Merck + Co., Inc.

Owen B McManus

Maria L Garcia

Gregory J Kaczorowski

Deborah L Zink

Otto D Hensens

Seok H Lee

Robert A Giacobbe

Richard J Swanson

Reid J Leonard

Kimberly L Folander

William Strohl

Richard L Monaghan

Michael A Goetz

Gary S Kath

Jan S Tkacz

Tina Garyantes

Paul R Augustine

Randal M Bugianesi

Paul B Bennett

John P Imredy

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

Methods of identifying activators and inhibitors of voltage-gated ion channels are provided in which the methods employ electrical field stimulation of the cells in order to manipulate the open/close state transition of the voltage-gated ion channels. This allows for more convenient, more precise experimental manipulation of these transitions, and, coupled with efficient methods of detecting the result of ion flux through the channels, provides methods that are especially suitable for high throughput screening.

Electrical field stimulation of eukaryotic cells

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

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

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 compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof which are useful as potassium channel antagonists, particularly Maxi-K channel antagonists, and thus useful in treating Alzheimer's Disease and other cognitive disorders. This invention is also related to a method of making the compound of formula (I).

Indole diterpene alkaloid compounds

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

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Skillman, NJ, United States of America

Owen B McManus