Merck + Co., Inc.

Evotec Oai

Gregory J Kaczorowski

Maria L Garcia

Owen B McManus

William H Parsons

Richard J Swanson

Reid J Leonard

Kimberly L Folander

David A Claremon

Nigel J Liverton

Michael H Fisher

Stephen Colin Price

Deborah L Zink

Frank Kayser

Otto D Hensens

Kathleen M Rupprecht

Jianming Bao

Christopher F Claiborne

Edward Andrew Boyd

Robert K Baker

William Strohl

Richard L Monaghan

Ying-Duo Gao

Wayne J Thompson

Peter T Meinke

Seok H Lee

Shouwu Miao

Robert A Giacobbe

Michael A Goetz

Andrew Kotliar

Jan S Tkacz

Peter K Siegl

Jennifer Chee

Stephan K Grant

John Stibbard

William A Schmalhofer

Chou Juitsai Liu

Richard E Middleton

This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Ophthalmic compositions for treating ocular hypertension

This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.

Maxi-k channel blockers, methods of use and process for making the same

This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.

Method for treating ocular hypertension

The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Carbocyclic potassium channel inhibitors

The present invention provides assays in which intracellular chelators are used to alter the kinetics of signal generation triggered by divalent cations, particularly calcium influx into the cell. The use of an intracellular chelator in the assay can delay and prolong the signal, allowing the signal to be detected by automated instrumentation without the need for simultaneous liquid handling at the time of detection.

High throughput screening by measurement of intracellular calcium levels

DNA encoding the .beta. subunit of a mammalian maxi-K potassium channel

Disclosed are nucleic acids encoding the .beta. subunit of the mammalian large-conductance ('maxi-K') potassium channel, cells transformed with such nucleic acids, and .beta. subunit proteins produced by the transformed cells. Within the invention are recombinant host cells expressing .alpha..beta. heteromultimers. Such cells or preparations made from them may be used to screen for pharmacologically active modulators of maxi-K channel activity. Such modulators are potentially useful in treating asthma, pregnant human myometrium, hypertension and angina, cerebral ischemia, and conditions where stimulation of neurotransmitter release is desired, such as in Alzheimer's disease and stimulation of damaged nerves.

Screening array using cells expressing recombinant .alpha. and .beta.

The present invention relates to novel potassium channel agonists which are useful in activating the calcium activated Maxi-K potassium channel in mammalian neuronal and smooth muscle tissue. The claimed compounds are of the general formula: ##STR1## In addition, a novel microbiological process for producing the claimed compounds is described.

Biologically active compounds

Pharmaceutical compositions and methods useful in the treatment of cardiac arrhythmias are described.

Antiarrhythmic compositions and method

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Edison, NJ, United States of America

Gregory J Kaczorowski