N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase

N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula I: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, dela...

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Main Authors MURAGLIA ESTER, SUMMA VINCENZO, GARDELLI CRISTINA, ROWLEY MICHAEL, PESCATORE GIOVANNA, NIZI EMANUELA, ORVIETO FREDERICA, PETROCCHI ALESSIA, SCARPELLI RITA, CRESCENZI BENEDETTA, PACE PAOLA, POMA MARCO
Format Patent
LanguageChinese
English
Published 19.10.2011
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula I: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are 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 ascompounds 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 otherantivirals, 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.
Bibliography:Application Number: CN201110092480