Claims for Patent: 6,727,256

Summary for Patent: 6,727,256

Title:	Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
Abstract:	Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHCH2—Ar—, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or C1-4alkoxy groups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di[C1-4alkyl]amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl, or R3 represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R3 represents a group of formula (a) wherein each R5 is independently selected from halogen, C1-4alkyl, C1-4alkoxy; and n is 0 to 3; each R4 is independently hydroxy, halogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, amino, C1-4alkylamino, di[C1-4alkyl]amino, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, C1-4alkylcarbonyl, carboxy, carbamoyl, C1-4alkoxycarbonyl, C1-4alkanoylamino, N-(C1-4alkyl)carbamoyl, N,N-di(C1-4alkyl)carbamoyl, cyano, nitro and trifluoromethyl; and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.
Inventor(s):	Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
Assignee:	Novartis AG , Glaxo Group Ltd
Application Number:	US09/582,746
Patent Claims:	1. A compound of the formula and a pharmaceutically acceptable salt or solvates thereof. 2. a compound selected from the group: a pharmaceutically acceptable salt or solvates thereof. 3. A pharmaceutical composition, comprising a compound of claim 2 or a pharmaceutically acceptable salt or solvate thereof, together with one or more of pharmaceutically acceptable carriers, diluents or excipients. 4. A pharmaceutical composition as claimed in claim 3 in unit dosage form. 5. A method of treatment of a human or animal subject suffering from breast, or head and neck cancers; which comprises administering to said subject an effective amount of a compound as claimed in claim 2 or a pharmaceutically acceptable salt or solvate thereof. 6. The method of claim 5, wherein the compound inhibits at least one protein tyrosine kinase selected from c-erbB-2, c-erbB-4, and EGFr. 7. The method of claim 5, wherein the compound inhibits at least two protein tyrosine kinases selected from c-erbB-2, c-erbB-4, and EGFr. 8. The method of claim 5, wherein the compound inhibits c-erbB-2, c-erbB-4, and EGFr.