Allergan, Inc.

Euro-celtique S.a.

State Board of Higher Education for and on Behalf of the University of

Lloyd Jay Dolby

Michael E Garst

Shervin Esfandiari

Mark Chasin

David J Cavalla

Alfred Arthur Avey, Jr

Nestor A Fedoruk

Vivian Rose MacKenzie

Richard William Frith

David Charles Muchmore

Peter Hofer

Joseph S Adorante

George R Ehring

Mark R Hansen

Jeremiah Marsden

Jia Chian Li

Ellen Chao

Howard B Rind

Herman Ng

Hau Ton

Thomas C Malone

Stephen M Coutts

T Scott Shoupe

Geoffrey Kenneth Cooper

Michael S Garst

Natalie C Chamberlain

John David Cavalla

Charles David Muchmore

The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R, R, R, R, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.

Benzimidazole derivatives as selective blockers of persistent sodium current

The present invention provides a method of making an imidazole 2-thione which comprises the step(s) of reducing a thiohydantoin to said imidazole-2-thione.

[object Object]

The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.

Process for the synthesis of imidazoles

A method of 4-substituted imidazole-2-ones and thiones which comprises reacting a methylene urea or methylene thiourea wherein said methylene is substituted with the 4-subsituent and a cyano or alkycarboxylate group to provide said 4-substituted imidazole 2-one or thione.

Method of making imidazole-2-ones and 2-thiones

Synthetic methods for preparing isomerically pure N-arylsulfonyl derivatives of proton pump inhibitors which include a substituted benzimidazole nucleus are shown by the synthetic schemes and experimental description.

Process for preparing isomerically pure prodrugs of proton pump inhibitors

The present invention provides a method of making an imidazole-2-thione which comprises the steps of reacting a vicinal diamine with a compound having a thiocarbonyl moiety and oxidizing the resulting reaction product to obtain said imidazole-2-thione.

Method of making imidazole-2-thiones

Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.

Benzoxazoles

Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of:

Phenyl-triazole compounds for PDE-IV inhibition

Phenylpyridyl compounds for inhibiting phosphodiesterase IV and methods

Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2 and Z are described herein. The compounds possess improved PDE IV inhibition as compared to rolipram as well as with improved selectivity with regard to PDE III inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

Aryl imidazole compounds having phosphodiesterase IV inhibitory activity

Novel compounds which are effective PDE IV inhibitors are disclosed The compounds possess similar or improved PDE IV inhibition as compared to rolipram, with improved selectivity with regard to, e.g., PDE III inhibition. Preferred compounds are 3-(3-cyclopentyloxy-4-methoxy-benzylamino)-4-hydroxymethyl pyrazole and 3-(3-cyclopentyloxy-4-methoxybenzylamino)-4-methoxymethylpyrazole.

Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods

Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds have the formula: ##STR1## wherein: R.sub.1 and R.sub.2 may be the same or different and each is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety;

Growing community of inventors

Eugene, OR, United States of America

Lloyd Jay Dolby