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US Army

Generated: May 25, 2018

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Claims for Patent: 6,727,256

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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 CR.sup.1 and V is N; or Y is N and V is CR.sup.1 ; or Y is CR.sup.1 and V is CR.sup.2 ; or Y is CR.sup.2 and V is CR.sup.1 ; R.sup.1 represents a group CH.sub.3 SO.sub.2 CH.sub.2 CH.sub.2 NHCH.sub.2 --Ar--, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy groups; R.sup.2 is selected from the group comprising hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylamino and di[C.sub.1-4 alkyl]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 R.sup.3 group and optionally substituted by at least one independently selected R.sup.4 group; R.sup.3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl, or R.sup.3 represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R.sup.3 represents a group of formula (a) wherein each R.sup.5 is independently selected from halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy; and n is 0 to 3; each R.sup.4 is independently hydroxy, halogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.1-4 alkoxy, amino, C.sub.1-4 alkylamino, di[C.sub.1-4 alkyl]amino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, C.sub.1-4 alkylcarbonyl, carboxy, carbamoyl, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoylamino, N-(C.sub.1-4 alkyl)carbamoyl, N,N-di(C.sub.1-4 alkyl)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): Carter; Malcolm Clive (Ware, GB), Cockerill; George Stuart (Bedford, GB), Guntrip; Stephen Barry (Hertford, GB), Lackey; Karen Elizabeth (Hillsborough, NC), Smith; Kathryn Jane (Bishop's Stortford, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:09/582,746
Patent Claims: 1. A compound of the formula ##STR54##

and a pharmaceutically acceptable salt or solvates thereof.

2. a compound selected from the group: ##STR55##

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.

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