公开(公告)号：EP2453885A1

公开(公告)日：2012-05-23

申请号：EP10734866.6

申请日：2010-07-12

申请人： Targacept, Inc.

发明人： DUNBAR, Geoffrey C. ,  BEAVER, Jessica ,  TOLER, Steven M.

IPC分类号： A61K31/13 ,  A61P25/24

CPC分类号： A61K31/13 ,  A61K2300/00

摘要： The present invention relates to exo-S-mecamylamine and the use of exo-S-mecamylamine in medical treatments.

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.