Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Sharp & Dhome Corp.

Nancy J Kevin

Ralph A Rivero

William J Greenlee

Prasun K Chakravarty

Xin Gu

Thomas F Walsh

Sherman Tim Waddell

Scott William Bagley

James R Tata

Eric E Allen

Daljit S Dhanoa

Kenneth J Fitch

Douglas J Pettibone

David L Williams

Theodore P Broten

James M Balkovec

Scott D Edmondson

Ying-Duo Gao

Zhuyan Guo

Santhosh Francis Neelamkavil

Joseph Leslie Duffy

Richard B Toupence

Zahid Hussain

Remond Moningka

Jay M Matthews

Andrew William Stamford

Amjad Ali

Donald W Graham

Younong Yu

Nathan B Mantlo

Zhijian Lu

Yuan Cheng

Mitree M Ponpipom

Songnian Lin

David Askin

Kevin Tyler Chapman

Richard John Varsolona

Alan W Hruza

Subharekha Raghavan

Bing Li

Rajan Anand

Yeon-Hee Lim

Yu Jiang

Weiguo Liu

Ahmet Kekec

Jiayi Xu

Heping Wu

Thomas A Rano

Fengqi Zhang

R Scott Hoerrner

Gool F Patel

Deyou Sha

Susan D Aster

Gerard R Kieczykowski

Joseph D Armstrong, Iii

Tomasz W Glinka

Gioconda V Gallo-Etienne

Anjan Chakrabarti

Craig A Parish

Tracy Huening

Robert M Purick

Puneet Kumar

Hiroki Sone

Brian Anthony Kirk

Fred Fleitz

Daniel E Petrillo

Weijuan Tang

Joseph L Duffy

Andrew M Stamford

The present invention relates to tyrosine-specific functionalized insulin analogs and processes of making such tyrosine-specific functionalized insulin analogs using R-3H-1,2,4-triazoline-3,5-(4H)diones (PTAD).

Tyrosine-specific functionalized insulin and insulin analogs

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor XIa inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase Type 1 enzyme (11&#x3b2;-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11&#x3b2;-HSD-1.

Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Triazole derivatives as inhibitors of 11-&#x3b2;-hydroxysteroid dehydrogenase-1

Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Pyrazole carboxamides of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Pyrazole carboxamides as inhibitors of 11-&#x3b2;-hydroxysteroid dehydrogenase-1

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

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

Substituted biphenylmethylimidazopyridines

Substituted heterocycles attached through a methylene bridge to novel substituted phenyl thiophene or phenyl furan derivative of the Formula I are useful as angiotensin II antagonists. ##STR1##

Angiotensin II antagonists incorporating a substituted thiophene or furan

Substituted imidazoles attached through a methylene bridge to novel substituted phenyl thiophene or phenyl furan derivative of the Formula I are useful as angiotensin II antagonists. ##STR1##

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

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East Brunswick, NJ, United States of America

Nancy J Kevin