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    NOVEL AMINOPYRIDINE DERIVATIVE HAVING AURORA-A-SELECTIVE INHIBITORY ACTIVITY
    8.
    发明公开
    NOVEL AMINOPYRIDINE DERIVATIVE HAVING AURORA-A-SELECTIVE INHIBITORY ACTIVITY 有权
    氨基嘧啶衍生物麻醉剂AURORA-A-SELEKTIVER HEMMENDER WIRKUNG

    公开(公告)号：EP2017279A1

    公开(公告)日：2009-01-21

    申请号：EP07742848.0

    申请日：2007-04-25

    申请人： BANYU PHARMACEUTICAL CO., LTD.

    发明人： KATO, Tetsuya ,  KAWANISHI, Nobuhiko ,  MITA, Takashi ,  NAGAI, Keita ,  NONOSHITA, Katsumasa ,  OHKUBO, Mitsuru

    IPC分类号： C07D487/08 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K45/08 ,  A61P35/00 ,  A61P43/00

    CPC分类号： C07D487/08

    摘要： The present invention relates to a compound of general formula I:

    wherein:
    n 1 and n 2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; R e is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of R a1 and R a1 ', (ii) either one of R a2 and R a2 ', (iii) either one of R b1 and R b1 ', and (iv) either one of R b2 and R b2 ', are combined to form -(CH 2 ) n - where n is 1, 2 or 3; and among R a1 , R a1 ', R a2 , R a2 ', R b1 , R b1 ', R b2 and R b2 ', the groups which do not form -(CH 2 ) n - are each independently hydrogen atom, etc.; X 1 , X 2 , X 3 and X 4 are each independently CH, N, etc.; Y 1 , Y 2 , Y 3 and Y 4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group,

    or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译： 本发明涉及通式I的化合物：其中：n 1和n 2相同或不同，为0或1; R是芳基，杂芳基等; R e为氢原子或低级烷基; 从（a）R a1和R a1'中的任一个，（ii）R a2和R a2'中的任一个，（iii）R b1和R b1'中的任一个和（iv） ）R b2和R b2'中的任一个组合形成 - （CH 2）n - ，其中n为1,2或3; 在R a1，R a1'，R a2，R a2'，R b1，R b1'，R b2和R b2'中，不形成 - （CH 2）n - 的基团各自独立地为氢原子等 。 X 1，X 2，X 3和X 4各自独立地为CH，N等; Y 1，Y 2，Y 3和Y 4相同或不同，为CH或N等; W是5元芳杂环基，或其药学上可接受的盐或酯。

    SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON
    10.
    发明公开
    SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON 审中-公开
    SELEKTIVE INHIBITOREN GEGEN CDK4 UND CDK6 MIT AMINOTHIAZOLSKELETT

    公开(公告)号：EP1754706A1

    公开(公告)日：2007-02-21

    申请号：EP05743671.9

    申请日：2005-05-19

    申请人： BANYU PHARMACEUTICAL CO., LTD.

    发明人： IWASAWA, Yoshikazu ,  SHIBATA, Jun ,  SHIMAMURA, Tadashi ,  KURIHARA, Hideki ,  MITA, Takashi ,  KAWANISHI, Nobuhiko ,  HASHIHAYATA, Takashi ,  KAWAMURA, Mikako ,  SAGARA, Takeshi ,  ARAI, Sachie ,  HIRAI, Hiroshi

    IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61P35/00 ,  A61P43/00

    CPC分类号： C07D417/14 ,  C07D417/12 ,  C07D491/08

    摘要： The present invention relates to a compound represented by Formula [I]:

    wherein
    X is O, S, NH or CH 2 ;
    Y 1 , Y 2 , Y 3 , Y 4 and Y 5 , which may be identical or different, are each CH or N; however, at least one of Y 1 , Y 2 , Y 3 , Y 4 and Y 5 is N;
    Z 1 and Z 2 , which may be identical or different, are each CH or N;
    n is an integer from 1 to 3;
    R 1 is a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group;
    R 2 and R 3 , which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aromatic heterocyclic ring, or the like; and
    R 4 is a hydrogen atom, a lower alkyl group, a C 3 -C 6 cycloalkyl group or the like,
    or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译： 本发明涉及由式[I]表示的化合物：其中X是O，S，NH或CH 2; Y 1，Y 2，Y 3，Y 4和Y 5可以相同或不同，分别为CH或N; 然而，Y 1，Y 2，Y 3，Y 4和Y 5中的至少一个为N; Z 1和Z 2可以相同或不同，各自为CH或N; n为1〜3的整数， R 1为C 3〜C 8环烷基，C 6〜C 10芳基，脂肪族杂环或芳香族杂环，双环脂肪族饱和烃基， R 2和R 3可以相同或不同，分别为氢原子，低级烷基，低级烯基，C 3〜C 8环烷基，C 6〜C 10芳基，芳香族杂环 环等; R 4为氢原子，低级烷基，C 3〜C 6环烷基等，或其药学上可接受的盐或酯，以及对Cdk4和/或Cdk6的选择性抑制剂或含有 化合物或其药学上可接受的盐或酯。