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    NITROGENOUS-RING ACYLGUANIDINE DERIVATIVE
    4.
    发明申请
    NITROGENOUS-RING ACYLGUANIDINE DERIVATIVE 有权
    硝基环丙酰胺衍生物

    公开(公告)号：US20120142727A1

    公开(公告)日：2012-06-07

    申请号：US13388872

    申请日：2010-08-05

    申请人： Isao Kinoyama ,  Takehiro Miyazaki ,  Yohei Koganemaru ,  Takuya Washio ,  Wataru Hamaguchi

    发明人： Isao Kinoyama ,  Takehiro Miyazaki ,  Yohei Koganemaru ,  Takuya Washio ,  Wataru Hamaguchi

    IPC分类号： A61K31/472 ,  C07D217/14 ,  C07D215/60 ,  A61P25/00 ,  A61K31/4709 ,  A61P25/28 ,  A61P25/18 ,  C07D215/48 ,  A61K31/47

    CPC分类号： C07D215/48 ,  C07D215/54 ,  C07D215/60 ,  C07D217/02 ,  C07D217/14 ,  C07D217/16 ,  C07D217/22 ,  C07D401/04

    摘要： [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided.[Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.

    摘要翻译： 提供了一种基于5-羟色胺5-HT5A受体调节作用预防或治疗痴呆，精神分裂症等的优异剂。 [解决方案]确认酰基胍衍生物（下式I，Z 1，Z 2，Z 3，Z 4和Z 5中的任一个为氮原子，其余为碳原子），其特征在于胍 通过羰基与喹啉或异喹啉的一个环键合，并且环状基团与另一个环键合，表现出基于5-HT5A受体调节作用的有效的5-HT5A受体调节作用和优异的药理作用，因此可以 是预防或治疗痴呆，精神分裂症，双相情感障碍或注意缺陷多动障碍的优良药剂。 因此，本发明已经完成。

    Benzimidazolylidene propane-1,3-dione derivative or salt thereof
    7.
    发明授权
    Benzimidazolylidene propane-1,3-dione derivative or salt thereof 失效
    苯并咪唑基丙烷-1,3-二酮衍生物或其盐

    公开(公告)号：US08076367B2

    公开(公告)日：2011-12-13

    申请号：US12726506

    申请日：2010-03-18

    申请人： Masaaki Hirano ,  Eiji Kawaminami ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Kei Ohnuki ,  Kazuyoshi Obitsu ,  Toshiyuki Kusayama

    发明人： Masaaki Hirano ,  Eiji Kawaminami ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Kei Ohnuki ,  Kazuyoshi Obitsu ,  Toshiyuki Kusayama

    IPC分类号： A01N43/52

    CPC分类号： C07D401/06

    摘要： Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.

    摘要翻译： 提供了可用作GnRH受体拮抗剂的化合物。 本发明人进一步研究了丙-1,3-二酮衍生物，结果确认了具有2-（1,3-二氢-2H-苯并咪唑-2-亚基）的丙-1,3-二酮或化合物 其具有被衍生自1-羟甲基的基团取代的苯或噻吩环，除了其优异的GnRH受体拮抗作用外，显示出优异的可利用性，从而完成本发明。 由于本发明的化合物显示出优异的可利用性，除了其强的GnRH受体拮抗作用外，可以预期其在生物体中具有优异的药物作用，并且可用于治疗性激素依赖性疾病如前列腺癌 ，乳腺癌，子宫内膜异位症，子宫平滑肌瘤，良性前列腺肥大等。 此外，由于本发明的化合物在人体中的代谢稳定性优异，药物相互作用也较少，因此作为上述疾病的药物具有更优选的特性。