- NEW PROCESS FOR THE PREPARATION OF ARYL SUBSTITUTED OLEFINIC AMINES
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An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N- methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.
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- HYDROXYBENZOATE SALTS OF METANICOTINE COMPOUNDS
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Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The forma
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Page/Page column 43-44
(2008/06/13)
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- Compounds capable of activating cholinergic receptors
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The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.
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- Compounds capable of activating cholinergic receptors
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The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.
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- Pharmaceutical compositions and methods for use
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Pharmaceutical compositions incorporate aryl substituted olefinic amine compounds. Representative compounds are (3E)-N-methyl-4-[3-(5-nitro-6-aminopyridin)yl]-3-buten-1-amine, (3E)-N-methyl-4-[3-(5-(N-benzylcarboxamido)pyridin)yl]-3-buten-1-amine, (4E)-N-methyl-5-[5-(2-aminopyrimidin)yl]-4-penten-2-amine, (4E)-N-methyl-5-(3-(5-aminopyridin)yl)-4-penten-2-amine, (3E)-N-methyl-4-(3-(5-isobutoxypyridin)yl)-3-buten-1-amine, (3E)-N-methyl-4-(3-(1-oxopyridin)yl)-3-buten-1-amine, (3E)-N-methyl-4-(3-(5-ethylthiopyridin)yl)-3-buten-1-amine, (4E)-N-methyl-5-(3-(5-trifluoromethylpyridin)yl)-4-penten-2-amine and (4E)-N-methyl-5-(3-(5-hydroxypyridin)yl)-4-penten-2-amine.
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- Pharmaceutical compositions for the prevention and treatment of central nervous system disorders
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A pharmaceutical composition incorporates a pharmaceutically effective amount of at least two components, one of those components being a nicotinic compound capable of interacting with nicotinic cholinergic receptors (e.g., a nicotinic agonist, such as E-
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