Targacept, Inc.

Catalyst Biosciences, Inc.

Attenua, Inc.

John Genus

Gary Maurice Dull

Merouane Bencherif

Anatoly A Mazurov

Lan Miao

Julio A Munoz

James R Moore

Srinivasa Rao Akireddy

Jacob Mathew

Daniel Yohannes

Timothy J Cuthbertson

Pieter Albert Otten

Scott R Breining

Philip S Hammond

Kristen G Jordan

Nikolai Fedorov

Gregory J Gatto

Thomas Wännman

Sondra Pfeiffer

Inigo Pfeiffer

Lisa Benson

Tommi Ratilainen

Janna Hellström

Niklas Wahlström

Joesph Pike Mitchener, Jr

Teresa Y Phillips

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 formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine compound) or to another pharmaceutically acceptable salt form.

Hydroxybenzoate salts of metanicotine compounds

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 formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.

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.

Process for the preparation of aryl substituted olefinic amines

The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.

Synthesis and novel salt forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine

The present invention relates to (2S,3R)-N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.

(2S,3R)-N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms, and methods of use thereof

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Winston-Salem, NC, United States of America

John Genus