76 results about "Carbonic anhydrase inhibitor" patented technology

The present invention relates to the combination of a methylxanthine and a carbonic anhydrase activator to provide synergistic effects. The invention further relates to the improved/enhanced cognitive ability of individuals, particularly those suffering from various disorders, such as Alzheimer's Disease, stroke, hypoxia, general dementia, ADHD, mental retardation, and "sun down" syndrome.

A sterile aqueous formulation of a carbonic anhydrase inhibitor such as brinzolamide in combination with polymers like Soluplus® and a surfactant like polysorbate 80, as well as methods of preparation thereof, is disclosed. The formulation relates to the highly solubilized or an amorphous form of poorly insoluble drugs/active ingredient(s) to improve its bio-availability and manufacturability.

This invention relates generally to methods and pharmaceutical formulations useful in treating patients suffering from sleep apnea, including obstructive sleep apnea syndrome (OSAS). Treatment is effected by administering a carbonic anhydrase inhibitor to the patient in combination with an aldosterone antagonist. Formulations containing a therapeutically effective amount of a carbonic anhydrase inhibitor and a therapeutically effective amount of an aldosterone antagonist are provided as well.

Carbonic anhydrase inhibitors for the prevention and treatment of diabetic retinopathy and various other retinopathies.

This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing or modulating carbonic anhydrase activity in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of glaucoma, epileptic seizures, Idiopathic intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, periodic paralysis and dural ectasia, congestive heart failure, drug induced edema, diuretic, intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.

Pharmaceutical ophthalmic compositions comprising active ingredient(s) such as carbonic anhydrase inhibitor (CAI) or combinations and processes for making such compositions and the use of these compositions in patient populations including pediatric populations. A process for preparing an ophthalmic composition comprising a carbonic anhydrase inhibitor, which comprises a) preparing a slurry comprising a carbonic anhydrase inhibitor and a surfactant; b) preparing a polymer slurry comprising a polymer and water; c) preparing a solution comprising tonicity and preservative agents; d) mixing the polymer slurry of step b and the solution of step c, to form a vehicle concentrate and adjusting pH; e) adding the slurry of step a, to the vehicle concentrate of step d and mixing to homogenize; f) autoclaving the mixture of step e; g) sizing the mixture of step f, under aseptic condition.

The present invention relates to an ophthalmic composition comprising at least two active pharmaceutical ingredients. In particular, the active pharmaceutical ingredients are selected from the group consisting of: an alpha 2 adrenergic receptor agonist; a beta-adrenergic receptor agonist; an immunosuppressant; a lymphocyte associated antigen antagonist; an anti-inflammatory; a beta-blocker; a prostaglandin analog; a histamine receptor antagonist; a carbonic anhydrase inhibitor; and an antibiotic. In some embodiments, the composition of the invention is a nanoemulsion formulation. In one particular embodiment, the first active pharmaceutical ingredient is an alpha 2 adrenergic receptor agonist. The present invention also provides a method for treating various clinical conditions associated with an eye disorder or eye disease using the composition of the invention.

Derivatives of boron cluster compounds of general formula I and their pharmaceutically acceptable salts and solvates, and their specific inhibition effect on the enzyme carbonic anhydrase IX, a protein overexpressed in cancer tissues. Methods of synthesis and the use of the novel derivatives. These inhibitors of human carbonic anhydrase IX can be used as active compounds of pharmaceuticals for diagnostics and/or therapy of cancer diseases.

The present invention relates to a pharmaceutical cocktail and methods of cancer treatment. In particular, one such cocktail comprises a combination of effective amounts of a lactate transporter inhibitor, a carbonic anhydrase inhibitor, a sodium potassium chloride cofactor (NKCC) transporter inhibitor, a member of the hydroxycinnamate class of drugs or a derivative thereof, and/or an angiogenesis inhibitor, including a vascular endothelial growth factor (VEGF) inhibitor such as bevacizumab in combination with blood vessel occlusion. As most cancers in an untreated state uses both aerobic and anaerobic/glycolytic pathways treatments contemplated herein can affect both metabolic pathways.

The invention belongs to the field of anti-arteriosclerosis drugs, and particularly relates to application of a carbonic anhydrase inhibitor to preparation of the anti-arteriosclerosis drugs. The study finds for the first time that carbonic anhydrase 1 (CA1) is highly expressed in arteriosclerosis calcified tissue, and CA1 is related to vascular smooth muscle calcification and affects cell proliferation and apoptosis. Methazolamide, the inhibitor of CA1, can significantly reduce the progression of atherosclerosis and inhibit atherosclerotic inflammatory factors. The results suggest that calcification plays an important role in atherosclerosis, and CA1-dominated calcification promotes the course of the atherosclerosis. Methazolamide has a potential therapeutic effect on the atherosclerosisby inhibiting expression of CA1. The findings not only further explain the close relationship between the atherosclerosis and the calcification, but also explore the calcification mechanism of the atherosclerosis, and further prove that inhibition of the calcification is a key point in the treatment of the atherosclerosis. The application of the carbonic anhydrase inhibitor to the preparation of the anti-arteriosclerosis drugs provides new ideas for the treatment of the atherosclerosis.

