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    5-substituted picolinic acid compounds and their method of use
    4.
    发明授权
    5-substituted picolinic acid compounds and their method of use 失效
    5-取代吡啶甲酸化合物及其使用方法

    公开(公告)号：US06194442B1

    公开(公告)日：2001-02-27

    申请号：US09460483

    申请日：1999-12-14

    申请人： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    发明人： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    IPC分类号： A61K3144

    CPC分类号： A61K31/44 ,  Y02A50/411

    摘要： The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).

    摘要翻译： 本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用 在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。

    5-substituted picolinic acid compounds production by Marasmiellus sp
    5.
    发明授权
    5-substituted picolinic acid compounds production by Marasmiellus sp 失效
    由马拉斯马司属（Malasmiellus sp。）生产的5-取代吡啶甲酸化合物

    公开(公告)号：US06416979B1

    公开(公告)日：2002-07-09

    申请号：US09657730

    申请日：2000-09-08

    申请人： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    发明人： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    IPC分类号： C12P1712

    CPC分类号： A61K31/44

    摘要： The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).

    摘要翻译： 本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用 在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。