Murthy, Srinivasa V.,Mazurov, Anatoly A.,Xiao, Yun-De,Hammond, Philip S.,Akireddy, Srinivasa Rao
申请号：
AU2008232787
公开号：
AU2008232787B2
申请日:
2008.03.27
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
Compounds, pharmaceutical compositions including the compounds, and methodsof 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 affinityto, neuronal nicotinic receptors of the a4ß2 subtype in the central nervoussystem (CNS). The compounds and compositions can be used to treat and/or preventa wide variety of conditions or disorders, such as those disorders characterizedby dysfunction of nicotinic cholinergic neurotransmission, including disordersinvolving neuromodulation of neurotransmitter release, such as dopamine release.CNS disorders, which are characterized by an alteration in normal neurotransmitterrelease, are another example of disorders that can be treated and/or prevented.The compounds can: (i) alter the number of nicotinic cholinergic receptors ofthe brain of the patient, (ii) exhibit neuroprotective effects, and (iii) whenemployed in effective amounts, not result in appreciable adverse side effects(e.g. side effects such as significant increases in blood pressure and heartrate, significant negative effects upon the gastrointestinal tract, and significanteffects upon skeletal muscle).
