| 摘要 |
<p>Fused pyrimidines of formula (I); wherein A represents a thiophene or furan ring; nis 1 or 2; R1 is a group of formula (1); wherein m is 0 or 1; R30 isH or C1-C6 alkyl; R4 and R5 form, together withthe N atom to which they are attached, a 5- or 6- membered saturated N-containing heterocyclicgroup which includes 0 or 1 additional heteroatoms selected from N, S and O, whichmay be fused to a benzene ring and which is unsubstituted or substituted; or oneof R4 and R5 is alkyl and the other is a 5- or 6- membered saturatedN-containing heterocyclic group as defined above or an alkyl group which is substitutedby a 5- or 6- membered saturated N- containing heterocyclic group as defined above;R2 is selected from formula (a); wherein R6 and R7 form, togetherwith the nitrogen atom to which they are attached, a morpholine, thiomorpholine,piperidine, piperazine, oxazepane or thiazepane group which is unsubstitutedor substituted; and formula (b); wherein Y is a C2-C4 alkylenechain which contains, be tween constituent carbon atoms of the chain and/or atone or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and whichis unsubstituted or substituted ; and R3 in an indole group which isunsubstituted or substituted ; and the pharmaceutically acceptable salt thereofhave activity as inhibitors of PI3K and may thus be used to treat diseased and disordersarising from abnormal cell growth, function or behaviour associated with PI3kinase such as cancer, immune disorders, cardiovascular disease, viral infection,inflammation, metabolism/endocrine disorders and neurological disorders.Processes for synthesizing the compounds are also described.</p> |
