Cotelle Philippe
Universite de lille 1 - chimie, batiment C3 2eme etage cite scicentifique villeneuve d'ascq 59650, UMR CNRS 8009, France.
Expert Opin Ther Pat. 2009 Jan;19(1):87-93. doi: 10.1517/13543770802603577.
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.
自2007年10月发现MK-0518（拉替拉韦，首个获美国食品药品监督管理局批准的整合酶抑制剂）以来，默克公司的研究人员一直在为与拉替拉韦相关的新型原创杂环申请专利，这些杂环是强效链转移抑制剂。在最近的专利成果中，六氢二氮杂萘并萘啶三酮具有特殊之处，即拥有两种不同的手性来源，也就是一个不对称碳原子和一个呈现阻转异构现象的八元杂环。本专利中所要求保护的不同合成异构体均有描述，并针对其立体异构性对它们的生物学性质进行了评论。
