Patent Number: 6,169,091

Title: Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

Abstract: Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R.sup.3 is a group ZR.sup.4 wherein Z is joined to R.sup.4 through a (CH.sub.2)p group in which p is 0, 1, or 2 and Z represents a group V(CH.sub.2), V(CF.sub.2), (CH.sub.2)V, (CF.sub.2)V, V(CRR'), V(CHR) or V where R and R' are each C.sub.1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O).sub.m or NR.sup.b where R.sup.b is hydrogen or R.sup.b is C.sub.1-4 alkyl; and R.sup.4 is an optionally substituted C.sub.3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R.sup.3 is a group ZR.sup.4 in which Z is NR.sup.b, and NR.sup.b and R.sup.4 together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors. The compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer. ##STR1##

Inventors: Cockerill; George Stuart (Stevenage, GB), Guntrip; Stephen Barry (Stevenage, GB), McKeown; Stephen Carl (Stevenage, GB), Page; Martin John (Abingdon, GB), Smith; Kathryn Jane (Stevenage, GB), Vile; Sadie (Stevenage, GB), Hudson; Alan Thomas (Otford, GB), Barraclough; Paul (Maidstone, GB), Franzmann; Karl Witold (London, GB)

Assignee: Glaxo Wellcome Inc.

International Classification: C07D 471/00 (20060101); C07D 495/04 (20060101); C07D 495/00 (20060101); C07D 471/04 (20060101); C07D 487/04 (); A61K 031/4745 ()

Expiration Date: 01/02/2018