di-alkylamino, alkyl or aryl or heteroaryl amide, NR.sup.20 COR.sup.22, NR.sup.20 SO.sub.2 R.sup.22, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, NR.sup.20 CON(R.sup.20).sub.2, OC(O)R.sup.20, OC(O)N(R.sup.20).sub.2, SR.sup.20, S(O)R.sup.22, SO.sub.2 N(R.sup.20).sub.2, CN, or OR.sup.20 ;R.sup.5 is selected from the group consisting of C.sub.1-5 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, which alkyl, alkenyl, alkynyl, aryl, heterocyclyl and heteroaryl are optionally substituted with from 1 to 3 substituents independently selected from the group consisting of halo, alkyl, NO.sub.2, heterocyclyl, aryl, heteroaryl, CF.sub.3, CN, OR.sup.20, SR.sup.20, N(R.sup.20).sub.2, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, S(O).sub.3 R.sup.20, P(O)(OR.sup.20).sub.2, SO.sub.2 NR.sup.20 COR.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 COR.sup.22, NR.sup.20 CO.sub.2 R.sup.22, NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 C(NR.sup.20)NHR.sup.23, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, CONR.sup.20 SO.sub.2 R.sup.22, NR.sup.20 SO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, OCONR.sub.20 SO.sub.2 R.sup.22, OC(O)R.sup.20, C(O)OCH.sub.2 OC(O)R.sup.20, and OCON(R.sup.20).sub.2 and each optional alkyl, heteroaryl, aryl, and heterocyclyl substituent is further optionally substituted with halo, NO.sub.2, alkyl, CF.sub.3, amino, mono- or di-alkylamino, alkyl or aryl or heteroaryl amide, NR.sup.20 COR.sup.22, NR.sup.20 SO.sub.2 R.sup.22, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, NR.sup.20 CON(R.sup.20).sub.2, OC(O)R.sup.20, OC(O)N(R.sup.20).sub.2, S(O).sub.3 R.sup.20, P(O)(OR.sup.20).sub.2, SR.sup.20, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, CN, or OR.sup.20 ;R.sup.6 is selected from the group consisting of H, C.sub.1-6 alkyl and aryl optionally substituted with halo, CN, CF.sub.3, OR.sup.20 and N(R.sup.20).sub.2 ;R.sup.7 and R.sup.8 are each independently selected from the group consisting of H, and C.sub.1 -C.sub.15 alkyl optionally substituted with one aryl substituent that is optionally substituted with halo or CF.sub.3 ;R.sup.20 is selected from the group consisting of H, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, alkenyl, alkynyl, heterocyclyl, aryl, and heteroaryl substituents are optionally substituted with from 1 to 3 substituents independently selected from halo, alkyl, mono- or dialkylamino, alkyl or aryl or heteroaryl amide, CN, O--C.sub.1-6 alkyl, CF.sub.3, aryl, and heteroaryl; andR.sup.22 is selected from the group consisting of hydrogen, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, alkenyl, alkynyl, heterocyclyl, aryl, and heteroaryl substituents are optionally substituted with from 1 to 3 substituents independently selected from the group consisting of halo, alkyl, mono- or dialkylamino, alkyl or aryl or heteroaryl amide, CN, O--C.sub.1-6 alkyl, CF.sub.3, aryl, and heteroaryl wherein when Z.dbd.NR.sup.8 then R.sup.5 and R.sup.8 may bond to form a 4 or 5 or 6 membered saturated or unsaturated ring; wherein when X.sup.1.dbd.NR.sup.6 and when Z.dbd.NR.sup.8, then R.sup.6 and R.sup.8 may bond to form a 4 or 5 or 6 membered saturated or unsaturated ring; and wherein when X.sup.1.dbd.NR.sup.6 and Y.dbd.O or S, then R.sup.5 and R.sup.6 may bond to form a 5 or a 6 membered saturated or unsaturated ring.