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1. 发明申请

US20080200551A1 Flourene Derivative 审中-公开
标题翻译： Flourene衍生物
公开(公告)号：US20080200551A1
公开(公告)日：2008-08-21
申请号：US10568684
申请日：2005-02-17
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Koichiro Harada , Jiro Fujiyasu , Yuji Koga , Makoto Oku , Toshio Okazaki , Shinobu Akuzawa , Toshihiro Watanabe
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Koichiro Harada , Jiro Fujiyasu , Yuji Koga , Makoto Oku , Toshio Okazaki , Shinobu Akuzawa , Toshihiro Watanabe
IPC分类号： A61K31/166 , C07C233/78 , A61P25/06
CPC分类号： C07D311/96 , A61K31/166 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/385 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K31/438 , C07C279/22 , C07D207/20 , C07D209/54 , C07D209/96 , C07D211/70 , C07D221/20 , C07D233/50 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D303/06 , C07D305/14 , C07D307/94 , C07D309/06 , C07D309/20 , C07D317/12 , C07D319/14 , C07D327/04 , C07D335/04 , C07D339/06
摘要： This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof.The compound of the invention has an advantage in that it has high affinity for serotonin receptor subtypes, particularly for 5-HT2B receptor and 5-HT7 receptor, and shows excellent pharmacological effects in comparison with the conventional compounds which have only one of the antagonistic activities of 5-HT2B receptor and 5-HT7 receptor, this is useful as a prophylactic antimigraine agent having high safety and excellent effect.
摘要翻译：本发明涉及具有胍基等官能团通过羰基与芴结构连接的特征结构的新型芴衍生物或其盐。本发明的化合物具有的优点在于其对5-羟色胺受体亚型具有高亲和力，特别是对于5-HT 2B受体和5-HT 7受体，并且显示出优异的与仅具有5-HT 2B受体和5-HT 7受体的拮抗活性的常规化合物相比，药理作用可用作预防性抗偏头痛药剂安全性高，效果好。

2. 发明申请

US20100168096A1 ACYLGUANIDINE DERIVATIVE OR SALT THEREOF 失效
标题翻译：乙酰胺衍生物或其盐
公开(公告)号：US20100168096A1
公开(公告)日：2010-07-01
申请号：US11997956
申请日：2006-08-07
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
IPC分类号： A61K31/5377 , C07C69/76 , C07D209/56 , C07D401/02 , C07D413/02 , C07D221/16 , C07D211/00 , A61K31/24 , A61K31/403 , A61K31/4439 , A61K31/4355 , A61P1/06 , A61P1/12
CPC分类号： C07D209/88 , C07D221/16 , C07D265/38 , C07D333/78 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D471/04 , C07D491/10 , C07D495/10
摘要： [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine.[Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
摘要翻译： [问题]提供可用于预防和/或治疗5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛 [解决方法]发现具有三环结构的酰基胍衍生物或其药学上可接受的盐具有对5-HT 2B受体和5-HT7受体的强拮抗作用。此外，与单次使用对任一受体选择性拮抗剂的情况相比，本发明对两种受体具有拮抗作用的化合物显示出优异的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。

3. 发明授权

US08076348B2 Acylguanidine derivative or salt thereof 失效
标题翻译：酰基胍衍生物或其盐
公开(公告)号：US08076348B2
公开(公告)日：2011-12-13
申请号：US11997956
申请日：2006-08-07
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
IPC分类号： A61K31/435
CPC分类号： C07D209/88 , C07D221/16 , C07D265/38 , C07D333/78 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D471/04 , C07D491/10 , C07D495/10
摘要： [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine.[Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
摘要翻译： [问题]提供可用于预防和/或治疗5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛 [解决方法]发现具有三环结构的酰基胍衍生物或其药学上可接受的盐具有对5-HT 2B受体和5-HT7受体的强拮抗作用。此外，与单次使用对任一受体选择性拮抗剂的情况相比，本发明对两种受体具有拮抗作用的化合物显示出优异的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。

