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10 条记录 (耗时 0.137 秒)

    2-piperidone compounds
    7.
    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。

    Agent for inducing apoptosis
    9.
    发明授权
    Agent for inducing apoptosis 失效
    诱导细胞凋亡的药物

    公开(公告)号：US06548536B2

    公开(公告)日：2003-04-15

    申请号：US09793654

    申请日：2001-02-27

    申请人： Mitsunobu Hara ,  Takayuki Nakashima ,  Yutaka Kanda ,  Masami Hamano ,  Shun-ichi Ikeda ,  Yuko Uosaki ,  Yoko Takata ,  Junji Kanazawa

    发明人： Mitsunobu Hara ,  Takayuki Nakashima ,  Yutaka Kanda ,  Masami Hamano ,  Shun-ichi Ikeda ,  Yuko Uosaki ,  Yoko Takata ,  Junji Kanazawa

    IPC分类号： A61K3134

    CPC分类号： C07D407/14 ,  A61K31/00 ,  A61K31/365 ,  C07H17/08

    摘要： Agents for inducing apoptosis comprising a tetrocarcin derivative represented by the following formula (I) or a salt thereof as an active ingredient (---- represents a single bond or a double bond; j and k represent 0 or 1; R1 to R3, R7 to R10 and R14 represent a hydrogen atom, a lower alkyl group and the like; R4, R11, R12, R13 and R15 to R18 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like; R5 and R6 represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a group represented by the following formula (B) (R32 represents a formyl group and the like, R33 to R35 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like); R19 represents a hydroxyl group, a lower alkoxyl group, a lower alkanoyloxy group and the like). The agents are useful as medicaments for preventive and/or therapeutic treatment of diseases resulting from increased expression of Bcl-2 family proteins, for example, cancers, AIDS and the like.

    摘要翻译： 用于诱导凋亡的药剂，其包含由下式（I）表示的四环卟啉衍生物或其盐作为活性成分（----表示单键或双键; j和k表示0或1; R 1至R 3， R 7〜R 10和R 14表示氢原子，低级烷基等; R 4，R 11，R 12，R 13，R 15〜R 18表示氢原子，羟基，低级烷基等; R 5，R 6表示 氢原子，羟基，低级烷基，下式（B）表示的基团（R32表示甲酰基等，R33〜R35表示氢原子，羟基，低级烷基， 类似）; R 19表示羟基，低级烷氧基，低级烷酰氧基等）。 这些药剂可用作预防和/或治疗由Bcl-2家族蛋白（例如癌症，AIDS等）表达增加而引起的疾病的药物。

    UCF116 derivatives
    10.
    发明授权
    UCF116 derivatives 失效
    UCF116衍生物

    公开(公告)号：US06407087B1

    公开(公告)日：2002-06-18

    申请号：US09605014

    申请日：2000-06-27

    申请人： Mitsunobu Hara ,  Shiro Akinaga ,  Yutaka Kanda ,  Timothy S. Powers ,  David A. Johnson

    发明人： Mitsunobu Hara ,  Shiro Akinaga ,  Yutaka Kanda ,  Timothy S. Powers ,  David A. Johnson

    IPC分类号： C07D22506

    CPC分类号： C07D401/12 ,  C07D225/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

    摘要： UCF116 derivatives represented by formula (I): wherein Q represents and R represents hydrogen, C(═O)R1a (wherein R1a represents methyl, ethyl, propyl, isopropyl, 2,2-dimethylpropyl, pentyl, alkyl having 6 to 10 carbon atoms, 1-propenyl, isopropenyl, 2-methyl-1-propenyl, substituted or unsubstituted alicyclic alkyl having 3 to 5 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aralkyloxy, or substituted lower alkyl), C(═X)NHR1b (wherein X represents an oxygen or sulfur atom, and R1b represents substituted or unsubstituted lower alkyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group), or SO2R1c (wherein R1c represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, or substituted or unsubstituted lower alkenyl), with the proviso that, when Q is R is not benzoyl; salts thereof; isomers thereof; hydrates thereof; or solvates thereof.

    摘要翻译： 由式（I）表示的UCF116衍生物：其中Q表示并且R表示氢，C（= O）R 1a（其中R 1a表示甲基，乙基，丙基，异丙基，2,2-二甲基丙基，戊基，具有6至10个碳原子的烷基， 取代或未取代的芳基，取代或未取代的芳烷基，取代或未取代的杂环基，取代或未取代的芳烷氧基或取代或未取代的低级烷基 烷基），C（= X）NHR1b（其中X表示氧或硫原子，并且R1b表示取代或未取代的低级烷基，取代或未取代的脂环族烷基，取代或未取代的低级烷氧基羰基，取代或未取代的芳基，取代或未取代的芳烷基， 或取代或未取代的杂环基）或SO 2 R 1c（其中R 1c表示取代或未取代的低级烷基，取代或未取代的芳基，取代基 芳基或未取代的芳烷基，取代或未取代的杂环基或取代或未取代的低级烯基），条件是当Q不是苯甲酰基时; 的盐; 异构体; 其水合物; 或溶剂化物。