New hexahydrodiazocino-naphthyridine triones as HIV-1 integrase inhibitors: WO2008048538 A1.
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.
Cotelle
Philippe
P
Universite de lille 1 - chimie, batiment C3 2eme etage cite scicentifique villeneuve d'ascq 59650, UMR CNRS 8009, France. philippecotelle@univ-lille1.fr
D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy* / Q000503:physiopathology; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009287:Naphthyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010330:Patents as Topic; D011760:Pyrrolidinones / Q000494:pharmacology; D000068898:Raltegravir Potassium; D013237:Stereoisomerism
D019428:HIV Integrase Inhibitors; D009287:Naphthyridines; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium