Method of reducing intraocular pressure in humans
AssigneeInotek Pharmaceuticals Corporation
InventorsNorman N. Kim, William K. McVicar, Thomas G. McCauley, Prakash Jagtap
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Abstract
Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).
Claims20
A method of reducing intraocular pressure (IOP) in a human subject in need thereof by administering about 0.05 mg/ml to about 7.0 mg/ml of a compound of Formula II, or a pharmaceutically acceptable salt thereof, to an affected eye of the human subject,
- wherein R1 is selected from —(CO)C1-C6 alkyl;
- —(CO)CH(halo)2;
- —(CO)phenyl;
- —(CO)C1-C10 optionally branched aliphatic;
- —(CO)C3-C8 cycloalkyl which is optionally substituted with one or more of hydroxy or —(CH2)nOH wherein n is 1-6;
- —(CO)aryl which is optionally substituted with one or more of hydroxy or —(CH2)nOH wherein n is 1-6;
- and —(CO)C3-C7 heterocyclyl which is optionally substituted with one or more of hydroxy or —(CH2)nOH, wherein n is 1-6;
- R2 is selected from —H and halo;
- and
- R3 is selected from —H, hydroxy, —O(CO)CH(halo)2, —O(CO)(CH2)2CH3, —O(CO)CH(CH3)2, and —O(CO)CH2C(CH3)3.
A method of treating diseases and conditions selected from the group consisting of normal-tension glaucoma, primary open angle glaucoma (POAG) and ocular hypertension (OHT), the method comprising administering a compound of Formula II, or a pharmaceutically acceptable salt thereof, to an affected eye of a human subject in need thereof,
- wherein R1 is selected from —(CO)C1-C6 alkyl;
- —(CO)CH(halo)2;
- —(CO)phenyl;
- —(CO)C1-C10 optionally branched aliphatic;
- —(CO)C3-C8 cycloalkyl which is optionally substituted with one or more of hydroxy or —(CH2)nOH wherein n is 1-6;
- —(CO)aryl which is optionally substituted with one or more of hydroxy or —(CH2)nOH wherein n is 1-6;
- and —(CO) C3-C7 heterocyclyl which is optionally substituted with one or more of hydroxy or —(CH2)nOH, wherein n is 1-6;
- R2 is selected from —H and halo;
- and
- R3 is selected from —H, hydroxy, —O(CO)CH(halo)2, —O(CO)(CH2)2CH3, —O(CO)CH(CH3)2, and —O(CO)CH2C(CH3)3.
Dependencies are inferred from the claim text.