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12 条记录 (耗时 0.018 秒)

    Hexa-cyclic compound
    1.
    发明授权
    Hexa-cyclic compound 失效
    六环化合物

    公开(公告)号：US5834476A

    公开(公告)日：1998-11-10

    申请号：US989420

    申请日：1997-12-12

    申请人： Hirofumi Terasawa ,  Akio Ejima ,  Satoru Ohsuki ,  Kouichi Uoto

    发明人： Hirofumi Terasawa ,  Akio Ejima ,  Satoru Ohsuki ,  Kouichi Uoto

    IPC分类号： C07D491/22 ,  C07D495/22 ,  A61K31/40 ,  A61K31/435 ,  C07D471/22

    CPC分类号： C07D491/22 ,  C07D495/22

    摘要： A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.

    摘要翻译： 一种新颖的六环化合物，喜树碱的衍生物，具有以下通式：该化合物通过缩合闭合反应由氨基酮化合物和吡喃并吲哚化合物制备。 水溶性丰富，抗肿瘤活性优良，安全性高，可用作治疗各种肿瘤的抗肿瘤药物。

    Pyrazole derivatives
    3.
    发明授权
    Pyrazole derivatives 失效
    吡唑衍生物

    公开(公告)号：US06552018B1

    公开(公告)日：2003-04-22

    申请号：US09688787

    申请日：2000-10-17

    申请人： Akio Ejima ,  Satoru Ohsuki ,  Hitoshi Ohki ,  Hiroyuki Naito

    发明人： Akio Ejima ,  Satoru Ohsuki ,  Hitoshi Ohki ,  Hiroyuki Naito

    IPC分类号： C07D40104

    CPC分类号： C07D231/12 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

    摘要： The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.

    摘要翻译： 本发明涉及吡唑衍生物，其盐或含有该取代基的吡唑衍生物，其盐或其代表物的顺式和反式，其通式（I）表示：其中G表示由下式表示的含氮饱和杂环结构：这些 化合物对5-FU抗性肿瘤表现出抗肿瘤活性，对P糖蛋白表达，多重耐药性肿瘤有影响。 显示50％抑制肿瘤细胞生长的吡唑衍生物的实例是3- [4-（3-氯-5-氟苯基）-1-哌嗪基] -1- [1-（3-氯-2-吡啶基）-5 - 甲基-4-吡唑基）-1-反丙烯盐酸盐。 由式（I）表示的化合物的合成可以通过各种途径中的任何一种制备，例如曼尼希反应，维蒂希反应，还原胺化或烯丙基取代。

    PYRAZOLOPYRIMIDINE DERIVATIVE
    5.
    发明申请
    PYRAZOLOPYRIMIDINE DERIVATIVE 有权
    吡唑并嘧啶衍生物

    公开(公告)号：US20100113410A1

    公开(公告)日：2010-05-06

    申请号：US12442094

    申请日：2007-09-14

    申请人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

    发明人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

    IPC分类号： A61K31/519 ,  C07D495/16 ,  C07D487/04 ,  C07D495/20 ,  A61K31/5377 ,  A61P35/00

    CPC分类号： C07D495/16 ,  C07D495/20 ,  C07D495/22 ,  C07D498/22

    摘要： Problem to be Solved To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity. Solution The present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).

    摘要翻译： 要解决的问题提供抑制HSP90的作用的新型化合物，特别是抑制HSP90作为伴侣蛋白的功能并具有抗肿瘤活性的新化合物。 溶液本发明提供了具有抑制HSP90的ATP酶活性且具有抗肿瘤活性的各种取代基的式（1）表示的吡唑并嘧啶化合物，包含由式（1）表示的化合物的HSP90抑制剂，包含化合物 （1）代表的抗癌剂，包含由式（1）表示的化合物的抗癌剂，包含式（1）表示的化合物的药物组合物和使用式（1）表示的化合物治疗癌症的方法 ）。

