INHIBIDORES NO NUCLEOSIDICOS DE LA TRANSCRIPTASA INVERSA

• Main Authors: ST-ONGE, MIGUEL, GAUVREAU, DANNY, COTE, BERNARD, LI, CHUN SING, BURCH, JASON, NGUYEN, NATALIE
• Format: Patent
• Language: Spanish
• Published: 28.02.2013
• 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

SE REFIERE A COMPUESTOS DERIVADOS DE 1-[(5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-PIRIDIN-2(1H)-ONA DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C10), CICLOALQUILO(C3-C8) O ARILO; R2 Y R3 SON CADA UNO H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), NO2, CICLOALQUILO(C3-C8), ENTRE OTROS; R4 ES H, ALQUILO(C1-C6), HALOGENO, FLUOROALQUILO(C1-C6), ENTRE OTROS; R5 ES H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: 3-CLORO-5-({1-[(4-METIL-5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-2-OXO-4-(TRIFLUOROMETIL)-1,2-DIHIDROPIRIDIN-3-IL}OXI)BENZONITRILO; 3-CLORO-5-({4-CLORO-1-[(4-METIL-5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-2-OXO-1,2-DIHIDROPIRIDIN-3-IL}OXI)BENZONITRILO; 3-({5-BROMO-4-CLORO-1-[(4-METIL-5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-2-OXO-1,2-DIHIDROPIRIDIN-3-IL}OXI)-5-CLOROBENZONITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA TRANSCRIPTASA INVERSA DEL VIH SIENDO UTILES EN EL TRATAMIENTO DE LA INFECCION POR VIH The invention relates to a pharmaceutical composition comprising an effective amount of the compound: or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and further comprising an effective amount of an anti-HIV agent. The invention further relates to use of said pharmaceutical composition for the prophylaxis or treatment of infection by HIV or for the prophylaxis, treatment, or delay in the onset of AIDS in a subject in need thereof.