发明公开
EP2509982A1 3,6-DIAZABICYCLO[3.1.1]HEPTANES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
审中-公开
3,6-二氮杂双环[3.1.1] HEPTANE ALS NEURONALE NIKOTINISCHE ACETYLCHOLINRECEPTORLIGANDEN
- 专利标题： 3,6-DIAZABICYCLO[3.1.1]HEPTANES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
- 专利标题（中）： 3,6-二氮杂双环[3.1.1] HEPTANE ALS NEURONALE NIKOTINISCHE ACETYLCHOLINRECEPTORLIGANDEN
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申请号： EP10787978.5申请日： 2010-12-03
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公开(公告)号： EP2509982A1公开(公告)日： 2012-10-17
- 发明人: AKIREDDY, Srinivasa Rao , BHATTI, Balwinder Singh , HEEMSTRA, Ronald Joseph , MURTHY, Srinivasa V. , STRACHAN, Jon-Paul , XIAO, Yunde
- 申请人： Targacept, Inc.
- 申请人地址： 200 East First Street, Suite 300 Winston-Salem, NC 27101-4165 US
- 专利权人： Targacept, Inc.
- 当前专利权人： Targacept, Inc.
- 当前专利权人地址： 200 East First Street, Suite 300 Winston-Salem, NC 27101-4165 US
- 代理机构： Crowhurst, Charlotte Waveney
- 优先权： US267218P 20091207
- 国际公布： WO2011071758 20110616
- 主分类号： C07D487/08
- IPC分类号： C07D487/08 ; A61K31/4995 ; A61P25/00 ; A61P25/16 ; A61P25/28
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.
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.
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