Patent ID: 6452009
Filing Date: 2002-09-17
Classification: C07D,C40B,G01N

Abstract:
A single compound of the formula: wherein: R1 and R2 are, independently, selected from the group consisting of a hydrogen atom, C1 to C12 alkyl, C1 to C12 substituted alkyl, C2 to C12 alkenyl, C2 to C12 substituted alkenyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, C7 to C18 phenylalkyl, C7 to C18 substituted phenylalkyl, C1 to C12 heterocyclicalkyl, C1 to C12 substituted heterocyclicalkyl, heteroaryl, substituted heteroaryl, heterocycle and substituted heterocycle; R3 is selected from the group consisting of C1 to C12 alkyl, C1 to C12 substituted alkyl, phenyl, substituted phenyl, heteroaryl, substituted heteroaryl, carboxy, protected carboxy, cyano, protected (monosubstituted) amino, (disubstituted) amino, C1 to C12 acyl, C1 to C12 substituted acyl, C1 to C12 alkoxycarbonyl, C1 to C12 substituted alkoxycarbonyl, C1 to C12 alkylaminocarbonyl, C1 to C12 substituted alkylaminocarbonyl, phenylaminocarbonyl, substituted phenylaminocarbonyl, heterocycle, substituted heterocycle, naphthyl, substituted naphthyl, C3 to C7 cycloalkyl, C3 to C7 substituted cycloalkyl, C5 to C7 cycloalkenyl and C5 to C7 substituted cycloalkenyl; R4 is selected from the group consisting of the formula: -D-W-E- â€ƒwherein: W is absent or selected from the group consisting of C3 to C7 cycloalkylene, C3 to C7 substituted cycloalkylene, C5 to C7 cycloalkenylene, C5 to C7 substituted cycloalkenylene, arylene, substituted arylene, heterocyclene, substituted heterocyclene, heteroarylene and substituted heteroarylene; and D, which is directly attached to the nitrogen depicted in the formula, and E, one of which may be absent, are independently absent or independently selected from the group consisting of C1 to C12 alkylene, C2 to C12 alkenylene, C2 to C12 alkynylene, C1 to C12 substituted alkylene, C2 to C12 substituted alkenylene, C2 to C12 substituted alkynylene, C3 to C7 cycloalkylene, C3 to C7 substituted cycloalkylene, C5 to C7 cycloalkenylene, C5 to C7 substituted cycloalkenylene, C7 to C18 phenylalkylene, C7 to C18 substituted phenylalkylene, C1 to C12 heterocyclicalkylene and C1 to C12 substituted heterocyclicalkylene; and the formula: â€ƒwherein: R8 and R9 are together or independently selected from the group consisting of a hydrogen atom, C1 to C12 alkyl, C2 to C12 alkenyl, C2 to C12 alkynyl, C1 to C12 substituted alkyl, C2 to C12 substituted alkenyl, C2 to C12 substituted alkynyl, C1 to C12 acyl, C1 to C12 substituted acyl, C3 to C7 cycloalkyl, C3 to C7 substituted cycloalkyl, C5 to C7 cycloalkenyl, C5 to C7 substituted cycloalkenyl, a heterocyclic ring, substituted heterocyclic ring, heteroaryl, substituted heteroaryl, C7 to C18 phenylalkyl, C7 to C16 substituted phenylalkyl, C1 to C12 heterocyclicalkyl, C1 to C12 substituted heterocyclicalkyl, C7 to C18 phenylalkoxy, C7 to C18 substituted phenylalkoxy, phenyl, substituted phenyl, naphthyl, substituted naphthyl, cyclic C2 to C7 alkylene, substituted cyclic C2 to C7 alkylene, cyclic C2 to C7 heteroalkylene, substituted cyclic C2 to C7 heteroalkylene, carboxy, protected carboxy, hydroxymethyl, protected hydroxymethyl, amino and amino-protecting group; and m and n are independently 0, 1, 2, 3 or 4; R5 is absent or selected from the group consisting of â€”Oâ€”, â€”Sâ€”, amino, (monosubstituted) amino, protected (monosubstituted) amino, the formula -D-W-E- as defined herein, the formula K-L-M, wherein K and M are, independently, selected from the group consisting of amino, (monosubstituted) amino and protected (monosubstituted) amino, and L is absent or selected from the group consisting of C1 to C12 alkylene, C1 to C12 substituted alkylene, C2 to C12 alkenylene, C2 to C12 substituted alkenylene, C3 to C7 cycloalkylene, C3 to C7 substituted cycloalkylene, C5 to C7 cycloalkenylene, C5 to C7 substituted cycloalkenylene, arylene, substituted