    Hexa-cyclic compound
    6.
    发明授权
    Hexa-cyclic compound 失效
    六环化合物

    公开(公告)号：US5637770A

    公开(公告)日：1997-06-10

    申请号：US455718

    申请日：1995-05-31

    申请人： Hirofumi Terasawa ,  Akio Ejima ,  Satoru Ohsuki ,  Kouichi Uoto

    发明人： Hirofumi Terasawa ,  Akio Ejima ,  Satoru Ohsuki ,  Kouichi Uoto

    IPC分类号： C07D491/22 ,  C07D495/22 ,  C07C233/05

    CPC分类号： C07D491/22 ,  C07D495/22

    摘要： A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.

    摘要翻译： 一种新颖的六环化合物，喜树碱的衍生物，具有以下通式：该化合物通过缩合闭合反应由氨基酮化合物和吡喃并吲哚化合物制备。 水溶性丰富，抗肿瘤活性优良，安全性高，可用作治疗各种肿瘤的抗肿瘤药物。

    Pyrazolopyrimidine derivative
    7.
    发明授权
    Pyrazolopyrimidine derivative 有权
    吡唑并嘧啶衍生物

    公开(公告)号：US08158638B2

    公开(公告)日：2012-04-17

    申请号：US12442094

    申请日：2007-09-14

    申请人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

    发明人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

    IPC分类号： A61K31/505 ,  A61K31/415 ,  C07D491/00 ,  C07D487/02

    CPC分类号： C07D495/16 ,  C07D495/20 ,  C07D495/22 ,  C07D498/22

    摘要： Problem to be SolvedTo provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity.SolutionThe present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).

    摘要翻译： 要解决的问题提供抑制HSP90的作用的新型化合物，特别是抑制HSP90作为伴侣蛋白的功能并具有抗肿瘤活性的新化合物。 溶液本发明提供了具有抑制HSP90的ATP酶活性且具有抗肿瘤活性的各种取代基的式（1）表示的吡唑并嘧啶化合物，包含由式（1）表示的化合物的HSP90抑制剂，包含化合物 （1）代表的抗癌剂，包含由式（1）表示的化合物的抗癌剂，包含式（1）表示的化合物的药物组合物和使用式（1）表示的化合物治疗癌症的方法 ）。

    Hexa-cyclic compound
    8.
    发明授权
    Hexa-cyclic compound 失效
    六环化合物

    公开(公告)号：US06407115B1

    公开(公告)日：2002-06-18

    申请号：US08451993

    申请日：1995-05-26

    申请人： Hirofumi Terasawa ,  Akio Ejima ,  Satoru Ohsuki ,  Kouichi Uoto

    发明人： Hirofumi Terasawa ,  Akio Ejima ,  Satoru Ohsuki ,  Kouichi Uoto

    IPC分类号： C07D49122

    CPC分类号： C07D491/22 ,  C07D495/22

    摘要： Accordingly, an object of this invention is to provide a hexa-cyclic compound represented by the following general formula: wherein R1 and R2 individually represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group (“C1-6 alkyl group means an alkyl group having 1 to 6 carbon atoms. Hereinafter defined in the same manner.) The present inventors have conducted extensive studies for the purpose of obtaining camptothecin derivatives with more excellent activity and higher safety, as well as excellent characteristics required for a drug to be administered, and found that hexa-cyclic compounds obtained by the addition of a water-soluble ring to camptothecin had characteristics superior to camptothecin. This finding has led to the completion of this invention.

    摘要翻译： 因此，本发明的目的是提供由以下通式表示的六环化合物：其中R 1和R 2各自表示氢原子，羟基，C 1-6烷基（“C 1-6烷基” 具有1〜6个碳原子的烷基，以下相同的方式定义。）本发明人为了得到活性更高，安全性更好的喜树碱衍生物进行了广泛的研究， 并且发现通过向喜树碱中加入水溶性环获得的六环化合物具有优于喜树碱的特征，这一发现导致本发明的完成。