Provided is a technology for suppressing discoloration of a halo-isoquinoline derivative-containing aqueous composition during high-temperature storage. Provided is an aqueous composition containing a compound of formula (1):

Novel fluorinated benzenesulfonamides compounds of general formula (I)

can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.

The present invention relates in general to the use of amphiphilic graft-type copolymers of polyaspartamide for the ophthalmic administration of drugs, such as for example steroidal and non-steroidal anti-inflammatory agents, antimicrobial agents such as aminoglycosides, macrolides, cephalosporin, tetracycline, quinolones, penicillin, beta-lactams, anti-glaucoma agents such as prostaglandins, alpha- and beta-blockers, inhibitors of carbonic anhydrase, cannabinoids, antiviral agents, diagnostic agents, anti-angiogenic agents, antioxidants.

A stable liposomal formulation for ocular delivery of a carbonic anhydrase inhibitor. The formulation contains (i) a liposome that includes a lipid bilayer formed of a phosphatidylcholine, and (ii) a carbonic anhydrase inhibitor encapsulated in the liposome. Also provided is a method for treating an ocular disorder with the formulation.

The present invention falls within the field of biomedicine. Specifically, the present invention relates to the use of carbonic anhydrase II for the manufacture of a medicament for the prevention and/or treatment of the damage caused by ischemia, ischemia followed by reperfusion or toxins, acute failure or rejection of a transplanted organ, preferably the kidney. In a preferred embodiment, the toxin is cisplatin.

This invention relates to methods of treating mammals at risk or affected by spinal cord edema by administering a carbonic anhydrase inhibitor that crosses the blood-spinal cord barrier. Among the conditions treated are, but not limited to, spinal cord injury, spinal cord tumors and vascular malformations, spinal infections, transverse myelitis, multiple sclerosis, syringomyelia and the pre-syrinx state.

The present invention provides a process of manufacturing a sterile, ophthalmic pharmaceutical suspension comprising sterile active ingredient(s) such as sterile carbonic anhydrase inhibitors (CAIs) wherein the process does not involve the use of any special equipment's such as ball mill, milling bottle and/or jet mill The present process is simple, cost effective and efficient.

The present invention provides an ophthalmic composition comprising a hyperbranched polymer. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polymer increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as polysorbate, hydroxypropyl methyl cellulose or hydroxyethyl cellulose, and beta-blockers, such as carteolol, levobunolol, betaxolol, metipranolol, timolol or propranolol.

The invention discloses a thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and a preparation method thereof. In the inhibitor, a natural small-molecule inhibitor with a sulfonamide group is modified onto thermosensitive cyclodextrin with temperature response, an inhibitory effect on carbonic anhydrase is achieved through the sulfonamide group, and the reversible regulation of the activity of carbonic anhydrase is achieved through the thermosensitive effect of an alkoxy ether chain. When temperature is below a phase-transition temperature, the alkoxy ether chain stretches, the sulfonamide group can have good supramolecular interaction with carbonic anhydrase, and thereby the activity of carbonic anhydrase is inhibited. When temperature is above the phase-transition temperature, because the alkoxy ether chain is dehydrated to collapse to generate powerful steric resistance, destroying the supramolecular interaction between the sulfonamide group and carbonic anhydrase, and thereby the activity of the enzyme recovers again. Moreover, compared with other carbonic anhydrase inhibitors, the thermosensitive cyclodextrin-based carbonic anhydrase inhibitor is lower in toxicity and wider in resource, thus having high application value in the field of biomedical materials.

The invention relates to an acetazolamide derivative, a preparation method thereof and an application of the acetazolamide derivative in preparation of a medicine for treating coronary heart disease.The acetazolamide derivative is an acetazolamide derivative I obtained by bonding a carbonic anhydrase inhibitor acetazolamide Ac and a non-steroidal anti-inflammatory drug which is represented by aspirin As and has a carboxylic acid group through a linking group, and the structural general formula is shown as a formula 1 shown in the specification, wherein in the formula 1, OOC-NSAID represents anon-steroidal anti-inflammatory drug in which one carboxylic acid proton is lost, representative are acetazolamide derivatives containing aspirin or indomethacin, and the acetazolamide derivative I has good activity of inhibiting carbonic anhydrase 9, can effectively improve myocardial anoxia injury in an anoxia microenvironment, and is applied to preparation of the medicine for treating coronaryheart disease.