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    Radicicol derivatives
    6.
    发明授权
    Radicicol derivatives 失效
    蓝霉素衍生物

    公开(公告)号：US5977165A

    公开(公告)日：1999-11-02

    申请号：US958285

    申请日：1997-10-27

    申请人： Tsutomu Agatsuma ,  Yutaka Saitoh ,  Yoshinori Yamashita ,  Tamio Mizukami ,  Shiro Akinaga ,  Katsushige Gomi ,  Kazuhito Akasaka ,  Isami Takahashi

    发明人： Tsutomu Agatsuma ,  Yutaka Saitoh ,  Yoshinori Yamashita ,  Tamio Mizukami ,  Shiro Akinaga ,  Katsushige Gomi ,  Kazuhito Akasaka ,  Isami Takahashi

    IPC分类号： C07D313/00 ,  A61K31/335

    CPC分类号： C07D313/00

    摘要： The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R.sup.4 --O--N (wherein R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl); and R.sup.3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R.sup.3 are combined with each other to represent a single bond; Y represents R.sup.4B --O--N (wherein R.sup.4B has the same meaning as R.sup.4). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.

    摘要翻译： 本发明涉及由下式（I）表示的根赤壳菌素衍生物或其药理学上可接受的盐：其中R1和R2相同或不同，各自代表氢，烷酰基，烯酰基或叔丁基二甲基甲硅烷基; （1）当X表示卤素时，Y表示氧原子或R4-O-N（其中R4表示氢或取代或未取代的低级烷基）; 和R3表示氢，烷酰基，烯酰基等; 和（2）当X和R 3相互结合以表示单键时; Y表示R4B-O-N（其中R4B与R4相同）。 本发明的根皮霉素衍生物显示出酪氨酸激酶抑制活性和药理活性，如抗肿瘤，抗微生物或免疫抑制作用。

    2-piperidone compounds
    9.
    发明授权
    2-piperidone compounds 失效
    2-哌啶酮化合物

    公开(公告)号：US06492392B1

    公开(公告)日：2002-12-10

    申请号：US09481542

    申请日：2000-01-12

    申请人： Yutaka Kanda ,  Rieko Tanaka ,  Mitsunobu Hara ,  Jun Eishima ,  Shiro Akinaga ,  Tadashi Ashizawa

    发明人： Yutaka Kanda ,  Rieko Tanaka ,  Mitsunobu Hara ,  Jun Eishima ,  Shiro Akinaga ,  Tadashi Ashizawa

    IPC分类号： A61K31445

    CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D405/14 ,  C07D409/14

    摘要： The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful as medicaments, as well as antitumor agents containing these compounds. The 2-piperidone compound is represented by the following formula (I): wherein R1 represents —(CH2)nR1a {wherein n is an integer of from 0 to 5, and R1a represents amino, lower alkylamino, di(lower alkyl)amino, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group}, and R2 and R3 independently represent lower alkyl which may be substituted by lower alkoxycarboyl; lower alkenyl, aralkyl or lower alkynyl which may be substituted by substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; substituted or unsubstituted aryl; or a substituted or unsubstituted heterocyclic group.

    摘要翻译： 本发明提供了具有抑制肿瘤细胞增殖的有效活性的2-哌啶酮化合物或其药学上可接受的盐，因此可用作药物，以及含有这些化合物的抗肿瘤剂。 2-哌啶酮化合物由下式（I）表示：其中R1表示 - （CH2）nR1a {其中n为0-5的整数，R1a表示氨基，低级烷基氨基，二（低级烷基）氨基，取代的 或未取代的芳基，或取代或未取代的杂环基}，R2和R3独立地表示可以被低级烷氧基羰基取代的低级烷基; 可被取代或未取代的芳基或取代或未取代的杂环基取代的低级烯基，芳烷基或低级炔基; 取代或未取代的芳基; 或取代或未取代的杂环基。