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：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：EP2139857A1

公开(公告)日：2010-01-06

申请号：EP08732913.2

申请日：2008-03-27

申请人： Targacept Inc.

发明人： HAMMOND, Philip, S. ,  MAZUROV, Anatoly, A. ,  XIAO, Yun-De ,  MURTHY, Srinivasa, V. ,  AKIREDDY, Srinivasa, Rao

IPC分类号： C07D209/52 ,  C07D221/22 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  A61K31/403 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/5355 ,  A61K31/541 ,  A61P25/00

CPC分类号： C07D209/52 ,  C07D221/22 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06

摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4ß2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, such as those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

公开(公告)号：EP1802601A1

公开(公告)日：2007-07-04

申请号：EP05798620.0

申请日：2005-09-19

申请人： Targacept, Inc.

发明人： BHATTI, Balwinder, Singh ,  BREINING, Scott, R. ,  HAMMOND, Philip, S. ,  KLUCIK, Jozef ,  XIAO, Yun-De

IPC分类号： C07D401/04 ,  A61K31/438 ,  A61P25/04

CPC分类号： C07D413/04 ,  C07D401/04

摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle).