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43 results about "Diazoxide" patented technology

This medication is used to treat very low blood sugar (hypoglycemia).

Novel non-selective cation channel in neuronal cells and methods for treating brain swelling

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.
Owner:U S GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS

Salts of potassium ATP channel openers and uses thereof

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.
Owner:ESSENTIALIS INC

Composition, synthesis and therapeutic applications of polyamines

InactiveUS20050085555A1Chromium concentration were decreasedIncrease excretionBiocideGroup 5/15 element organic compoundsAntidoteRisk stroke
This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists / partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicty of neutoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure.
Owner:MURPHY MICHAEL A

Salts of potassium atp channel openers and uses thereof

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.
Owner:ESSENTIALIS INC

Salts of potassium atp channel openers and uses thereof

InactiveUS20090062264A1Inhibit and prevent progressionReducing insulin dosingMetabolism disorderDigestive systemDiseasePotassium channel opener
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.
Owner:ESSENTIALIS INC

Salts of potassium atp channel openers and uses thereof

InactiveUS20120238554A1Inhibit and prevent progressionReducing insulin dosingOrganic chemistryMetabolism disorderDiseasePotassium
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.
Owner:ESSENTIALIS INC

Compounds for the Treatment of Inflammation of the Central Nervous System

InactiveUS20070254871A1Antibacterial agentsNervous disorderBenzothiadiazinesTriazole antifungals
KATP channel openers (KCOs) are useful for the prophylactic and / or therapeutic treatment of CNS chronic inflammation associated with a disease or state in a mammal, including a human. The administration of KCOs, including the groups of benzopirans, cyanoguanidines, thioformamides, benzothiadiazines, pyridyl nitrates, pyrimidine sulfates, cyclobutenediones, DHP-related compounds, tertiary carbinols, 6-sulfonil-chromenes, 1,2,3-triazoles, pyridothiadiazines, benzothiazines, halogenquinazolins and phenylbenzimidazoles, and in particular, the compound diazoxide, result in a reduction of reactive microglial response in various CNS pathologies such as axonal injury, brain tumors, traumatic damage, neurodegeneration, spinal cord injury, infectious and autoimmune diseases. KCOs, isotopically modified, are also useful for the preparation of diagnostic agents for detection and follow-up of CNS chronic inflammation.
Owner:NEUROTEC PHARMA

Diazoxide For Use In The Treatment Of Amyotrophic Lateral Sclerosis (ALS)

The invention relates to the diazoxide or a pharmaceutically acceptable salt thereof for use as a medicament at low doses to treat amyotrophic lateral sclerosis.
Owner:NEUROTEC PHARMA

Small molecule inhibitors targeted at Bcl-2

The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and / or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2 / Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
Owner:RGT UNIV OF MICHIGAN +1

Novel non-selective cation channel in neuronal cells and method for treating brain swelling

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.
Owner:UNIV OF MARYLAND

Organic preserving solution and its preparation method

InactiveCN101167450ASlow down biochemical reactionsDelay dissipationDead animal preservationSodium lactateMannitol
The invention belongs to the technology of medical biology and relates to organ preservative fluid and the method for making same. The procedure to prepare 1000ml of the fluid is as follows, tetrahydrobiopterin 1.57mg and diazoxide 6.92mg are dissolved in 1ml of dimethyl sulfoxide to act as mother liquid, CaCl2 of 0.1mol / L is prepared for backup, double distilled water 800ml is charged in a container of 1000ml, KCl 1.12g, MgCl2 2.64g, manna sugar 10.93g, histidine 4.63g, glutathion 0.92g and glutavene 3.74g are sequentially charged and agitated to limpidity, 6.90ml of sodium lactate is charged and agitated to limpidity, CaCl2 2.5ml of 0.1mol / L is charged and agitated to limpidity, and backup liquid and mother liquid are charged and agitated to limpidity. The pH is adjusted to 7.3-7.5, the osmotic pressure is adjusted to 320Osm / L, and the volume of double distilled water is set to 1000ml. The fluid is stored in low temperature of 4 DEG C.
Owner:ZHEJIANG UNIV

