- FUSED BICYCLOHETEROCYCLE SUBSTITUTED QUINUCLIDINE DERIVATIVES
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Compounds of formula (I) wherein n is 0, 1, or 2; A is N or N+-O-; X is O, S, -NH-, and -N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by a7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.
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Page/Page column 64
(2010/11/08)
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- 3-quinuclidinyl amino-substituted biaryl derivatives
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Compounds of formula (I) wherein n is 0, 1, or 2; Y is O, S, —NH—, and —N-alkyl-; Ar1 is both 6-membered aromatic rings; Ar2 is 5- or 6-membered aromatic rings with a —NR8R9 group, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.
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Page/Page column 19
(2010/02/12)
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- Fused bicycloheterocycle substituted quinuclidine derivatives
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Compounds of formula (I) wherein n is 0, 1, or 2; A is N or N+—O?; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.
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Page/Page column 27
(2010/02/12)
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- Fused bicycloheterocycle substituted quinuclidine derivatives
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Compounds of formula (I) wherein n is 0, 1, or 2; A is N or N+—O—; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.
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- (+)-3-[2-(Benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]-octane as potent agonists for the α7 nicotinic acetylcholine receptor
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A series of 3-substituted 1-azabicyclo[2.2.2]octanes was discovered as the α7 nicotinic acetylcholine (α7) receptor agonists. It was found that (+)-3-[2-(benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]octane (+)-15b has potent agonistic activity for the α7 receptor.
- Tatsumi, Ryo,Seio, Kohji,Fujio, Masakazu,Katayama, Jiro,Horikawa, Takashi,Hashimoto, Kenji,Tanaka, Hiroshi
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p. 3781 - 3784
(2007/10/03)
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- Agonists and antagonists to nicotine as smoking deterents
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Agonists and antagonists to nicotine are used as smoking deterrents.The nicotinic antagonists have the following structural requirements:(1) Aromatic, cycloalkyl, and heterocyclic carbamic acid esters of di- and trialkylaminoalkyl alcohols.(2) Aromatic, cycloalkyl, and heterocyclic thiocarbamic acid esters of di- and trialkylaminoalkyl alcohols.(3) Aromatic, cycloalkyl, and heterocyclic carboxylic acid esters of di- and trialkylaminoalkyl alcohols.(4) Aromatic, cycloalkyl, and heterocyclic carboxylic acid esters of heterocyclic amino alcohols.(5) Lobelia alkaloids: lobeline, lobelanine, and lobelanidine.The nicotinic agonists (nicotine-like) have the following structural requirements:(1) methylcarbamic acid esters of di- and trialkylaminoalkyl alcohols.(2) methylthiocarbamic acid esters of di- and trialkylaminoalkyl alcohols.
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