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    Il-5 inhibiting 6-azauracil derivatives
    1.
    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：US06803364B1

    公开(公告)日：2004-10-12

    申请号：US09868384

    申请日：2001-08-29

    申请人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Jean Fernand Armand Lacrampe ,  Werner Constant Johan Embrechts ,  Jerome Michel Claude Fortin

    发明人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Jean Fernand Armand Lacrampe ,  Werner Constant Johan Embrechts ,  Jerome Michel Claude Fortin

    IPC分类号： C07D25306

    CPC分类号： C07D253/075 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    摘要： The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR3 or a direct bond; or —X—R2 is CN; R1 is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R2 is aryl, Het1, optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R3 is H or C1-4alkyl; R4 and R5 are —C(═O)—Z—R14, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(═O)O, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with —C(═O)—Z—R14, Het3, R6 or NR7R8; Z is O, S, NH, —CH2O or —CH2—S—; R14 is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het5, phenyl; or R14 is an oxygen containing radical; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het5 are optionally substituted heterocycles; Het4 is a monocyclic heterocycle; provided however that R2 is other than NH2C(═O), C1-6alkylOC(═O)C1-6alkyl; and R11 is other than COOH, C1-4alkylOC(═O), NH2C(═O), C1-4alkylNH2C(═O), OHC1-4alkylNH2C(═O), C1-4alkylC(═O)NH2C(═O), C3-7cycloalkylNH2C(═O); and R7, R8, R9, R10, R12, R13, R15 and R16 are other than C1-4alkylC(═O)OC1-4alkylC(═O), OHC1-4alkylC(═O); and Het3 is other than a monocyclic heterocycle substituted with COOH or C1-4alkylOC(═O); and the compounds of formula (I) contain at least one —C(═O)—Z—R14 moiety: to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺或其立体化学异构形式，其中p为0至4; q为0〜5; X是O，S，NR 3或直接键; 或-X-R 2为CN; R 1是H，OH，卤素，NH 2，单或二（C 1-4烷基）NH 2，C 1-6烷基，C 1-6烷基O，C 3-7环烷基，芳基，芳基C 1-6烷基，NH 2 C 1-4烷基，单或二 （C 1-4烷基）NH 2 C 1-4芳基或单或二（C 1-4烷基）NH 2 C 1-4烷基NH 2; R 2是芳基，Het 1，任选取代的C 3-7环烷基，任选取代的C 1-6烷基; R 3是H或C 1-4烷基; R 4和R 5是-C（= O）-ZR 14，C 1-6烷基，卤素，多卤代C 1-6烷基，OH，巯基，C 1-6烷基O，C 1-6烷硫基，C 1-6烷基C（= O ）O，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或被-C（= O）-ZR 14，Het 3取代的C 1-4烷基， R 6或NR 7 R 8; Z是O，S，NH，-CH 2 O或-CH 2 -S-; R 14是H，C 1-20酰基，任选取代的C 1-20烷基，任选取代的C 3-20烯基，C 3-20炔基，C 3-7环烷基，多卤代C 1-20烷基，Het 5，苯基; 或R 14是含氧基团; 芳基是任选取代的苯基; Het 1，Het 2，Het 3和Het 5是任选取代的杂环; Het 4是单环杂环; 但是R 2不是NH