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14 条记录 (耗时 0.028 秒)

    5-substituted picolinic acid compounds and their method of use
    1.
    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
    2.
    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。

    Rapamycin producer
    8.
    发明授权
    Rapamycin producer 失效
    雷帕霉素生产者

    公开(公告)号：US5674732A

    公开(公告)日：1997-10-07

    申请号：US325378

    申请日：1994-10-26

    申请人： Hiroyuki Nishida ,  Tatsuo Sakakibara ,  Yuji Yamauchi ,  Taisuke Inagaki ,  Yasuhiro Kojima ,  Nakao Kojima

    发明人： Hiroyuki Nishida ,  Tatsuo Sakakibara ,  Yuji Yamauchi ,  Taisuke Inagaki ,  Yasuhiro Kojima ,  Nakao Kojima

    IPC分类号： C12N1/20

    CPC分类号： C12R1/045

    摘要： The present invention provides a novel culture which belongs to Actinoplanes (Actinoplanes sp. FERM BP-3832). This culture is capable of producing rapamycin more than ten times efficiently than the cultures which have been reported (e.g., Streptomyces hygroscopicus ATCC 29253). The present invention provides a process for the production of rapamycin which comprises cultivating Actinoplanes sp. FERM BP-3832 and thereafter isolating rapamycin from the fermentation mixture.

    摘要翻译： PCT No.PCT / US93 / 01534 Sec。 371日期：1994年10月26日 102（e）日期1994年10月26日PCT 1993年2月26日PCT PCT。 公开号WO93 / 22446 日期：11月11日，11日本发明提供了属于动植物平面（Actinoplanes sp.FERM BP-3832）的新型培养物。 该培养物能够比已报道的培养物（例如，吸水链霉菌ATCC 29253）有效地产生雷帕霉素的十倍以上。 本发明提供了一种雷帕霉素的生产方法，其包括培养飞蓟素sp。 FERM BP-3832，然后从发酵混合物中分离雷帕霉素。

    Macrocyclic lactone compounds and their production process
    9.
    发明授权
    Macrocyclic lactone compounds and their production process 失效
    大环内酯化合物及其生产工艺

    公开(公告)号：US06187568B1

    公开(公告)日：2001-02-13

    申请号：US09378062

    申请日：1999-08-20

    申请人： Hiroyuki Nishida ,  Yuji Yamauchi ,  Taisuke Inagaki ,  Yasuhiro Kojima ,  Nakao Kojima

    发明人： Hiroyuki Nishida ,  Yuji Yamauchi ,  Taisuke Inagaki ,  Yasuhiro Kojima ,  Nakao Kojima

    IPC分类号： C12P1718

    CPC分类号： C07D498/18 ,  C12P17/188

    摘要： This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocylic lactone compound from the fermentation broth. The compounds produced by this process include a compound of the following formula: The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.

    摘要翻译： 本发明提供了一种制备大环内酯化合物的方法，其包括培养活性平板体。 FERM BP-3832，在L-脯氨酸，L-羟脯氨酸或L-乳酸的存在下，然后从发酵液中分离大环内酯化合物。 通过该方法制备的化合物包括下式的化合物：本发明还涉及包含该化合物的药物组合物，其可用作免疫抑制，抗真菌剂，抗肿瘤剂等。