Targacept, Inc.

Catalyst Biosciences, Inc.

Attenua, Inc.

Yunde Xiao

Srinivasa Rao Akireddy

Balwinder Singh Bhatti

Matt S Melvin

Ronald Joseph Heemstra

Jason Daniel Speake

Daniel Yohannes

Anatoly A Mazurov

Lan Miao

Srinivasa V Murthy

Craig Harrison Miller

Scott R Breining

Philip S Hammond

Regina C Whitaker

Jon-Paul Strachan

The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for use, and their pharmaceutical compositions.

Nicotinic receptor non-competitive antagonists

The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.

Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the &#x3b1;4&#x3b2;2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes

The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).

3,6-diazabicyclo[3.1.1]heptanes as neuronal nicotinic acetycholine receptor ligands

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Clemmons, NC, United States of America

Yunde Xiao