- 专利标题: Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication
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申请号: US10563691申请日: 2004-12-20
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公开(公告)号: US07449463B2公开(公告)日: 2008-11-11
- 发明人: Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
- 申请人: Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
- 申请人地址: IE County Cork
- 专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人地址: IE County Cork
- 代理商 Mary Appollina
- 优先权: EP03104810 20031218; EP04105312 20041026
- 国际申请: PCT/EP2004/053620 WO 20041220
- 国际公布: WO2005/058871 WO 20050630
- 主分类号: A61K31/535
- IPC分类号: A61K31/535 ; C07D413/00
摘要:
The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.