Université de Lille Nord de France, Chimie Moléculaire et Formulation, Villeneuve d'Ascq , France.
Expert Opin Ther Pat. 2011 Nov;21(11):1799-804. doi: 10.1517/13543776.2011.624272. Epub 2011 Oct 6.
Since the discovery of raltegravir, the first FDA-approved integrase inhibitor, Merck and other pharmaceutical companies have continued their research programs in order to introduce novel molecules as second generation integrase inhibitors. Elvitegravir (Japan Tobacco/Gilead) and dolutegravir (Shionogi/GlaxoSmithKline) are in advanced stages of clinical development. Bristol-Myers Squibb has developed molecules leading to BMS-707035, which was stopped at the Phase II clinical trial stage. Herein is presented the last patent from this company where, in particular, new 3-hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones are synthesized and their biological properties given.
自拉替拉韦（raltegravir）被发现以来，这是首个获得美国食品药品监督管理局（FDA）批准的整合酶抑制剂，默克（Merck）和其他制药公司继续开展他们的研究项目，以推出新型分子作为第二代整合酶抑制剂。艾维雷格（elvitegravir）（日本烟草公司/吉利德公司）和多替拉韦（dolutegravir）（盐野义/葛兰素史克公司）均处于临床开发的后期阶段。百时美施贵宝（Bristol-Myers Squibb）公司开发的分子最终导致了 BMS-707035 的产生，该药在二期临床试验阶段被停止。本文呈现了该公司的最后一项专利，特别是新的 3-羟基-6,7-二氢嘧啶并[2,1-c][1,4]恶嗪-4（9H）-酮的合成及其生物学特性。
