HIDROXIPIRIMIDINA CARBOXAMIDAS N-SUSTITUIDAS INHIBIDORAS DE HIV INTEGRASA

• Main Authors: CRESCENZI, BENEDETTA IRBM, NIZI, EMANUELA IRBM, GARDELLI, CRISTINA IRBM, ORVIETO, FEDERICA IRBM, MURAGLIA, ESTER IRBM, PACE, PAOLA IRBM
• Format: Patent
• Language: Spanish
• Published: 01.09.2006
• Edition: 4
• 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

Un compuesto de **fórmula** en la que R1 es (1) ¿H, (2) -alquilo C1-6, que opcionalmente está sustituido con uno o más sustituyentes, cada uno de los cuales es, independientemente, halógeno, -OH, -CN, -O-alquilo C1-6, -O-haloalquilo C1-6, -C(=O)Ra, -CO2Ra, -SRa, - S(=O)Ra, -N(RaRb), -C(=O)-alquilo C0-6-N(RaRb), N(Ra)- C(=O)alquilo C0-6-N(RbRc), -SO2Ra, -N(Ra)SO2Rb, - SO2N(RaRb), -N(Ra)-C(=O)Rb, o ¿N(Ra)C(=O)C(=O)N(RaRb), (3) -Rk, (4) ¿alquilo C1-6 ¿Rk, en el que el alquilo opcionalmente está sustituido con uno o más sustituyentes, cada uno de los cuales es, independientemente, halógeno, -OH, -CN, -O- alquilo C1-6, -O-haloalquilo C1-6, -N(RaRb), - N(Ra)CO2Rb, -N(Ra)C(=O) -alquilo C0-6-N(RbRc) o ¿N(Ra)-alquilo C2-6-OH, con la condición de que ¿OH no esté unido al carbono alfa a N(Ra); o una de sus sales farmacéuticamente aceptable. N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: 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.