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。

公开(公告)号：EP2242364A1

公开(公告)日：2010-10-27

申请号：EP09701707.3

申请日：2009-01-15

申请人： Targacept Inc.

发明人： BEAVER, Jessica ,  BREINING, Scott ,  DULL, Gary, Maurice ,  GATTO, Gergory, J. ,  GENUS, John ,  MATHEW, Jacob ,  MUNOZ, Julio, A. ,  PFEIFFER, Inigo ,  TOLER, Steve ,  WAMSLEY, James ,  XIE, Jianxun

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D491/10

CPC分类号： C07D487/10

摘要： A novel scalable synthesis for the preparation of 7-(3- pyridinyI)- 1,7- diazaspiro[4.4)nonane has been developed, and7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane salts have been formed with succinic acid and oxalic acid. Additionally, 7-(3-pyridinyl)-1,7- diazaspiro[4.4]nonane has been separated into its stereoisomers via resolution with L and D di-p-toluoyltartaric acids, giving (R)- and (S)-7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane of high enantiomeric purity. Numerous solid salts of the resulting (R)- and (S)-7-(3-pyridinyl)-1,7- diazaspiro[4.4}nonane have been prepared. Methods for the preparation of the racemic and enantiomeric salts, pharmaceutical compositions comprising such salts, and uses thereof are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.

公开(公告)号：EP2021325A2

公开(公告)日：2009-02-11

申请号：EP07761996.3

申请日：2007-05-08

申请人： AstraZeneca AB ,  Targacept Inc.

发明人： BOHLIN, Martin, Hans ,  DULL, Gary, M. ,  ERIKSSON, Caroline ,  MILLER, Craig, H. ,  MUNOZ, Julio, A. ,  SEBHATU, Tesfai

IPC分类号： C07D213/38

CPC分类号： C07D213/65

摘要： Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.

公开(公告)号：EP2389378A1

公开(公告)日：2011-11-30

申请号：EP10701307.0

申请日：2010-01-25

申请人： Targacept, Inc.

发明人： BENCHERIF, Merouane ,  FEDOROV, Nikolai ,  HAUSER, Terry ,  JORDAN, Kristen ,  LETCHWORTH, Sharon, Rae ,  MAZUROV, Anatoly ,  MUNOZ, Julio, A. ,  SPEAKE, Jason ,  YOHANNES, Daniel

IPC分类号： C07D453/02 ,  A61K31/439 ,  A61P3/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/28 ,  A61P29/00

CPC分类号： A61K31/444 ,  C07D453/02

摘要： The present invention relates to compounds 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 dysfunction of the central nervous system (CNS).

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.

公开(公告)号：EP1814852A2

公开(公告)日：2007-08-08

申请号：EP05819967.0

申请日：2005-11-09

申请人： Targacept, Inc.

发明人： MUNOZ, Julio, A. ,  GENUS, John ,  MOORE, James, R.

IPC分类号： C07D213/46 ,  A61K31/4406

CPC分类号： C07D213/38 ,  C07D213/65 ,  C07D213/73 ,  C07D213/75 ,  C07D401/12

摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.

摘要翻译： 通过给需要其的患者施用E-metanicotine型化合物的羟基苯甲酸盐组合物来治疗易患或患有病症和病症（例如中枢神经系统病症）的患者。 E-甲草烟碱化合物的羟基苯甲酸盐的形成也可用于纯化E-甲草烟碱化合物，因为羟基苯甲酸盐倾向于结晶出来，留下杂质例如Z-花青霉素化合物和其中双键迁移的化合物， 解。 如果需要，可以将羟基苯甲酸盐转化为游离碱（E-烟碱酸）或另一种药学上可接受的盐形式。

公开(公告)号：EP2389378B1

公开(公告)日：2014-06-25

申请号：EP10701307.0

申请日：2010-01-25

申请人： Targacept, Inc.

发明人： BENCHERIF, Merouane ,  FEDOROV, Nikolai ,  HAUSER, Terry ,  JORDAN, Kristen ,  LETCHWORTH, Sharon, Rae ,  MAZUROV, Anatoly ,  MUNOZ, Julio, A. ,  SPEAKE, Jason ,  YOHANNES, Daniel

IPC分类号： C07D453/02 ,  A61K31/439 ,  A61P3/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/28 ,  A61P29/00

CPC分类号： A61K31/444 ,  C07D453/02

公开(公告)号：EP2021326A1

公开(公告)日：2009-02-11

申请号：EP07783431.5

申请日：2007-05-08

申请人： Targacept, Inc.

发明人： DULL, Gary, Maurice ,  MUNOZ, Julio, A.

IPC分类号： C07D213/63 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D213/65

摘要： Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4- penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.