Merck + Co., Inc.

Merck Sharp + Dohme Corp.

David L Williams

Thomas F Walsh

Daljit S Dhanoa

Kenneth J Fitch

William J Greenlee

Prasun K Chakravarty

Scott William Bagley

James R Tata

Ralph A Rivero

Nancy J Kevin

Douglas J Pettibone

Theodore P Broten

Daniel F Veber

Richard B Toupence

Elizabeth M Naylor

Anna Chen

Jay M Matthews

James C Barrow

Leonardus H T Van Der Ploeg

Kevin R Lynch

Andrew D Howard

Scott E Wolkenberg

James J Mulhearn

Scott T Harrison

Gerard R Kieczykowski

Qingyun Liu

Eric Hostetler

Cyrille Sur

Theodore N Mellin

Qingping Jiang

Ruiping Wang

Alison Strack

The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH. 

Substituted azabenzoxazoles

A new neuromedin U receptor, designated NMUR2 has been found, which is involved in modulation of feeding behavior in mammals. Ligands of this receptor are able to modulate eating, and weight gain. Amino acid sequences of the human and rat forms, as well as their nucleic acid sequences are given.

Neuromedin U receptor NMUR2 and nucleotides encoding it

Phenoxyphenylacetic acid derivatives

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

Biphenyl compounds useful or endothelin antagonists

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, cerebral 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 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.

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, 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

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

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Telford, PA, United States of America

David L Williams