Process for the preparation of an HIV integrase inhibitor, WO-2012138670, Gilead sciences inc
Li, Wenjie; De Croos, Philomen; Fandrick, Keith, R.; Gao, Joe, Ju; Haddad, Nizar; Lu, Zhi-Hui; Qu, Bo; Rodriguez, Sonia; Senanayake, Chris, H.; Zhang, Yongda; Tang, Wenjun, PUB 11 OCT 2012, Drug BI-224436 ((Tentative))
GILEAD, under license from BOERINGER ING, is developing BI-224436, a HIV-1 non-catalytic site integrase inhibitor, for the potential oral treatment of HIV infection . By September 2011, BI-224436 had been advanced into phase I trials .
BI 224436 is an investigational new drug under development for the treatment of HIV infection. BI 224436 is the first non-catalytic site integrase inhibitor (NCINI). It inhibits HIV replication via binding to a conserved allosteric pocket of the HIV integrase enzyme. This makes the drug distinct in mechanism of action compared to raltegravir and elvitegravir,