Gilead Sciences, Inc.

4 Aza Bioscience Nv

Steven Cesar Alfons De Jonghe

William John Watkins

Lee Shun Chong

Piet André Maurits Maria Herdewijn

Ling-Jie Gao

Piet Andre Maurits Maria Herdewijn

Jennifer R Zhang

William A Lee

Wolfgang Pfleiderer

Steven S Bondy

Mark Jozef Albert Waer

Piet AndréMaurits Maria Herdewijn

Arnaud Didier Marie Marchand

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

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

This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C. 

Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections

Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C.

Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for treating hepatitis C

This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro-derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

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Brussels, Belgium

Steven Cesar Alfons De Jonghe