4. 发明申请

US20080171788A1 Medicament For Irritable Bowel Syndrome 审中-公开
标题翻译：肠易激综合征药物
公开(公告)号：US20080171788A1
公开(公告)日：2008-07-17
申请号：US11883651
申请日：2006-02-07
申请人： Shinobu Akuzawa , Hiroyuki Ito , Toshihiro Watanabe , Hiroyoshi Yamada
发明人： Shinobu Akuzawa , Hiroyuki Ito , Toshihiro Watanabe , Hiroyoshi Yamada
IPC分类号： A61K31/166 , C07C233/00 , A61K31/352 , A61K31/215 , C07C69/76 , C07C63/33 , C07C43/21 , A61K31/085 , C07C279/02 , A61K31/16 , A61K31/343 , A61K31/438 , C07D311/96 , C07D221/20 , A61K31/403 , C07D209/54 , A61P1/04
CPC分类号： A61K31/438 , A61K31/085 , A61K31/16 , A61K31/166 , A61K31/215 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/385 , A61K31/403 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K45/06 , C07D209/54 , C07D221/20 , C07D233/88 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D303/06 , C07D305/14 , C07D307/94 , C07D319/14 , C07D327/02 , C07D333/50 , C07D335/04 , A61K2300/00
摘要： The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors.The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.
摘要翻译：本发明涉及一种用于IBS的药物，其包含对5-HT受体具有选择性结合亲和力的5-HT 2B和5-HT 7受体的双重拮抗剂， 2B和5-HT 7受体。本发明的药物组合物作为对IBS的治疗效果优异的药物是有用的，并且在IBS的现有疗法中显示减轻的副作用，因为与独立使用5- 对5-HT 2B受体具有选择性结合亲和力的HT 2B受体拮抗剂或对5-羟色胺受体具有选择性结合亲和力的5-HT 7受体拮抗剂， HT 7受体。

5. 发明授权

US08222274B2 Pyrrole derivative or salt thereof 失效
标题翻译：吡咯衍生物或其盐
公开(公告)号：US08222274B2
公开(公告)日：2012-07-17
申请号：US12278609
申请日：2007-02-19
申请人： Ryushi Seo , Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Shinobu Akuzawa
发明人： Ryushi Seo , Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Shinobu Akuzawa
IPC分类号： C07D401/12 , C07D207/327 , C07D401/04 , C07D403/06 , C07D405/06 , C07D405/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D413/04 , A61K31/40 , A61K31/4025 , A61K31/422 , A61K31/439 , A61K31/454 , A61P1/00
CPC分类号： C07D207/34 , C07D401/04 , C07D401/10 , C07D403/04 , C07D407/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D453/02
摘要： [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).[Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
摘要翻译： [问题]提供可用于预防和/或治疗其中涉及5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）。 [解决方法]发现特征在于3-位的胍基羰基或酰氨基作为取代基的吡咯衍生物或其药学上可接受的盐对5- HT2B受体和5-HT7受体。此外，与对于任一种受体选择性拮抗剂单独使用的情况相比，具有对两种受体具有拮抗作用的本发明化合物显示出良好的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）。

6. 发明申请

US20090036421A1 Pyrrole Derivative or Salt Thereof 失效
标题翻译：吡咯衍生物或其盐
公开(公告)号：US20090036421A1
公开(公告)日：2009-02-05
申请号：US12278609
申请日：2007-02-19
申请人： Ryushi Seo , Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Shinobu Akuzawa
发明人： Ryushi Seo , Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Shinobu Akuzawa
IPC分类号： A61K31/4025 , A61P1/00 , C07D207/34 , C07D401/12 , A61K31/4439 , A61K31/4035 , A61K31/439 , A61K31/454 , C07D403/12 , C07D409/06
CPC分类号： C07D207/34 , C07D401/04 , C07D401/10 , C07D403/04 , C07D407/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D453/02
摘要： [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).[Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
摘要翻译： [问题]提供可用于预防和/或治疗其中涉及5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）。 [解决方法]发现特征在于3-位的胍基羰基或酰氨基作为取代基的吡咯衍生物或其药学上可接受的盐对5- HT2B受体和5-HT7受体。此外，与对于任一种受体选择性拮抗剂单独使用的情况相比，具有对两种受体具有拮抗作用的本发明化合物显示出良好的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）。

7. 发明申请

US20090062363A1 AMIDE DERIVATIVE OR SALT THEREOF 失效
标题翻译：酰胺衍生物或其盐
公开(公告)号：US20090062363A1
公开(公告)日：2009-03-05
申请号：US12279221
申请日：2007-02-07
申请人： Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Ryushi Seo , Shinobu Akuzawa
发明人： Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Ryushi Seo , Shinobu Akuzawa
IPC分类号： A61K31/4184 , C07D209/42 , C07D235/24 , A61K31/404
CPC分类号： C07D209/08 , C07D209/12 , C07D209/14 , C07D209/20 , C07D215/48 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/26 , C07D265/36 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08
摘要： [Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).[Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
摘要翻译： [问题]提供可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）。 [解决方法]发现特征在于含氮双环杂环（例如吲哚等）或其药学上可接受的盐的酰胺衍生物对5种 -HT2B受体和5-HT7受体。此外，与对于任一种受体选择性拮抗剂单独使用的情况相比，具有对两种受体具有拮抗作用的本发明化合物显示出良好的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）。

