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1.发明授权MORPHOLINYL CONTAINING BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权MORPHOLINYLHALTIGE的苯并咪唑为复制呼吸道合胞病毒的抑制剂
公开(公告)号：EP1697345B1
公开(公告)日：2008-03-12
申请号：EP04817576.4
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/06 , A61K31/4184 , C07D413/14 , A61P11/00 , A61P31/12
CPC分类号： C07D413/12 , C07D401/06 , C07D401/14 , C07D413/14
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. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.
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2.发明授权5- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权5-或6-取代的苯并咪唑衍生物作为呼吸道合胞病毒的复制的抑制剂
公开(公告)号：EP1697347B1
公开(公告)日：2011-02-23
申请号：EP04804954.8
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/14 , A61K31/4184 , A61P11/00 , A61P31/12 , C07D401/06 , C07D405/14
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Arl or a monocyclic or bicyclic heterocycle; one of R 2a and R2b is cyanoCl-6alkyl, cyanoC2-6alkenyl, Ar3Cl-6alkyl, Het-C1-6alky1, N(R8aR8b)Cl-6alkyl, Ar3C2-6alkenyl, Het-C2-6alkenyl, Ar3 aminoCl-6alkyl, HetaminoCl-6alkyl, Ar3thioC1-6 alkyl, Het-thioC1-6alkyl, Ar3sulfonylC1-6 alkyl, HetsulfonylC1-6alkyl, Ar3aminocarbonyl, Het-aminocarbonyl, Ar3(CH2)naminocarbonyl, Het-(CH2)naminocarbonyl, Ar3carbonylamino, Het-carbonylamino, Ar3(CH2)ncarbonylamino, Het-(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a is hydrogen, then R3 is hydrogen; in case R2b is hydrogen, the R3 is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
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3.发明授权AMINOBENZIMIDAZOLES AND BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权氨基苯并咪唑和苯并咪唑为复制呼吸道合胞病毒的抑制剂
公开(公告)号：EP1697343B1
公开(公告)日：2009-07-01
申请号：EP04804949.8
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/06 , A61K31/4184 , C07D401/14 , C07D405/14 , C07D401/12 , A61P11/00 , A61P31/12
CPC分类号： C07D401/06 , C07D235/20 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/02 , C07D405/14 , C07D471/04 , C07F9/65583
摘要： Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula (I) the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct bond or C1-10alkanediyl optionally substituted with one or more hydroxy, C1-6alkyloxy, Ar1Cl-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio, HO(-CH2-CH2-O)n-, C1-6alkyloxy(-CH2-M2-O)n- or Ar1Cl-6alkyloxy(-CH2-C2-O)n-; R1 is Ar1 or a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(C1-4alkyl)amino; 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. Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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4.发明公开AMINOBENZIMIDAZOLES AND BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权氨基苯并咪唑和苯并咪唑为复制呼吸道合胞病毒的抑制剂
公开(公告)号：EP1697343A1
公开(公告)日：2006-09-06
申请号：EP04804949.8
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/06 , A61K31/4184 , C07D401/14 , C07D405/14 , C07D401/12 , A61P11/00 , A61P31/12 , C07D235/00 , C07D213/00
CPC分类号： C07D401/06 , C07D235/20 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/02 , C07D405/14 , C07D471/04 , C07F9/65583
摘要： Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula (I) the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct bond or C1-10alkanediyl optionally substituted with one or more hydroxy, C1-6alkyloxy, Ar1Cl-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio, HO(-CH2-CH2-O)n-, C1-6alkyloxy(-CH2-M2-O)n- or Ar1Cl-6alkyloxy(-CH2-C2-O)n-; R1 is Ar1 or a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(C1-4alkyl)amino; 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. Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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5.发明公开5- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATIORY SYNCYTIAL VIRUS REPLICATION 有权5-或6-取代的苯并咪唑衍生物作为呼吸道合胞病毒的复制的抑制剂
公开(公告)号：EP1697347A1
公开(公告)日：2006-09-06
申请号：EP04804954.8
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/14 , A61K31/4184 , A61P11/00 , A61P31/12 , C07D401/06 , C07D405/14 , C07D235/00 , C07D213/00 , C07D211/00
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Arl or a monocyclic or bicyclic heterocycle; one of R 2a and R2b is cyanoCl-6alkyl, cyanoC2-6alkenyl, Ar3Cl-6alkyl, Het-C1-6alky1, N(R8aR8b)Cl-6alkyl, Ar3C2-6alkenyl, Het-C2-6alkenyl, Ar3 aminoCl-6alkyl, HetaminoCl-6alkyl, Ar3thioC1-6 alkyl, Het-thioC1-6alkyl, Ar3sulfonylC1-6 alkyl, HetsulfonylC1-6alkyl, Ar3aminocarbonyl, Het-aminocarbonyl, Ar3(CH2)naminocarbonyl, Het-(CH2)naminocarbonyl, Ar3carbonylamino, Het-carbonylamino, Ar3(CH2)ncarbonylamino, Het-(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a is hydrogen, then R3 is hydrogen; in case R2b is hydrogen, the R3 is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
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6.发明公开MORPHOLINYL CONTAINING BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权MORPHOLINYLHALTIGE的苯并咪唑为复制呼吸道合胞病毒的抑制剂
公开(公告)号：EP1697345A1
公开(公告)日：2006-09-06
申请号：EP04817576.4
申请日：2004-12-20
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/06 , A61K31/4184 , C07D413/14 , A61P11/00 , A61P31/12 , C07D235/00 , C07D213/00
CPC分类号： C07D413/12 , C07D401/06 , C07D401/14 , C07D413/14
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. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.
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