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    Aminopyridine derivatives having aurora a selective inhibitory action
    1.
    发明授权
    Aminopyridine derivatives having aurora a selective inhibitory action 有权
    具有极光选择性抑制作用的氨基吡啶衍生物

    公开(公告)号：US07834018B2

    公开(公告)日：2010-11-16

    申请号：US12315425

    申请日：2008-12-03

    申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    IPC分类号： A61K31/497 ,  C07D241/04 ,  C07D295/00

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

    摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m1和m2为1,2或3; n1和n2为0或1; 我是1到m1中任何一个的整数; j为1〜m2的整数， R是芳基，杂芳基或环烷基，其中任一个可以被取代; Rai和Rai'是氢原子等，Rbj和Rbj'是氢原子等; Rc，Rd和Re为氢原子等; X1是CH，CX1a或N; X2是CH，N等; X3是CH，N等; X4是CH或N; Y1，Y2和Y3各自独立地为CH或N; Z1和Z2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。

    METHOD OF ASSUMING DRUG SENSITIVITY TO CDK4 INHIBITOR
    3.
    发明申请
    METHOD OF ASSUMING DRUG SENSITIVITY TO CDK4 INHIBITOR 审中-公开
    对CDK4抑制剂的药物敏感性的方法

    公开(公告)号：US20090081645A1

    公开(公告)日：2009-03-26

    申请号：US11659258

    申请日：2005-08-02

    申请人： Hidehito Kotani ,  Hiraku Itadani ,  Kazunori Yamanaka ,  Tomohiro Eguchi ,  Toshiyasu Shimomura

    发明人： Hidehito Kotani ,  Hiraku Itadani ,  Kazunori Yamanaka ,  Tomohiro Eguchi ,  Toshiyasu Shimomura

    IPC分类号： C12Q1/68 ,  C12N15/11 ,  C07K16/18

    CPC分类号： C12Q1/485

    摘要： It is intended to provide a gene for assuming drug sensitivity, which is to be used for assuming the drug sensitivity to a CDK4 inhibitor based on the expression amount in a test tissue or a test cell, selected from the group consisting of p16 gene, p18 gene and p27 gene. It is also intended to provide a method of assuming the drug sensitivity to a CDK4 inhibitor by using the expression amount of the above gene in a test tissue or a test cell as an indication.

    摘要翻译： 旨在提供用于假定药物敏感性的基因，其用于基于在选自p16基因，p18的测试组织或测试细胞中的表达量来假定对CDK4抑制剂的药物敏感性 基因和p27基因。 还旨在提供一种通过使用在测试组织或测试细胞中的上述基因的表达量作为指示来确定对CDK4抑制剂的药物敏感性的方法。

    Novel aminopyridine derivatives having aurora a selective inhibitory action
    5.
    发明申请
    Novel aminopyridine derivatives having aurora a selective inhibitory action 有权
    具有极光选择性抑制作用的新型氨基吡啶衍生物

    公开(公告)号：US20090149470A1

    公开(公告)日：2009-06-11

    申请号：US12315425

    申请日：2008-12-03

    申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    IPC分类号： A61K31/497 ,  C07D409/14 ,  A61P35/00

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

    摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m1和m2为1,2或3; n1和n2为0或1; 我是1到m1中任何一个的整数; j为1〜m2的整数， R是芳基，杂芳基或环烷基，其中任一个可以被取代; Rai和Rai'是氢原子等，Rbj和Rbj'是氢原子等; Rc，Rd和Re为氢原子等; X1是CH，CX1a或N; X2是CH，N等; X3是CH，N等; X4是CH或N; Y1，Y2和Y3各自独立地为CH或N; Z1和Z2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。

    Novel aminopyridine derivatives having aurora a selective inhibitory action
    6.
    发明申请
    Novel aminopyridine derivatives having aurora a selective inhibitory action 有权
    具有极光选择性抑制作用的新型氨基吡啶衍生物

    公开(公告)号：US20060106029A1

    公开(公告)日：2006-05-18

    申请号：US11258447

    申请日：2005-10-25

    申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    IPC分类号： A61K31/496 ,  C07D417/14 ,  C07D403/14

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

    摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m 1和m 2是1,2或3; n 1和n 2是0或1; i是1〜m1的任一个的整数; j为1〜m 2的整数; R是芳基，杂芳基或环烷基，其中任一个可以被取代; R a a和R a'是氢原子等，R bj和R b'是氢原子 等等 R c，R d和R e是氢原子等; X 1是CH，CX 1a，或N; X 2是CH，N等; X 3是CH，N等; X 4是CH或N; Y 1，Y 2和Y 3各自独立地为CH或N; Z 1和Z 2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。

    Method for evaluation of compound using RSK1
    7.
    发明申请
    Method for evaluation of compound using RSK1 审中-公开
    使用RSK1评估化合物的方法

    公开(公告)号：US20100151050A1

    公开(公告)日：2010-06-17

    申请号：US11921621

    申请日：2006-06-06

    申请人： Shinji Mizuarai ,  Hidehito Kotani ,  Toshiyasu Shimomura ,  Eri Taniguchi

    发明人： Shinji Mizuarai ,  Hidehito Kotani ,  Toshiyasu Shimomura ,  Eri Taniguchi

    IPC分类号： A61K33/24 ,  C12Q1/68

    CPC分类号： G01N33/5011 ,  G01N2333/91215

    摘要： A method for evaluation of a compound comprising the steps of introducing an RSK1 gene into a cell to prepare a cell capable of expressing RSK1, contacting a compound to be evaluated with the cell, and detecting the specific binding of the compound to RSK1; and a compound given by the method. The compound can be used as a potentiator of cisplatin. The method enables to find a gene which acts specifically on a cell of cancer induced by the abnormality in p53 or enhanced MAPK pathway and to evaluate a compound by using the gene.

    摘要翻译： 一种化合物评价方法，其特征在于，包括以下步骤：将RSK1基因引入细胞，制备能够表达RSK1的细胞，使待评价的化合物与细胞接触，检测该化合物与RSK1的特异性结合; 和该方法给出的化合物。 该化合物可用作顺铂的增效剂。 该方法能够找到特异性地对由p53或增强的MAPK通路异常诱导的癌细胞起作用的基因，并通过使用该基因来评估化合物。

    Aminopyridine derivatives having Aurora A selective inhibitory action
    9.
    发明授权
    Aminopyridine derivatives having Aurora A selective inhibitory action 有权
    具有极光A的氨基吡啶衍生物选择性抑制作用

    公开(公告)号：US07491720B2

    公开(公告)日：2009-02-17

    申请号：US11258447

    申请日：2005-10-25

    申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

    IPC分类号： C07D241/00 ,  C07D241/02 ,  A01N43/58 ,  A61K31/50

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

    摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m1和m2为1,2或3; n1和n2为0或1; 我是1到m1中任何一个的整数; j为1〜m2的整数， R是芳基，杂芳基或环烷基，其中任一个可以被取代; Rai和Rai'是氢原子等，Rbj和Rbj'是氢原子等; Rc，Rd和Re为氢原子等; X1是CH，CX1a或N; X2是CH，N等; X3是CH，N等; X4是CH或N; Y1，Y2和Y3各自独立地为CH或N; Z1和Z2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。