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1. 发明申请

US20060281725A1 Agents and crystals for improving excretory potency of urinary bladder 审中-公开
标题翻译：用于改善膀胱排泄功效的药剂和晶体
公开(公告)号：US20060281725A1
公开(公告)日：2006-12-14
申请号：US11475881
申请日：2006-06-28
申请人： Yuji Isihara , Takayuki Doi , Hiroshi Nagabukuro , Yuji Ishichi
发明人： Yuji Isihara , Takayuki Doi , Hiroshi Nagabukuro , Yuji Ishichi
IPC分类号： A61K31/553 , A61K31/55 , A61K31/4745 , A61K31/454 , A61K31/453 , A61K31/452 , A61K31/473
CPC分类号： A61K31/00 , A61K31/343 , A61K31/382 , A61K31/395 , A61K31/404 , A61K31/435 , A61K31/445 , A61K31/452 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/473 , A61K31/4745 , A61K31/55 , A61K31/553 , A61K45/06 , C07D211/26 , C07D211/32 , C07D273/06 , C07D401/06 , C07D471/06 , C07D487/04 , A61K2300/00
摘要： Agents for improving potentcy of the urinary bladder which comprise an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholinesterase and an action to improve the excretory potency of the urinary bladder. As an example, crystals of of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.
摘要翻译：用于改善膀胱的潜力的药剂，其包含具有乙酰胆碱酯酶抑制作用的非氨基甲酸酯型胺化合物。特别地，提供三环，缩合，杂环衍生物的结晶，其具有抑制乙酰胆碱酯酶的优异作用和提高膀胱排泄能力的作用。例如，8- [3- [1 - [（3-氟苯基） - 甲基] -4-哌啶基] -1-氧代丙基] -1,2,5,6-四氢-4H-吡咯并[3 ，2,1-ij]喹啉-4-酮或其盐和含有它们的药物组合物。

2. 发明申请

US20050197362A1 Preventives/remedies for urinary disturbance 失效
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20050197362A1
公开(公告)日：2005-09-08
申请号：US10935646
申请日：2004-09-08
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61P13/00 , A61P13/08 , A61P43/00 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/22 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要翻译：含有具有乙酰胆碱酯酶抑制作用的化合物和α1拮抗作用的化合物的预防/补救措施，其显示出改善膀胱尿功能的优异效果（即，改善尿流率和排尿效率的效果）而不影响尿压或血压。

3. 发明授权

US08252814B2 Agents and crystals for improving excretory potency of urinary bladder 失效
标题翻译：用于改善膀胱排泄功效的药剂和晶体
公开(公告)号：US08252814B2
公开(公告)日：2012-08-28
申请号：US12219198
申请日：2008-07-17
申请人： Yuji Ishihara , Takayuki Doi , Hiroshi Nagabukuro , Yuji Ishichi
发明人： Yuji Ishihara , Takayuki Doi , Hiroshi Nagabukuro , Yuji Ishichi
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： A61K31/00 , A61K31/343 , A61K31/382 , A61K31/395 , A61K31/404 , A61K31/435 , A61K31/445 , A61K31/452 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/473 , A61K31/4745 , A61K31/55 , A61K31/553 , A61K45/06 , C07D211/26 , C07D211/32 , C07D273/06 , C07D401/06 , C07D471/06 , C07D487/04 , A61K2300/00
摘要： Agents for improving potency of the urinary bladder which comprise an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholinesterase and an action to improve the excretory potency of the urinary bladder. As an example, crystals of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.
摘要翻译：用于提高膀胱效能的药剂，其包含具有乙酰胆碱酯酶抑制作用的非氨基甲酸酯型胺化合物。特别地，提供三环，缩合，杂环衍生物的结晶，其具有抑制乙酰胆碱酯酶的优异作用和提高膀胱排泄能力的作用。例如，8- [3- [1 - [（3-氟苯基） - 甲基] -4-哌啶基] -1-氧代丙基] -1,2,5,6-四氢-4H-吡咯并[ 2,1-ij]喹啉-4-酮或其盐和含有它们的药物组合物。

