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    1-substituted tetrahydroisoquinoline compound
    5.
    发明授权
    1-substituted tetrahydroisoquinoline compound 有权
    1-取代的四氢异喹啉化合物

    公开(公告)号：US08263607B2

    公开(公告)日：2012-09-11

    申请号：US12600503

    申请日：2008-05-20

    申请人： Jun-ichi Shishikura ,  Makoto Inoue ,  Takashi Ogiyama ,  Koichi Yonezawa ,  Susumu Yamaki ,  Kazuhiro Yokoyama ,  Shuichirou Kakimoto ,  Hidetsugu Okada

    发明人： Jun-ichi Shishikura ,  Makoto Inoue ,  Takashi Ogiyama ,  Koichi Yonezawa ,  Susumu Yamaki ,  Kazuhiro Yokoyama ,  Shuichirou Kakimoto ,  Hidetsugu Okada

    IPC分类号： C07D217/04 ,  C07D491/04 ,  A61K31/472

    CPC分类号： C07D217/04 ,  C07D217/14 ,  C07D217/16 ,  C07D221/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D491/06

    摘要： Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating various pains such as neuropathic pain and nociceptive pain, headaches such as migraine and cluster headache, central nervous system diseases such as anxiety, depression, epilepsy, cerebral stroke and restless legs syndrome, abdominal symptoms such as abdominal pain and abdominal distension, stool abnormalities such as diarrhea and constipation, digestive system diseases such as irritable bowel syndrome, urinary system diseases such as overactive bladder and interstitial cystitis, etc.

    摘要翻译： 提供可用作N型Ca2 +通道阻断剂的化合物。 通过对具有阻塞N型Ca 2+通道作用的化合物的深入研究，本发明人发现在1位具有取代基的本发明的四氢异喹啉化合物具有阻断N型Ca 2+通道的作用 抗痛知性疼痛作用，抗神经病性疼痛作用，腹痛抑制作用和阿片样物质诱导的便秘改善作用，并且基于这些发现完成了本发明。 本发明的化合物可以用作预防和/或治疗诸如神经性疼痛和伤害性疼痛，头痛如偏头痛和丛集性头痛，中枢神经系统疾病如焦虑，抑郁，癫痫，脑的各种疼痛的药物组合物 中风和不宁腿综合症，腹痛，腹胀等腹部症状，腹泻便秘等粪便异常，肠易激综合征等消化系统疾病，膀胱过多膀胱炎，间质性膀胱炎等泌尿系统疾病等。

    1-SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUND
    6.
    发明申请
    1-SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUND 有权
    1-取代的四氢喹啉化合物

    公开(公告)号：US20100168154A1

    公开(公告)日：2010-07-01

    申请号：US12600503

    申请日：2008-05-20

    申请人： Jun-Ichi Shishikura ,  Makoto Inoue ,  Takashi Ogiyama ,  Koichi Yonezawa ,  Susumu Yamaki ,  Kazuhiro Yokoyama ,  Shuichirou Kakimoto ,  Hidetsugu Okada

    发明人： Jun-Ichi Shishikura ,  Makoto Inoue ,  Takashi Ogiyama ,  Koichi Yonezawa ,  Susumu Yamaki ,  Kazuhiro Yokoyama ,  Shuichirou Kakimoto ,  Hidetsugu Okada

    IPC分类号： A61K31/437 ,  C07D217/04 ,  C07D491/04 ,  A61K31/4725 ,  A61K31/472 ,  A61P25/00

    CPC分类号： C07D217/04 ,  C07D217/14 ,  C07D217/16 ,  C07D221/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D491/06

    摘要： Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating various pains such as neuropathic pain and nociceptive pain, headaches such as migraine and cluster headache, central nervous system diseases such as anxiety, depression, epilepsy, cerebral stroke and restless legs syndrome, abdominal symptoms such as abdominal pain and abdominal distension, stool abnormalities such as diarrhea and constipation, digestive system diseases such as irritable bowel syndrome, urinary system diseases such as overactive bladder and interstitial cystitis, etc.

    摘要翻译： 提供可用作N型Ca2 +通道阻断剂的化合物。 通过对具有阻塞N型Ca 2+通道作用的化合物的深入研究，本发明人发现在1位具有取代基的本发明的四氢异喹啉化合物具有阻断N型Ca 2+通道的作用 抗痛知性疼痛作用，抗神经病性疼痛作用，腹痛抑制作用和阿片样物质诱导的便秘改善作用，并且基于这些发现完成了本发明。 本发明的化合物可以用作预防和/或治疗诸如神经性疼痛和伤害性疼痛，头痛如偏头痛和丛集性头痛，中枢神经系统疾病如焦虑，抑郁，癫痫，脑的各种疼痛的药物组合物 中风和不宁腿综合症，腹痛，腹胀等腹部症状，腹泻便秘等粪便异常，肠易激综合征等消化系统疾病，膀胱过多膀胱炎，间质性膀胱炎等泌尿系统疾病等。