Targacept, Inc.

Thomas Jeffrey Clark

Balwinder Singh Bhatti

Craig Harrison Miller

Jeffrey Daniel Schmitt

Gary Maurice Dull

Lan Miao

Dwo Lynm

Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.

Pharmaceutical compositions and methods for use

The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridinyl diazabicyclic compounds, such as (1S,4S)-2-(5-(3-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(3-thienyl)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(4-fluorophenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, and (1S,4S)-2-(5-benzoyl-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.

Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an alkylene or alkylidene unit to an azabicyclic moiety.

The present invention relates to diazabicyclic compounds, and preferably N-aryl diazabicyclic compounds. Of particular interest are 2-pyridyl diazabicyclic compounds, such as (1S,4S)-2-(3-pyridyl)-2,5-diazabicyclo&lsqb;2.2.1&rsqb;heptane. Other exemplary compounds of the present invention include: (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo&lsqb;2.2.1&rsqb;heptane, (1S,4S)-2-(5-pyrimidinyl)-2,5-diazabicyclo&lsqb;2.2.1&rsqb;heptane and (1S,4S)-2-(6-chloro-3-pyridazinyl)-2,5-diazabicyclo&lsqb;2.2.1&rsqb;heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.

Growing community of inventors

High Point, NC, United States of America

Thomas Jeffrey Clark