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    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    1.
    发明授权
    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权
    氨基苯并咪唑衍生物作为复制呼吸道合胞病毒的抑制剂

    公开(公告)号：EP1711485B1

    公开(公告)日：2009-05-13

    申请号：EP04804953.0

    申请日：2004-12-20

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： BONFANTI, Jean-François ,  ANDRIES, Koenraad, Jozef, Lodewijk ,  JANSSENS, Frans, Eduard ,  SOMMEN, François, Maria ,  GUILLEMONT, Jerôme, Emile, Georges ,  LACRAMPE, Jean, Fernand, Armand

    IPC分类号： C07D401/06 ,  A61K31/4184 ,  C07D401/14 ,  C07D405/14 ,  A61P11/00 ,  A61P31/12

    CPC分类号： C07D405/14 ,  C07D401/06 ,  C07D401/14

    摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)„oxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4 alkylcarbonyl, Ar2carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)n carbonyl, aminocarbonyloxy, C1-4 alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2- 4-alkyloxy, C1-4 alkoxycarbonyl(CH2)noxy, mono­or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each 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 C 1-6alkyl, and R2b is hydrogen; 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.

    1,3-DIHYDRO-BENZIMIDAZOL-2-YLIDENE AMINES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    2.
    发明公开
    1,3-DIHYDRO-BENZIMIDAZOL-2-YLIDENE AMINES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权
    用于治疗或预防病毒感染SUITABLE 1,3-二氢-2- YLIDENAMINE

    公开(公告)号：EP1951704A1

    公开(公告)日：2008-08-06

    申请号：EP06708798.1

    申请日：2006-03-17

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： BONFANTI, Jean-François ,  FORTIN, Jérôme, Michel, Claude ,  DORANGE, Ismet

    IPC分类号： C07D401/06 ,  C07D401/14 ,  A61K31/4184 ,  A61P11/00

    CPC分类号： C07D401/06 ,  C07D235/30 ,  C07D401/14

    摘要： Novel 1,3-dihydro-benzimidazo l-2-ylidene amine derivatives of formula (I) the addition salts and stereochemically iso meric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl subst ituted with one or two Ar2 radicals; C1-66alkyl subst ituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; -CO-Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono-or di(C1-6alkyl)amino ; R1 is Ar2, -CO-Ar2 or a monocyclic or bicyclic heterocycle which may optionally be subst ituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: (b) wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar11, R10a-O-, R10a-S-, -N(R5aR5b), R10a-O-C(=O)-, N(R5aR5b)-C(=O)-, R10a-C(=O)-NR5b-, R10b-C(=O)-O-; and R8 and/or R9 may also be hydrogen; which are RSV inhibitors. Compositions containing these compounds and processes for preparing these compounds and compositions.

    2-SUBSTITUTED BENZIMIDAZOLES
    4.
    发明公开
    2-SUBSTITUTED BENZIMIDAZOLES 有权
    2-取代的苯并咪唑

    公开(公告)号：EP1896450A1

    公开(公告)日：2008-03-12

    申请号：EP06777372.1

    申请日：2006-06-20

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： BONFANTI, Jean-François ,  MULLER, Philippe ,  FORTIN, Jérôme, Michel, Claude ,  DOUBLET, Frédéric, Marc, Maurice

    IPC分类号： C07D401/06 ,  C07D235/30 ,  A61K31/4184 ,  A61P11/00

    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 subst ituted 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, HetC1-6alkylsulfo nyl, Het-C1-6alkylcarbonyl; Het is an optionally substituted heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    HETEROCYCLYLAMINOALKYL SUBSTITUTED BENZIMIDAZOLES
    6.
    发明公开
    HETEROCYCLYLAMINOALKYL SUBSTITUTED BENZIMIDAZOLES 有权
    杂环酰胺基烷基取代的苯并咪唑

    公开(公告)号：EP1896449A1

    公开(公告)日：2008-03-12

    申请号：EP06763809.8

    申请日：2006-06-20

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： BONFANTI, Jean-François ,  MULLER, Philippe ,  FORTIN, Jérôme, Michel, Claude ,  DOUBLET, Frédéric, Marc, Maurice

    IPC分类号： C07D401/06 ,  A61K31/4184 ,  A61P11/00

    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).

