Philip S. Hammond;Anatoly Mazurov;Yun-De Xiao;Srinivasa V. Murthy;Srinivisa Rao Akireddy
发明人:
Philip S. Hammond,Anatoly Mazurov,Yun-De Xiao,Srinivasa V. Murthy,Srinivisa Rao Akireddy
申请号：
US12593779
公开号：
US08198296B2
申请日:
2008.03.27
申请国别(地区):
US
年份:
2012
代理人:
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 α4β2 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).
