Abstract: A method of reducing intraocular eye pressure by topically applying to an affected eye a small but therapeutically effective intraocular eye pressure reducing amount of a compound which is a 2-deoxyglucose or hexose or pentose derivative of ethacrynic acid.
Type:
Grant
Filed:
February 23, 1996
Date of Patent:
October 15, 1996
Assignee:
University of Iowa Research Foundation
Inventors:
Charles F. Barfknecht, Ronald D. Schoenwald
Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon atoms, that may be derived from a lower alkanol.
Type:
Grant
Filed:
November 30, 1994
Date of Patent:
September 24, 1996
Assignee:
Allergan
Inventors:
Joseph S. Adorante, Elizabeth WoldeMussie, Guadalupe Ruiz
Abstract: This invention relates to novel aqueous ophthalmic compositions containing vitamin E or ester thereof as an active ingredient, sorbic acid or salts thereof as a preservative, and surfactant. The composition of this invention is useful for treatment of various eye diseases, especially for cataract.
Abstract: A drug delivery ophthalmic insert prepared by forming a water soluble solid polymer into a paste by the addition of a small fixed amount of water, drying the paste and then sectioning the paste into a plurality of rod shaped inserts is provided. The insert is rendered suitable for prolonged and sustained delivery of medication to the eye since it is formed by the addition of a small amount of water and has a surface area less than about 3 mm.sup.2. Specific water soluble solid polymers which may be used include methylcellulose, hydroxyethyl cellulose, alginic acid and combinations thereof as well as mixtures of pilocarpine dispersed in methylcellulose and its combinations.
Abstract: A method for treatment of ocular hypertension which comprises ocularly administering, to a subject in need of such treatment, an oculo-hypotensively synergistic combination of(a) a 15-ketoprostaglandin or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof, and(b) a carbonate dehydratase inhibitor in an amount effective in treatment of ocular hypertension.
Abstract: The present invention provides a novel drug for treating glaucoma. The present invention relates to a therapeutic agent for glaucoma which comprises an aminoalkoxybibenzyl represented by the formula (I): ##STR1## or a hydrate or pharmaceutically acceptable salt thereof as an active ingredient.
Abstract: The present invention provides a method of treating glaucoma which comprises administering to a subject an effective amount of an oligonucleotide which may be substituted or modified in its phosphate, sugar, or base, so as to decrease intraocular pressure and thereby treat the glaucoma.
Type:
Grant
Filed:
January 19, 1994
Date of Patent:
August 13, 1996
Assignees:
The Trustees of Columbia University in the City of New York, Washington University
Abstract: A method of retarding and ameliorating eye diseases and injuries is disclosed. The method comprises administering astaxanthin in a therapeutically-effective amount to prevent, retard or treat eye and central nervous system diseases or injuries, such as age-related macular degeneration and other central nervous system degenerative diseases, photic injury, ischemic diseases, and inflammatory diseases.
Type:
Grant
Filed:
October 27, 1994
Date of Patent:
June 18, 1996
Assignee:
Board of Trustees of the University of Illinois
Abstract: The invention relates to an ophthalmic solution for topical application to the eye in order to lower increased intraocular pressure of the aqueous humor, containing a quantity of a polyhydroxyalcohol such as sorbitol, mannitol, inositol or xylitol or mixtures thereof, effective for lowering the intraocular pressure of aqueous humor, in a carrier tolerated by the eye, the use thereof and the preparation thereof.
Type:
Grant
Filed:
August 19, 1993
Date of Patent:
June 18, 1996
Assignee:
Basotherm GmbH
Inventors:
Helmut Franz, Hannes E. Kompa, Tibor Rozman
Abstract: A method for inducing prolonged pseudoaccommodation includes the instillation of an ophthalmic formulation into an eye for contracting the iris sphincter muscle, but not the ciliary muscle, in order to cause sphincter muscle contraction for a period of greater than about one hour per installation. The method further provides for the stabilization of an implanted intraocular lens immediately after surgery and for reducing glare following radial keratotomy.
Type:
Grant
Filed:
April 13, 1993
Date of Patent:
May 28, 1996
Assignee:
Allergan, Inc.
