Patent ID: 6407083
Filing Date: 2002-06-18
Classification: C07D,C07J

Abstract:
A method of treating cancers comprising administering an effective amount of at least one compound of the following formula: wherein:R1 is selected from a group consisting of: hydrogen; C1-C6 alkyl; ar(C1-C6)alkyl; ar(C1-C6)alkyl substituted on aryl by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; aryl; aryl substituted by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; â€”COR8; â€”COOR8; â€”CONH2; â€”CONR8R9; â€”(CH2)pR10; and â€”(CH2)pVect; R2 is selected from the group consisting of: hydrogen; C1-C6 alkyl; ar(C1-C6)alkyl; ar(C1-C6)alkyl substituted on aryl by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; aryl; aryl sustituted by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; â€”COR8; â€”COOR8; â€”CONH2; â€”CONR8R9; â€”(CH2)pR10; and â€”(CH2)pVect; R3 is selected from the group consisting of: hydrogen; C1-C6 alkyl; ar(C1-C6)alkyl; ar(C1-C6)alkyl substituted on aryl by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; aryl; aryl substituted by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; â€”COR8; â€”COOR8; â€”CONH2; â€”CONR8R9; â€”(CH2)pR10; and â€”(CH2)pVect; R4 is â€”NO2; R5 is selected from the group consisting of: hydrogen; C1-C6 alkyl; â€”COR8; â€”COOR8; â€”CONR8R9; â€”(CH2)pR10; â€”(CH2)pVect; â€”N+R113Yâˆ’; â€”SO3âˆ’Z+ and â€”CO231Z+; X is (CR6R7)n; R6 is selected from the group consisting of: hydrogen; C1-C6 alkyl; â€”COR8; â€”COOR8; â€”CONR8R9; â€”(CH2)pR10; and â€”(CH2)pVect; R7 is selected from the group consisting of: hydrogen; C1-C6 alkyl; â€”COR8; â€”COOR8; â€”CONR8R9; â€”(CH2)pR10; and â€”(CH2)pVect; R8 is selected from the group consisting of: C1-C6 alkyl; ar(C1-C6)alkyl; ar(C1-C6)alkyl substituted on aryl by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; aryl; aryl substituted by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; heteroaryl; heteroaryl substituted by one or more identical or different groups selected from: C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; and â€”(CH2)pVect; R9 is selected from the group consisting of: hydrogen; C1-C6 alkyl; ar(C1-C6)alkyl; ar(C1-C6)alkyl substituted on aryl by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; aryl; aryl substituted by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; and â€”(CH2)pVect; R10 is selected from the group consisting of: hydrogen; â€”N+R113Yâˆ’; â€”SO3âˆ’Z+ and â€”CO2âˆ’Z+; R11 is selected from the group consisting of: hydrogen; C1-C6 alkyl; ar(C1-C6)alkyl; ar(C1-C6)alkyl substituted on aryl by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; aryl; aryl substituted by one or more identical or different groups selected from C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, hydroxyl, nitro, amino, C1-C6 alkylamino, di(C1-C6-alkyl)amino, sulfonyl, sulfonamide, sulfo(C1-C6-alkyl), â€”CO2H, and â€”CO2â€”(C1-C6)alkyl; vect=W is either a single bond with â€”(CH2)pâ€”, or a heteroatom selected from the group consisting of O, N and S, bound to â€”(CH2)pâ€”; Yâˆ’ is the anion of a pharmaceutically acceptable acid; Z+ is the cation of a pharmaceutically acceptable base; n=0 or 1; m=0 or 1; p=2 to 10; and their pharmaceutically acceptable salts of acids or bases; and a pharmaceutically acceptable carrier, excipient or vehicle;with the proviso that there can not be more than one Vect substituent within each molecule of said formula I.