Amelioration of cataracts, macular degeneration and other ophthalmic diseases

A technology for macular degeneration, diseases, applied in the direction of skin diseases, sensory diseases, organic active ingredients, etc.

Inactive Publication Date: 2008-01-09
OTHERA HLDG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Follow-up work at the National Institutes of Health also aimed to identify potent hydro

Method used

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  • Amelioration of cataracts, macular degeneration and other ophthalmic diseases
  • Amelioration of cataracts, macular degeneration and other ophthalmic diseases
  • Amelioration of cataracts, macular degeneration and other ophthalmic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0113] Example 1: Determination of the stability of ester compounds in aqueous humor

[0114] Methods: A 0.1-0.5% solution of the ester compound was prepared in a buffer (pH 4.5-5.0) containing DPTA or EDTA. The solution was filled into brown glass vials, which were sealed and placed in a temperature-controlled container maintained at 40°C. Sample vials were removed periodically and stored at 0-5°C until analyzed by HPLC, GC or GC / MS and found to be stable after 3 months under these conditions.

[0115] In order to be effective as an anti-cataract drug, the agent must be able to penetrate the lens. This can be included in methods of selecting anti-cataract compounds. The method for tempol-H is described as follows:

Embodiment 2

[0116] Example 2: Drug Permeation of Organ Cultured Rat Lenses

[0117] In contrast to drugs previously tested as anti-cataract agents, tempol-H and tempol have a remarkable ability to penetrate the lens tissue from the surrounding fluid. The assay described in this section measures the time period, active compound concentration and compound distribution in the lens following incubation with the rat lens under the organ culture conditions.

[0118] METHODS: Rat lenses were cultured as follows: Rat lenses were obtained from Sprague-Dawley rats. The lens was incubated in a 24-well culture plate filled with modified TC-199 medium, and placed in an atmosphere containing 95% air / 5% CO 2 atmosphere in a 37 °C incubator. The lenses were incubated in 2 ml of medium adjusted to 300 milliosmosm (mOsm). The lenses were incubated for 1-24 hours in medium containing 4.0 mM tempol-H or 4.0 mM oxidized form of tempol. At appropriate times, the lenses were removed from the medium, blotted...

Embodiment 3

[0122] Example 3: 1-oxyl-4-(3'-ethoxy-2',2'dimethyl)propanecarbonyloxy-2,2,6,6-tetramethylpiperidine

[0123]

[0124] In dry DMF (10 mL), 3-ethoxy-2,2-dimethylpropionic acid (750 mg, 7.13 mmol; prepared according to the method described in J.Org.Chem., 38, 2349, 1975, To the stirred solution, the contents of which are incorporated herein by reference), was added 1,1'-carbonyldiimidazole (1.27 g, 7.84 mmol) in small proportions. Vigorous gas evolution was observed. The solution was heated at 100°C for 1 hour. To this mixture was added tempol (900 mg, 5.23 mmol) and 1,8-diazabicyclo[5,4,0]undec-7-ene (DBU) (800 mg, 5.26 mmol) and heating was continued for 12 hours. The reaction mixture was concentrated under reduced pressure. The residue was dissolved in ethyl acetate (100 mL) and washed with 1N HCl, saturated NaHCO 3 Washed successively with brine, dried over anhydrous sodium sulfate, and concentrated in vacuo to give a red solid (1.48 g). It was subjected to silica ge...

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Abstract

Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age-related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula where R1 and R2 are, independently, H or C1 to C3 alkyl ; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl ; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl ; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.

Description

[0001] Cross References to Related Applications [0002] This application is a continuation-in-part of U.S. Application 10 / 440,583, filed May 19, 2003, and also claims priority to U.S. Provisional Application 60 / 523,803, filed November 20, 2003, each of which is hereby incorporated by reference in its entirety . field of invention [0003] The present invention relates to compositions for improving the development of cataracts in the eyes of patients and methods for achieving these improvements. In a preferred embodiment of the invention, cataract development or growth is substantially stopped. The invention also relates to the treatment and certain other uses of macular degeneration in the eye. According to a preferred embodiment, said composition of the present invention can be administered to a patient without injection and can be formulated as eye drops for such administration. This invention also provides methods of treating cataracts and macular degeneration as a mean...

Claims

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Application Information

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IPC IPC(8): A61K31/445A61K
CPCC07D401/12A61K9/0048C07D211/94A61K31/4525A61K31/198C07D405/12A61K38/063A61K31/145C07D487/04A61K31/445C07D413/12A61K9/0051A61K45/06A61P1/00A61P17/14A61P27/02A61P27/06A61P27/12A61P39/00A61P39/06A61P43/00A61K2300/00A61K31/435
Inventor 威廉·L·马蒂尔甘希亚姆·帕蒂尔
Owner OTHERA HLDG
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