Patent ID: 6677452
Filing Date: 2004-01-13
Classification: C07B,C07D,C40B

Abstract:
A combinatorial library of two or more compounds of the formula: wherein:X is selected from the group consisting of â€”C(O)â€” and â€”S(O2)â€”; one of R1, R2, R3 and R4 is the formula â€”Xâ€”Nâ€”R7R8, wherein X is a carbonyl group (â€”C(O)â€”) or a sulfonyl group (â€”S(O2)â€”); R7 is selected from the group consisting of a hydrogen atom, C1 to C12 alkyl, C1 to C12 substituted alkyl, phenyl, substituted phenyl, heterocycle, substituted heterocycle, C3 to C7 cycloalkyl, C3 to C7 substituted cycloalkyl, C5 to C7 cycloalkenyl, C5 to C7 substituted cycloalkenyl, C2 to C12 alkenyl, C2 to C12 substituted alkenyl, C7 to C18 phlenylalkyl, C7 to C18 substituted phenylalkyl, C1 to C12 heterocycloalkyl and C1 to C12 substituted heterocycloalkyl; and R8 is selected from the group consisting of a hydrogen atom, C1 to C12 alkyl, C1 to C12 substituted alkyl, non-aromatic heterocycle, non-aromatic substituted heterocycle, C3 to C7 cycloalkyl, C3 to C7 substituted cycloalkyl, C5 to C7 cycloalkenyl, C5 to C7 substituted cycloalkenyl, C2 to C12 alkenyl, C2 to C12 substituted alkenyl, C7 to C18 phenylalkyl, C7 to C18 substituted phenylalkyl, C1 to C12 heterocycloalkyl and C1 to C12 substituted heterocycloalkyl; the remaining R1, R2, R3 and R4 are, independently, selected from the group consisting of a hydrogen atom, hydroxy, protected hydroxy, nitro, cyano, 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 suibstituted phenylalkyl, C1 to C12 heterocycloalkyl, C1 to C12 substituted heterocycloalkyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, cyclic C3 to C7 allkylene, substituted cyclic C3 to C7 alkylene, cyclic C2 to C7 heteroalkylene, substituted cyclic C2 to C7 heteroalkylene, carboxy, protected carboxy, hydroxymethyl, protected hydroxymethyl, protected amino, (monosubstituted)amino, protected (monosubstituted)amino, (disubstituted)amino, C1 to C12 alkylamino, C1 to C10 substituted alkylamino, carboxamide, protected carboxamide, C1 to C10 alkylthio, C1 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; R5 is the formula â€”DWEâ€”, wherein (i) D and E are each â€”NHâ€” and W is selected from the group consisting of C2 to C12 alkylene, C2 to C12 alkenylene, C2 to C12 alkynylene, C2 to C12 substituted alkylene, C2 to C12 substituted alkenylene, C2 to C12 substituted alkynylene, C7 to C18 phenylalkylene, C7 to C18 substituted phenylalkylene, C1 to C12 heterocycloalkylene and C1 to C12 substituted heterocycloalkylene phenylene, substituted phenylene, C3 to C7 cycloalkylene, C3 to C7 substituted cycloalkylene, C5 to C7 cycloalkenylene, C5 to C7 substituted cycloalkenylene, heterocyclene and substituted heterocyclene; or (ii) D, W and E together form a non-aromatic heterocyclene or substituted non-aromatic heterocyclene having at least two ring nitrogen atoms, one ring nitrogen atom directly attached to Xâ€”R6 depicted in the above formula and the other ring nitrogen atom directly attached to the pyridine depicted in the above formula; and R6 is 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 heterocycloalkyl, C1 to C12 substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, heterocycle and substituted heterocycle, wherein said heterocycle is a five-membered to eight-membered ring; wherein R7 or R8 can be attached to a functionalized resin; or a pharmaceutically acceptable salt of a compound thereof.