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3,6-diazabicyclo 3.1.1 heptanes as neuronal nicotinic acetylcholine receptor ligands

机译:3,6-二氮杂双环[3.1.1]庚烷作为神经元烟碱型乙酰胆碱受体配体

摘要

"3,6-diazabicyclo [3.1.1] heptanes as acetylcholine neuronal nocotinic receptor ligands". The present invention relates to compounds which bind and modulate the activity of neuronal nicotinic acetylcholine receptors (nrrs), processes for the preparation of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds for the treatment of such compounds. of a wide variety of conditions and disorders, including those associated with central nervous system (CNS) dysfunction. The present invention includes compounds that bind with high affinity to nnrs of the & 4b2 subtypes or the & 6-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) qx-xr3, -c (o) o- (chh2 ) qx-r3, or -c (o) nh- (ch2) qx-r3; q is 1,2,3,41,5, or 6; x is -o-, -s-, -nh-, or -nhc (o) -; R2 is h or alkyl; R3 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, or heterocyclic.
机译:“ 3,6-二氮杂双环[3.1.1]庚烷作为乙酰胆碱神经元的Nocotinic受体配体”。本发明涉及结合和调节神经元烟碱乙酰胆碱受体(nrrs)活性的化合物,制备此类化合物的方法,含有此类化合物的药物组合物,以及使用此类化合物治疗此类化合物的方法。各种疾病和病症,包括与中枢神经系统(CNS)功能障碍有关的疾病和病症。本发明包括以高亲和力与&4b2亚型或含&6亚型或两种nnr亚型的nnrs结合的化合物。式(i)其中:每个m相同且为0或1:每个n相同且为0或1;当每个m为0时,则每个n为1;当每个m为1时,则每个n为0; r1是-c(o)-r3,-c(o)o-r3,-c(o)nh-r3,-c(o)-(ch2)qx-xr3,-c(o)o-(chh2 )qx-r3或-c(o)nh-(ch2)qx-r3; q是1,2,3,41,5或6; x是-o-,-s-,-nh-或-nhc(o)-; R 2是h或烷基; R 3是烷基,烯基,炔基,环烷基,环烯基,环炔基,芳基,杂芳基或杂环。

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