Merck + Co., Inc.

Elizabeth M Naylor

Prasun K Chakravarty

Ann E Weber

Michael H Fisher

Thomas F Walsh

William J Greenlee

Anna Chen

Emma R Parmee

Scott William Bagley

James R Tata

Hyun O Ok

Daljit S Dhanoa

Kenneth J Fitch

Thomas L Shih

David L Williams

Arthur A Patchett

Tesfaye Biftu

Wallace T Ashton

Danqing D Feng

Gui-Bai Liang

Robert J Mathvink

Chan-Hwa Kuo

Dong Ok

Amide derivatives are selective &bgr;,adrenergic receptor agonists with very little &bgr;,and &bgr;,adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

Amide derivatives as &bgr; 3 agonists

Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

Oxadiazole benzenesulfonamides as selective .beta..sub.3 Agonist for the

Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

Substituted sulfonamides as selective .beta.-3 agonists for the

Substituted phthalazinones as neurotensin antagonists

Substituted sulfonamides as selective .beta..sub.3 agonists for the

Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.

Quinazolinones substituted with phenoxyphenylacetic acid derivatives

Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.

Benzimidazolinones substituted with phenoxyphenylacetic acid derivatives

Phenoxyphenylacetic acids and derivatives of general structural formula I have endothelin ##STR1## antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.

Six-membered ring fused imidazoles substituted with phenoxyphenylacetic

There are disclosed substituted imidazole derivatives of Formula I which are useful as angiotensin II antagonists. ##STR1##

Imidazole angiotensin II antagonists incorporating acidic functional

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Scotch Plains, NJ, United States of America

Elizabeth M Naylor