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PYRIMIDINE DERIVATIVES, CHARACTERISED BY ANTIPROLIFERATIVE ACTIVITY, AND PHARMACEUTICAL COMPOSITION

机译:嘧啶衍生物,具有抗增殖活性和药物成分

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to new pyrimidine derivatives of formula I and their pharmaceutically acceptable salts, which are selective inhibitors of kinases KDR, FGFR and PDGFR and can be used for treatment of oncological diseases. Compound of formula I corresponds to structural formula , where R1 is selected from group, including H, COR4 and COOCHR5OCOR4; R2 and R3 are independently selected from group, including C1-6alkyl, C1-6alkyl, substituted with not more than 4 groups, which are independently selected from group, including -NR5R6,-R5, -OR5-phenyl,-phenyl, substituted with not more than 2 groups, which are independently selected from group, including OR5 and -C1-4alkyl and heteroaryl, representing aromatic heterocyclic ring system, which contains not more than two rings and includes from 1 to 3 nitrogen atoms, and heterocyclyl, representing saturated cyclic radical, which includes from 1 to 3 nitrogen atoms; R5 and R6 are independently selected from group H and C1-5alkyl. Invention also relates to pharmaceutical compositions, containing said compounds of formula I and intermediate products.;EFFECT: obtaining new pyrimidine derivatives, which can be used for treating oncological diseases.;17 cl, 2 tbl, 27 ex
机译:发明领域本发明涉及式I的新嘧啶衍生物及其药学上可接受的盐,它们是激酶KDR,FGFR和PDGFR的选择性抑制剂,可用于治疗肿瘤疾病。式I的化合物对应于结构式,其中R 1 选自H,COR 4 和COOCHR 5 OCOR 4 。 R 2 和R 3 独立地选自C 1-6 烷基,C 1-6 烷基,被不超过4个基团取代,独立地选自-NR 5 R 6 ,-R 5 ,- OR 5 -苯基,-苯基,被不超过2个基团取代,这些基团独立选自OR 5 和-C 1-4 <代表芳族杂环系统的烷基和杂芳基,其包含不超过两个的环并包含1至3个氮原子;以及杂环基,其代表饱和的环状基团,其包含1至3个氮原子; R 5 和R 6 独立地选自基团H和C 1-5 烷基。本发明还涉及包含所述式I化合物和中间产物的药物组合物;效果:获得新的嘧啶衍生物,其可用于治疗肿瘤疾病。17 cl,2 tbl,27 ex

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