您的位置: 首页 > 农业专利 > 详情页

Analogi 5'-monofosforanu 2',3'-dideoksy-3'-fluorotymidyny (FLTMP), ich zastosowanie oraz farmaceutycznie dopuszczalna forma farmaceutyczna
专利权人:
INSTYTUT BIOCHEMII I BIOFIZYKI POLSKIEJ AKADEMII NAUK
发明人:
MIAZGA AGNIESZKA,AGNIESZKA MIAZGA,ZIEMKOWSKI PRZEMYS&Lstrok,AW,PRZEMYSŁAW ZIEMKOWSKI,KULIKOWSKI TADEUSZ,TADEUSZ KULIKOWSKI,HAMY FRANCOIS,FRANCOIS HAMY,LOUVEL SEVERINE,SEVERINE LOUVEL,KLIMKAIT THOMAS,T,ZIEMKOWSKI PRZEMYSŁAW,THOMAS KLIMKAIT,KLIMKAIT
申请号:
PL391676
公开号:
PL218333B1
申请日:
2010.06.30
申请国别(地区):
PL
年份:
2014
代理人:
摘要:
Analogs of 3'-fluorothymidine 5'-monophosphate (FLTMP), preferably intended 2',3'-dideoxy-3'-fluoro-²-D- erythro -pentofuranoside of thymine 5'-monophosphate (FLTMP): 3'-fluoro-2-thiothymidine 5'-monophosphate intended 2',3'-dideoxy-3'-fluoro-²-D- erythro -pentofuranoside of 2-thiothymine 5'-monophosphate; 3'-fluoro-4-thiothymidine 5'-monophosphate is intended 2',3'-dideoxy-3'-fluoro-²-D- erythro -pentofuranoside of 4-thiothymine 5'-monophosphate (4-SFLTMP). This invention includes also medical use of analogues of 3'-fluorothymidine 5'-monophosphate (FLTMP), according to the invention, Formula 1 , for therapy of infections caused by the human immunodeficiency virus (HIV-1) wild type strain and strains showing resistance and multidrug resistance. The inventors unexpectedly discovered that proposed new FLTMP analogs with thiosubstituent at 2 or 4 position of FLT pyrimidine ring and monophosphate group at 5'-0-of 2,3-dideoxyribose exert very potent inhibitory activity against drug and multidrug resistant HIV-1 strains, as well as show high selectivity and good solubility in water. This invention also includes pharmaceutical acceptable form of drug, which according to the invention, contain known acceptable media and auxiliary substances, containing, as an active compounds analogues of general Formula 1 , in which X , Y and R have the above-mentioned importance, especially the relationship being dilithium salt of 2-SFLTMP and 4-SFLTMP.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充