Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Merck Sharp + Dohme Corp.

Istituto Di Ricerche Di Biologia P. Angeletti S.p.a.

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.r.l.

Barbara Pacini

Cristina Gardelli

Steven Harper

Maria Emilia Di Francesco

Vincenzo Summa

Alessia Petrocchi

Frank Narjes

Marco Poma

Paola Pace

Emanuela Nizi

Victor Giulio Matassa

Malte Meppen

Ester Murgalia

Malcolm MacCoss

Philippe L Durette

David Brian Olsen

Monica Donghi

The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I). 

Nucleoside cyclic phosphoramidates for the treatment of RNA-dependent RNA viral infection

The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention. 

Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection

4,5-Dihydroxypyrimidine-6-carboxamides of formula:  are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R, R, Rand Rare defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Dihydroxypyrimidine carboxamide inhibitors of HIV integrase

4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R, R, Rand Rare defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described 

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Rome, Italy

Barbara Pacini