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    Hexa-cyclic compound
    3.
    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。

    Hexa-cyclic compound
    4.
    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。

    Hexa-cyclic compound
    6.
    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。

    Method for treating leukemia with a hexa-cyclic compound
    7.
    发明授权
    Method for treating leukemia with a hexa-cyclic compound 失效
    用六环化合物治疗白血病的方法

    公开(公告)号：US5770605A

    公开(公告)日：1998-06-23

    申请号：US811239

    申请日：1997-03-03

    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 ,  A61K31/47

    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 antitumor activity and a high degree of safety, and can be applied as an antitumor 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，具有优异的抗肿瘤活性和高度的安全性，可用作治疗各种肿瘤的抗肿瘤药物。

    Pentacyclic compound
    9.
    发明授权
    Pentacyclic compound 有权
    五环化合物

    公开(公告)号：US06545151B2

    公开(公告)日：2003-04-08

    申请号：US09759378

    申请日：2001-01-16

    申请人： Hirofumi Terasawa ,  Tsunehiko Soga ,  Takashi Ishiyama

    发明人： Hirofumi Terasawa ,  Tsunehiko Soga ,  Takashi Ishiyama

    IPC分类号： C07D49308

    CPC分类号： C07D493/08 ,  C07D305/14

    摘要： The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].

    摘要翻译： 本发明涉及由式（1）表示的具有抗肿瘤活性的新型紫杉醇衍生物[式（I）中，R 1为苯基，R 2为烷基，烯基，炔基 ，环烷基或烷氧基，R3：氢原子，羟基，卤素原子，烷氧基，-O-R31基，酰氧基或-O-CO-R31基（其中R31 ：烷基氨基，烯基，炔基，环烷基，芳基或杂环基），R4和R5：氢原子，烷基，烯基，炔基，芳基或 杂环基，Z 1：氢原子，羟基，卤原子或烷基，Z 2：氢原子，羟基，卤素原子或烷基，Z 3：烷基，烯基， 炔基，环烷基，芳基或杂环基]。

    Pentacyclic Compound
    10.
    发明授权
    Pentacyclic Compound 失效
    五环化合物

    公开(公告)号：US06646123B2

    公开(公告)日：2003-11-11

    申请号：US10126653

    申请日：2002-04-22

    申请人： Hirofumi Terasawa ,  Tsunehiko Soga ,  Takashi Ishiyama

    发明人： Hirofumi Terasawa ,  Tsunehiko Soga ,  Takashi Ishiyama

    IPC分类号： C07D49308

    CPC分类号： C07D493/08 ,  C07D305/14

    摘要： The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R311 an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].

    摘要翻译： 本发明涉及由式（1）表示的具有抗肿瘤活性的新型紫杉醇衍生物[在式（I）中，R 1：苯基，R 2：烷基，烯基 基团，炔基，环烷基或烷氧基，R 3：氢原子，羟基，卤素原子，烷氧基，基团-OR 31，酰氧基或基团， O-CO-R 31（其中R 31：烷基氨基，烯基，炔基，环烷基，芳基或杂环基），R 4和R 5 >：氢原子，烷基，烯基，炔基，芳基或杂环基，Z 1：氢原子，羟基，卤素原子或烷基，Z 2 >：氢原子，羟基，卤素原子或烷基，Z 3：烷基，烯基，炔基，环烷基，芳基或杂环基]。