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公开(公告)号:US08106190B2
公开(公告)日:2012-01-31
申请号:US12094298
申请日:2006-11-29
申请人: Takahiro Kuramochi , Ryoji Hirabayashi , Yohei Koganemaru , Ryosuke Munakata , Koichi Yonezawa , Tetsuo Kiso
发明人: Takahiro Kuramochi , Ryoji Hirabayashi , Yohei Koganemaru , Ryosuke Munakata , Koichi Yonezawa , Tetsuo Kiso
IPC分类号: C07D265/30 , C07D265/36 , C07D405/04 , C07D413/00
CPC分类号: C07D295/135 , A61K31/167 , C07C37/18 , C07C237/40 , C07C2601/14 , C07C2602/10 , C07D207/09 , C07D207/14 , C07D209/34 , C07D209/48 , C07D209/96 , C07D211/58 , C07D213/38 , C07D213/74 , C07D213/80 , C07D215/227 , C07D215/38 , C07D217/02 , C07D265/36 , C07D277/64 , C07D279/16 , C07D295/13 , C07D295/185 , C07D307/14 , C07D307/22 , C07D309/14 , C07D319/12 , C07D319/18 , C07D321/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D453/02 , C07C39/27
摘要: To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation.The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.
摘要翻译: 基于对辣椒素受体VR1活化的抑制作用,提供用于治疗或预防伤害性疼痛,神经性疼痛,癌症疼痛,头痛,膀胱功能障碍等的新颖优异的药剂。 本发明是通过确认苯甲酰胺衍生物,其特征在于具有苯环,其中单环在酰氨基的氮原子上缩合,并且具有低级烷基氨基或被环基取代的氨基 所述酰胺基的相邻位置对VR1的活化具有强烈的抑制作用,并且基于此起到优异的药理作用,并且发现其可以成为治疗或预防VR1涉及的疾病如伤害性疼痛,神经性疼痛,癌症疼痛, 头痛,膀胱功能障碍等。
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公开(公告)号:US07585878B2
公开(公告)日:2009-09-08
申请号:US10560282
申请日:2004-06-10
申请人: Takahiro Kuramochi , Norio Asai , Kazuhiro Ikegai , Seijiro Akamatsu , Hironori Harada , Noriko Ishikawa , Shohei Shirakami , Satoshi Miyamoto , Toshihiro Watanabe , Tetsuo Kiso
发明人: Takahiro Kuramochi , Norio Asai , Kazuhiro Ikegai , Seijiro Akamatsu , Hironori Harada , Noriko Ishikawa , Shohei Shirakami , Satoshi Miyamoto , Toshihiro Watanabe , Tetsuo Kiso
IPC分类号: C07D413/02 , C07D403/02 , A61K31/538 , A61K31/404
CPC分类号: C07C237/40 , A61K31/167 , A61K31/428 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D209/08 , C07D209/34 , C07D213/75 , C07D215/38 , C07D217/04 , C07D223/16 , C07D231/56 , C07D235/06 , C07D241/42 , C07D249/18 , C07D263/58 , C07D265/36 , C07D277/64 , C07D277/82 , C07D279/16 , C07D295/155 , C07D307/79 , C07D317/66 , C07D333/54 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要: There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like.A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).
摘要翻译: 提供了具有辣椒素受体VR1抑制活性的化合物,并且可用作各种疼痛的治疗剂,包括炎性疼痛和神经源性疼痛,偏头痛,丛集性头痛,包括膀胱活动过度的膀胱疾病等。 一种苯甲酰胺衍生物或其盐,其中苯环通过酰胺键连接到D环(单环或双环烃环或单环或双环杂芳族环),苯环直接键合到E环(单环 或双环烃环或单环或双环杂芳族环),并且苯环通过L(低级亚烷基)进一步与A(氨基部分,单环或双环杂环)键合。
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公开(公告)号:US06664283B1
公开(公告)日:2003-12-16
申请号:US10031404
申请日:2002-05-15
IPC分类号: A61K31415
CPC分类号: A61K31/429 , A61K31/00
摘要: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.
摘要翻译: 本发明涉及用于神经性疼痛的药物,其包含用于全身给药的mGluR1受体拮抗剂。 可以通过本发明提供治疗各种神经性疼痛的药物。
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公开(公告)号:US20130165491A1
公开(公告)日:2013-06-27
申请号:US13820873
申请日:2010-09-06
申请人: Tetsuo Kiso , Mina Tsukamoto
发明人: Tetsuo Kiso , Mina Tsukamoto
IPC分类号: C07D249/08 , C07D403/04
CPC分类号: C07D249/08 , A61K31/4196 , C07D403/04 , C07D413/12
摘要: [Problem]Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain.[Means for Solution]The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11β-hydroxydehydrogenase type 1 (11β-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11β-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).
