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    PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    11.
    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.

    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    12.
    发明授权
    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines 有权
    N- [4-（杂芳基甲基）苯基] - 杂芳基胺

    公开(公告)号：US06486187B1

    公开(公告)日：2002-11-26

    申请号：US09624966

    申请日：2000-07-25

    申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    IPC分类号： A61K31422

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as 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和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

    IL-5 inhibiting 6-azauracil derivatives
    13.
    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：US06469001B1

    公开(公告)日：2002-10-22

    申请号：US09856625

    申请日：2001-05-22

    申请人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Davy Petrus Franciscus Maria Petit ,  Jean Fernand Armand Lacrampe

    发明人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Davy Petrus Franciscus Maria Petit ,  Jean Fernand Armand Lacrampe

    IPC分类号： C07D253075

    CPC分类号： C07D253/075 ,  C07D417/10

    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, wherein p is 0 to 3; q is 0 to 5; —A—B— is —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with Het3, R6 or NR7R8; R2 represents aryl, Het1, C3-7cycloalkyl, cyano, C1-6alkyl, —C(═Q)—X2—R15 or C1-6alkyl substituted with one or two substituents selected from hydroxy, cyano, amino, mono- or di(C1-4alkyl)amino, C1-6alkyloxy, C1-6alkylsulfonyloxy, C1-6alkyloxycarbonyl, C3-7cycloalkyl, aryl, aryloxy, arylthio, Het1, Het1 oxy, Het1 thio and —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloallcyl, aryl; where X2 is a direct bond, R15 is also halo or Het1; where X2 is NR5, R15 is also hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(═O), R15 is replaced by R11; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; Q is O, S or NR3; X2 is O, S, NR5, C(═O)—NH—NH, NH—NH—C(═O) or a direct bond; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl—C(═O)—O—R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl—C(═O)—O—R14, —C(═O)—O—R14,. —Y—C1-4alkanediyl—C(═O)—O—R14, aryl, aryloxy, arcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3, Het4 and C(═O)Het3; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 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和立体化学异构形式，其中p为0-3; q为0〜5; -A-B-是 - （CH 2）r - ， - （CH 2）t -O-， - （CH 2）t -S（= O）u - 或 - （CH 2）t -NR 3 - ; r为2〜4; t为1〜3; 你是0到2; X1是O，S，NR3或直接键; R 1和R 4是C 1-6烷基，卤素，多卤代C 1-6烷基，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，R 6，NR 7 R 8或被Het 3， 或NR7R8; R 2表示芳基，Het 1，C 3-7环烷基，氰基，C 1-6烷基，-C（= Q）-X 2 -R 15或被一个或两个选自羟基，氰基，氨基，单 - 或二 1-4烷基）氨基，C 1-6烷氧基，C 1-6烷基磺酰氧基，C 1-6烷氧基羰基，C 3-7环烷基，芳基，芳氧基，芳硫基，Het 1，Het 1氧基，Het 1硫基和-C（= Q）-X 2 -R 15; R3是氢或C1-4烷基; R 15是氢，任选取代的C 1-6烷基，C 3-7环烷基，芳基; 其中X2是直接键，R15也是卤素或Het1; 其中X2是NR5，R15也是羟基; 其中X2是C（= O）-NH-NH或NH-NH-C（= O），R15被R11代替; R5是氢，C1-6烷基，