- 专利标题: Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
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申请号: US10596519申请日: 2004-12-20
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公开(公告)号: US07355051B2公开(公告)日: 2008-04-08
- 发明人: Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , François Maria Sommen , Jerôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe
- 申请人: Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , François Maria Sommen , Jerôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe
- 申请人地址: IE County Cork
- 专利权人: Tibotec Pharmaceuticals
- 当前专利权人: Tibotec Pharmaceuticals
- 当前专利权人地址: IE County Cork
- 优先权: EP03104802 20031218
- 国际申请: PCT/EP2004/053606 WO 20041220
- 国际公布: WO2005/058873 WO 20050630
- 主分类号: C07D401/106
- IPC分类号: C07D401/106
摘要:
The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1−6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1−4alkoxy, C1−4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1−4alkyl-carbonyl, Ar2carbonyl, C1−4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1−4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1−4alkoxy-carbonyl(CH2)noxy, mono- or di(C1−4alkyl)aminocarbonyl, mono- or di(C1−4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1−4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1−6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1−6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1−6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1−6alkyl, and R2b is hydrogen; t is 1, 2 or 3; Ar1 is phenyl or substituted phenyl; and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
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