8. 发明授权

US07985764B2 Amide derivative or salt thereof 失效
标题翻译：酰胺衍生物或其盐
公开(公告)号：US07985764B2
公开(公告)日：2011-07-26
申请号：US12279221
申请日：2007-02-07
申请人： Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Ryushi Seo , Shinobu Akuzawa
发明人： Hidetaka Kaku , Hiroyoshi Yamada , Daisuke Kaga , Ryushi Seo , Shinobu Akuzawa
IPC分类号： C07D209/08 , A61K31/404
CPC分类号： C07D209/08 , C07D209/12 , C07D209/14 , C07D209/20 , C07D215/48 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/26 , C07D265/36 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08
摘要： It was found that a compound according to the following formula: or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compound shows good pharmacological action as compared to antagonists selective for only one of these receptors. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
摘要翻译：发现根据下式的化合物或其药学上可接受的盐对5-HT2B和5-HT7受体具有强拮抗作用。此外，与仅对这些受体中的一种选择性的拮抗剂相比，该化合物显示出良好的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）。

9. 发明申请

US20080161419A1 Prophylactic Antimigraine Agents 审中-公开
标题翻译：预防性抗偏头痛药
公开(公告)号：US20080161419A1
公开(公告)日：2008-07-03
申请号：US10589892
申请日：2005-02-17
申请人： Shinobu Akuzawa , Toshihiro Watanabe
发明人： Shinobu Akuzawa , Toshihiro Watanabe
IPC分类号： A61K45/00 , A61P25/06
CPC分类号： A61K31/166 , A61K31/454 , A61K31/505 , C07D339/06
摘要： The present invention relates to prophylactic antimigraine agents comprising as an active ingredient a dual antagonist for the 5-HT2B and 5-HT7 receptors, the antagonist having a binding affinity selective for the 5-HT2B and 5-HT7 receptors.Since these prophylactic antimigraine agents show an excellent pharmacological effect in comparison with the cases in which a 5-HT2B receptor antagonist having a selective binding affinity to the 5-HT2B receptor or a 5-HT7 receptor antagonist having a selective binding affinity to the 5-HT7 receptor is used alone, they are useful as drugs which are excellent in prophylaxis of migraine and in which the side effects found in the existing prophylactic antimigraine agents are reduced.
摘要翻译：本发明涉及含有5-HT 2B和5-HT 7受体的双重拮抗剂作为活性成分的预防性抗偏头痛药，所述拮抗剂具有结合亲和选择性对于5-HT 2B和5-HT 7受体。由于与对5-HT 2B受体具有选择性结合亲和力的5-HT 2B受体拮抗剂相比，这些预防性抗偏头痛药物显示出优异的药理作用或对5-HT 7受体具有选择性结合亲和力的5-HT 7受体拮抗剂单独使用，它们可用作预防偏头痛的药物并且其中在现有的预防性抗偏头痛药中发现的副作用减少。

10. 发明申请

US20110158930A1 METHOD FOR TREATMENT OF IRRITABLE BOWEL SYNDROME 审中-公开
标题翻译：用于治疗可重要的牙龈综合征的方法
公开(公告)号：US20110158930A1
公开(公告)日：2011-06-30
申请号：US13061384
申请日：2009-08-27
申请人： Takuya Hirata , Toshiyuki Funatsu , Yoshihiro Keto , Shinobu Akuzawa
发明人： Takuya Hirata , Toshiyuki Funatsu , Yoshihiro Keto , Shinobu Akuzawa
IPC分类号： A61K31/78 , C07D403/06 , A61P1/00 , A61P1/12
CPC分类号： A61K31/4184 , A61K31/78
摘要： A method for treatment of a patient suffering from irritable bowel syndrome with diarrhea or mixed irritable bowel syndrome, which comprises administering to the patient a therapeutically effective amount of ramosetron or a pharmaceutically acceptable salt thereof in combination with a therapeutically effective amount of polycarbophil or a pharmaceutically acceptable salt thereof.
摘要翻译：一种用于治疗患有腹泻或混合性肠易激综合征的肠易激综合征的患者的方法，其包括向患者施用治疗有效量的雷莫司琼或其药学上可接受的盐与治疗有效量的聚卡波非或药学上其可接受的盐。

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