Inventors:
Elizabeth WoldeMussie, Roger F. Steinert, Guadalupe Ruiz
Abstract: In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as the active ingredient one or more N-substituted 2-(1H) pyridone(s). The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.
Abstract: An ophthalmic pharmaceutical composition containing an association of N-acetyl-cysteine and polyvinylalcohol useful for the treatment of keratoconjunctivitis sicca.
Type:
Grant
Filed:
March 17, 1994
Date of Patent:
April 23, 1996
Assignee:
Zambon Group S.p.A.
Inventors:
Federico Stroppolo, Daniele Bonadeo, Francesco Tocchini, Annibale Gazzaniga
Abstract: Compounds structurally related to ethacrynic acid are described. The compounds are useful for controlling intraocular pressure. Unlike ethacrynic acid, the compounds of the present invention are capable of effectively penetrating the cornea. Methods of controlling intraocular pressure via topical application of one or more of the compounds to the eye and topical ophthalmic compositions useful in the treatment of glaucoma are also described.
Abstract: Ophthalmic pharmaceutical compositions useful in controlling elevated intraocular pressure associated with glaucoma and other ophthalmic conditions are described. A method of controlling elevated intraocular pressure with those compositions is also described. The compositions contain a combination of an alpha-2 agonist (e.g., para-amino clonidine) and a beta blocker (e.g., betaxolol).
Abstract: The present invention relates to a method of treating cranial fluid volume dysfunctions such as glaucoma in an individual, comprising administering compounds which effect an increase in cyclic GMP at the site of the dysfunction or at the site of synthesis or removal of the accumulating fluid. In particular, the method of treatment involves the topical use of hydralazine, non-organic nitrites or nitroglycerine, and the systematic use of hydralazine or non-organic nitrites.
Abstract: The present invention provides the fumarate salt of 4-(diethyl-3-(1-methyloctyl)-7,8,9,10-tetrahydro-6,6,9-trimethyl-6H-dibenz o[b,d]pyran-1-ol, 4-diethyl-amino)butyric acid ester, i.e. the compound having the following structure (I): ##STR1## and methods of treatment, particularly treatment of glaucoma, and pharmaceutical compositions that utilize or comprise the fumarate salt (I).
Abstract: A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of .beta.-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.
Type:
Grant
Filed:
January 5, 1993
Date of Patent:
February 27, 1996
Inventors:
Jonathan C. Javitt, Norman B. Javitt, Peter McDonnell
Abstract: An ophthalmic pharmaceutical composition containing an association of N-acetyl-cysteine and polyvinylalcohol useful for the treatment of keratoconjunctivitis sicca.
Type:
Grant
Filed:
June 3, 1994
Date of Patent:
January 30, 1996
Assignee:
Zambon Group S.p.A.
Inventors:
Federico Stroppolo, Daniele Bonadeo, Francesco Tocchini, Annibale Gazzaniga
Abstract: The present invention provides therapeutic agents comprising cyclopentane heptane or heptenoic acid, 2 arylalkyl or arylalkenyl and derivatives thereof, wherein the carboxylic acid of the parent compound is converted to a hydroxyl or ester group. These therapeutic agents are potent ocular hypotensives as well as having other therapeutic uses.
Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.
Abstract: The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
Type:
Grant
Filed:
December 3, 1993
Date of Patent:
December 19, 1995
Assignees:
The Rockefeller University, Alteon Inc.
Inventors:
Peter C. Ulrich, Anthony Cerami, Dilip R. Wagle
Abstract: Methods and compositions for preventing or treating non-inflammatory elevated intraocular pressure associated with administered or endogenous steroids including administering to a mammalian organism a composition including (a) an ophthalmologically effective amount of a non-steroidal cyclooxygenase inhibitor, and (b) a pharmaceutically acceptable carrier, to reduce or prevent an elevation of intraocular pressure and/or protein marker induction induced by chronic exposure to glucocorticoids.
