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    5- or 6-substituted benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
    3.
    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复制的抑制剂

    公开(公告)号：US08278455B2

    公开(公告)日：2012-10-02

    申请号：US12253450

    申请日：2008-10-17

    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

    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

    IPC分类号： A61K31/4439 ,  C07D401/06

    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 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 Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)namino-carbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(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.

    摘要翻译： 本发明涉及对呼吸道合胞病毒复制具有抑制活性的5-或6-取代苯并咪唑衍生物，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式，其中Q 是Ar 2，R 6，被R 6取代的吡咯烷基，被R 6取代的哌啶基或被R 6取代的高哌啶基，G是直接键或任意取代的C 1-10烷二基; R1是Ar1或单环或双环杂环; R2a和R2b之一是氰基C 1-6烷基，氰基C 2-6烯基，Ar 3 C 1-6烷基，Het 1 C 1-6烷基，N（R 8 a R 8 b）C 1-6烷基，Ar 3 C 2-6烯基，Het 1 C 2-6烯基，Ar 3氨基C 1-6烷基，Het 1氨基C 1-6烷基，Ar 3硫代C 1-6烷基， （CH 2）n氨基 - 羰基，Het 1（CH 2）n氨基羰基，Ar 3羰基氨基，Het 1羰基氨基，Ar 3（CH 2）n - 羰基氨基，Het 1（CH 2）n - 羰基氨基，和另一个（CH 2）n C 1 -C 6烷基， R2a和R2b是氢; 在R2a为氢的情况下，R3为氢; 在R2b为氢的情况下，R3为氢或C1-6烷基。 它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

    1-[2-AMINO-3-(SUBSTITUTED ALKYL)-3H-BENZIMIDAZOLYLMETHYL]-3-SUBSTITUTED-1,3-DIHYDRO-BENZOIMIDAZOL-2-ONES AND STRUCTURAL ANALOGS
    5.
    发明申请
    1-[2-AMINO-3-(SUBSTITUTED ALKYL)-3H-BENZIMIDAZOLYLMETHYL]-3-SUBSTITUTED-1,3-DIHYDRO-BENZOIMIDAZOL-2-ONES AND STRUCTURAL ANALOGS 有权
    1- [2-氨基-3-（取代的烷基）-3H-苯并咪唑基]乙基] -3-取代的1,3-二氢苯并咪唑-2-酮和结构模拟物

    公开(公告)号：US20100183552A1

    公开(公告)日：2010-07-22

    申请号：US11993109

    申请日：2006-06-20

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

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

    IPC分类号： A61K38/21 ,  A61K38/19 ,  A61P31/12 ,  C07D471/04 ,  A61K31/437 ,  C07D413/14 ,  A61K31/5377

    CPC分类号： C07D471/04 ,  C07D401/14

    摘要： Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH— or —CH═CH—CH═N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    摘要翻译： 式（I）的RSV复制抑制剂，其可以由式（I）表示其盐和立体化学异构形式，其中R是式Q的基团是氢或任选被杂环取代的C 1-6烷基或Q是C1- 被烷基和-OR4基团取代的6个烷基; Alk是C1-6烷二基; X是O或S; -a1 = a2-a3 = a4-是-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-或-CH = CH-CH = N- R1是Ar或杂环; R 2是氢，C 1-6烷基，取代的C 1-6烷基，C 3-7环烷基; R3是氢，C1-6烷基，氰基，氨基羰基，多卤代C 1-6烷基，C 2-6烯基或C 2-6炔基; R4是氢或C1-6烷基; Ar是苯基或取代的苯基; Het是杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

    2-substituted benzimidazoles
    6.
    发明授权
    2-substituted benzimidazoles 有权

    公开(公告)号：US07884215B2

    公开(公告)日：2011-02-08

    申请号：US11993136

    申请日：2006-06-20

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

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

    IPC分类号： C07D295/00

    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).

    Heterocyclylaminoalkyl substituted benzimidazoles
    7.
    发明授权
    Heterocyclylaminoalkyl substituted benzimidazoles 有权

    公开(公告)号：US08178694B2

    公开(公告)日：2012-05-15

    申请号：US11993126

    申请日：2006-06-20

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

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

    IPC分类号： A61K31/5377 ,  C07D413/14

    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, isoxazo lyl, 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, benzoxazo lyl, 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).

    1-[[2-amino-3-(substituted alkyl)-3H-benzimidazolyl[methyl]-3-substituted-1,3-dihydro-benzoimidazol-2-ones and structural analogs
    8.
    发明授权
    1-[[2-amino-3-(substituted alkyl)-3H-benzimidazolyl[methyl]-3-substituted-1,3-dihydro-benzoimidazol-2-ones and structural analogs 有权
    1 - [[2-氨基-3-（取代的烷基）-3H-苯并咪唑基[甲基] -3-取代-1,3-二氢 - 苯并咪唑-2-酮和结构类似物

    公开(公告)号：US08034835B2

    公开(公告)日：2011-10-11

    申请号：US11993109

    申请日：2006-06-20

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

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

    IPC分类号： C07D235/04 ,  C07D403/02 ,  A01N43/52 ,  A61K31/415

    CPC分类号： C07D471/04 ,  C07D401/14

    摘要： Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH— or —CH═CH—CH═N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    摘要翻译： 式（I）的RSV复制抑制剂，其可以由式（I）表示其盐和立体化学异构形式，其中R是式Q的基团是氢或任选被杂环取代的C 1-6烷基或Q是C1- 被烷基和-OR4基团取代的6个烷基; Alk是C1-6烷二基; X是O或S; -a1 = a2-a3 = a4-是-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-或-CH = CH-CH = N- R1是Ar或杂环; R 2是氢，C 1-6烷基，取代的C 1-6烷基，C 3-7环烷基; R3是氢，C1-6烷基，氰基，氨基羰基，多卤代C 1-6烷基，C 2-6烯基或C 2-6炔基; R4是氢或C1-6烷基; Ar是苯基或取代的苯基; Het是杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

    2-SUBSTITUTED BENZIMIDAZOLES
    9.
    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).