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    SUBSTANCE FA-70D, PROCESS FOR PRODUCING THE SAME, AND USES THEREOF
    2.
    发明公开
    SUBSTANCE FA-70D, PROCESS FOR PRODUCING THE SAME, AND USES THEREOF 失效
    SUBSTANZ FA-70D，HERSTELLUNGSVERFAHREN UND VERWENDUNGEN

    公开(公告)号：EP0822260A1

    公开(公告)日：1998-02-04

    申请号：EP97904590.3

    申请日：1997-02-20

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： KITANO, Shizuo ,  SASAKI, Toru ,  YOSHIDA, Kenichiro ,  OTANI, Toshio ,  YU, Lei ,  WU, Yun ,  KATSUNUMA, Nobuhiko

    IPC分类号： C12P21/02 ,  C07K5/068 ,  A61K38/05

    CPC分类号： C07K5/06095 ,  A61K38/00 ,  C12P21/02

    摘要： Substance FA-70D which has the following formula (1) or its salt, a method for its production, a pharmaceutical composition comprising the compound as an active ingredient, a method of treating osteoporosis which comprises administering the compound, use of the compound as a drug, and a microorganism capable of producing Substance FA-70D.

    This compound has specific inhibitory activity against cathepsin series proteases and is of value as a therapeutic drug for various diseases with which these enzymes are associated, particularly osteoporosis.

    摘要翻译： 具有下式（1）的物质FA-70D或其盐，其制备方法，包含该化合物作为活性成分的药物组合物，治疗骨质疏松症的方法，其包括施用该化合物，使用该化合物作为 药物和能够产生物质FA-70D的微生物。 该化合物对组织蛋白酶系列蛋白酶具有特异性抑制活性，作为与这些酶相关的各种疾病，特别是骨质疏松症的治疗药物是有价值的。

    IT-62-B SUBSTANCE AND MEDICINAL COMPOSITION CONTAINING THE SAME
    4.
    发明公开
    IT-62-B SUBSTANCE AND MEDICINAL COMPOSITION CONTAINING THE SAME 失效
    DIE SUBSTANZ IT-62-B UND SIE ENTHALTENDE MEDISINISCHE ZUBEREITUNGEN

    公开(公告)号：EP0721985A1

    公开(公告)日：1996-07-17

    申请号：EP95925105.9

    申请日：1995-07-12

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： KAWAUCHI, Takashi ,  SASAKI, Toru ,  MATSUMOTO, Hiroshi ,  OTANI, Toshio ,  CHEN, Ru-Xian ,  HUANG, Ming-Yu ,  YOSHIDA, Ken-ichiro

    IPC分类号： C12P19/56 ,  C07H15/252 ,  A61K31/71

    CPC分类号： C07H15/252 ,  C07H17/00 ,  C12P19/56

    摘要： An IT-62-B substance represented by formula (1), a process for producing the same, a medicinal composition containing the same as the active ingredient, and a method of treating bacterium-induced infectious diseases and tumors by administering the same. The compound has antibacterial activities against gram-positive bacteria and part of gram-negative bacteria and also has an excellent antitumor activity against, for example, human nasopharyngeal cancer, thus being useful as a medicine.

    摘要翻译： 由式（1）表示的IT-62-B物质，其制备方法，含有该活性成分的药物组合物，以及通过施用该细菌诱导的感染性疾病和肿瘤的方法。 该化合物对革兰氏阳性菌和革兰氏阴性细菌的一部分具有抗菌活性，并且对于例如人鼻咽癌具有优异的抗肿瘤活性，因此可用作药物。

    NOVEL 3-(SUBSTITUTED METHYL)-4-OXA-1-AZABICYCLO 3.2.0]HEPTAN-7-ONE DERIVATIVES USEFUL AS ANTITUMOR AGENTS
    6.
    发明公开
    NOVEL 3-(SUBSTITUTED METHYL)-4-OXA-1-AZABICYCLO 3.2.0]HEPTAN-7-ONE DERIVATIVES USEFUL AS ANTITUMOR AGENTS 失效
    3-（取代的甲基）-4-氧杂-1-AZABICYCLO¬3.2.0庚-7-酮衍生物作为抗肿瘤剂

    公开(公告)号：EP0688324A1

    公开(公告)日：1995-12-27

    申请号：EP95904658.0

    申请日：1995-01-06

    申请人： TAIHO PHARMACEUTICAL CO., LTD. ,  SYNPHAR LABORATORIES INC.

    发明人： SINGH, Rajeshwar ,  YAMASHITA, Tomohiro ,  FIAKPUI, Charles ,  THOMAS, George ,  HA, Chan ,  MATSUMOTO, Hiroshi ,  OTANI, Toshio ,  OIE, Shinji ,  MICETICH, Ronald

    IPC分类号： A61K31 ,  A61P35 ,  C07D503

    CPC分类号： C07D503/00 ,  Y02P20/55

    摘要： The present invention is based on the discovery that certain 3-(substituted methyl)-4-oxa-1-azabicyclo[3.2.0]heptan-7-one derivatives of formula (I) or a pharmaceutically acceptable salt thereof are useful as antitumor agents against sensitive and resistant tumor cells. In Formula (I) X is NH or O, when X is NH, R is hydrogen, -COR1, wherein R1 is (i) a C1-C6 alkyl group which may be substituted by 1-3 substituents selected from halogen, hydroxy, formyloxy, azido, carboxyl, heteroaryl or acetamide, (ii) a C2-C4 alkenyl group, (iii) a C2-C4 alkynyl group, (iv) a C3-C6 cycloalkyl group, (v) a phenyl group which may be substituted by 1-3 substituents selected from hydroxy, halogen, C1-C6 alkoxy group or cyano, (vi) a C5-C6 heteroaryl group, (vii) an NR2R3 wherein R2 and R3 are the same or different and each is a hydrogen, C1-C6 alkyl group or (7-oxo-1-aza-4-oxabicyclo[3.2.0]hept-3-yl)methyl group or (viii) benzyloxy group; -SO2R4 wherein R4 is a C1-C6 alkyl group or a phenyl group which may be substituted by 1-3 substituents selected from C1-C6 alkyl group, halogen or C1-C6 alkoxy group; 1-2 amino acid residue which may be substituted with protective group; when X is O, R is 1-2 amino acid residue which may be substituted with protective group.