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    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    9.
    发明授权
    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权
    PIPERIDINAMINO - 苯并咪唑衍生物AL呼吸道合胞病毒复制抑制剂

    公开(公告)号：EP1723136B1

    公开(公告)日：2011-03-09

    申请号：EP04804942.3

    申请日：2004-12-20

    申请人： Tibotec Pharmaceuticals

    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： C07D401/14 ,  A61K31/4184 ,  C07D417/14 ,  A61P11/00 ,  A61P31/12

    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 (I) their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1-6alkyl optionally substituted with trifluorornethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4 alkoxy, 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-odi(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 Cl-10 loalkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6 salkyl 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.

    BROADSPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    10.
    发明授权
    BROADSPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 有权
    取代的苯并咪唑磺酰胺衍生物用作广谱HIV蛋白酶抑制剂

    公开(公告)号：EP1485358B1

    公开(公告)日：2011-02-02

    申请号：EP03714954.9

    申请日：2003-03-12

    申请人： Tibotec Pharmaceuticals

    发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain ,  WIGERINCK, Piet, Tom, Bert, Paul ,  VOETS, Marieke, Christiane, Johanna ,  VENDEVILLE, Sandrine, Marie, Helene ,  DE KOCK, Herman, Augustinus ,  VERGOUWEN, Bernhard, Joanna, Bernard

    IPC分类号： C07D235/32 ,  A61K31/415 ,  C07D493/04 ,  C07D235/30 ,  C07D407/12 ,  C07D417/12 ,  C07D413/12 ,  C07D401/12 ,  A61P31/18

    CPC分类号： C07D401/12 ,  A61K31/415 ,  C07D235/30 ,  C07D235/32 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D493/04

    摘要： The present invention concerns the compounds having the formula (I), wherein N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aRl0b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8-C1-6alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1-6alkanediyl-C(=O)-, C1-6 alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2-; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6 alkyl, optionally substituted amino­-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6 alkyloxy­carbonylamino or amino; and in case _A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and _A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2, R12 , is H, - NH2, _NR5AR6, - C1-6alkyl or alkyl-W-R14 , wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4alkyl and R13 is H, C1-6-alkyl, optionally substituted by aryl, Het1, Het2, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C1-4alkyl.