    摘要翻译： 式（I）的RSV复制的杂环氨基烷基取代的苯并咪唑类抑制剂：其中Q为氢，任选被杂环取代的C 1-6烷基或Q为被-OR 4和杂环取代的C 1-6烷基; 其中所述杂环是恶唑烷，噻唑烷，1-氧代 - 噻唑烷，1,1-二氧代噻唑烷，吗啉基，硫代吗啉基，1-氧代 - 硫代吗啉基，1,1-二氧代硫代吗啉基，六氢氧氮杂，六氢硫氮杂， 二氢 - 六氢硫氮杂，吡咯烷，哌啶，高哌啶，哌嗪; 该杂环可以被1-2个取代基取代; 每个Alk是C 1-6链烷二基; 哌嗪基，吗啉基，硫代吗啉基，吡啶基，吡嗪基，哒嗪基，嘧啶基，呋喃基，四氢呋喃基，噻吩基，吡咯基，噻唑基，恶唑基，咪唑基，异噻唑基，吡唑基，异恶唑基， 苯并噻吩基，苯并咪唑基，苯并恶唑基，苯并噻唑基，吡啶并吡啶基，萘并噻唑基，1H-咪唑并[4,5-b]吡啶基，3H-咪唑并[4,5-b]吡啶基，咪唑并[1,2-a] - 二氢-1,4-二氧杂环己烯并[2,3-b]吡啶基; R 3是羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，氰基C 1-6烷基，氨基羰基-C 1-6 - 烷基，一或二（C 1-6烷基）氨基羰基-C 1-6 - 烷基，羧基-C 1-6 - C6烷氧基羰基-C1-6烷基; R2，R4和R5是氢或C1-6烷基; 噻吩基，噻唑基，咪唑基，异噻唑基，吡唑基，异恶唑基，恶二唑基，喹啉基，喹喔啉基，苯并呋喃基，苯并噻吩基，苯并咪唑基，苯并恶唑基，苯并噻唑基，吡啶并吡啶基，萘基吡啶基 ，1H-咪唑并〔4,5-b〕吡啶基，3H-咪唑并〔4,5-b〕吡啶基，咪唑并〔1,2-a〕吡啶基和2,3-二氢-1,4-二氧杂环己烯并〔2,1- 3-b]吡啶基; Ar是任选取代的苯基; 含有化合物（I）的药物组合物和用于制备化合物（I）的方法。

    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    7.
    发明公开
    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权
    氨基苯并咪唑衍生物作为复制呼吸道合胞病毒的抑制剂

    公开(公告)号：EP1711485A1

    公开(公告)日：2006-10-18

    申请号：EP04804953.0

    申请日：2004-12-20

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： BONFANTI, Jean-François ,  ANDRIES, Koenraad, Jozef, Lodewijk ,  JANSSENS, Frans, Eduard ,  SOMMEN, François, Maria ,  GUILLEMONT, Jerôme, Emile, Georges ,  LACRAMPE, Jean, Fernand, Armand

    IPC分类号： C07D401/06 ,  A61K31/4184 ,  C07D401/14 ,  C07D405/14 ,  A61P11/00 ,  A61P31/12

    CPC分类号： C07D405/14 ,  C07D401/06 ,  C07D401/14

    摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)„oxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4 alkylcarbonyl, Ar2carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)n carbonyl, aminocarbonyloxy, C1-4 alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2- 4-alkyloxy, C1-4 alkoxycarbonyl(CH2)noxy, mono­or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each 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 C 1-6alkyl, and R2b is hydrogen; 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.