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    HETEROCYCLYLAMINOALKYL SUBSTITUTED BENZIMIDAZOLES
    1.
    发明申请
    HETEROCYCLYLAMINOALKYL SUBSTITUTED BENZIMIDAZOLES 有权

    公开(公告)号：US20100272683A1

    公开(公告)日：2010-10-28

    申请号：US11993126

    申请日：2006-06-20

    申请人： Jean-Francois Bonfanti

    发明人： Jean-Francois Bonfanti

    IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61K38/21 ,  A61K38/19 ,  A61P31/12 ,  A61P31/14

    CPC分类号： C07D401/06 ,  C07D401/14

    摘要： Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono- or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6 alkyl; R2, R4 and R5 are hydrogen or C1-6alkyl; Het is pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]-pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl and 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; Ar is optionally substituted phenyl; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    2-SUBSTITUTED BENZIMIDAZOLES
    2.
    发明申请
    2-SUBSTITUTED BENZIMIDAZOLES 有权

    公开(公告)号：US20100092426A1

    公开(公告)日：2010-04-15

    申请号：US11993136

    申请日：2006-06-20

    申请人： Jean-Francois Bonfanti ,  Philippe Muller ,  Jérôme Michel Claude Fortin ,  Frédéric Marc Maurice Doublet

    发明人： Jean-Francois Bonfanti ,  Philippe Muller ,  Jérôme Michel Claude Fortin ,  Frédéric Marc Maurice Doublet

    IPC分类号： C07D401/06 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/4439 ,  A61P31/12 ,  A61K38/21 ,  A61K38/19

    CPC分类号： C07D401/06 ,  C07D235/30

    摘要： Inhibitors of RSV replication of formula (I) the addition salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydro-thiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar2 or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydro-furanyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono- or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 and R4 are hydrogen, C1-6alkyl, Ar2, Ar2C1-6alkyl, C1-6alkylcarbonyl, Ar2carbonyl, Ar2C1-6alkylcarbonyl, C1-6alkylsulfonyl, aminosulfonyl, Ar1sulfonyl, Ar1C1-6alkylsulfonyl, C1-6alkyloxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)-aminoC1-6alkyl, hydroxyC1-6alkyl, aminocarbonylC1-6alkyl, C1-4alkyloxycarbonyl-C1-6alkyl, hydroxycarbonylC1-6alkyl, aminosulfonylC1-6alkyl, Het, Het-C1-6alkyl, Het-carbonyl, Het-sulfonyl, HetC1-6alkylsulfonyl, Het-C1-6alkylcarbonyl; Het is an optionally substituted heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
    4.
    发明申请
    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权

    公开(公告)号：US20070093659A1

    公开(公告)日：2007-04-26

    申请号：US10596519

    申请日：2004-12-20

    申请人： Jean-Francois Bonfanti ,  Koenraad Andries ,  Frans Janssens ,  Francois Sommen ,  Jerome Guillemont ,  Jean Lacrampe

    发明人： Jean-Francois Bonfanti ,  Koenraad Andries ,  Frans Janssens ,  Francois Sommen ,  Jerome Guillemont ,  Jean Lacrampe

    IPC分类号： C07D473/00

    CPC分类号： C07D401/14 ,  C07D417/14

    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, C1-4alkylcarbonyl, 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.