Warner-lambert Company

Basf Aktiengesellschaft

Other

Medicis Pharmaceutical Corporation

Graceway Pharmaceuticals, LLC

Catherine R Kostlan

David T Connor

Thomas R Belliotti

Jagadish C Sircar

Daniel L Flynn

Paul C Unangst

James Bernard Kramer

Michael D Mullican

Gary P Shrum

Wiaczeslaw A Cetenko

Michael William Wilson

Hamish John Allen

Kenneth Dale Brady

John C Hodges

Diane H Boschelli

Subhashis Banerjee

Robert V Talanian

Raj Neil Raheja

Meera Tugnait

Donald E Nies

Kimberly Wade

Bruce D Roth

Bernard Gaudilliere

Henry Jacobelli

Steven Robert Miller

Nigel P Walker

William Glen Harter

Hans Peter Albrecht

Jack Jie Li

Wen-Song Yue

The present invention is directed to the topical application of the malonamide ACAT inhibitors described by Formula I. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin.

Method for decreasing sebum production

A compound selected from those of formula (I):wherein:

Oxo-azabicyclic compounds

The present invention relates to compounds that are inhibitors of interleukin-1&bgr; converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1&bgr; converting enzyme.

Sulfonamide interleukin-1&bgr; converting enzyme inhibitors

The present invention relates to N-substituted derivatives of glutamic acid of pharmaceutical interest, to pharmaceutical compositions which include compounds of the invention and pharmaceutically acceptable carriers, to methods of their preparation, and to their use in purification of interleukin-1.beta. converting enzyme (ICE).

N-substituted glutamic acid derivatives with interleukin-1.beta.

N-substituted glutamic acid derivatives with interleukin-1 .beta.

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

The present invention is novel compounds which are 3,5-di-tertiary-butyl-4-hydroxyphenyl substituted 1,2,4- and 1,3,4-thiadazoles 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 the like.

3,5-di-tertiary-butyl-4-hydroxyphenyl-1,3,4-thiadiazoles, and

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

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

Novel heterocyclic methyl derivatives of biphenyl oxadiazoles and thiadiazoles are described, as well as methods for the preparation of said derivatives and pharmaceutical compositions of the same, which are useful as antagonists of the angiotensin II enzyme and thus useful in treating hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.

Biphenyl oxadiazoles and thiadiazoles as angiotensin II antagonists

The present invention is novel compounds which are 2-heterocyclic-4,6-ditertiarybutyl-5-hydroxy-1,3-pyrimidines, where heterocyclic is selected from imidazole, thiazole, and oxazole, and pharmaceutically acceptable additional 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.

2-heterocyclic-5-hydroxy-1,3-pyrimidines useful as antiinflammatory

The present invention is novel compounds which are 2-substituted-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 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 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-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines useful as

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

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Saline, MI, United States of America

Catherine R Kostlan