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PYRIDINE 2,3-d PYRIMIDINE DERIVATIVES AS SELECTIVE KDR AND FGFR INHIBITORS

机译:吡啶[2,3-d]嘧啶衍生物作为选择性KDR和FGFR抑制剂

摘要

FIELD: chemistry, pharmaceutics.;SUBSTANCE: invention relates to novel derivatives of pyridine [2,3-d] pyrimidine of general formula (I) and their pharmaceutically acceptable salts, which possess properties of KDR and FGFR inhibitors. Compounds can be applied to produce medications for treatment of cancer, for instance, of mammary gland, large intestine, lungs and prostate gland. In general formula (I) , Ar and Ar' independently on each other are selected from group that includes phenyl; phenyl substituted with 1-3 substituents selected from group C1-C4alkyl, hydroxy, halogen, halogen-substituted C1-C4alkyl, C1-C4alkoxy; 6-member nitrogen-containing heteroaryl and 6-member nitrogen-containing heteroaryl substituted with C1-C4alkoxygroup, on condition that Ar standing for heteroaryl does not represent 2-pyridyl, and standing for substituted heteroaryl does not represent substituted 2-pyridyl, R1 is selected from group including phenyl, C1-C10alkyl, C1-C10alkyl independently containing substituents selected from group that includes phenyl, C3-C6cycloalkyl. Invention also relates to intermediate compounds for compounds of general formula (I) and to pharmaceutical compositions.;EFFECT: obtaining derivatives and their pharmaceutically acceptable salts which possess properties of selective KDR and FGFR inhibitors.;21 cl, 2 tbl, 20 ex
机译:发明领域本发明涉及具有KDR和FGFR抑制剂性质的通式(I)的吡啶[2,3-d]嘧啶的新型衍生物及其药学上可接受的盐。该化合物可用于生产用于治疗例如乳腺,大肠,肺和前列腺的癌症的药物。在通式(I)中,,彼此独立地从组中选择Ar和Ar'包括苯基;被1-3个选自C 1 -C 4 烷基的取代基取代的苯基,羟基,卤素,被卤素取代的C 1 -C < Sub> 4 烷基,C 1 -C 4 烷氧基;在Ar代表杂芳基不表示2-的条件下,被C 1 -C 4 烷氧基取代的6元含氮杂芳基和6元含氮杂芳基吡啶基,并且代表取代的杂芳基不代表取代的2-吡啶基,R 1 选自苯基,C 1 -C 10 烷基,C 1 -C 10 烷基独立地包含选自以下的取代基,所述取代基包括苯基,C 3 -C 6 环烷基。本发明还涉及通式(I)的化合物的中间体化合物和药物组合物。效果:获得具有选择性KDR和FGFR抑制剂特性的衍生物及其药学上可接受的盐。21 cl,2 tbl,20 ex

著录项

  • 公开/公告号RU2345077C2

    专利类型

  • 公开/公告日2009-01-27

    原文格式PDF

  • 申请/专利权人 F.KHOFFMANN-LJA ROSH AG;

    申请/专利号RU20050122901

  • 发明设计人 LJU TSZINTSZUN (US);LJUK KINCHUN (US);

    申请日2003-12-11

  • 分类号C07D471/04;C07D239/30;C07D239/48;C07D401/08;A61K31/519;A61P35;

  • 国家 RU

  • 入库时间 2022-08-21 19:10:44

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