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1. 发明授权

US08273883B2 Method for producing optically active 2-arylpiperazine derivative 失效
标题翻译：光学活性2-芳基哌嗪衍生物的制备方法
公开(公告)号：US08273883B2
公开(公告)日：2012-09-25
申请号：US12449460
申请日：2008-02-05
申请人： Masatoshi Ohnuki , Akira Nishiyama , Masaru Mitsuda
发明人： Masatoshi Ohnuki , Akira Nishiyama , Masaru Mitsuda
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07B53/00 , C07D241/04
摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.
摘要翻译：本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。

2. 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。

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