发明公开
- 专利标题: Amides of diazabicycloalkanes selective for nicotinic acetylcholine receptor sub-types
- 专利标题(中): 酰胺二氮杂双环链烷酸脱乙酰壳多糖
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申请号: EP10075738.4申请日: 2007-11-01
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公开(公告)号: EP2284171A1公开(公告)日: 2011-02-16
- 发明人: Mazurov, Anatoly , Miao, Lan , Xiao, Yun-de , Hammond, Philip S. , Miller, Craig H. , Akireddy, Srinivasa Rao , Murthy, V Srinivasa , Whitaker, Regina C. , Breining, Scott R. , Melvin, Matt S.
- 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: US856079P 20061102
- 主分类号: C07D471/08
- IPC分类号: C07D471/08 ; A61P25/00 ; A61K31/407 ; C07D487/04
摘要:
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroraryl carboxylic acids and certain diazabicycloalkanes. The 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, particularly CNS disorders. 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).
Formula I:
wherein n has the value of 0 or 1, and
Cy is a heteroaryl group chosen from the group of 2-furanyl, 3-furanyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 1,3,4-oxadiazol-2-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 1,3,4-thiadiazol-2-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl and 4-pyridinyl.
Formula I:
wherein n has the value of 0 or 1, and
Cy is a heteroaryl group chosen from the group of 2-furanyl, 3-furanyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 1,3,4-oxadiazol-2-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 1,3,4-thiadiazol-2-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl and 4-pyridinyl.
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