Patent ID: 6552065
Filing Date: 2003-04-22
Classification: A61P,C04B,C07C,C07D

Abstract:
A compound of the formula (I) whereinR1 is H, halo, or a straight chain C1-C6 alkyl; R2 is selected from H, C1-C10 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, C4-C9 heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, â€”(CH2)nC(O)R6, â€”(CH2)nOC(O)R6, amino acyl, HONâ€”C(O)â€”CH&boxH;C(R1)-aryl-alkyl- and â€”(CH2)nR7; R3 and R4 are the same or different and independently H, C1-C6 alkyl, acyl or acylamino, or R3 and R4 together with the carbon to which they are bound represent C&boxH;O, C&boxH;S, or C&boxH;NR8; R5 is selected from polyheteroaryl which is substituted or unsubstituted indol-3-yl; n, n1, n2 and n3 are the same or different and independently selected from 0-6, when n, is 1-6, each carbon atom can be optionally and independently substituted with R3 and/or R4; X and Y are the same or different and independently selected from H, halo, C1-C4 alkyl, NO2, C(O)R1, OR9, SR9, CN, and NR10R11; R6 is selected from H, C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, cycloalkylalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, OR12, and NR13R14; R7 is selected from OR15, SR15, S(O)R16, SO2R17, NR13R14, and NR12SO2R6; R8 is selected from H, OR15, NR13R14, C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; R9 is selected from C1-C4 alkyl and C(O)-alkyl; R10 and R11 are the same or different and independently selected from H, C1-C4 alkyl, and â€”C(O)-alkyl; R12 is selected from H, C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, C4-C9 heterocycloalkylalkyl, aryl, mixed aryl and non-aryl polycycle, heteroaryl, arylalkyl, and heteroarylalkyl; R13 and R14 are the same or different and independently selected from H, C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, amino acyl, or R13 and R14 together with the nitrogen to which they are bound are C4-C9 heterocycloalkyl, heteroaryl, polyheteroaryl, non-aromatic polyheterocycle or mixed aryl and non-aryl polyheterocycle; R15 is selected from H, C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and (CH2)mZR12; R16 is selected from C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, aryl, heteroaryl, polyheteroaryl, arylalkyl, heteroarylalkyl and (CH2)mZR12; R17 is selected from C1-C6 alkyl, C4-C9 cycloalkyl, C4-C9 heterocycloalkyl, aryl, aromatic polycycle, heteroaryl, arylalkyl, heteroarylalkyl, polyheteroaryl and NR13R14; m is an integer selected from 0 to 6; and Z is selected from O, NR13, S and S(O); or a pharmaceutically acceptable salt thereof.