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Diazabicyclic aryl derivatives as cholinergic receptor modulators and nicotinic acetylcholine receptor ligands

机译:二氮杂双环芳基衍生物作为胆碱能受体调节剂和烟碱乙酰胆碱受体配体

摘要

Disclosed are 1,4-diaza-bicyclo[3.2.2]nonane derivatives as represented by Formula I, which are cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters, wherein n is 1, 2 or 3; and A represents a phenyl, a thiadiazolyl, a pyridyl or a pyridazinyl group; B represents a phenyl group, a thiadiazolyl group, a pyridyl group or a pyridazinyl group, which may optionally be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, hydroxy. alkoxy, cyano-alkyl, halo, trihaloalkyl, trihaloalkoxy, cyano, amino, nitro, and -NH(CO)R""; wherein R"" represents hydrogen, alkyl or cycloalkyl; and L represents a linking group selected from C2-alkynyl, -O-, -S-CH2-, -SO-, -S-, -NHCO-, -NHCONH- or -NH(SO2)-.
机译:公开了由式I表示的1,4-二氮杂-双环[3.2.2]壬烷衍生物,其为烟碱乙酰胆碱受体上的胆碱能配体以及单胺受体和转运蛋白的调节剂,其中n为1、2或3; A表示苯基,噻二唑基,吡啶基或哒嗪基。 B代表苯基,噻二唑基,吡啶基或哒嗪基,它们可以任选地被选自烷基,环烷基,羟基的取代基取代一次或多次。烷氧基,氰基烷基,卤素,三卤代烷基,三卤代烷氧基,氰基,氨基,硝基和-NH(CO)R“”;其中R””代表氢,烷基或环烷基; L表示选自C 2-炔基,-O-,-S-CH 2-,-SO-,-S-,-NHCO-,-NHCONH-或-NH(SO 2)-的连接基团。

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