SMEJLL Dzheffri Brjus (NZ),СМЕЙЛЛ Джеффри Брюс (NZ),PATTERSON Adam Vorn (NZ),ПАТТЕРСОН Адам Ворн (NZ),LU Go-Ljan (NZ),ЛУ Го-Лян (NZ),LI Kho Khuat (NZ),ЛИ Хо Хуат (NZ),AShOORZADEKh Amir (NZ),АШООРЗАДЕХ,SMEJLL DZHEFFRI BRJUS,СМЕЙЛЛ Джеффри Брюс,PATTERSON ADAM VORN,ПАТТЕРСОН Адам Ворн,LU GO-LJAN,ЛУ Го-Лян,LI KHO KHUAT,ЛИ Хо Хуат,ASHOORZADEKH AMIR,АШООРЗАДЕХ Амир,ANDERSON ROBERT FORBZ,АНДЕРСОН Роберт Ф
申请号：
RU2012112396/04
公开号：
RU0002568639C2
申请日:
2010.09.02
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
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) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy- and R3 is chloro； (b) R2 and R3, together with the carbon atom with which they are bonded, form 1-(3-fluorobenzyl)-1H-pyrazole； (c) R2 is 2-pyridinylmethoxy and R3 is chloro； (d) R2 and R3 are both chloro； (e) R2 is chloro and R3 is bromo； (f) R2 and R3 are both bromo； (g) R2 is fluoro and R3 is ethynyl； (h) R2 is chloro and R3 is ethynyl； (i) R2 is bromo and R3 is ethynyl； (j) except in cases when R2 is in position 3 coupled with R3 in position 4, R2 is bromo and R3 is fluoro； (k) R2 is 2-pyridinylmethoxy and R3 is fluoro； or (1) R2 is 2-pyridinylmethoxy and R3 is bromo； or (2) at least one of R1,R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy, and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the rest is independently selected from H, halogen and C2-C4alkynyl, under the condition that when one of R1, R2 and R3 is benzyloxy 2-pyridinylmethoxy, the other two of R1, R2 and R3 may not be H； or (3) two of R1, R2 and R3, together with carbon atoms with which they are bonded, form 1-(3-fluorobenzyl)-1H-pyrazole, and the rest is selected from H, halogen and C2-C4alkynyl； R4 is selected from H, methyl, ethyl, trifluoromethyl, -CN, -CONH2 and propyn-1-yl, and R5 is C1-C6alkyl.EFFECT: compounds can be used in treating cancer, which is mediated by the activity of said kinase.12 cl, 16 dwg, 6 tblИзобретение относится к пиридо[3,4-d]пиримидиновым соединениям формулы (III), обладающим свойствами ингибитора киназы Pan-erbB. Соединения могут быть использованы при лечении рака, опосредованного активностью указанной киназы. В соединенииформулы (III), где X представляет собой галогенид, (1) R1 представляет собой Н, и (a) R2 представляет собой (3-хлорбензил)о