Use of a combination of diazoxide and metformin for treating obesity or obesity related disorders

The present invention relates to a method for suppressing the fasting plasma insulin level and / or postabsorptive insulin level in a mammal in need thereof, said method comprising administering to said mammal a pharmaceutically effective amount of a combination of a potassium channel activator and an anti-diabetic drug. The present invention also relates to a method for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising administering to said mammal a pharmaceutically effective amount of a combination of a potassium channel activator and an anti-diabetic drug.
Owner:COOP MIRZORG U A ARNHEM

Salts of potassium atp channel openers and uses thereof

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.
Owner:ESSENTIALIS INC

Salts of potassium ATP channel openers and uses thereof

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.
Owner:ESSENTIALIS INC

Method of treatment of retinal ischemia with diazoxide

A composition including diazoxide (7-chloro-3-methyl-2H-1,2,4-benzothiadiazine-1,1-dioxide) for the treatment and / or prevention of retinal ischemia and of diseases associated with retinal ischemia. The composition can also contain riluzole, a derivative active in neuroprotection of the latter, or a pharmaceutically acceptable salt of the latter.
Owner:CENT NAT DE LA RECHERCHE SCI +1

Method of treatment of retinal ischemia with diazoxide

A composition including diazoxide (7-chloro-3-methyl-2H-1,2,4-benzothiadiazine-1,1-dioxide) for the treatment and / or prevention of retinal ischemia and of diseases associated with retinal ischemia. The composition can also contain riluzole, a derivative active in neuroprotection of the latter, or a pharmaceutically acceptable salt of the latter.
Owner:CENT NAT DE LA RECHERCHE SCI +1

Use of monoamine oxidase inhibitors to improve epithelial biology

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.
Owner:PROCTER & GAMBLE CO

Diazoxide For Use In The Treatment Or Prevention Of A Central Nervous System (CNS) Autoimmune Demyelinating Disease

InactiveUS20130039905A1Improving clinical manifestationNervous disorderAntibody ingredientsNervous systemAutoimmunity
The invention relates to the use of diazoxide or a pharmaceutically acceptable salt thereof at low doses to treat a CNS autoimmune demyelinating disease selected from selected from multiple sclerosis (MS), clinically isolated syndrome (CIS), tumefactive (tumor-like) M S, Marburg's acute M S, Balós's concentric sclerosis, acute disseminated encephalomyelitis (ADEM), post-vaccinal encephalitis (PVE), post-infectious encephalomyelitis (PIE) and neuromyelitis optica (NMO).
Owner:NEUROTEC PHARMA

Therapeutic polyamine compositions and their synthesis

InactiveUS20140057877A1Chromium concentration were decreasedIncrease excretionBiocideCopper organic compoundsAntidoteRisk stroke
This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists / partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be utilized to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure.
Owner:MURPHY MICHAEL A +1

Method for preparing diazoxide

The invention discloses a method for preparing diazoxide. The method comprises the following steps: reacting o-aminobenzenesulfonamide with N-chlorosuccinimide in a chlorine solvent to obtain 2-amino-5-chlorobenzenesulfonamide, mixing the 2-amino-5-chlorobenzenesulfonamide, an imidazolium salt and an amide solvent, and heating the obtained mixture to react to obtain the diazoxide; or mixing o-aminobenzenesulfonamide, the imidazolium salt and the amide solvent, heating for a reaction to obtain a compound IV, and reacting the compound IV with N-chlorosuccinimide in the chlorine solvent so as toobtain the diazoxide. The invention also discloses an application of imidazole hydrochloride as a catalyst in the preparation of diazoxide. The method avoids the problems that chlorosulfonyl isocyanate and strong acid (sulfuric acid) which have high corrosivity and toxicity are used in the reaction process and the reaction temperature is high (240-250 DEG C), and the reaction steps are short; thetotal yield of the two steps can reach 90% or above; and compared with publicly reported diazoxide preparation methods, the synthesis method of the invention overcomes numerous defects, so that the synthesis method is suitable for industrial production.
Owner:SUZHOU UNIV

