Process for the preparation of an HIV integrase inhibitor, WO-2012138670, Gilead Sciences Inc

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,

(2S)-[4-(3,4-Dihydro-2H-chromen-6-yl)-3-quinolinyl][(2-methyl-2-propanyl)oxy]acetic acid

http://en.wikipedia.org/wiki/BI_224436

WO-2012138670

http://worldwide.espacenet.com/publicationDetails/originalDocument?CC=WO&NR=2012138670A1&KC=A1&FT=D&ND=3&date=20121011&DB=EPODOC&locale=en_EP

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