| 简介 |
FIELD : chemistry.SUBSTANCE : invention relates to pyrido[3, 4-d]pyrimidine compounds of formula (III), having Pan-erbB kinase inhibiting properties. In the compound of formula, where X is a halide, (1) Ris H, and (a) Ris (3-chlorobenzyl)oxy- and Ris chloro; (b) Rand R, together with the carbon atom with which they are bonded, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) Ris 2-pyridinylmethoxy and Ris chloro; (d) Rand Rare both chloro; (e) Ris chloro and Ris bromo; (f) Rand Rare both bromo; (g) Ris fluoro and Ris ethynyl; (h) Ris chloro and Ris ethynyl; (i) Ris bromo and Ris ethynyl; (j) except in cases when Ris in position 3 coupled with Rin position 4, Ris bromo and Ris fluoro; (k) Ris 2-pyridinylmethoxy and Ris fluoro; or (1) Ris 2-pyridinylmethoxy and Ris bromo; or (2) at least one of R, Rand Ris selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy, and when at least one of R, Rand Ris not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the rest is independently selected from H, halogen and C-Calkynyl, under the condition that when one of R, Rand Ris benzyloxy 2-pyridinylmethoxy, the other two of R, Rand Rmay not be H; or (3) two of R, Rand R, together with carbon atoms with which they are bonded, form 1-(3-fluorobenzyl)-1H-pyrazole, and the rest is selected from H, halogen and C-Calkynyl; Ris selected from H, methyl, ethyl, trifluoromethyl, -CN, -CONHand propyn-1-yl, and Ris C-Calkyl.EFFECT : compounds can be used in treating cancer, which is mediated by the activity of said kinase.12 cl, 16 dwg, 6 tbl |
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