Aventis Pharmaceuticals Inc.

Francis A Volz

Daniel Gerard McGarry

Christopher J Burns

Gregory H Merriman

Alexandre Gross

William P Dankulich

Liang Ma

Patrick Shum

David Rampe

Jeffrey Stephen Sabol

Garth E Ringheim

Timothy Francis Gallagher

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

This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).

Substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans

This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Substituted (aminoiminomethyl or aminomethyl) benzoheteroaryl compounds

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Neshanic Station, NJ, United States of America

Francis A Volz