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1.发明公开(R) -3- (E) -2- (PYRR0LIDIN-3-YL) VINYL) -5- (TETRAHYDR0PYRAN-4-YL0XY) PYRIDINE, ITS SALTS, ITS SYNTHESIS AND ITS USE AS LIGAND FOR NICOTINIC ACETYLCHOLINERGIC RECEPTORS 审中-公开（R）-2-（E）-2-（吡咯烷-3-基）乙烯基）-5-（四氢吡喃-4-基氧基）吡啶，其盐，其合成，以及其作为烟碱乙酰胆碱受体的配体的使用
公开(公告)号：EP2358705A1
公开(公告)日：2011-08-24
申请号：EP09775410.5
申请日：2009-11-30
申请人： Targacept Inc.
发明人： AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , CUTHBERTSON, Timothy, J. , DULL, Gary, Maurice , GATTO, Gregory, J. , GENUS, John , HAMMOND, Philip, S. , MITCHENER, Joseph, Pike, Jr. , MUNOZ, Julio, A. , OTTEN, Pieter, Albert , YOHANNES, Daniel , FEDOROV, Nikolai
IPC分类号： C07D405/14 , A61P25/00 , A61K31/4439
CPC分类号： A61K31/4439 , C07D405/14
摘要： The present invention relates to (R) -3- ( (E) -2- (pyrrolidin-3-yl) vinyl) -5- (tetrahydropyran-4-yloxy) pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions. The present invention relates also the use of this compound in the manufacture of a medicament for the treatment of CNS related disorders.
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2.发明公开DERIVATIVES OF OXABISPIDINE AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开OXABISPIDIN作为配体为神经元烟碱型乙酰胆碱受体衍生物
公开(公告)号：EP2356125A1
公开(公告)日：2011-08-17
申请号：EP09774421.3
申请日：2009-07-01
申请人： Targacept, Inc.
发明人： MAZUROV, Anatoly , MIAO, Lan , XIAO, Yun-de , YOHANNES, Daniel , AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , KOMBO, David , MURTHY, V. Srinivasa , FEDOROV, Nikolai , SHOWALTER, Todd
IPC分类号： C07D498/04 , A61K31/5386 , A61P25/00
CPC分类号： C07D498/04
摘要： The present invention relates to compounds of formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with d sfunction of the central nervous s stem (CNS).
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3.发明授权A process for the preparation of tert-butyl (R)-3-vinylpyrrolidine-1-carboxylate and intermediates therefor 有权一种制备叔丁基（R）-3-乙烯基吡咯烷-1-甲酸叔丁酯和为此有用的中间体过程
公开(公告)号：EP2358670B1
公开(公告)日：2012-10-24
申请号：EP09775409.7
申请日：2009-11-30
申请人： Targacept Inc.
发明人： AKIREDDY, Srinivisa, Rao , BHATTI, Balwinder Singh , CUTHBERTSON, Timothy, J. , MILLER, Craig, Harrison , MITCHENER, JR., Joseph, Pike
IPC分类号： C07D207/06 , C07D207/08
CPC分类号： A61K31/4439 , C07D405/14
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公开(公告)号：EP2358670A2
公开(公告)日：2011-08-24
申请号：EP09775409.7
申请日：2009-11-30
申请人： Targacept Inc.
发明人： AKIREDDY, Srinivisa, Rao , BHATTI, Balwinder Singh , CUTHBERTSON, Timothy, J. , MILLER, Craig, Harrison , MITCHENER, JR., Joseph, Pike
IPC分类号： C07D207/06 , C07D207/08
CPC分类号： A61K31/4439 , C07D405/14
摘要： The present invention relates to a method of making tert-butyl (R)-3-vinylpyrrolidine-1-carboxylate through the intermediacy of one or more of diethyl (R)-2-(1-(tert- butoxycarbonyl)pyrrolidin-3-yl)malonate, (R)-2-(1-(tert-butoxycarbonyl)pyrrolidin-3-yl)malonic acid, tert-butyl (R)-3-(2-hydroxyethyl)pyrrolidine-1 -carboxylate, and test-butyl (R)-3-(2- iodoethyl)pyrrolidine- 1 -carboxylate.
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