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    Benzimidazolylidene propane-1,3-dione derivative or salt thereof
    1.
    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。

    BENZIMIDAZOLYLIDENE PROPANE-1,3-DIONE DERIVATIVE OR SALT THEREOF
    2.
    发明申请
    BENZIMIDAZOLYLIDENE PROPANE-1,3-DIONE DERIVATIVE OR SALT THEREOF 失效
    苯并咪唑啉酮1,3-丙二醇衍生物或其盐

    公开(公告)号：US20100173946A1

    公开(公告)日：2010-07-08

    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： A61K31/4439 ,  C07D405/10 ,  A61K31/4184 ,  C07D407/14 ,  A61P13/08 ,  A61P35/00

    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。

    Propane-1,3-Dione Derivative or Salt Thereof
    3.
    发明申请
    Propane-1,3-Dione Derivative or Salt Thereof 失效
    丙烷-1,3-二酮衍生物或其盐

    公开(公告)号：US20090018177A1

    公开(公告)日：2009-01-15

    申请号：US10588485

    申请日：2005-06-02

    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： A61K31/4184 ,  C07D235/06 ,  A61P35/04

    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。

    Benzimidazolylidene propane-1,3 dione derivative or salt thereof
    4.
    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：US07709519B2

    公开(公告)日：2010-05-04

    申请号：US10588485

    申请日：2005-06-02

    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。