Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-12-22
2002-06-04
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S912000
Reexamination Certificate
active
06399655
ABSTRACT:
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a method for the prophylactic treatment of cataracts.
BACKGROUND OF THE INVENTION
The lens of the eye is a transparent, bi-convex body, which functions as a refractive device to focus light onto the retina. A cataract is an opacity of the lens that adversely affects visual acuity. Cataracts are the leading cause of blindness in the world and incidence of cataract-induced blindness is expected to increase, especially in developing countries. Cataracts can appear at all ages, but are most commonly associated with aging adults—approximately 90% of adults 70 years and older experience symptoms of cataracts. Cataract surgery accounts for the largest single item in Medicare expenditures. In the United States, approximately 1.2 million cataract surgeries are performed every year at a cost of over $3 billion (Taylor,
Journal of the American College of Nutrition,
12(2): 138-146 (1993)).
The precise cause of cataract formation is unclear. Alteration in cell structure, formation of water pockets, and accumulation of high molecular weight proteins are but a few of the changes in lens architecture associated with cataract formation. Loss of transparency has been linked to formation of opaque fibers in the layers of the lens, as well as loss of transparency of previously clear fibers due to protein damage. Accumulation of extracellular materials and pigment also result in loss of transparency and scattering of light.
Various factors, besides age, have been associated with a predisposition to cataracts. Increased risk of cataract formation has been linked to exposure to ultraviolet light, infection, injury to the eye or the head region, exposure to radiation or toxic substances and prolonged use of corticosteroid drugs. These factors, alone or in concert, predispose one to cataracts by affecting the fibers and the biochemical reactions occurring naturally in the lens. Systemic disease, such as diabetes mellitus, also increases the risk of cataracts. In fact, it has been estimated that diabetics are three to four times more likely to develop cataracts than non-diabetics (Bunce et al.,
Annual Review of Nutrition
10: 223-254 (1990)). While the mechanism of action is unclear, it is believed that osmotic pressure increases with an increase in sugar molecules in the lens and leads to swelling of the lens and subsequently clouded vision.
Symptoms of cataracts include blurred and double vision, color confusion and reduced vision at night and in low light. As vision gradually deteriorates over time, affected individuals lose the ability to accomplish everyday tasks. Decreased vision results in difficulty in reading and watching television. Many have difficulty driving, especially at night. As such, many patients must alter their lifestyles and give up much of their independence. Cataract patients also have an increased risk of injury due to impaired vision.
Unless cataracts seriously interfere with vision and lifestyle, vision correction is accomplished by the prescribing of glasses or contact lenses. Ultimately, however, surgery is required to remove the cataract, once contact lenses and glasses are insufficient to maintain vision. Surgery is comprised of cataract extraction, wherein the affected lens is removed, and, in most cases, replaced with an artificial lens. Cataract surgery can be an outpatient procedure and accomplished with local anesthetic. Still, many complications can arise during and after surgery. Tearing of the capsule of the lens can cause the posterior capsule to rupture, thereby losing the lens to the vitreous cavity. Hemorrhage during surgery can stimulate inflammation and accelerate opacification of the capsule. Epithelial cells can invade the wound into the cornea, iris, and lens capsule, thereby causing uveitis and corneal decompensation. Retinal detachment is also a risk following cataract surgery. A rise in intraocular pressure is common after cataract surgery and causes glaucoma-like symptoms.
Given the prevalence of cataracts, the absence of any mode of prevention of cataracts, and the absence of any mode of treatment beyond surgery, there remains a need for an effective prophylactic treatment of cataracts. Accordingly, it is a principal object of the present invention to provide a method of prophylactically treating cataracts. This and other objects of the present invention will become apparent from the detailed description provided herein.
BRIEF SUMMARY OF THE INVENTION
The present invention is directed to a method for the prophylactic treatment of cataract. The method involves the administration of a compound of the formula:
wherein V, W and X are selected from the group consisting of hydro, hydroxyl, alkoxy, halo, an ester, an ether, a carboxylic acid group, a pharmaceutically acceptable salt of a carboxylic acid group, and —SR, in which R is hydrogen or an alkyl group, Y is selected from the group consisting of oxygen, sulfur, C(OH), and C═O, and Z is selected from the group consisting of hydro and C(O)OR
1
, wherein R
1
is an alkyl. Preferably, the alkoxy is a C
1
-C
6
alkoxy. Preferably, the halo is fluorine, chlorine or bromine. Preferably, the ester is a C
1
-C
6
ester. Preferably, the ether is a C
1
-C
6
ether. Preferred pharmaceutically acceptable salts of the carboxylic acid group include sodium and potassium salts. Preferably, the alkyl groups are C
1
-C
6
alkyl groups. Desirably, the compound of Formula I is genistein.
DETAILED DESCRIPTION OF THE INVENTION
The present invention is predicated on the discovery that compounds of Formula I are effective in the prevention of cataracts. Accordingly, the present invention provides a method for the prophylactic treatment of cataracts. By “prophylactic” is meant the protection, in whole or in part, against cataract formation. The present inventive method is particularly useful in the inhibition of age-related cataracts and diabetic cataracts. However, the present inventive method is also useful in the treatment of cataracts that have been or are being treated with surgery, cataracts that occur after surgical removal of an existing opacified lens, i.e., secondary cataracts, cataracts that occur after retinal detachment and surgery to repair the retinal detachment, cataracts associated with trauma to the eye or head, cataracts associated with tumors, cataracts associated with exposure to radiation, and cataracts associated with toxicity. The present inventive method is also useful in the prophylactic treatment of cataracts resulting from systemic disorders, for example, but not limited to, galactosemia, Farry's disease, Lowe's syndrome, Alport's syndrome and dystrophia myotonica, as well as dermatologic disorders, such as atopy, ichthyosis, Rothmund-Thompson syndrome, Werner's syndrome, incontinentia pigment and Cockayne's syndrome. The present inventive method is also useful in the prevention of cataract formation due to central nervous system disorders, such as neurofibromatosis type II, Zellweger syndrome and Norrie's disease, and local ocular disease, such as glaucoma, uveitis, retinitis pigmentosa, gyrate atrophy, degenerative myopia, ischemia and infection.
The method comprises the administration of a compound of Formula I in an amount sufficient to treat the lens for cataract prophylactically. Accordingly, a compound for use in the method of the present invention is a compound of the following formula:
wherein V, W and X are selected from the group consisting of hydro, hydroxyl, alkoxy, halo, an ester, an ether, a carboxylic acid group, a pharmaceutically acceptable salt of a carboxylic acid group, and —SR, in which R is hydrogen or an alkyl group, and Y is selected from the group consisting of oxygen, sulfur, C(OH), and C═O, and Z is selected from the group consisting of hydro and C(O)OR
1
, wherein R
1
is an alkyl. Preferably, the alkoxy is a C
1
-C
6
alkoxy. Preferably, the halo is fluorine, chlorine or bromine. Preferably, the ester is a C
1
-C
6
ester. Preferably, the ether is a C
1
-C
6
Fay Zohreh
Johns Hopkins University School of Medicine
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