Celltech Therapeutics Limited

David Festus Moffat

Peter David Davis

Jeremy Martin Davis

Mark James Batchelor

Martin Clive Hutchings

David Mark Parry

Fused polycyclic 2-aminopyrimidines of formula (1) are described: wherein

Fused polycyclic 2-aminopyrimidine derivatives

Compounds of general formula (1) ##STR1## are described wherein: Ar is an optionally substituted aromatic group;

2-Pyrimidineamine derivatives and processes for their preparation

Compounds of general formula (1): ##STR1## are described wherein Het is an optionally substituted heteroaromatic group; R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group; R.sup.2 is a hydrogen or halogen atom or a group --X.sup.1 --R.sup.2a where X.sup.1 is a direct bond or a linker atom or group, and R.sup.2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.3 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.

Substituted 2-pyrimidineamines and processes for their preparation

Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;

Compounds of formula (1) are described: ##STR1## and the salts, solvates, hydrates and N-oxides thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.

Substituted 2-anilinopryimidines useful as protein kinase inhibitors

2-Anilinopyrimidines, processes for their preparation, pharmaceutical compositions containing them, their use in medicine. In a preferred embodiment, the compounds have the general formula (1): ##STR1## wherein R.sup.1 is preferably methoxy; R.sup.2 and R.sup.3 are preferably methyl; R.sup.4 is preferably a hydrogen atom; R.sup.5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.6 is a hydrogen or halogen atom or an amino (--NH.sub.2), substituted amino, nitro, carboxyl (--CO.sub.2 H), esterified carboxyl or --X.sup.1 R.sup.6a where X.sup.1 is a direct bond or a linker atom or group and R.sup.6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom or group; and R.sup.7 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group. Compounds of the invention are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, p59.sup.fyn, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.

Substituted 2-anilinopyrimidines useful as protein kinase inhibitors

Compounds of general formula (1) are described: ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;

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Maidenhead, United Kingdom

David Festus Moffat