| 摘要 |
Pyrimidines of formula (1) are described, wherein R1 is a -XR6 group; R2 and R3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, -OH, -OR10 [where R10 is an optionall y substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic , aromatic or heteroaromatic group] -SH, -NO2, -CN, -SR10, -COR10, S(O)R10, - SO2R8, -SO2N(R8)(R9), -CO2R8, -CON(R8)(R9), -CSN(R8)(R9), -NH2 or substitute d amino group; R4 is a X1R11 group where X1 is a covalent bond or a -C(R12)(R1 3)- [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alky l or haloalkyl group] or -C(O)- group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R5 is a halogen atom or an alkynyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis.
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