Patented small molecule inhibitors of HIV-1 integrase: a 10-year saga

Validation of integrase as a suitable therapeutic target for the development of drugs against HIV infection; discovery of diketo acid derivatives as bona fide inhibitors of integrase and the recent news of Phase 11 clinical trials with S-1360 are major findings fuelling the recent surge of interest in the development of integrase inhibitors. Herein, the first review of the entire patent literature for small molecule intergrase inhibitors is presented. The emphasis is based on compounds with potential to serve as leads, therefore, no attempt are made to include: antibodies, oligonucleotides or polypeptides.