Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity

專利類型

發明

專利國別 (專利申請國家)

南韓

專利申請案號

10-2010-7006286

專利證號

10-1535691

專利獲證名稱

Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity

專利所屬機關 (申請機關)

中央研究院

獲證日期

2015/07/03

技術說明

「克流感」目前是治療H5N1、H1N1流感患者的唯一口服藥，但抗藥性是其隱憂。我們因此開發兩種新途徑，以木糖或溴苯作為起始物，合成「克流感」和「零流感」（將「克流感」化學結構內的羧酸基團以磷酸基團取代）。與「克流感」同屬流感病毒的神經醯胺酶抑制劑的「零流感」，在酵素活性、保護細胞等實驗上，都顯示比「克流感」效果更好，同時，實驗小鼠服用「零流感」後，也較服用「克流感」者之存活率更高，小鼠恢復體重的情形也較明顯。因此，口服性「零流感」極具開發為流感新藥的潛力。 Influenza remains a major health problem for humans and animals. Tamiflu is an orally administrated anti-influenza drug by inhibiting the activity of neuraminidase (NA). Recent reports on the drug resistant avian flu infections and the side effects in children receiving Tamiflu treatments suggest that new chemical identities for neuraminidase inhibitors are needed for the battle against the threat of the pandemic flu. We have thus discovered two enantioselective synthetic routes to the anti-flu drug Tamiflu, as well as the novel and more potent phosphonate compounds including Tamiphosphor, using D-xylose or bromobenzene as the starting material. Tamiphosphor proves to be more effective due to its higher enzyme inhibition. Survival rates and recovery rates of infected mice treated with Tamiphosphor both show better results. Tamiphosphor has a great potential to become a new orally available anti-influenza drug.

備註

本部(收文號1110010228)同意該校111年2月21日智財字第1111700342號函申請終止維護專利(中央研究院)

連絡單位 (專責單位/部門名稱)

智財技轉處

連絡電話

02-2787-2508

網址