Southern Research Institute

Merck Sharp + Dohme Corp.

Anita T Fowler

John A Secrist, Iii

F George Njoroge

Frank W Bennett

Ashok Arasappan

Subramaniam Ananthan

Joseph A Maddry

Robert C Reynolds

Hollis S Kezar, Iii

Cecil D Kwong

Abhijit Roychowdhury

Neng-Yang Shih

John J Piwinski

John A Montgomery

Srikanth Venkatraman

Vinay M Girijavallabhan

Francisco Velazquez

Feng Geng

Vishal Verma

Yuhua Huang

Jeremy Clark

Joseph A Kozlowski

Ling Tong

Malcolm Maccoss

Bandarpalle B Shankar

Seong Heon Kim

Regina Huelgas

John A Iii Secrist

Hollis S Iii Kezar

George F Njoroge

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 

Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections

2-Chloro-9-(2-deoxy-2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

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2-Chloro-9-(2-deoxy-2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

Method for synthesizing 2-chloro-9-(2-fluoro-&#x3b2;-D-arabinofuranosyl)-9H-purin-6-amine

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Irondale, AL, United States of America

Anita T Fowler