摘要翻译: [问题]提供了一种药物,特别是可用于治疗疼痛的药物组合物。 [解决方案]本发明人为了提供疼痛治疗剂而对具有疼痛的模型动物进行了广泛的研究。 结果发现,1α-(11β-HSD1)抑制剂,特别是在三唑环3位(或5位)具有环状基团的三唑化合物具有良好的效果, 改善慢性疼痛。 也就是说,根据本发明,包含11beta-HSD1抑制剂,特别是本发明的三唑化合物作为活性成分的药物组合物可用于治疗疼痛(特别是神经性疼痛或纤维肌痛) 。
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公开(公告)号:US07855198B2
公开(公告)日:2010-12-21
申请号:US12496993
申请日:2009-07-02
申请人: Takahiro Kuramochi , Norio Asai , Kazuhiro Ikegai , Seijiro Akamatsu , Hironori Harada , Noriko Ishikawa , Shohei Shirakami , Satoshi Miyamoto , Toshihiro Watanabe , Tetsuo Kiso
发明人: Takahiro Kuramochi , Norio Asai , Kazuhiro Ikegai , Seijiro Akamatsu , Hironori Harada , Noriko Ishikawa , Shohei Shirakami , Satoshi Miyamoto , Toshihiro Watanabe , Tetsuo Kiso
IPC分类号: C07D413/10 , C07D413/14 , A61K31/538
CPC分类号: C07C237/40 , A61K31/167 , A61K31/428 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D209/08 , C07D209/34 , C07D213/75 , C07D215/38 , C07D217/04 , C07D223/16 , C07D231/56 , C07D235/06 , C07D241/42 , C07D249/18 , C07D263/58 , C07D265/36 , C07D277/64 , C07D277/82 , C07D279/16 , C07D295/155 , C07D307/79 , C07D317/66 , C07D333/54 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要: There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like.A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).
摘要翻译: 提供了具有辣椒素受体VR1抑制活性的化合物,并且可用作各种疼痛的治疗剂,包括炎性疼痛和神经源性疼痛,偏头痛,丛集性头痛,包括膀胱活动过度的膀胱疾病等。 一种苯甲酰胺衍生物或其盐,其中苯环通过酰胺键连接到D环(单环或双环烃环或单环或双环杂芳族环),苯环直接键合到E环(单环 或双环烃环或单环或双环杂芳族环),并且苯环通过L(低级亚烷基)进一步与A(氨基部分,单环或双环杂环)键合。
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公开(公告)号:US20090270365A1
公开(公告)日:2009-10-29
申请号:US12496993
申请日:2009-07-02
申请人: Takahiro KURAMOCHI , Norio ASAI , Kazuhiro IKEGAI , Seijiro AKAMATSU , Hironori HARADA , Noriko ISHIKAWA , Shohei SHIRAKAMI , Satoshi MIYAMOTO , Toshihiro WATANABE , Tetsuo KISO
发明人: Takahiro KURAMOCHI , Norio ASAI , Kazuhiro IKEGAI , Seijiro AKAMATSU , Hironori HARADA , Noriko ISHIKAWA , Shohei SHIRAKAMI , Satoshi MIYAMOTO , Toshihiro WATANABE , Tetsuo KISO
IPC分类号: A61K31/55 , C07D413/02 , C07D223/04 , C07D401/04 , A61K31/5377 , A61K31/497 , A61P29/00
CPC分类号: C07C237/40 , A61K31/167 , A61K31/428 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D209/08 , C07D209/34 , C07D213/75 , C07D215/38 , C07D217/04 , C07D223/16 , C07D231/56 , C07D235/06 , C07D241/42 , C07D249/18 , C07D263/58 , C07D265/36 , C07D277/64 , C07D277/82 , C07D279/16 , C07D295/155 , C07D307/79 , C07D317/66 , C07D333/54 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要: There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like.A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).
