Patent ID: 6245743
Filing Date: 2001-06-12
Classification: A61K,C07K

Abstract:
A compound represented by the formula: ##STR47##wherein:m=0,1,2,3,4;n=0,1,2,3,4;p=0,1,2,3,4;q=0,1,2,3,4;Y=CHO, COCF.sub.3, COCF.sub.2 CF.sub.3, COCO.sub.2 R.sub.7, COCONR.sub.8 R.sub.9, B(OR.sub.10).sub.2 ; where: R.sub.7, R.sub.8, R.sub.9, R.sub.10 are the same or different and =H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, arylC.sub.1-3 alkyl, heteroarylC.sub.1-3 alkyl;A=piperdinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, C.sub.3-6 heteroaryl, or is absent;R.sub.1 =H or C.sub.1-3 alkyl;J=O or H.sub.2 ;R.sub.2 =H or C.sub.1-3 alkyl;D=N,CH, NCH.sub.2, NCH.sub.2 CH.sub.2, CHCH.sub.2 ;R.sub.3 =H or C.sub.1-3 alkyl;E=O or H.sub.2 ;R.sub.4 =H or CH.sub.3 ;Q=piperdinyl, pyrrolidinyl, C.sub.3-8 cycloalkyl, phenyl, substituted phenyl, naphthyl, pyridyl, or is absent;G=N, CH, or is H;R.sup.5 =H or C.sub.1-3 alkyl, or is absent if G is H;R.sub.6 =H or CH.sub.3 ;W=H, arylacyl, heteroarylacyl, arylC.sub.1-3 alkylsulfonyl, arylsulfonyl, substituted arylsulfonyl, arylC.sub.1-4 alkenylsulfonyl, C.sub.1-8 alkylsulfonyl, heteroarylC.sub.1-3 alkylsulfonyl, heteroarylsulfonyl, aryloxycarbonyl, C.sub.1-6 alkyloxycarbonyl, arylC.sub.1-3 alkyloxycarbonyl, arylaminocarbonyl, C.sub.1-6 -alkylaminocarbonyl, arylC.sub.1-3 alkylaminocarbonyl, HOOCC-C.sub.0-3 alkylcarbonyl, or is absent if G is H;X=H, C.sub.1-3 alkyl, NR'R"", NH--C(NR'R"").dbd.NH, NH--C(NHR').dbd.NR"", S--C(NR'R"").dbd.NH, S--C(NHR').dbd.NR"", C(NR'R"").dbd.NH, C(NHR').dbd.NR"", or CR'.dbd.NR""; where: R',R"" are the same or different and .dbd.H. C.sub.1-6 alkyl, C.sub.1-3 arylalkyl, aryl or where R'R"" forms a cyclic ring containing (CH.sub.2).sub.p where p=2-5, with the proviso that when X is H or C.sub.1-3 alkyl, then A must contain at least one N atom;Z=H, C.sub.1-3 alkyl, NR'NR"", NH--C(NR'R"")NH, NH--C(NHR').dbd.NR"", S--C(NR'R"").dbd.NH, S--C(NHR').dbd.NR"", C(NR'R"").dbd.NH, C(NHR').dbd.NR"", or CR'=NR""; where: R',R"" are the same or different and .dbd.H, C.sub.1-6 alkyl, C.sub.1-3 arylalkyl, aryl or where R'R"" forms a cyclic ring containing (CH.sub.2)p where p=2-5, with the proviso that when Z is H or C.sub.1-3 alkyl, then Q must contain at least one N atom;and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.