Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma
AssigneeAlcon Inc.
InventorsMark R. Hellberg, Abbot F. Clark, Iok-Hou Pang, Peggy Elizabeth Hellberg, Loretta Graves McNatt, Wan-Heng Wang
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Abstract
The use of inhibitors of GSK-3 useful for treating glaucoma is disclosed.
Claims19
A method for treating glaucomatous optic neuropathy comprising administering to a patient in need thereof a therapeutically effective amount of a composition comprising at least one glycogen synthase kinase-3 (GSK-3) inhibitor in a pharmaceutically acceptable carrier, wherein said GSK-3 inhibitor is a compound of the formula:
- wherein R1 and R2independently═
- R3═H, C1-6alkyl, (un)substituted phenyl, C1-6alkyl-NR6R7, C1-7cycloalkyl, C1-6alkyl-OR6, C1-6alkylC(O)2R5, or C1-6alkylC(O)NR6R7;
- R4═H, or one or more substituents C1-6alkyl, (un)substituted phenyl, —OR6, —SR6, halogen, (un)substituted phenoxy, —CN, —NO2, C1-6alkyl-NR6R7, —NR6R7, C1-7cycloalkyl, (un)substituted heterocyclyl, —C(O)2R5, C1-6alkylC(O)2R5, or C1-6alkylC(O)NR6R7;
- and
- R5, R6, R7═H, or C1-6alkyl, (un)substituted phenyl.
A method for lowering intraocular pressure (IOP) in a patient in need thereof said method comprising administering to said patient a therapeutically effective amount of a composition comprising at least one glycogen synthase kinase-3 (GSK-3) inhibitor in a pharmaceutically acceptable vehicle, wherein said GSK-3 inhibitor is a compound of the formula:
- wherein R1 and R2independently═
- R3═H, C1-6alkyl, (un)substituted phenyl, C1-6alkyl-NR6R7, C1-7cycloalkyl, C1-6alkyl-OR6, C1-6alkylC(O)2R5, or C1-6alkylC(O)NR6R7;
- R4═H, or one or more substituents C1-6alkyl, (un)substituted phenyl, —OR6, —SR6, halogen, (un)substituted phenoxy, —CN, —NO2, C1-6alkyl-NR6R7, —NR6R7, C1-7cycloalkyl, (un)substituted heterocyclyl, —C(O)2R5, C1-6alkylC(O)2R5, or C1-6alkylC(O)NR6R7;
- and
- R5, R6, R7═H, C1-6alkyl, or (un)substituted phenyl.
A method for preventing or inhibiting glaucomatous optic neuropathy and controlling intraocular pressure (IOP) in a patient in need thereof, said method comprising at least one glycogen synthase kinase-3 (GSK-3) inhibitor in a pharmaceutically acceptable carrier, wherein said GSK-3 inhibitor is a compound of the formula:
- wherein R1 and R2 independently═
- R3═H, C1-6alkyl, (un)substituted phenyl, C1-6alkyl-NR6R7, C1-7cycloalkyl, C1-6alkyl-OR6, C1-6alkylC(O)2R5, C1-6alkylC(O)NR6R7;
- R4═H, or one or more substituents C1-6alkyl, (un)substituted phenyl, —OR6, —SR6, halogen, (un)substituted phenoxy, —CN, —NO2, C1-6alkyl-NR6R7, —NR6R7, C1-7cycloalkyl,(un)substituted heterocyclyl, —C(O)2R5, C1-6alkylC(O)2R5, or C1-6alkylC(O)NR6R7;
- and
- R5, R6, R7═H, C1-6alkyl, or (un)substituted phenyl.
The method of 17, wherein said glaucoma is normal-tension glaucoma.
Dependencies are inferred from the claim text.