发明名称 DERIVATIVES OF SUBSTITUTED QUINAZOLINES AND THEIR USING AS TYROSINE KINASE INHIBITORS
摘要 FIELD: organic chemistry, biochemistry, medicine, pharmacy. SUBSTANCE: invention proposes compounds of the formula (I): or their pharmaceutically acceptable salts wherein X represents phenyl ring substituted with halogen atom or dimethylamino-group; Z represents -NH-; each among R1,R3,R4 represents hydrogen atom; R2 is taken among different unsaturated acyl groups enumerated in claim 1 under condition that when R2 is taken among the group consisting of: or then R5 represents independently and solely hydrogen atom, alkyl comprising 1-6 carbon atoms or carboxy-group; X doesn't represent phenyl ring substituted solely with one or some halogen atoms. Compounds are inhibitors of tyrosine kinase and can be used for treatment of cancer and some renal diseases, such as polycystic renal disease. Invention relates also to method for inhibition of biological effect of protein tyrosine kinase with damaged regulation in mammal, treatment or inhibition of tumors growth in mammal, to pharmaceutical composition inhibiting activity of receptor protein tyrosine kinase, epidermal growth factor of cells and to method for preparing compound of the formula (I). EFFECT: valuable medicinal properties of compounds. 20 cl, 5 tbl, 82 ex
申请公布号 RU2227798(C2) 申请公布日期 2004.04.27
申请号 RU20000105243 申请日期 1998.07.29
申请人 UAJT KHOLDINGZ KORPOREJSHN 发明人 VISSNER ALLAN;TSOU KHVEJ-RU;DZHONSON BERNARD DIN;KHAMANN FILIP ROSS;ZANG NAN
分类号 A61K31/505;A61K31/517;A61P13/12;A61P35/00;A61P43/00;C07D239/94;C07D401/12;C07D405/12 主分类号 A61K31/505
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