43 results about "Diazoxide" patented technology

The present invention is directed to therapeutic compounds, treatment methods, and kits affecting the NCCa-ATP channel of neural tissue, including neurons, glia and blood vessels within the nervous system, and methods of using same. The NCCa-ATP channel is newly expressed in neural tissue following injury such as ischemia, and is regulated by the sulfonylurea receptor SUR1, being inhibited by sulfonylurea compounds, e.g., glibenclamide and tolbutamide, and opened by diazoxide. Antagonists of the NCCa-ATP channel, including SUR1 antagonists, are useful in the prevention, diminution, and treatment of injured or diseased neural tissue, including astrocytes, neurons and capillary endothelial cells, that is due to ischemia, tissue trauma, brain swelling and increased tissue pressure, or other forms of brain or spinal cord disease or injury. Agonists of the NCCa-ATP channel may be are useful in the treatment neural tissue where damage or destruction of the tissue, such as a gliotic capsule, is desired.

Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.

The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analog, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

The present invention relates to the use of an effective amount of at least one potassium KvI.3 channel inhibitor or of an effective amount of at least one compound having in addition to its potassium KvI.3 channel inhibiting properties also CBx modulating properties and / or potassium K(atp) channel opening properties for the manufacture of a medicament for the prophylaxis, treatment, delayed progression, delayed onset and / or inhibition of various medical conditions in subjects in need thereof . The diseases are obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity , asthma, glucose metabolism - in particular, insulin resistance, hyperglycaem ea and / or glucose intolerance - neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripher al vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration , pain - including neuropathic pain and chronic pain - and impotence. The compounds are a.o. 4, 5-dihydropyrazole derivatives, imidazole derivatives, diazoxide, NN414, R(+) -WIN55212-2, HU-308, Rimonaband, SR-147778.

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and / or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

The invention relates to a synthetic method of diazoxide (I). The synthetic method comprises the following steps of (a) carrying out catalytic hydrogenation reduction on 5-chlorine-2-nitrobenzenesulfonamide (II) in a solvent A through raney nickel so as to obtain 5-chlorine-2-aminobenzenesul fonamide (III), wherein the reduction reaction temperature ranges from 20 to 40 DEG C, the reduction reaction pressure ranges from 3 to 10kg / cm<2>, and the reduction reaction time ranges from 3 to 5 hours; (b) acetylizing the 5-chlorine-2-aminobenzenesul fonamide (III) in a solvent B through an acylation reagent with the existence of an inorganic substance acid-binding agent, carrying out ring-closure reaction on a product in a high-boiling-point inert solvent C, and obtaining a diazoxide (I) crude product, wherein the acetylation reaction temperature ranges from 0 to 30 DEG C, the acetylation time ranges from 2 to 10 hours, the ring-closure reaction temperature ranges from 240 to 250 DEG C, and the ring-closure reaction time ranges from 0.5 to 1.5 hours; (c) refining the diazoxide (I) crude product through ethyl alcohol with the concentration being 80 percent, and obtaining a diazoxide (I) finished product.

The invention discloses a method for preparing diazoxide, which comprises anthranilamide and N ‑chlorosuccinimide is reacted in a chlorine solvent to obtain 2‑amino‑5‑chlorobenzenesulfonamide, and 2‑amino‑5‑chlorobenzenesulfonamide, imidazolium salt and amide solvent are mixed and reacted by heating to obtain di Azrazine; or anthranilamide, imidazolium salt and amide solvent are mixed and reacted by heating to obtain compound IV; then compound IV and N - Chloro-succinimide is reacted in a chlorine solvent to obtain diazoxide; the invention also discloses the application of imidazole hydrochloride as a catalyst in the preparation of diazoxide. The invention avoids the problems of using highly corrosive and highly toxic chlorosulfonyl isocyanate, strong acid (sulfuric acid) and high reaction temperature (240-250°C) in the reaction process, and the reaction steps are short; the total yield of the two steps can be It reaches more than 90%, and compared with the preparation method of diazoxide that has been publicly reported, the synthetic route provided by the present invention overcomes many shortcomings, so it is more suitable for industrial production.