Type:
Grant
Filed:
December 22, 1993
Date of Patent:
December 12, 1995
Assignee:
The Regents of the University of California
Inventors:
Jon R. Polansky, Ernest Bloom, Donald J. Fauss
Abstract: Topical ophthalmic medicament delivery system combining an aqueous ophthalmic gel suspension at a pH equal to or greater than 7.5 and an osmotic pressure of from 10 to about 400 mOsM containing a pharmaceutically effective mount of one or more ophthalmic medicaments of from about 0.05% to about 10% by weight, based on the total weight of the suspension, of a carboxyl-containing polymer prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less then about 5% by weight of a cross-linking agent. The systems have a viscosity of from about 1,000 to about 30,000 centiposes prior to administration to the eye and remain a gel in the eye for a prolonged period of time allowing for the sustained release of one or medicaments such as amine containing antibiotics alone or in combination with cortiscosteroids.
Type:
Grant
Filed:
May 24, 1994
Date of Patent:
December 12, 1995
Assignee:
InSite Vision Incorporated
Inventors:
Rajesh Patel, Lyle Bowman, Margarita Vildaver, Raymond Chen
Abstract: Intraocular pressure is lowered in the eye of a mammal by administration of a pharmaceutical composition containing as active ingredient a compound of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, wavy lines connected to the olefinic bond represent cis or trans configuration about the olefinic bond; R.sub.1 represents H, or CO-R.sub.3 where R.sub.3 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; R.sub.2 represents H or lower alkyl of 1 to 6 carbons, and n is an integer between 0 and 8.
Type:
Grant
Filed:
September 24, 1992
Date of Patent:
November 21, 1995
Assignee:
Allergan, Inc.
Inventors:
Michael E. Garst, Robert M. Burk, Ming F. Chan, Michael B. Roof
Abstract: A device for pinpoint application of micro-quantities of a pharmacologically suitable composition to the outer hard coat of the eye, comprises a micro-container with a fixation element. The micro-container comprises a bore whose aperture is adapted to contact the eye surface, and the fixation element is adapted for reversibly adhering to the eye surface.
Abstract: A preparation for reducing intraocular pressure consisting essentially of a therapeutically effective amount of the fixed combination of dipivalylepinephrine and carbachol (preparation 1) or dipivalylepinephrine and beta-blocker (preparation 2). The preparations may be prepared both as a solution and as a suspension. Either preparation is administered twice daily.
Abstract: A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of a glaucoma disorder. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R.sup.
Abstract: Disclosed is an intraocular pressure reducing method and composition wherein 11-acyl prostaglandins are contained in a pharmaceutically acceptable excipient for topical application to the surface of the eye.
Abstract: Reversibly gelling aqueous and oil emulsions are disclosed which can be modified to incorporate oil soluble pharmaceutical compounds for delivery to physiological systems in a soluble form and which undergo significant changes in viscosity in response to substantially simultaneous changes in both temperature and pH. The compositions are formed of relatively low concentrations of a stable combination of at least one pH-sensitive reversibly gelling polymer, at least one temperature-sensitive reversibly gelling polymer and at least one organic oil. The compositions can be formulated to exhibit a sol-gel transition over a wide range of conditions and viscosities and may be modified to incorporate a pharmaceutical compound for utilization as droppable or injectable drug delivery systems which will gel following administration to a physiological system for the sustained delivery of such pharmaceutical compounds.
Abstract: A method of reducing elevated intraocular pressure which comprises administering the compound of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof to patients suffering from abnormally elevated intraocular pressure is provided. A pharmaceutical formulation containing the compound of the formula (1) as an essential component is also provided.
Abstract: Low-tension glaucoma is treated by topical administration to the eye of an amount of a calcium channel blocking agent effective to increase blood flow to the optic nerve head. Calcium channel blocking agents of Class I are especially useful, and among these a preferred agent is verapamil hydrochloride.
Abstract: The use is described of acetyl D-carnitine and its pharmacologically acceptable salts in the therapeutic treatment of glaucoma. The medicament may be administered orally or parenterally or be applied as a collyrium containing approximately 1-10% w/v of acetyl D-carnitine.
Abstract: Ischemic disorders of the retina and associated tissues of the posterior segment of the eye are treated by topical administration to the eye of an amount of a calcium channel blocking agent effective to increase blood flow to those tissues. Calcium channel blocking agents of Class I are especially useful, and among these a preferred agent is verapamil hydrochloride.
