Allergan, Inc.

Shervin Esfandiari

Lloyd Jay Dolby

Michael E Garst

Alfred Arthur Avey, Jr

Vivian Rose MacKenzie

David Charles Muchmore

Joseph S Adorante

George R Ehring

Mark R Hansen

Nestor A Fedoruk

Jeremiah Marsden

Jia Chian Li

Ellen Chao

Howard B Rind

Herman Ng

Hau Ton

Thomas C Malone

Geoffrey Kenneth Cooper

Michael S Garst

Natalie C Chamberlain

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.

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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

The invention is directed to a process for reducing or reductively cleaving an organic compound susceptible to dissolving metal reduction comprising exposing the organic compound to a solution of lithium in a polyamine including at least two amino groups, selected from the group consisting of primary and secondary amino groups and mixtures thereof, e.g. ethylenediamine and R--NH.sub.2, optionally containing a lower alkyl alcohol, wherein R is chosen from the group consisting of ethyl, propyl, and butyl, including all straight and branched chain isomers thereof, for a time sufficient to effect reduction.

Lithium and amine dissolving metal reduction

A process of preparing lactam derivatives of pilocarpine is disclosed. The process involves condensation of a dihydroxybutene and alkyl orthoester to form a lactone intermediate which is oxidized to trans-pilopic acid. This lactone ring is reacted with a benzylamine and the benzyl group removed with a novel dissolving metal reduction mixture to yield the key intermediate IV ##STR1## which can be elaborated to pilolactam through a known sequence of steps.

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Eugene, OR, United States of America

Shervin Esfandiari