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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。

    Furopyridine antibacterials
    8.
    发明授权
    Furopyridine antibacterials 失效
    呋喃西林抗菌剂

    公开(公告)号：US06277860B1

    公开(公告)日：2001-08-21

    申请号：US09430763

    申请日：1999-10-29

    申请人： Yutaka Sugie ,  Akemi Sugiura ,  Nobuji Yoshikawa ,  Susan J. I Truesdell ,  John W. Wong

    发明人： Yutaka Sugie ,  Akemi Sugiura ,  Nobuji Yoshikawa ,  Susan J. I Truesdell ,  John W. Wong

    IPC分类号： A61K31436

    CPC分类号： C07D491/04 ,  C07D491/14

    摘要： This invention provides a compound of formula (I): or pharmaceutically acceptable salts thereof, wherein X1 and X2 are C or N, respectively; R1 and R2 are independently phenyl optionally substituted with a hydroxy group with proviso that X1 and X2 are not simultaneously C or N, when X1 is N, R1 is absent, and when X2 is N, R2 is absent; R3 is methyl or hydroxymethyl; R4 is formyl, hydroxymethyl or hydroxy C3-6 alkenyl; R5 is hydroxy, C3-6 alkenyl or hydroxy C3-6 alkenyl; or R4 and R5, together with the carbon atoms in the furopyridine ring to which they are attached, may form the following ring (to be fused with the furopyridine ring): with the proviso that when R3 is methyl and R5 is 2-buten-2-yl, X2 is not N. These compounds and pharmaceutical compositions containing such compounds are useful for treating infectious diseases caused by bacteria.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中X 1和X 2分别是C或N; R1和R2独立地为羟基取代的苯基，条件是X1和X2不同时为C或N，当X1为N时，R1不存在，当X2为N时，R2为不; R3是甲基或羟甲基; R4是甲酰基，羟甲基或羟基C 3-6烯基; R5是羟基，C3-6烯基或羟基C3-6烯基; 或R 4和R 5与它们所连接的呋喃啶环中的碳原子一起形成以下环（与呋喃啶环稠合）：条件是当R 3为甲基且R 5为2-丁烯基时， 2-这些化合物和含有这些化合物的药物组合物可用于治疗由细菌引起的感染性疾病。