公开(公告)号：EP0861253A1

公开(公告)日：1998-09-02

申请号：EP96934612.0

申请日：1996-10-10

申请人： GLAXO GROUP LIMITED

发明人： COCKERILL, George, Stuart, Glaxo Wellcome plc ,  GUNTRIP, Stephen, Barry, Glaxo Wellcome plc ,  McKEOWN, Stephen, Carl, 0laxo Wellcome plc ,  PAGE, Martin, John, Glaxo Wellcome plc ,  SMITH, Kathryn, Jane, Glaxo Wellcome plc ,  VILE, Sadie, Glaxo Wellcome plc ,  HUDSON, Alan, Thomas ,  BARRACLOUGH, Paul ,  FRANZMANN, Karl, Witold

IPC分类号： A61K31 ,  A61P7 ,  A61P9 ,  A61P35 ,  A61P43 ,  C07D471 ,  C07D491 ,  C07D495

CPC分类号： C07D471/04 ,  C07D495/04

摘要： 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 R3 is a group ZR4 wherein Z is joined to R4 through a (CH¿2?)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR'), V(CHR) or V where R and R' are each C1-4 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)m or NR?b¿ where Rb is hydrogen or Rb is C¿1-4? alkyl; and R?4¿ is an optionally substituted C¿3-6? cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R?3¿ is a group ZR4 in which Z is NRb, and NR?b and R4¿ 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.