Gilead Sciences, Inc.

Schering-plough Animal Health Corporation

Lee Shun Chong

William John Watkins

Jennifer R Zhang

Aesop Cho

Thorsten A Kirschberg

James Ming Chen

Maria Fardis

Xiaowu Chen

Hyung-Jung Pyun

Adrian S Ray

Carina E Cannizzaro

Richard L Mackman

Sundaramoorthi Swaminathan

Choung U Kim

Christopher P Lee

David A Oare

Constantine G Boojamra

Alan X Huang

Steven Cesar Alfons De Jonghe

William A Lee

David Y Markevitch

Vidya K Prasad

Ralph F Hirschmann

Haolun Jin

Edward Doerffler

Manoj C Desai

Scott E Lazerwith

Peter H Nelson

Eda Y Canales

Michael O'Neil Hanrahan Clarke

Qi Liu

Willard Lew

Piet André Maurits Maria Herdewijn

Ling-Jie Gao

Rosemarie Sherlock

Kuei-Ying Lin

Philip Anthony Morganelli

Steven H Krawczyk

Michael Mertzman

Lijun Zhang

Steven S Bondy

Michael O' Neil Hanrahan Clarke

Craig S Gibbs

Piet Andre Maurits Maria Herdewijn

Rosemarie O'Shea

Michael Graupe

Scott J Hecker

Hong Yang

Michael L Mitchell

Randall Halcomb

Tomasz W Glinka

Chien-hung Chou

Dale Edward Shuster

Randall L Halcomb

Daniel B Tumas

Ruchika Mishra

Piet AndréMaurits Maria Herdewijn

Hans C Reiser

Brian Gallagher

Hans Reiser

Hong Ye

Sundaramoorthi Swaninathan

Michael O'neil Clarke

Michael O'neil Hanrahan Clarke

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: Ris hydrogen, NR'R″, Calkyl, arylCalkyl or Ccycloalkyl; Ris amino, Calkyl, Calkenyl, Ccycloalkyl, Ccycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted Calkyl or Ccycloalkyl-Calkyl; Ris hydrogen or Calkyl, or Rand Rtogether with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, Calkylene, Calkenylene or Calkynylene; Ris halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, Calkyl-carbonyl or Calkyl; provided that Ris not phenyl substituted with morpholino when Ris H and Ris H, and provided that when NRRis piperazinyl, said NRRis either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: Ris hydrogen, NR'R&#x2033;, Calkyl, arylCalkyl or Ccycloalkyl; Ris amino, Calkyl, Calkenyl, Ccycloalkyl, Ccycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted Calkyl or Ccycloalkyl-Calkyl; Ris hydrogen or Calkyl, or Rand Rtogether with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, Calkylene, Calkenylene or Calkynylene; Ris halogen, heteroaryl or aryl; R&#x2032; and R&#x2033; are each independently hydrogen, Calkyl-carbonyl or Calkyl; provided that Ris not phenyl substituted with morpholino when Ris H and Ris H, and provided that when NRRis piperazinyl, said NRRis either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

Substituted pteridines useful for the treatment and prevention of viral infections

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Antiviral phosphonate analogs

Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

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Inhibitors of flaviviridae viruses

Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I): wherein:

Pyrido(3,2-d)pyrimidines useful for treating viral infections

This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: Ris selected from the group consisting of hydrogen, NR'R&#x2033; and Calkyl; &#x2014;A is selected from the group consisting of a bond, O, S(O), Calkylene, Calkenylene and Calkynylene; Ris selected from the group consisting of Calkyl, Calkenyl, Ccycloalkyl, Ccycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; &#x2014;Y is selected from the group consisting of a single bond, Calkylene, Calkenylene, and Calkynylene; n is 0, 1 or 2; and Ris selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-&#x39b;/-oxide, a solvate or a pro-drug thereof.

4,6-di- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections

This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: Ris amino, Ris hydrogen, and Rand Rtogether provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.

Pyrido(3,2-d)pyridmidines useful for treating viral infections

Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (Ia): wherein, R, Rand Rare defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, for use in the treatment of hepatitis C. 

2,4,6-trisubstituted pyrido(3,2-d)pyrimidines useful for treating viral infections

Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections. 

Growing community of inventors

Newark, CA, United States of America

Lee Shun Chong