US2012258966A1PendingUtilityA1
Pharmaceutical compounds
Est. expiryOct 25, 2024(expired)· nominal 20-yr term from priority
Inventors:Stephen Joseph ShuttleworthAdrian FolkesIrina ChuckowreeNan Chi WanTimothy C. HancoxStewart J. BakerSukhjit SohalMohammed A. Latif
A61P 43/00A61P 37/02A61P 5/00A61P 35/00A61P 37/00A61P 3/04A61P 9/00A61P 3/10A61P 31/12A61P 35/02C07D 495/04A61P 29/00A61P 3/00A61P 25/00C07D 491/04A61K 31/519
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Claims
Abstract
Fused pyrimidines of formula (I): wherein R 1 -R 3 , A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
Claims
exact text as granted — not AI-modified1 . A method of treating a disease or disorder arising from abnormal cell growth, function or behavior associated with PI3 kinase, which method comprises administering to a patient in need thereof a compound which is a fused pyrimidine of formula (I):
wherein
A represents a thiophene or furan ring;
n is 1 or 2;
R 1 is a group of formula:
wherein
m is 0 or 1;
R 30 is H or C 1 -C 6 alkyl;
R 4 and R 5 form, together with the N atom to which they are attached, a 5- or 6-membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R 4 and R 5 is alkyl and the other is a 5- or 6-membered saturated N-containing heterocyclic group as defined above or an alkyl group which is substituted by a 5- or 6-membered saturated N-containing heterocyclic group as defined above;
R 2 is selected from:
wherein R 6 and R 7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane or thiazepane group which is unsubstituted or substituted; and
wherein Y is a C 2 -C 4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted;
and R 3 is an indazole group which is unsubstituted or substituted;
or a pharmaceutically acceptable salt thereof.Cited by (0)
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