PYRIDINONE DIKETO ACIDS: INHIBITORS OF HIV REPLICATION IN COMBINATION THERAPY

• Main Authors: CHI, GUOCHEN, UCHIL, VINOD R, SEO, BYUNG I, NAIR, VASU
• Format: Patent
• Language: English; French
• Published: 24.01.2008
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV integrase, is de scribed. These compounds are useful in the prevention or treatment of infect ion by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carr iers, used alone or in combination with antivirals, immunomodulators, antibi otics, vaccines, and other therapeutic agents, especially other anti-HIV com pounds (including other anti-HIV integrase agents), which can be used to cre ate combination anti-HIV cocktails. Methods of treating AIDS and ARC and met hods of treating or preventing infection by HIV are also described. Compound s of the present application include those of formula I and include tautomer s, regioisomers, geometric isomers, and pharmaceutically acceptable salts th ereof, wherein the pyridinone scaffold and R groups are as otherwise defined in the specification. These are combined, with any number of typical other anti-HIV agents (including other integrase-based anti-HIV agents) and other combination therapeutic agents described herein, to provide an effective tre atment modality for HIV infections, including AIDS and ARC.