发明公开
EP2402356A3 Modified 2',3'-dideoxynucleosides for treatment infections caused by human immunodeficiency virus (HIV) multidrug resistant strains, method of their synthesis and the pharmaceutical agent containing these nucleosides
审中-公开
它们的合成和药物包含已修饰的2”，3'-二脱氧核苷造成的耐人类免疫缺陷病毒的多种药物株（HIV）感染的治疗方法，这些核苷
- 专利标题： Modified 2',3'-dideoxynucleosides for treatment infections caused by human immunodeficiency virus (HIV) multidrug resistant strains, method of their synthesis and the pharmaceutical agent containing these nucleosides
- 专利标题（中）： 它们的合成和药物包含已修饰的2”，3'-二脱氧核苷造成的耐人类免疫缺陷病毒的多种药物株（HIV）感染的治疗方法，这些核苷
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申请号： EP10172854.1申请日： 2010-08-15
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公开(公告)号： EP2402356A3公开(公告)日： 2012-07-18
- 发明人: ZIEMKOWSKI, Przemyslaw , MIAZGA, Agnieszka , KULIKOWSKI, Tadeusz , KLIMKAIT, Thomas , LOUVEL, Severine , HAMY, Francois , Lipniacki, Andrzej , PIASEK, Andrzej
- 申请人： Instytut Biochemii I Biofizyki Pan
- 申请人地址： Ul. Pawinskiego 5A 02-106 Warszawa PL
- 专利权人： Instytut Biochemii I Biofizyki Pan
- 当前专利权人： Instytut Biochemii I Biofizyki Pan
- 当前专利权人地址： Ul. Pawinskiego 5A 02-106 Warszawa PL
- 代理机构： Brodowska, Iwona
- 优先权： PL39169410 20100630
- 主分类号： C07H19/073
- IPC分类号： C07H19/073 ; A61K31/7068 ; A61P31/18
摘要：
2',3'-Dideoxy-3'-fluoro-4-thiothymidine (4-SFLT) derivatives according to the invention substituted at 5'-O position of 4-SFLT with 12-tetradodecanoyl, 12-bromododecanoyl, 12-metoxydodecanoyl, 12-ethylothiododecanoyl, 11-ethylothioundecanoyl or 12-azidodocanoyl group (represented by the symbols WA18, WA19, WA21,WA22,WA23 and WA20 in the deCIPhR™ cell system exert high antiviral activity against wild type HIV-1 strain, as well as against its drug and multidrug resistant strains, and moreover very low citotoxicity (CC 50 > 200 µM) and very high selectivity.
The compounds, because of lack of toxicity may be applied at all AIDS phases i.e. also them the T4 lymphocytes level in patients drops down below 200/ µL of peripheral blood.
2',3'-Dideoxy-3'-fluoro-4-thiothymidine derivatives according to the invention are synthesized by the transformation of the known compound 2',3'-dideoxy-3'-fluoro-4-thiothymidine (4-SFLT).
The compounds, because of lack of toxicity may be applied at all AIDS phases i.e. also them the T4 lymphocytes level in patients drops down below 200/ µL of peripheral blood.
2',3'-Dideoxy-3'-fluoro-4-thiothymidine derivatives according to the invention are synthesized by the transformation of the known compound 2',3'-dideoxy-3'-fluoro-4-thiothymidine (4-SFLT).
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