发明名称 Azaindoles As Respiratory Syncytial Virus Antiviral Agents
摘要 Azaindoles having inhibitory activity on RSV replication and having the formula I;;compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
申请公布号 US2015231119(A1) 申请公布日期 2015.08.20
申请号 US201514704292 申请日期 2015.05.05
申请人 Janssen R&D Ireland 发明人 COOYMANS Ludwig Paul;DEMIN Samuël Dominique;HU Lili;JONCKERS Tim Hugo Maria;RABOISSON Pierre Jean-Marie Bernard;TAHRI Abdellah;VENDEVILLE Sandrine Marie Helene
分类号 A61K31/437 主分类号 A61K31/437
代理机构 代理人
主权项 1. A method of treating a respiratory syncytial viral (RSV) infection comprising administering to a warm-blooded animal 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 independently is C or N with at least one X being N; each Y independently is C or N; R1 is present where X═C and each R1 is independently selected from the group consisting of H, OH, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkoxy, N(R6)2, CO(R7), CH2NH2, CH2OH, CN, C(═NOH)NH2, C(═NOCH3)NH2, C(═NH)NH2, CF3, OCF3, B(OH)2 and B(O—C1-C6alkyl)2; R1 is absent where X is N; R2 is selected from the group consisting of H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkoxy, and CO(R7); R3 is —(CR8R9)n—R10; R4 is selected from the group consisting of H, C1-C10alkyl, CH2CF3C3-C7cycloalkyl, C2-C10alkenyl, SO2—R8, or a 4 to 6 membered saturated ring containing an oxygen atom; R5 is present where Y is C, and is selected from the group consisting of H, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkoxy, CO(R7), CF3 and halogen; R5 is absent where Y is N; R6 is selected from the group consisting of H, C1-C6alkyl, COOCH3, and CONHSO2CH3; R7 is 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; n is an integer from 2 to 6; R8 and R9 are each independently chosen from H, C1-C10alkyl, or C3-C7cycloalkyl; or R8 and R9 taken together form a 4 to 6 membered aliphatic ring that optionally contains a heteroatom selected from the group N, S, O; R10 is selected from the group consisting of H, C1-C6alkyl, OH, CN, F, CF2H, CF3, CONR8R9, COOR8, CONR8SO2R9, CON(R8)SO2N(R8R9), NR8R9, NR8COOR9, OCOR8, NR8SO2R9, SO2NR8R9, SO2R8 or a 4 to 6 membered saturated ring containing an oxygen atom.
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