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    1,3-DIHYDRO-BENZIMIDAZOL-2-YLIDENE AMINES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    86.
    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.

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    88.
    发明公开
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒的大环内酯类抑制剂

    公开(公告)号：EP1919899A1

    公开(公告)日：2008-05-14

    申请号：EP06778070.0

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd. ,  MEDIVIR AB

    发明人： DE KOCK, Herman Augustinus ,  SIMMEN, Kenneth Alan ,  JÖNSSON, Carl Erik Daniel ,  AYESA ALVAREZ, Susana ,  CLASSON, Björn Olof ,  NILSSON, Karl Magnus ,  ROSENQUIST, Åsa Annica Kristina ,  SAMUELSSON, Bengt Bertil ,  WALLBERG, Hans Kristian

    IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/538 ,  A61P31/14

    CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D487/04

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is -OR6, -NH-SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from formula (II) wherein said ring system may optionally be substituted with 1-3 substituents; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being optionally substituted with 1-3 substituents pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

    摘要翻译： 式（I）的HCV复制抑制剂及其N-氧化物，盐或立体异构体，其中每个虚线表示任选的双键; X是N，CH，其中X带有一个双键，它是C; R1是-OR6，-NH-SO2R7; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R3是氢，C1-6烷基，C1-6烷氧基C1-6烷基或C3-7环烷基; n是3,4,5或6; R 4和R 5与它们所连接的氮原子一起形成选自式（II）的双环系统，其中所述环系统可以任选地被1-3个取代基取代; R6是氢; 芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或用Het取代的C 1-6烷基; R7是芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或用Het取代的C 1-6烷基; 芳基是苯基或萘基，它们中的每一个可以任选被1-3个取代基取代; Het是含有1至4个各自独立地选自N，O或S的杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，并且任选地被1-3个取代基药物组合物取代，所述药物组合物含有化合物（I） 制备化合物（I）。 还提供了式（I）的HCV抑制剂与利托那韦的生物可用组合。

    2-SUBSTITUTED BENZIMIDAZOLES
    90.
    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).