Aventis Pharmaceuticals Inc.

David Rampe

Michel P Rathbone

Craig P Smith

Margaret Petty

Gregory H Merriman

Daniel Gerard McGarry

Alexandre Gross

Liang Ma

Patrick Shum

Jeffrey Stephen Sabol

Garth E Ringheim

Francis A Volz

Daniel G Mcgarry

Alexandre 245 Eighth Street Gross

The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R, R, R, R, R, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

Heterocyclic compounds as P2X7 ion channel blockers

N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.

Method of treating demyelinating diseases or conditions

Method of treating of demyelinating diseases or conditions

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Bernardsville, NJ, United States of America

David Rampe