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US 7,220,757 B2Granted
Compositions and methods for topical administration of 2-NH-heteroarylimidazoles
AssigneeReplidyne, Inc.
InventorsJohn Berge, Andrew Forrest, Dieter Hamprecht, Richard Jarvest
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I): are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.
Claims15
A method of treating a bacterial infection in a patient in need thereof comprising topically administering to the patient an antibacterially effective amount of a compound of the formula (I):
- in which:
- R1 is an optionally substituted aryl or an optionally substituted heteroaryl ring;
- R2 is a 5 or 6-membered heteroaryl ring which is optionally substituted with from 1 to 3 substituents selected from halo, cyano, hydroxy, (C1-6)alkyl (optionally substituted by halo, hydroxy, amino, mono to perfluoro(C1-3)alkyl, carboxy or (C1-6)alkoxycarbonyl), (C3-7)cycloalkyl, C(1–6)alkoxy, amino, mono- or di-(C1-6)alkylamino, acylamino, carboxy, (C1-6)alkoxycarbonyl, carboxy(C1-6)alkyloxy, (C1-6)alkylthio, (C1-6)alkylsulphinyl, (C1-6)alkylsulphonyl, sulphamoyl, mono- and di-(C1-6)alkylsulphamoyl, carbamoyl, mono- and di-(C1-6)alkylcarbamoyl, and heterocyclyl;
- X is CH2 or CHR3 in which R3 is C(1–6)alkyl or is linked to the ortho position of an aryl or heteroaryl ring of R1 to form a 5 to 7 membered ring optionally including oxygen or nitrogen as a ring atom;
- Y is C(1-3)alkylene or C(4-6)cycloalkylene;
- including tautomeric forms of the imidazole ring;
- and
- salts thereof, and
- excluding 8-[2-(benzylamino)ethylamino]theophylline.
6 more elements
A pharmaceutical composition for topical administration to a patient in need thereof comprising an antibacterially effective amount of a compound according to the formula (I):
- in which:
- R1 is an optionally substituted aryl or an optionally substituted heteroaryl ring;
- R2 is a 5 or 6-membered heteroaryl ring which is optionally substituted with from 1 to 3 substituents selected from halo, cyano, hydroxy, (C1-6)alkyl (optionally substituted by halo, hydroxy, amino, mono to perfluoro(C1-3)alkyl, carboxy or (C1-6)alkoxycarbonyl), (C3-7)cycloalkyl, C(1-6)alkoxy, amino, mono- or di-(C1-6)alkylamino, acylamino, carboxy, (C1-6)alkoxycarbonyl, carboxy(C1-6)alkyloxy, (C1-6)alkylthio, (C1-6)alkylsulphinyl, (C1-6)alkylsulphonyl, sulphamoyl, mono- and di-(C1-6)alkylsulphamoyl, carbamoyl, mono- and di-(C1-6)alkylcarbamoyl, and heterocyclyl;
- X is CH2 or CHR3in which R3is C(1-6)alkyl or is linked to the ortho position of an aryl or heteroaryl ring of R1 to form a 5 to 7 membered ring optionally including oxygen or nitrogen as a ring atom;
- Y is C(1-3)alkylene or C(4-6)cycloalkylene;
- including tautomeric forms of the imidazole ring;
- and
- salts thereof, and
- excluding 8-[2-(benzylamino)ethylamino]theophylline;
- wherein the compound of formula (I) is together with a topical additive.
7 more elements
Dependencies are inferred from the claim text.