摘要翻译: 提供了具有辣椒素受体VR1抑制活性的化合物,并且可用作各种疼痛的治疗剂,包括炎性疼痛和神经源性疼痛,偏头痛,丛集性头痛,包括膀胱活动过度的膀胱疾病等。 一种苯甲酰胺衍生物或其盐,其中苯环通过酰胺键连接到D环(单环或双环烃环或单环或双环杂芳族环),苯环直接键合到E环(单环 或双环烃环或单环或双环杂芳族环),并且苯环通过L(低级亚烷基)进一步与A(氨基部分,单环或双环杂环)键合。
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公开(公告)号:US09765040B2
公开(公告)日:2017-09-19
申请号:US13820873
申请日:2011-09-06
申请人: Tetsuo Kiso , Mina Tsukamoto
发明人: Tetsuo Kiso , Mina Tsukamoto
IPC分类号: C07D249/08 , C07D403/04 , A61K31/4196 , C07D413/12
CPC分类号: C07D249/08 , A61K31/4196 , C07D403/04 , C07D413/12
摘要: [Problem]Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain.[Means for Solution]The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11β-hydroxydehydrogenase type 1 (11β-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11β-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).
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公开(公告)号:US20090233900A1
公开(公告)日:2009-09-17
申请号:US12094298
申请日:2006-11-29
申请人: Takahiro Kuramochi , Ryoji Hirabayashi , Yohei Koganemaru , Ryosuke Munakata , Koichi Yonezawa , Tetsuo Kiso
发明人: Takahiro Kuramochi , Ryoji Hirabayashi , Yohei Koganemaru , Ryosuke Munakata , Koichi Yonezawa , Tetsuo Kiso
IPC分类号: A61K31/536 , C07D265/30 , A61K31/535 , C07D405/04 , A61K31/497 , C07D413/00 , A61K31/5377 , C07D265/36 , A61K31/397
CPC分类号: C07D295/135 , A61K31/167 , C07C37/18 , C07C237/40 , C07C2601/14 , C07C2602/10 , C07D207/09 , C07D207/14 , C07D209/34 , C07D209/48 , C07D209/96 , C07D211/58 , C07D213/38 , C07D213/74 , C07D213/80 , C07D215/227 , C07D215/38 , C07D217/02 , C07D265/36 , C07D277/64 , C07D279/16 , C07D295/13 , C07D295/185 , C07D307/14 , C07D307/22 , C07D309/14 , C07D319/12 , C07D319/18 , C07D321/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D453/02 , C07C39/27
摘要: To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation.The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.
摘要翻译: 基于对辣椒素受体VR1活化的抑制作用,提供用于治疗或预防伤害性疼痛,神经性疼痛,癌症疼痛,头痛,膀胱功能障碍等的新颖优异的药剂。 本发明是通过确认苯甲酰胺衍生物,其特征在于具有苯环,其中单环在酰氨基的氮原子上缩合,并且具有低级烷基氨基或被环基取代的氨基 所述酰胺基的相邻位置对VR1的活化具有强烈的抑制作用,并且基于此起到优异的药理作用,并且发现其可以成为治疗或预防VR1涉及的疾病如伤害性疼痛,神经性疼痛,癌症疼痛, 头痛,膀胱功能障碍等。
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公开(公告)号:US20070167444A1
公开(公告)日:2007-07-19
申请号:US10560282
申请日:2004-06-10
申请人: Takahiro Kuramochi , Norio Asai , Kazuhiro Ikegai , Seijiro Akamatsu , Hironori Harada , Noriko Ishikawa , Shohei Shirakami , Satoshi Miyamoto , Toshihiro Watanabe , Tetsuo Kiso
发明人: Takahiro Kuramochi , Norio Asai , Kazuhiro Ikegai , Seijiro Akamatsu , Hironori Harada , Noriko Ishikawa , Shohei Shirakami , Satoshi Miyamoto , Toshihiro Watanabe , Tetsuo Kiso
IPC分类号: A61K31/538 , A61K31/404 , C07D413/02 , C07D403/02
CPC分类号: C07C237/40 , A61K31/167 , A61K31/428 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D209/08 , C07D209/34 , C07D213/75 , C07D215/38 , C07D217/04 , C07D223/16 , C07D231/56 , C07D235/06 , C07D241/42 , C07D249/18 , C07D263/58 , C07D265/36 , C07D277/64 , C07D277/82 , C07D279/16 , C07D295/155 , C07D307/79 , C07D317/66 , C07D333/54 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要: There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).
摘要翻译: 提供了具有辣椒素受体VR1抑制活性的化合物,并且可用作各种疼痛的治疗剂,包括炎性疼痛和神经源性疼痛,偏头痛,丛集性头痛,包括膀胱活动过度的膀胱疾病等。 一种苯甲酰胺衍生物或其盐,其中苯环通过酰胺键连接到D环(单环或双环烃环或单环或双环杂芳族环),苯环直接键合到E环(单环 或双环烃环或单环或双环杂芳族环),并且苯环通过L(低级亚烷基)进一步与A(氨基部分,单环或双环杂环)键合。
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