New hexahydrodiazocino-naphthyridine triones as HIV-1 integrase inhibitors: WO2008048538 A1

Abstract

Since the discovery of MK-0518 (raltegravir, the first FDA-approved integrase inhibitor) in October 2007, Merck Co. researchers have continued to patent original new heterocycles related to raltegravir as powerful strand transfer inhibitors. Among the most recent patented works hexahydrodiazocino-naphthyridinetriones present the particularity to possess two different sources of chirality, that is, an asymmetric carbon and a heterocyclic eight-membered ring presenting atropisomerism. The different synthesized isomers claimed in this patent are described and their biological properties commented on in relation to stereoisomerism.

Keywords::

• AIDS
• diazocinonaphthyridinetriones
• HIV-1 integrase
• strand transfer inhibition