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53 条记录 (耗时 0.048 秒)

    Aminopyridine derivatives having Aurora A selective inhibitory action
    8.
    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。

    Isoxazolopyridone derivatives and their use
    10.
    发明授权
    Isoxazolopyridone derivatives and their use 失效
    异恶唑吡啶酮衍生物及其用途

    公开(公告)号：US07053219B2

    公开(公告)日：2006-05-30

    申请号：US10732988

    申请日：2003-12-10

    申请人： Masayuki Nakamura ,  Hideki Kurihara ,  Mitsuru Ohkubo ,  Naohiro Tsukamoto

    发明人： Masayuki Nakamura ,  Hideki Kurihara ,  Mitsuru Ohkubo ,  Naohiro Tsukamoto

    IPC分类号： C07D471/22 ,  A61K31/44

    CPC分类号： C07D498/04

    摘要： The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substituted phenyl or heteroaryl group, and R3a represents a methyl group, provided that, (1) when R1a is an unsubstituted phenyl group, then R2a must not be a para-substituted phenyl group of which the substituent is any of a methoxy group, a chloro group, a methyl group, a trifluoromethyl group, a fluoro group, a bromomethyl group or a dimethylaminomethyl group, and R2a must not be an unsubstituted heteroaryl group, and (2) when R1a is a 4-tolyl group or a 4-fluorophenyl group, then R2a must not be an unsubstituted phenyl group, a 4-methoxyphenyl group or a 4-fluorophenyl group, or their pharmaceutically-acceptable salts. The isoxazolopyridone derivatives or their pharmaceutically-acceptable salts of the invention have a metabotropic glutamic acid receptor-antagonistic effect, and are useful for remedy of, for example, anxiety disorders, psychosomatic disorders, obsessive-compulsive neurosis, bipolar disorders, melancholia, eating disorders, schizophrenia, multi-infarct dementia, Alzheimer disease, epilepsy, Parkinson disease, Huntington's chorea, pain or retrograde neurosis.

    摘要翻译： 本发明涉及式（Ia）的异恶唑吡啶酮衍生物：其中R 1a表示任选取代的杂芳基或苯基，R 2a表示任选取代的苯基或杂芳基 基团，且R 3a表示甲基，条件是（1）当R 1a为未取代的苯基时，R 2a必须 不是取代基是甲氧基，氯基，甲基，三氟甲基，氟基，溴甲基或二甲基氨基甲基中的任何一个的对位取代的苯基，R 2a， / SUP>不能是未取代的杂芳基，和（2）当R 1a是4-甲苯基或4-氟苯基时，R 2a不能 为未取代的苯基，4-甲氧基苯基或4-氟苯基，或其药学上可接受的盐。 本发明的异恶唑吡啶酮衍生物或其药学上可接受的盐具有代谢型谷氨酸受体拮抗作用，并且可用于治疗例如焦虑症，心理障碍，强迫性神经症，双相情感障碍，忧郁症，进食障碍 ，精神分裂症，多发性梗塞性痴呆，阿尔茨海默病，癫痫，帕金森病，亨廷顿舞蹈病，疼痛或逆行神经症。