Azabenzimidazoles as respiratory syncytial virus antiviral agents

摘要

A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof;;
compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions

主权项

1. A method of treating a respiratory syncytial viral (RSV) infection comprising administering to a subject in need thereof an anti-virally effective amount of a compound of formula I, or a N-oxide, addition salt, quaternary amine, or a stereochemically isomeric form thereof, wherein each X is independently C or N, wherein at least one X is N; each Y is independently C or N; each R1 is selected from the group consisting of H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkoxy, N(R5)2, CO(R6), CH2NH2, CH2OH, CN, C(═NOH)NH2, C(═NOCH3)NH2, C(═NH)NH2, CF3, OCF3, B(OH)2, and B(O—C1-C6alkyl)2, wherein if X is C, R1 is present, and if X is N, R1 is absent; R2 is —(CR7R8)n-R9; R3 is selected from the group consisting of H, C1-C10alkyl, C3-C7cycloalkyl, C2-C10alkenyl, SO2-R7, CH2CF3 and a 4 to 6 membered saturated ring containing an oxygen atom; each R4 is independently selected from the group consisting of H, C1-C6alkyl, C1-C6cycloalkyl, C1-C6alkoxy, CO(R7), COO(R7), CF3 and halogen, wherein if Y is C, R4 is present, and if Y is N, R4 is absent; each R5 is independently selected from the group consisting of H, C1-C6alkyl, COOCH3, and CONHSO2CH3; each R6 is independently selected from the group consisting of OH, O(C1-C6alkyl), NH2, NHSO2N(C1-C6alkyl)2, NHSO2NHCH3, NHSO2(C1-C6alkyl), NHSO2(C3-C7cycloalkyl), and N(C1-C6-alkyl)2; R7 and R8 are each independently selected from the group consisting of H, C1-C10alkyl, and C3-C7cycloalkyl, or R7 and R8 taken together form a 4 to 6 membered aliphatic ring, said ring optionally contains a heteroatom selected from the group consisting of N, S, and O; R9 is selected from the group consisting of H, R10, C1-C6alkyl, OH, CN, F, CF2H, CF3, CONR7R8, COOR7, CON(R7)SO2R8, CON(R7)SO2N(R7R8), NR7R8, NR7COOR8, OCOR7, O-Benzyl, NR7SO2R8, SO2NR7R8, SO2R2 , OCONR7R8, OCONR7R10, N(R7)CON(R7R8), N(R7)COOR10, phtalimido, 2-methyl-benzothiophene(1,1)dioxide, and a 4 to 6 membered saturated ring containing an oxygen atom; n is an integer from 2 to 6; and R10 is selected from the group consisting of C1-C6 alkyl, C3-C7cycloalkyl, phenyl, pyridine and pyrazole, wherein R10 is optionally substituted with one or more substituents comprising CF3, CH3, OCH3, OCF3 or halogen.