BALWINDER SINGH BHATTI,SRINIVASA RAO AKIREDDY,RONALD JOSEPH HEEMSTRA,SRINIVASA V. MURTHY,JON-PAUL STRACHAN,YUNDE XIAO
申请号:
MX2012006484
公开号:
MX2012006484A
申请日:
2010.12.03
申请国别(地区):
MX
年份:
2012
代理人:
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 R1 is -C(O)-R3, -C(O)O-R3, -C(O)NH-R3, -C(O)-(CH2)q-X-R3, -C(O)O-(CH2)q-X-R3, or -C(O)NH-(CH2)q-X-R3 q is 1, 2, 3, 4, 5, or 6 X is -0-, -S-, -NH-, or -NHC(O)- R2 is H or alkyl R3 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, or heterocyclic.La presente invención se relaciona con compuestos que se unen y modulan la actividad de receptores nicotínicos neuronales de acetilcolina, con procesos para preparar estos compuestos, con composiciones farmacéuticas que contienen estos compuestos, y con métodos para usar estos compuestos para tratar una amplia variedad de condiciones y trastornos, que incluyen aquellos asociados a la disfunción del sistema nervioso central (SNC).