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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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3.发明公开SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-(PYRROLIDIN-3-YLVINYL)PYRIMIDINE 有权5 - （（E）-2-（吡咯烷-3-基）乙基）吡咯烷酮的合成
公开(公告)号：EP2364307A1
公开(公告)日：2011-09-14
申请号：EP09775408.9
申请日：2009-11-30
申请人： Targacept Inc.
发明人： AKIREDDY, Srinivisa Rao , BHATTI, Balwinder, Singh , CUTHBERTSON, Timothy, J. , DULL, Gary, Maurice , MILLER, Craig, Harrison , MITCHENER, JR., Joseph, Pike , MUNOZ, Julio, A. , OTTEN, Pieter, Albert
IPC分类号： C07D403/06 , A61K31/505 , A61P25/00
CPC分类号： C07D403/06
摘要： The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
摘要翻译： 本发明涉及（R）-5 - （（E）-2-吡咯烷-3-基）嘧啶的立体有择合成，新的盐形式，以及这些盐的新颖多晶形式。
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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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