arylene, heterocyclene, substituted heterocyclene, heteroarylene and substituted heteroarylene, and the formula â€”NR12â€”, wherein R12 is selected from a hydrogen atom, C1 to C12 alkyl., C1 to C12 substituted alkyl, C7 to C18 phenylalkyl, C7 to C18 substituted phenylalkyl, C1 to C12 heterocyclicalkyl, C1 to C12 substituted heterocyclicalkyl, C7 to C18 phenylalkoxy, C7 to C18 substituted phenylalkoxy C1 to C12 acyl, C1 to C12 substituted acyl, phenylsulfonyl, substituted phenylsulfonyl, C1 to C10 alkylsulfonyl, C1 to C10 substituted alkylsulfonyl, C1 to C12 alkylaminocarbonyl, C1 to C12 substituted alkylaminocarbonyl, phenylaminocarbonyl, substituted phenylaminocarbonyl, C1 to C12 alkylaminothiocarbonyl, C1 to C12 substituted alkylaminothiocarbonyl, phenylaminothiocarbonyl, substituted phenylaminothiocarbonyl, amino, (monosubstituted) amino, (disubstituted) amino, protected (monosubstituted) amino, Ci to C12 alkylamino, C1 to C12 alkyl (monosubstituted) amino, C1 to C12 alkyl(disubstituted) amino, C1 to C12 alkyl protected (monosubstituted) amino, C1 to C12 substituted alkylamino, C1 to C12 substituted alkyl(monosubstituted) amino, C1 to C12 substituted alkyl(disubstituted) amino and C1 to C12 substituted alkyl protected (monosubstituted) amino; R6 is absent or selected from the group consisting of C1 to C12 alkylene, C1 to C12 substituted alkylene, C2 to C12 alkenylene and C2 to C12 substituted alkenylene; and R7 is selected from the group consisting of a hydrogen atom, a halide, â€”OR13, â€”CO2R13, â€”C(O)NR13R14 and â€”NR13R14, wherein R13 and R14 are independently selected from a hydrogen atom, C1 to C12 alkyl, C1 to C12 substituted alkyl, phenyl, substituted phenyl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl, C3 to C7 cycloalkyl, C3 to C7 substituted cycloalkyl, C5 to C7 cycloalkenyl, C5 to C7 substituted cycloalkenyl, C7 to C18 phenylalkyl, C7 to C12 substituted phenylalkyl, C1 to C12 heterocyclicalkyl, C1 to C12 substituted heterocyclicalkyl, C1 to C12 acyl, C1 to C12 substituted acyl, phenylsulfonyl, substituted phenylsulfonyl, C1 to C10 alkylsulfonyl, C1 to C10 substituted alkylsulfonyl, C1 to C12 alkylaminocarbonyl, C1 to C12 substituted alkylaminocarbonyl, phenylaminocarbonyl, substituted phenylaminocarbonyl, C1 to C12 alkylaminothiocarbonyl, C1 to C12 substituted alkylaminothiocarbonyl, phenylaminothiocarbonyl and substituted phenylaminothiocarbonyl; X, Y and Z are, independently, selected from the group consisting of a hydrogen atom, halo, hydroxy, protected hydroxy, cyano, nitro, C1 to C12 alkyl, C2 to C12 alkenyl, C2 to C12 alkynyl, C1 to C12 substituted alkyl, C2 to C12 substituted alkenyl, C2 to C12 substituted alkynyl, C1 to C12 alkoxy, C1 to C12 substituted alkoxy, C1 to C12 acyloxy, C1 to C12 acyl, C3 to C7 cycloalkyl, C3 to C7 substituted cycloalkyl, C5 to C7 cycloalkenyl, C5 to C7 substituted cycloalkenyl, heterocyclic ring, substituted heterocyclic ring, C7 to C18 phenylalkyl, C7 to C18 substituted phenylalkyl, C1 to C12 heterocyclicalkyl, C1 to C12 substituted heterocyclicalkyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, cyclic C2 to C7 alkylene, substituted cyclic C2 to C7 alkylene, cyclic C2 to C7 heteroalkylene, substituted cyclic C2 to C7 heteroalkylene, carboxy, protected carboxy, hydroxymethyl, protected hydroxymethyl, amino, protected amino, (monosubstituted) amino, protected (monosubstituted) amino, (disubstituted) amino, carboxamide, protected carboxamide, C1 to C10 alkylthio, C, to C10 substituted alkylthio, C1 to C10 alkylsulfonyl, C1 to C10 substituted alkylsulfonyl, C1 to C10 alkylsulfoxide, C1 to C10 substituted alkylsulfoxide, phenylthio, substituted phenylthio, phenylsulfoxide, substituted phenylsulfoxide, phenylsulfonyl and substituted phenylsulfonyl; b, c and d are, independently, 0 or 1 and, when 0, the absent carbonyl can be replaced with â€”SO2â€”; or a pharmaceutically acceptable salt of a compound thereof.