SUBSTITUTED PYRIDINE-PIPERAZINYL ANALOGUES AS RSV ANTIVIRAL COMPOUNDS

摘要

The invention concerns novel substituted pyridine-piperazinyl analogues of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.;

主权项

1. A compound of formula (I′) or a stereochemically isomeric form thereof, wherein: X and Y are each independently selected from CR6 or N, wherein R6 is selected from the group consisting of hydrogen, halo, hydroxy, cyano, polyhaloC1-4alkyl, C1-4alkyloxy, nitro, amino, mono- or di(C1-4alkyl)amino, and C1-4alkylcarbonyl; R1 and R2 are each independently selected from the group consisting of hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, polyhaloC1-4alkyl, polyhaloC1-4alkyloxy, cyano, nitro, and C1-4alkylcarbonyl; R3 is hydrogen or C1-6alkyl; R4 is selected from the group consisting of hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, polyhaloC1-4alkyl, polyhaloC1-4alkyloxy, cyano, nitro, and C1-4alkylcarbonyl; L1 is a direct bond; oxygen; or C1-4alkanediyl, wherein said C1-4alkanediyl is optionally substituted with one or two substituents each independently selected from the group consisting of hydroxy, and phenyl optionally substituted with C1-4alkyloxy; L2 is a direct bond, phenyl, or piperazine optionally substituted with hydroxy; and R5 is selected from the group consisting of C1-4alkyl, C3-6cycloalkyl, heteroalkyl, aryl and heteroaryl;
wherein said heteroalkyl is piperidinyl;wherein said aryl is phenyl, or naphthalenyl; wherein each aryl is optionally substituted with one or two substituents each independently selected from the group consisting of halo, hydroxy, C1-4alkyl, C1-4alkyloxy, C1-4alkylthio, polyhaloC1-4alkyl, C1-4alkyloxy, cyano, nitro, amino, o- or di(C1-4alkyl)amino, C1-4alkylcarbonyl, and C1-4alkyl(SO2)—NH—; andwherein said heteroaryl is selected from the group consisting of furanyl, thiophenyl, pyrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, 2,3-dihydro-benzo[1,4]dioxinyl, benzo[1,3]dioxolyl, 1-benzofuranyl, 2,3-dihydro-1-benzofuranyl, 1-benzothiophenyl, 1-benzopyrazolyl, 1,3-benzothiazolyl, and quinolinyl; wherein each heteroaryl is optionally substituted with one or two substituents each independently selected from the group consisting of C1-4alkyl, C1-4alkyloxy, hydroxyC1-4alkyl, cyanoC1-4alkyl, polyhaloC1-4alkyl, and C1-4alkyloxyC1-4alkyl; or a pharmaceutically acceptable acid addition salt thereof.