Sepracor, Inc.

Steven Brandt

James W Young

Charles M Zepp

David R Dodds

Jorge Luis Lopez

This invention relates to a method for the production of (2R,3S)-3-(4-methoxyphenyl)glycidic acids and esters thereof, which are synthetic intermediates for the production of the calcium antagonist diltiazem. The method involves the stereoselective enzymatic ester hydrolysis of racemic trans-3-(4-methoxyphenyl)glycidic acid ester to yield the resolved (2R,3S) compound as the ester. Membrane reactor methods and apparatus for the conduct of this enzymatic resolution process are also disclosed herein, as is the use of bisulfite anion in the aqueous reaction phase as a means of minimizing the inhibitory effect of an aldehyde reaction by-product on the reaction's progress. The benefits of selected solvent systems from which may be obtained highly resolved ester product are also disclosed. These enriched organic solutions may be used in subsequent transformations. Alternatively, optically pure product may be obtained directly therefrom.

Process for preparing optically active glycidate esters

Methods and compositions are disclosed utilizing the optically pure (&plus;) isomer of zopiclone. This compound is a potent drug for the treatment of sleep disorders, such as insomnia, and convulsive disorders, such as epilepsy. Similarly, these novel compositions and methods are useful for the treatment of sleep disorders and convulsive disorders while avoiding the concomitant liability of adverse effects associated with the racemic mixture of zopiclone. The optically pure (&plus;) isomer of zopiclone is also useful for treating disorders that are affected by the binding of agonists to central nervous system or peripheral benzodiazepine receptors. Also described are methods and compositions for treating disorders that are affected by binding of agonists to central nervous system or peripheral benzodiazepine receptors while avoiding the adverse effects associated with the administration of the racemic mixture of zopiclone.

Methods and compositions for treating disorders, using optically pure (&plus;) zopiclone

Methods and compositions are disclosed utilizing the optically pure (+) isomer of zopiclone. This compound is a potent drug for the treatment of sleep disorders, such as insomnia, and convulsive disorders, such as epilepsy. Similarly, these novel compositions and methods are useful for the treatment of sleep disorders and convulsive disorders while avoiding the concomitant liability of adverse effects associated with the racemic mixture of zopiclone. The optically pure (+) isomer of zopiclone is also useful for treating disorders that are affected by the binding of agonists to central nervous system or peripheral benzodiazepine receptors. Also described are methods and compositions for treating disorders that are affected by binding of agonists to central nervous system or peripheral benzodiazepine receptors while avoiding the adverse effects associated with the administration of the racemic mixture of zopiclone.

Methods and compositions for treating sleep disorders, convulsive

Disclosed is a method of inducing and maintaining anesthesia while avoiding concomitant liability of adverse effects comprising administering by inhalation to a warm blooded animal in need of anesthesia an amount sufficient to induce and maintain anesthesia but insufficient to cause said adverse effects, of (R)-isoflurane or (R)-desflurane, substantially free of its (S)-stereoisomer. Also disclosed are novel compositions of these compounds for use in the above disclosed method.

Methods of use and compositions of (R)-isoflurane and (R)-desflurane

Disclosed is a method of inducing and maintaining anesthesia while avoiding concomitant liability of adverse effects comprising administering by inhalation to a warm blooded animal in need of anesthesia an amount sufficient to induce and maintain anesthesia but insufficient to cause said adverse effects, of (S)-isoflurane or (S)-desflurane, substantially free of its (R)-stereoisomer. Also disclosed are novel compositions of these compounds for use in the above disclosed method.

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Marlborough, MA, United States of America

Steven Brandt