N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDE INHIBITORS OF HIV INTEGRASE

• Main Authors: ORVIETO, FEDERICA, SCARPELLI, RITA, GARDELLI, CRISTINA, PETROCCHI, ALESSIA, PACE, PAOLA, POMA, MARCO, SUMMA, VINCENZO, CRESCENZI, BENEDETTA, MURAGLIA, ESTER, PESCATORE, GIOVANNA, NIZI, EMANUELA, ROWLEY, MICHAEL
• Format: Patent
• Language: English; French
• Published: 01.05.2003
• Edition: 7
• 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

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 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. 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 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. L'invention concerne des 5-hydroxypyrimidin-6-one-4-carboxamides N-substitués représentés par la formule (I) utilisés comme inhibiteurs de l'intégrase du VIH et comme inhibiteurs de la réplication du VIH. R , R , R et R sont définis dans le descriptif. Les composés selon l'invention sont utiles pour prévenir et traiter une infection à VIH et pour prévenir, traiter et retarder l'apparition du SIDA. Ces composés sont utilisés pour lutter contre une infection à VIH et contre le SIDA, en tant que composés en soi, sous la forme de sels pharmaceutiquement acceptables. Ces composés et leurs sels peuvent être utilisés en tant qu'ingrédients dans des compositions pharmaceutiques, combinés éventuellement avec d'autres antiviraux, immunomodulateurs, antibiotiques ou vaccins. L'invention concerne également des méthodes permettant de prévenir, de traiter et de retarder l'apparition du SIDA ainsi que des méthodes permettant de prévenir ou de traiter une infection à VIH.