Warner-lambert Company

Pfizer Corporation

Thomas R Belliotti

Catherine R Kostlan

David T Connor

David Juergen Wustrow

Daniel L Flynn

Jagadish C Sircar

Lawrence D Wise

James Bernard Kramer

Wiaczeslaw A Cetenko

Justin Stephen Bryans

Andrew John Thorpe

Suzanne Ross Kesten

Donald E Nies

David Christopher Horwell

Po-wai Yuen

Diane H Boschelli

Jacob Bradley Schwarz

Thomas Capiris

Clifton J Blankley

Clare Octavia Kneen

Steven Robert Miller

Augustine Tobi Osuma

Robert Michael Schelkun

Thomas A Pugsley

Ihoezo Victor Ekhato

Mono-and disubstituted 3-propyl gamma-aminobutyric acids

The instant invention is improved gamma amino butyric acid analogs, processes for their preparation, and methods of using them as agents for treating epilepsy and other neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal damage, and inflammation.

Gamma amino butyric and acid analogs

Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Amines as pharmaceutical agents

The instant invention is a novel series of amino heterocycles useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, and sleep disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Amino heterocycles useful as pharmaceutical agents

This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.

Benzoxazinone dopamine D4 receptor antagonists

Compounds that are antagonists of dopamine D4 receptors, methods of treating psychosis and schizophrenia using the compounds, and pharmaceutically acceptable compositions that contain the dopamine D4 receptor antagonists are disclosed.

Dopamine D4 receptor antagonists

Substituted cyclohexylamines as central nervous systems agents

The present invention is novel compounds which are 4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidine substituted 1,2,4- and 1,3,4-thiadiazoles and oxadiazoles, and 1,2,4-triazoles, and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and particularly rheumatoid arthritis, osteoarthritis, other inflammatory conditions, psoriasis, allergic diseases, asthma, inflammatory bowel disease, GI ulcers, cardiovascular conditions, including ischemic heart disease and atherosclerosis, and ischemia-induced cell damage, particularly brain damage caused by stroke. They can also be used topically for treating acne, sunburn, psoriasis, and eczema. Also included are leukotriene mediated pulmonary, gastrointestinal, inflammatory, dermatological, and cardiovascular conditions. The disclosed compounds also have potential utility as antioxidants. The preferred use is in treating inflammatory conditions.

Substituted heteroaryl analogs of

Substituted 4,6-di-tertiary-butyl 5-hydroxy-pyrimidines

The present invention compounds are 5-hydroxy-2-pyrimidinylmethylene derivatives and pharmaceutically acceptable addition salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of, for example, inflammation and GI ulcers.

5-hydroxy-2-pyrimidinylmethylene derivatives useful as antiinflammatory

The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are described as having activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.

2-substituted amino-4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidines as

The present invention is novel compounds which are 5-hydroxy-2-pyrimidinylmethylene derivatives and pharmaceutically acceptable addition salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of, for example, preferably inflammation.

2-substituted amino-4, 6-di-tertiary-butyl-5-hydroxy-1, 3-pyrimidines as

The present invention is a novel compound which is a thiadiazole or oxadiazole analog of a fenamic acid having a substituted hydroxamate side chain and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use thereof. The invention compounds are now found to have activity as inhibitors of one or both of cyclooxygenase and 5-lipoxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like. Thus, the present invention is also a pharmaceutical composition or method of use thereof.

Thiadiazole or oxadiazole analogs of fenamic acids containing

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Ypsilanti, MI, United States of America

Thomas R Belliotti