DrugPatentWatch Database Preview
« Back to Dashboard
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)|
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.
For more information try a trial or see the plans and pricing
Serving hundreds of leading biopharmaceutical companies globally:
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.