Use of diazoxide for suppressing the plasma insulin level in a mammal

The present invention relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and / or postabsorptive insulin level in a mammal in need thereof, wherein the fasting and / or postabsorptive plasma insulin level is reduced to about 5 mU / l or less. The present invention also relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and / or postabsorptive insulin level in a mammal in need thereof for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising orally administering to said mammal in need thereof a daily dosage of about 5 mg to about 1200 mg, calculated on a Diazoxide active weight basis.
Owner:COOP MIRZORG U A ARNHEM

Diazoxide for use in the treatment of a central nervous system (CNS) autoimmune demyelinating disease

The invention relates to the use of diazoxide or a pharmaceutically acceptable salt thereof at low doses to treat a CNS autoimmune demyelinating disease selected from selected from multiple sclerosis (MS), clinically isolated syndrome (CIS), tumefactive (tumor-like) MS, Marburg's acute MS, Bal?s's concentric sclerosis, acute disseminated encephalomyelitis (ADEM), post-vaccinal encephalitis (PVE), post-infectious encephalomyelitis (PIE) and neuromyelitis optica (NMO).
Owner:NEUROTEC PHARMA

Organic preserving solution and its preparation method

The invention belongs to medical biology technology, and relates to an organ preservation solution and its preparation. According to the preparation steps per 1000ml, it comprises: taking 1.57mg of tetrahydrobiopterin and 6.92mg of diazoxide and dissolving them in 1ml of dimethyl sulfoxide As a mother liquor; prepare 0.1mol / L CaCl210ml for later use; add 800ml double distilled water into a 1000ml container, add KCl 1.12g, MgCl22.64g, mannitol 10.93g, histidine 4.63g, glutathione 0.92g, Sodium glutamate 3.74g, stir until clear; add sodium lactate 6.90ml, stir until clear; add 0.1mol / L CaCl22.5ml, stir until clear; add stock solution and mother liquor, stir until clear. The pH was adjusted to 7.3-7.5, the osmotic pressure was adjusted to 320Osm / L, and the volume was adjusted to 1000ml with double distilled water. Store at 4°C for low temperature storage.
Owner:ZHEJIANG UNIV

The synthetic method of diazoxide

InactiveCN106831648BChemical reaction diagramOrganic chemistrySynthesis methodsReaction temperature
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.
Owner:北京同济达药业有限公司

Application of potassium ATP channel regulator in preparation of medicine for resisting diabetic nephropathy

The invention discloses a novel pharmaceutical application of a potassium ATP channel regulator, namely application of the potassium ATP channel regulator (such as diazoxide, crocarine, pinadil, niacdil, alplecarine and the like) in preparation of a medicine for resisting diabetic nephropathy. The invention further provides application of a pharmaceutical composition taking the potassium ATP channel regulator as an active ingredient in prevention or treatment of diabetic nephropathy. A diabetic rat is modeled through streptozotocin (STZ), high fat diet is given to the rat after modeling to form the diabetic nephropathy, whether the rat enters the diabetic nephropathy or not is detected by taking microalbuminuria (mALB) as an index, and whether the model succeeds or not is observed by taking the weight and blood sugar level of the rat as indexes. Experimental results show that after the potassium ATP channel opener such as diazoxide is administered to the diabetic rat, the renal injury process of the diabetic rat can be delayed.
Owner:HANGZHOU QIAN BIOTECHNOLOGY LTD

Diazoxide for the treatment of Friedreich's Ataxia

A pharmaceutical preparation treats Friedreich's ataxia and treats or prevents pathologies related thereto. In particular, the pharaceutical preparation concerns the use of diazoxide or 7-chloro-3-methyl-4H-1,2,4 benzothiadiazine 1,1-dioxide, in combination with glucose and / or leucine, for the treatment of Friedreich's ataxia (FRDA) and for the treatment or prevention of pathologies related thereto.
Owner:UNIV DEGLI STUDI DI BARI
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