GAMMA-HIDROXI-2-(FLUOROALQUILAMINOCARBONIL)-1-PIPERAZINAPENTANAMIDAS COMO INHIBIDORES DE PROTEASA DEL VIH

• Main Authors: ZHANG FENGQI, KIRK BRIAN ANTHONY, RAGHAVAN SUBHAREKHA, KEVIN NANCY J, TATA JAMES R, CHAPMAN KEVIN T, CHENG YUAN, RANO THOMAS A, DUFFY JOSEPH LESLIE, LU ZHIJIAN, HUENING TRACY
• Format: Patent
• Language: Spanish
• Published: 12.10.2001
• Edition: 7
• Subjects: APPARATUS THEREFOR; BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; GENERAL METHODS OF ORGANIC CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; VINEGAR; WINE

SE REFIERE A PIPERAZINA 2 CARBOXAMIDO SUSTITUIDAS DE FORMULA I DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, CICLOALQUILO C3-C6, ENTRE OTROS; R2 Y R3 SON H, ALQUILO C1-C4 O JUNTO A C FORMAN CICLOALQUILO C3-C6; R4 ES ALQUILO C1-C6, CICLOALQUILO, ARILO, HETEROARILO, ENTRE OTROS; R5 ES CARBOCICLICO, HETEROCICLO, ENTRE OTROS; R6 ES ALQUILO C1-C6 FLUORADO; Ra Y Rb SON ALQUILO C1-C4 O JUNTO A N FORMAN AZACICLOALQUILO C3-C6. UN COMPUESTO PREFERIDO ES (OR,þS,2S)-N-((3S,4S)-3,4-DIHIDRO-3-HIDROXI-2H-1-BENZOPIRAN-4-IL)-4-(1-FLUORO[3,2-c]-PIRIDIN-2-IL-1-METILETIL)-þ-HIDROXI-O-(FENILMETIL)-2-[[(2,2,2-TRIFLUOROETIL)AMINO]CARBONIL]-1-PIPERAZINAPENTANAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A COMPOSICIONES QUE COMPRENDEN ADEMAS AGENTES ANTIVIRALES DE VIH/SIDA, INMUNOMODULADORES, AGENTES ANTIINFECCIOSOS, INHIBIDORES DE TRANSCRIPTASA INVERSA NUCLEOSIDO Y NO NUCLESIDO, INDINAVIR, RITONAVIR. EL COMPUESTO I ES UN INHIBIDOR DE PROTEASA DEL VIH gamma-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.