Agouron Pharmaceuticals, Inc.

Pfizer Corporation

Novo Nordisk A/s

Research Triangle Institute

Javier Gonzalez

John Howard Tatlock

Hui Li

Tanya Michelle Jewell

Allen Borchardt

Maria Angelica Linton

Angelica Linton

Min Teng

Yufeng Hong

Vlad Edward Gregor

Anthony Lai Ling

Michael David Johnson

Atsuo Kuki

Dan Kiel

Jesper F Lau

Jun Feng

Peter Madsen

Peter Scott Dragovich

Melwyn A Abreo

Daljit Singh Dhanoa

Christian Klarner Sams

Michael Bruno Plewe

Ru Zhou

Thomas Jay Prins

Lars Naerum

Shenghua Shi

F Ivy Carroll

Larry Kenneth Truesdale

Ulla Grove Sidelmann

Lotte Bjerre Knudsen

Ranjan Jagath Rajapakse

Richard A Bychowski

Tso-sheng Chou

Kimberly Ann Teston

The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4). 

Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same

The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, Rand R, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Inhibitors of Hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same

Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus 

Inhibitors of hepatitis C virus RNA-dependent RNA polymerase

Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.

Glucagon antagonists/inverse agonists

Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.

Non-peptide antagonists of GLP-1 receptor and methods of use

A powerful new anti-convulsant and anti-ischemic pharmaceutical, 5-aminocarbonyl-5H-dibenzo�a,d!cycloheptene-5,10-imine is prepared according to a novel synthesis which converts the starting material, commercially available dibenzosubernone to ADCI without the use of chromatographic purification, hazardous reagents or extreme conditions. The starting material is converted to the corresponding imine through ammonia exposure, and directly converted with acetone cyanohydrin in the presence of sodium cyanide to a 5-amino, 5-cyanocycloheptene intermediate. The intermediate is cyclized using bromine, followed by a reduction of the bromine-carbon bond using sodium cyanoborohydride. The target compound is obtained through selective hydrolysis. An overall yield of 46 percent or better is obtained.

Synthesis of 5-aminocarbonyl-5H-dibenzo�a,d!cyclohepten-5,10-imine

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Oceanside, CA, United States of America

Javier Gonzalez