| 主权项 |
1. A 2,4-diaminoquinazoline compound selected from:
(A) 2,4-diaminoquinazoline compounds selected from the group consisting of formulae I, II and III: wherein L1 is selected from the group consisting of a bond and a linker of empirical formula CpHqNrOsSt in which p is 2-20; q is 0-40; r is 0-3; s is 0-6; t is 0-2; R1 is selected from the group consisting of cycloalkyl, aryl, fused cycloalkylaryl, heterocyclyl, heteroaryl, substituted cycloalkyl, substituted aryl, substituted fused cycloalkylaryl, substituted heterocyclyl, and substituted heteroaryl; G is selected from the group consisting of —NR6—, —CH2—, SO2— and —CH2O—; G1 is selected from the group consisting of —O—, NR6—, —S— and —OCH(CH3)—; R2 is selected from the group consisting of cycloalkyl, aryl, fused cycloalkylaryl, heterocyclyl, heteroaryl; substituted cycloalkyl, substituted aryl, substituted fused cycloalkylaryl, substituted heterocyclyl, and substituted heteroaryl with the proviso that when G is —CH2— then R2 is other than phenyl or substituted phenyl; R6 is selected from the group consisting of hydrogen and C1-C6 alkyl; and Q is selected from the group consisting of —CH2OCH3, —CH2OCH2CH═CH2, C6-C20 hydrocarbon, heterocyclyl, and heteroaryl; substituted C6-C20 hydrocarbon, substituted heterocyclyl, and substituted heteroaryl; and —C(OH)Ar2, wherein Ar is phenyl or substituted phenyl, with the proviso that when G1 is —O— or —S—, then Q is other than 4-chlorophenyl; (B) 2,4-diaminoquinazoline compounds of formula IV: wherein G2 is selected from the group consisting of —O—, —S—, and —NH—; and R12 is selected from the group consisting of C7-C10 polycyclic hydrocarbon, substituted C7-C10 polycyclic hydrocarbon, and wherein the wavy line indicates the point of attachment; and wherein one or more carbon atoms in the cyclopentyl ring is optionally replaced by a heteroatom independently selected from the group consisting of N, O, and S; and R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, haloalkyl, hydroxy, carboxy, C1-C6 alkoxycarbonyl, carboxamido, cyano, formyl, nitro, amino, C1-C6 alkylamino, C1-C6 dialkylamino, mercapto, C1-C6 alkylthio, C1-C6 alkylsulfoxide, C1-C6 alkylsulfone, C1-C6 acylamino, amidino, phenyl, benzyl, phenoxy and benzyloxy, with the proviso that at least one of R3, R4, and R5 must be other than hydrogen; and (C) 2,4-diaminoquinazoline compounds of formula VI: wherein L is a linker of empirical formula CpHqNrOsSt in which p is 0-20; q is 0-40; r is 0-3; s is 0-6; t is 0-2; and R is selected from the group consisting of cycloalkyl, aryl, fused cycloalkylaryl, heterocyclyl, heteroaryl, C3-C10 alkyl and C3-C10 oxaalkyl; substituted cycloalkyl, substituted aryl, substituted fused cycloalkylaryl, substituted heterocyclyl, substituted heteroaryl, substituted C3-C10 alkyl, and substituted C3-C10 oxaalkyl; and R10 and R11 are independently selected from the group consisting of H, —NH2, —NH(alkyl), —NHOH, —NHO(alkyl), and acyl, with the proviso that at least one of R10 and R11 is other than H; or a pharmaceutically acceptable salt of such a compound, in any stereoisomeric or tautomeric form, or a mixture of any such compounds in any ratio. |
