公开(公告)号：US08207199B2

公开(公告)日：2012-06-26

申请号：US13054057

申请日：2009-07-13

申请人： Satoshi Aoki ,  Ryosuke Munakata ,  Noriyuki Kawano ,  Kiyohiro Samizu ,  Hiromasa Oka ,  Takahiro Ishii ,  Takashi Sugane

发明人： Satoshi Aoki ,  Ryosuke Munakata ,  Noriyuki Kawano ,  Kiyohiro Samizu ,  Hiromasa Oka ,  Takahiro Ishii ,  Takashi Sugane

IPC分类号： A61K31/4545 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14

CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.

摘要翻译： 提供了可用作治疗神经性疼痛的药物组合物的活性成分的化合物。 本发明人对具有FAAH抑制活性的化合物进行了广泛的研究，结果发现被N-（吡啶-3-基）氧基羰基 - 哌啶-4-基和苯基取代的唑化合物 或其药学上可接受的盐具有优异的FAAH抑制活性，从而完成了本发明。 确认本发明的化合物在具有神经性疼痛的大鼠模型中具有优异的FAAH抑制活性和抗异常性疼痛作用，因此可用作预防剂和/或治疗神经性疼痛的药剂。

公开(公告)号：US20110118311A1

公开(公告)日：2011-05-19

申请号：US13054057

申请日：2009-07-13

申请人： Satoshi Aoki ,  Ryosuke Munakata ,  Noriyuki Kawano ,  Kiyohiro Samizu ,  Hiromasa Oka ,  Takahiro Ishii ,  Takashi Sugane

发明人： Satoshi Aoki ,  Ryosuke Munakata ,  Noriyuki Kawano ,  Kiyohiro Samizu ,  Hiromasa Oka ,  Takahiro Ishii ,  Takashi Sugane

IPC分类号： A61K31/4545 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14 ,  A61P29/00

CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.

摘要翻译： 提供了可用作治疗神经性疼痛的药物组合物的活性成分的化合物。 本发明人对具有FAAH抑制活性的化合物进行了广泛的研究，结果发现被N-（吡啶-3-基）氧基羰基 - 哌啶-4-基和苯基取代的唑化合物 或其药学上可接受的盐具有优异的FAAH抑制活性，从而完成了本发明。 确认本发明的化合物在具有神经性疼痛的大鼠模型中具有优异的FAAH抑制活性和抗异常性疼痛作用，因此可用作预防剂和/或治疗神经性疼痛的药剂。