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    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    4.
    发明申请
    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开

    公开(公告)号：US20080146613A1

    公开(公告)日：2008-06-19

    申请号：US12030483

    申请日：2008-02-13

    申请人： Jean-Francois BONFANTI ,  Koenraad Jozef Lodewikjk Andries ,  Frans Eduard Janssens ,  Francois Maria Sommen ,  Jerome Emile Georges Guillemont ,  Jean Fernand Armand Lacrampe

    发明人： Jean-Francois BONFANTI ,  Koenraad Jozef Lodewikjk Andries ,  Frans Eduard Janssens ,  Francois Maria Sommen ,  Jerome Emile Georges Guillemont ,  Jean Fernand Armand Lacrampe

    IPC分类号： A61K31/4545 ,  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 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, C1-4alkyl-carbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, 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.

    IL-5 inhibiting 6-azauracil derivatives
    8.
    发明授权
    IL-5 inhibiting 6-azauracil derivatives 失效
    IL-5抑制6-氮尿嘧啶衍生物

    公开(公告)号：US06867207B2

    公开(公告)日：2005-03-15

    申请号：US09891888

    申请日：2001-06-26

    申请人： Jean Fernand Armand Lacrampe ,  Eddy Jean Edgard Freyne ,  Marc Gaston Venet ,  Gustaaf Maria Boeckx

    发明人： Jean Fernand Armand Lacrampe ,  Eddy Jean Edgard Freyne ,  Marc Gaston Venet ,  Gustaaf Maria Boeckx

    IPC分类号： A61P37/08 ,  C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D253/065 ,  A61K31/53 ,  A61K17/00

    CPC分类号： C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

    摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐及其立体化学异构形式，p和q分别为0,1,2,3或4，q也为5; X是O，S，NR 3或直接键; R 1是氢，羟基，卤素，任选取代的氨基，任选取代的C 1-6烷基，C 1-6烷氧基，C 3-7环烷基或芳基; R 2是芳基，Het 1，C 3-7环烷基，任选取代的C 1-6烷基; 并且如果X是O，S或NR 3，则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基，卤素，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3， 或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢，任选取代的C 1-4烷基，芳基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 9和R 10各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 11是羟基，巯基，氰基，硝基，卤素，三卤代甲基，C 1-4烷氧基，羧基，C 1-4烷氧基羰基，三卤代C 1-4烷基磺酰氧基，R 6，NR 7 R 8，C（= O） NR 7 R 8，芳基，芳氧基，芳基羰基，C 3-7环烷基，C 3-7环烷氧基，邻苯二甲酰亚胺-2-基，Het 3和C（= O）Het 3; R 12和R 13各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>，Het <