Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Wallace T Ashton

Richard L Tolman

William J Greenlee

Linda L Chang

Ann E Weber

Edward F Rogers

Matthew J Wyvratt

Malcolm MacCoss

Michael H Fisher

Mark T Goulet

Lin Chu

Arthur A Patchett

Prasun K Chakravarty

Charles G Caldwell

Peter Lin

Thomas F Walsh

Donald W Graham

Narindar N Girotra

Robert J Mathvink

Steven M Hutchins

Emma R Parmee

Mitree M Ponpipom

Hyun O Ok

Ralph A Rivero

Mu T Wu

Edward Walton

Arthur K Field

Hong Dong

John D Karkas

Christine L Cantone

Sander G Mills

Conrad P Dorn

Richard A Dybas

Nathan B Mantlo

Dooseop Kim

Jonathan R Young

Ying-Duo Gao

David G Hangauer

Robert L Bugianesi

Liping Wang

Daljit S Dhanoa

Joseph Leslie Duffy

Jinyou Xu

Kenneth J Fitch

Roy G Smith

Elizabeth M Naylor

Anna Chen

Jeannette E Brown

Giovanna Scapin

Louis Barash

Yi Tien Yang

Kelly Flanagan

Leah Bitalac Reigle

Ronald D Brown

Laura F Canning

The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. 

Bicyclic pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes

The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes

The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. 

The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-RV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

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

There are disclosed compounds of formula (I)

Antagonists of gonadotropin releasing hormone

There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

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.

Endothelin antagonists bearing pyridyl amides

Endothelin antagonists bearing 5-membered heterocyclic amides

Novel substituted 1,2,4-triazolin-3-ones of the formula (I) are useful as angiotensin II antagonists. ##STR1##

Substituted 1,2,4-triazolin-3-one compounds bearing acidic functional

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Clark, NJ, United States of America

Wallace T Ashton