920036-39-1Relevant articles and documents
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses
Su, Dai-Shi,Lim, John J.,Tinney, Elizabeth,Wan, Bang-Lin,Young, Mary Beth,Anderson, Kenneth D.,Rudd, Deanne,Munshi, Vandna,Bahnck, Carolyn,Felock, Peter J.,Lu, Meiquing,Lai, Ming-Tain,Touch, Sinoeun,Moyer, Gregory,DiStefano, Daniel J.,Flynn, Jessica A.,Liang, Yuexia,Sanchez, Rosa,Perlow-Poehnelt, Rebecca,Miller, Mike,Vacca, Joe P.,Williams, Theresa M.,Anthony, Neville J.
experimental part, p. 7163 - 7169 (2010/06/16)
Biaryl ethers were recently reported as potent NNRTIs. Herein we disclose a detailed SAR study that led to the biaryl ether 6. This compound possessed excellent potency against WT RT and key clinically observed RT mutants and had an excellent pharmacokinetic profile in rats, dogs, and rhesus macaques. The compound also exhibited a clean safety profile in preclinical safety studies.
HIV reverse transcriptase inhibitors
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Page/Page column 58, (2010/11/25)
Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.