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Thieno [3,2-d] pyrimidines as phosphatidylinositol-3-kinase inhibitors for the treatment of cancerous diseases
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
CHUCKOWREE, Irina,FOLKES, Adrian,GOLDSMITH, Paul,HANCOX, Timothy,SHUTTLEWORTH, Stephen
申请号:
ES07732675
公开号:
ES2562935T3
申请日:
2007.05.04
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound that is a condensed pyrimidine of formula (Ia): ** Formula ** wherein: X is S; R2 is a heteroaryl group selected from the following structures (a) to (j): wherein: each W is, independently, -CH or N; Y is N, O or S; and B is a saturated, unsaturated or unsaturated carbocyclic or heterocyclic ring of 5, 6 or 7 members, whose group is unsubstituted or substituted with an R20 group or with alkyl that is unsubstituted or substituted with an R20 group; R20 is selected from hydrogen, halogen, alkoxy, carbocyclyl, a 5- or 6-membered saturated N-containing heterocyclic group as defined above, OH, SR, CN, nitro, NR2, -COOR, -C (O) R, S (O) mR and -CONR2, wherein each R is H, unsubstituted alkyl or C3-C10 cycloalkyl and m is 1 or 2; and R3 is selected from: (a) a group of the following formula: ** Formula ** wherein B is a phenyl ring that is unsubstituted or substituted and Z is selected from H, -OR, -SR, -CH2OR , - CO2R, CF2OH, CH (CF3) OH, C (CF3) 2OH, - (CH2) qOR, - (CH2) qNR2, -C (O) N (R) 2, -NR2, -NRC (O) R , -S (O) mN (R) 2, - OC (O) R, OC (O) N (R) 2, NRS (O) mR, -RC (O) N (R) 2, CN and -NO2 , wherein each R is independently selected from H, C1-C6 alkyl, C3-C10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, the unsubstituted or substituted group being, m is 1 or 2 and q is 0 , 1 or 2; (b) a heteroaryl group containing 1, 2, 3 or 4 ring nitrogen atoms and 0, 1 or 2 additional heteroatoms selected from O and S, said monocyclic or bicyclic group being and being unsubstituted or substituted; and (c) a group comprising a benzene ring that is unsubstituted or substituted and that is fused to a heteroaryl group as defined above; 5 or one of its pharmaceutically acceptable salts.Un compuesto que es una pirimidina condensada de fórmula (Ia):**Fórmula** en donde: X es S; R2 es un grupo heteroarilo seleccionado de las siguientes estructuras (a) a (j): en donde: cada W es, independientemente, -CH o N; Y es N, O o S; y B es un anillo carbocíclico o hetero
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