4. 发明申请

US20090264467A1 Agents and crystals for improving excretory potency of urinary bladder 失效
标题翻译：用于改善膀胱排泄功效的药剂和晶体
公开(公告)号：US20090264467A1
公开(公告)日：2009-10-22
申请号：US12219198
申请日：2008-07-17
申请人： Yuji Ishihara , Takayuki Doi , Hiroshi Nagabukuro , Yuji Ishichi
发明人： Yuji Ishihara , Takayuki Doi , Hiroshi Nagabukuro , Yuji Ishichi
IPC分类号： A61K31/445
CPC分类号： A61K31/00 , A61K31/343 , A61K31/382 , A61K31/395 , A61K31/404 , A61K31/435 , A61K31/445 , A61K31/452 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/473 , A61K31/4745 , A61K31/55 , A61K31/553 , A61K45/06 , C07D211/26 , C07D211/32 , C07D273/06 , C07D401/06 , C07D471/06 , C07D487/04 , A61K2300/00
摘要： Agents for improving potency of the urinary bladder which comprise an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholinesterase and an action to improve the excretory potency of the urinary bladder. As an example, crystals of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.
摘要翻译：用于提高膀胱效能的药剂，其包含具有乙酰胆碱酯酶抑制作用的非氨基甲酸酯型胺化合物。特别地，提供三环，缩合，杂环衍生物的结晶，其具有抑制乙酰胆碱酯酶的优异作用和提高膀胱排泄能力的作用。例如，8- [3- [1 - [（3-氟苯基） - 甲基] -4-哌啶基] -1-氧代丙基] -1,2,5,6-四氢-4H-吡咯并[ 2,1-ij]喹啉-4-酮或其盐和含有它们的药物组合物。

5. 发明授权

US07138533B2 Preventives/remedies for urinary disturbance 失效
公开(公告)号：US07138533B2
公开(公告)日：2006-11-21
申请号：US10935646
申请日：2004-09-08
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： C07D307/78 , C07D307/87 , C07D307/93
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

6. 发明申请

US20060211675A1 Preventives/remedies for urinary disturbance 失效
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20060211675A1
公开(公告)日：2006-09-21
申请号：US11333375
申请日：2006-01-18
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： A61K31/55 , A61K31/549 , A61K31/553
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an al antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要翻译：包含具有乙酰胆碱酯酶抑制作用的化合物和具有改善膀胱尿功能的优异效果（即，改善尿流率和排尿效率）的优异效果的排尿障碍的预防/补救措施，而不影响尿压或血压。

7. 发明授权

US07462628B2 Preventives/remedies for urinary disturbance 失效
标题翻译：预防/治疗尿路障碍
公开(公告)号：US07462628B2
公开(公告)日：2008-12-09
申请号：US11333375
申请日：2006-01-18
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： A61K31/44 , C07D451/00 , C07D453/00 , C07D455/00
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要翻译：含有具有乙酰胆碱酯酶抑制作用的化合物和α1拮抗作用的化合物的预防/补救措施，其显示出改善膀胱尿功能的优异效果（即，改善尿流率和排尿效率的效果）而不影响尿压或血压。

8. 发明授权

US07132547B2 Preventives/remedies for urinary disturbance 有权
公开(公告)号：US07132547B2
公开(公告)日：2006-11-07
申请号：US10500217
申请日：2002-12-26
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： C07D235/24
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

9. 发明申请

US20060063769A1 Preventives/remedies for urinary disturbance 有权
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20060063769A1
公开(公告)日：2006-03-23
申请号：US10500217
申请日：2002-12-26
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： A61K31/517 , A61K31/454
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要翻译：含有具有乙酰胆碱酯酶抑制作用的化合物和α1拮抗作用的化合物的预防/补救措施，其显示出改善膀胱尿功能的优异效果（即，改善尿流率和排尿效率的效果）而不影响尿压或血压。

10. 发明申请

US20070021391A1 Preventive/remedy for urinary disturbance 审中-公开
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20070021391A1
公开(公告)日：2007-01-25
申请号：US10560754
申请日：2004-06-29
申请人： Takayuki Doi , Hiroshi Nagabukuro
发明人： Takayuki Doi , Hiroshi Nagabukuro
IPC分类号： A61K31/445 , A61K31/66
CPC分类号： A61K45/06 , G01N2333/916 , G01N2500/04
摘要： It is intended to provide a preventive/remedy for urinary disturbance containing a compound, which shows an acetylcholine esterase inhibitory activity but substantially has no butyrylcholine esterase inhibitory activity, showing no side effect and being safe and efficacious without inhibiting the urine collection function; a preventive/remedy for dry mouth induced by the administration of a remedy for urinary disturbance and a preventive or remedy for hyperactive bladder not accompanied by dry mouth; and a method of screening a substance preventing/treating urinary disturbance without inhibiting the urine collection function characterized by comprising measuring and comparing the acetylcholine esterase inhibitory activity and the butyrylcholine esterase inhibitory activity of a test compound.
摘要翻译：旨在提供含有化合物的尿失调的预防/治疗方法，其显示乙酰胆碱酯酶抑制活性，但基本上不具有丁酰胆碱酯酶抑制活性，在不抑制尿液收集功能的情况下不显示副作用并且安全有效; 用于治疗尿失禁引起的口干预防/补救措施以及未伴有口干的活动性膀胱的预防或补救措施; 以及在不抑制尿液收集功能的情况下筛选预防/治疗尿失调的物质的方法，其特征在于包括测定和比较测试化合物的乙酰胆碱酯酶抑制活性和丁酰胆碱酯酶抑制活性。

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