Abstract: A method for the treatment of ocular hypertension which comprises administering, to a subject in need of such treatment,(a) a .beta.-adrenergic blocker at the enhancement phase of aqueous humor production, and(b) a prostanoic acid compound at the suppression phase of aqueous humor production, andin an amount effective in treatment of ocular hypertension.
Abstract: A method of reducing elevated intraocular pressure which comprises administering the compound of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof to patients suffering from abnormally elevated intraocular pressure is provided. A pharmaceutical formulation containing the compound of the formula (1) as an essential component is also provided.
Abstract: Disclosed is a sustained release liquid aqueous ophthalmic delivery system and a method of providing a slow and sustained release of ophthalmic treating agents to the eye of a mammal which comprises administering to the eye of a said mammal an effective amount of a homogeneous liquid aqueous ophthalmic pharmaceutical composition, of pH between about 3.0 and about 6.2, which is adminstrable in drop form and which comprises an ophthalmically effective concentration of a said ophthalmic treating agent and about 0.05% to about 10% by weight of the polymer chitosan; said polymer consisting essentially of(A) monomeric .beta.(1.fwdarw.4)-D-glucosamine linked units and of(B) monomeric .beta.(1.fwdarw.
Abstract: A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of .beta.-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.
Type:
Grant
Filed:
January 5, 1993
Date of Patent:
May 23, 1995
Inventors:
Jonathan C. Javitt, Norman B. Javitt, Peter McDonnell
Abstract: Aminoglycosides, analogs and derivatives thereof, in the form of phosphate salts are described as well as the process for making and utilizing same. Aminoglycoside phosphate liposomes and nonguanadino aminoglycoside phosphate liposomes, their preparation and use, are particularly described.
Type:
Grant
Filed:
May 6, 1993
Date of Patent:
April 25, 1995
Assignee:
The Liposome Company, Inc.
Inventors:
Marcel B. Bally, Lois E. Bolcsak, Pieter R. Cullis, Andrew S. Janoff, Lawrence D. Mayer
Abstract: A method for treatment of ocular hypertension which comprises ocularly administering, to a subject in need of such treatment, an ocular-hypertension synergistic combination of(a) a 15-deoxy-prostaglandin compound, and(b) a .beta.-adrenergic blocker in an amount effective in treatment of ocular hypertension.
Abstract: The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
Abstract: A method for treatment of ocular hypertension which comprises ocularly administering, to a subject in need of such treatment, a oculo-hypotensively synergistic combination of(a) a 13,14-dihydro-15-ketoprostaglandin compound, and(b) a cholinergic agentin an amount effective in treatment of ocular hypertension.
Abstract: An ophthalmologic gel is disclosed having a viscosity in the range of about 10,000 to about 50,000 mPa.s and comprising (1) about 0.05 to about 3% by weight of one or more polyacrylates and (2) about 0.1 to about 10% by weight one or more water-soluble, physiologically compatible polymers selected from the group consisting of polyvinyl alcohol, dextran, and mixtures thereof.
Type:
Grant
Filed:
March 25, 1993
Date of Patent:
March 14, 1995
Assignee:
Medproject Pharma Entwicklungs und Vertriebs Gesellschaft
Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
Abstract: A disinfectant or preservative composition particularly adapted for use in ophthalmic preparations such as contact lens disinfecting, cleaning, cushioning, wetting, soaking and reconditioning solutions and additionally in topical medications and tear substitutes, which uses a hydrophilic polymeric antimicrobial agent, namely poly[oxyethylene(dimethylimino) (ethylene dimethylimino)ethylene dichloride] with additional agents including EDTA and alkali salts thereof and a boric acid/borate buffer system.
Abstract: An assay for determining patients either having Primary Open Angle Glaucoma or at risk of developing Primary Open Angle Glaucoma. The assay involves testing cells, preferably lymphocyte cells, for 3.alpha.-HSD activity and determining from the level of assayed activity whether the patient is either suffering from Primary Open Angle Glaucoma or at risk therefor.
Type:
Grant
Filed:
December 17, 1993
Date of Patent:
December 27, 1994
Assignee:
New York Medical College
Inventors:
A. Louis Southren, Bernard I. Weinstein, Gary G. Gordon