Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Cameron Cowden

Antony John Davies

Leslie Joseph Street

Jose Luis Castro Pineiro

William Robert Carling

Andrew Madin

Feng Xu

Chunhua Yang

Ian Frank Cottrell

Stephen Philip Keen

J Michael Williams

David R Lieberman

Brian Christopher Bishop

Gavin William Stewart

Marjorie See Waters

Karel Marie Joseph Brands

Daniel J Rush

James Francis McCabe

Gareth Edward Pearce

V Brett Cooper

Patricia Frech

Matthew M Bio

Kimberly A Petrillo

A process is provided for the preparation of branched-chain ribonucleosides of formula (I): from the 1,2-anhydroderivatives of formula (II). wherein PG is a hydroxyl protecting group, B is a purine or pyrimidine nucleobase, and Ris Calkyl. The compounds of formula (I) are inhibitors of HCV polymerase useful in the treatment of HCV infection.

Process for preparing branched ribonucleosides from 1,2-anhydroribofuranose intermediates

The present invention relates to the synthesis of intermediates for the preparation of compounds of formula (A): wherein n is 2 or 3 and various salt forms of these compounds. The compounds of formula (A) are useful as &#x3b1;&#x3bd;&#x3b2;3 receptor antagonists 

&#x3b1; v integrin receptor antagonists

7-(1,1 -Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo&lsqb;4,3-b&rsqb;pyridazine, and pharmaceutically acceptable salts thereof are selective ligands for GABA receptors useful in the treatment of disorders of the central nervous system.

Substituted triazolo-pyridazine derivative, pharmaceutical compositions made therefrom

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline Anhydrous Form B, 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type A Monohydrate, and 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type B monohydrate, or a pharmaceutically acceptable salt thereof.

Pyrazinone thrombin inhibitors

Growing community of inventors

Hoddesdon, United Kingdom

Cameron Cowden