公开(公告)号：EP2257549A1

公开(公告)日：2010-12-08

申请号：EP09716691.2

申请日：2009-03-04

申请人： Targacept Inc.

发明人： AKIREDDY, Srinivisa Rao ,  BHATTI, Balwinder Singh ,  BREINING, Scott R. ,  HAMMOND, Philip S. ,  HEEMSTRA, Ronald Joseph ,  MAZUROV, Anatoly ,  MELVIN, Matt S. ,  MIAO, Lan ,  MURTHY, V. Srinivasa ,  STRACHAN, Jon-Paul ,  XIAO, Yun-De

IPC分类号： C07D471/08 ,  A61K31/407 ,  A61P25/00

CPC分类号： C07D471/08

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

公开(公告)号：EP2576496A1

公开(公告)日：2013-04-10

申请号：EP11724498.8

申请日：2011-05-24

申请人： Targacept, Inc.

发明人： AKIREDDY, Srinivasa Rao ,  BHATTI, Balwinder Singh ,  HEEMSTRA, Ronald Joseph ,  MELVIN, Matt S. ,  SPEAKE, Jason ,  XIAO, Yunde ,  YOHANNES, Daniel

IPC分类号： C07C211/41 ,  A61K31/13 ,  A61P9/12 ,  A61P25/24

CPC分类号： A61K31/13 ,  A61K31/397 ,  A61K31/40 ,  C07C211/38 ,  C07C211/41 ,  C07D205/04 ,  C07D295/033

摘要： The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.

摘要翻译： 本发明涉及作为非竞争性拮抗剂调节烟碱受体的化合物，其合成方法，使用方法及其药物组合物。

公开(公告)号：EP2344496A1

公开(公告)日：2011-07-20

申请号：EP09792165.4

申请日：2009-09-02

申请人： Targacept Inc.

发明人： STRACHAN, Jon-Paul ,  BHATTI, Balwinder Singh ,  MAZUROV, Anatoly ,  KLUCIK, Jozef ,  XIAO, Yun-De ,  HAMMOND, Philip S. ,  KOMBO, David ,  MIAO, Lan ,  SPEAKE, Jason Daniel ,  YOHANNES, Daniel

IPC分类号： C07D471/08 ,  A61K31/407 ,  A61P25/00

CPC分类号： C07D471/08

摘要： The present invention relates to compounds of the following formulae I and II 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). Formula (I ), Formula (Il)

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

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.

公开(公告)号：EP2661421A2

公开(公告)日：2013-11-13

申请号：EP12731898.8

申请日：2012-01-05

申请人： Targacept, Inc.

发明人： AKIREDDY, Srinivasa Rao ,  BREINING, Scott R. ,  MELVIN, Matt S. ,  MURTHY, Srinivasa V. ,  MAZUROV, Anatoly A. ,  BHATTI, Balwinder Singh ,  STRACHAN, Jon-Paul ,  HEEMSTRA, Ronald Joseph ,  SHOWALTER, Todd ,  XIAO, Yunde ,  HAMMOND, Philip S. ,  MIAO, Lan ,  KOMBO, David ,  YOHANNES, Daniel ,  SPEAKE, Jason

IPC分类号： C07C211/35 ,  A61K31/13 ,  A61P9/12

CPC分类号： C07D493/08 ,  C07C211/38 ,  C07C2602/40 ,  C07C2602/42 ,  C07C2602/44

摘要： The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for their use, and their pharmaceutical compositions.

摘要翻译： 本发明涉及将烟碱受体调节为非竞争性拮抗剂的化合物，其合成方法，其使用方法及其药物组合物。

公开(公告)号：EP2509982A1

公开(公告)日：2012-10-17

申请号：EP10787978.5

申请日：2010-12-03

申请人： Targacept, Inc.

发明人： AKIREDDY, Srinivasa Rao ,  BHATTI, Balwinder Singh ,  HEEMSTRA, Ronald Joseph ,  MURTHY, Srinivasa V. ,  STRACHAN, Jon-Paul ,  XIAO, Yunde

IPC分类号： C07D487/08 ,  A61K31/4995 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D471/08 ,  C07D487/08

摘要： The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors (NNRs), 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). The present invention includes compounds which bind with high affinity to NNRs of either the α4β2 subtype, or the α6-containing subtype, or both NNR subtypes. Formula (I), wherein: each m is identical and is 0 or 1; each n is identical and is 0 or 1; when each m is 0, then each n is 1; when each m is 1, then each n is 0; R
1 is -C(O)-R
3 , -C(O)O-R
3 , -C(O)NH-R
3 , -C(O)-(CH
2 )
q -X-R
3 , -C(O)O-(CH
2 )
q -X-R
3 , or -C(O)NH-(CH
2 )
q -X-R
3 ; q is 1, 2, 3, 4, 5, or 6; X is -0-, -S-, -NH-, or -NHC(O)-; R
2 is H or alkyl; R
3 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, or heterocyclic.