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38 results about "Histamine Receptor Antagonists" patented technology

Nanoparticulate ebastine formulations

The invention is directed to compositions comprising at least one nanoparticulate H1-histamine receptor antagonist, such as ebastine or a salt or derivative thereof, having improved dissolution rate providing a faster onset of drug availability. The nanoparticulate H1-histamine receptor antagonist particles, such as ebastine, have an effective average particle size of less than about 2000 nm and are useful in the treatment of seasonal and perennial allergic rhinitis and related diseases.
Owner:ELAN PHRMA INT LTD

Compositions and methods for treatment of viral and bacterial infections

Compositions and methods are presented that are useful for treatment of viral and / or bacterial infections, and especially the common cold or flu. Particularly preferred combinations include those orally administered, preferably early in the course of the symptoms of the cold or flu, and comprising (a) an H2-histamine receptor antagonist and (b) acetaminophen, NSAID, or other anti-pyretic, analgesic agent.
Owner:EDALATPOUR NASROLA

Novel piperidine derivative

Provided are a histamine-H3 receptor antagonist; and a preventive and / or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute / congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit / hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific group; X3 represents Os—(CH2)m; R1 and R2 independently represent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
Owner:MSD KK

Use of Histamine H4 antagonist for the treatment of post-operative adhesions

The present invention includes methods for the inhibition of post-operative adhesion formation between tissue surfaces in a body cavity having been subjected to a surgical procedure, which methods involve administering a histamine H4 receptor antagonist, systemically, directly to tissue surfaces in the body cavity, or both, and to delivery vehicles and compositions suitable for use for local, non-systemic administration of a drug to the body and directly to tissue within a body cavity having been subjected to a surgical procedure.
Owner:JANSSEN PHARMA NV

Suspension composition for treating oral mucositis caused by chemoradiotherapy

InactiveCN102319208AGood dispersionProlongs the duration of action of anti-inflammatory and analgesicDigestive systemSolution deliveryClinical efficacyAnaerobic bacteria
The present invention discloses a suspension composition for treating oral mucositis caused by chemoradiotherapy, and relates to a new drug for treating oral mucositis. The suspension composition comprises: 1, local anesthetics; 2, histamine 1 receptor antagonists; 3, a mucosal repairing agent and a drug dispersing agent; 4, an anti-foaming agent; 5, microcrystalline cellulose; 6, unreactive assistant materials; 7, pure water. The preparation method comprises: 1, preparing a solution I; 2, preparing a solution II; 3, adding the solution I to the solution II at a stirring state, completely stirring, adjusting the pH value of the mixed solution to 6-9 to obtain the suspension composition. According to the present invention, the suspension composition provided by the present invention has characteristics of good uniformity and strong stability, is not easy to agglomerate when the suspension composition is placed for a long time; the preparation method has characteristics of simple process and low production cost; the suspension composition can be applicable for treating the oral mucositis caused by the chemoradiotherapy, and severe mouth ulcers caused by anaerobic bacteria; the suspension composition provides effects of analgesia, inflammation eliminating and mucosa repairing; the clinical efficacy of the suspension composition is obvious; the use of the suspension composition is convenient and safe.
Owner:何雪心 +1

Histamine h3 receptor agents, preparation and therapeutic uses

The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
Owner:ELI LILLY & CO

Histamine H3 receptor antagonists

Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
Owner:HIGH POINT PHARMA

Novel usage of rice, rice bran, or chaff extract as histamine receptor antagonist

InactiveCN103561755APrevent or improve sleep disordersNervous disorderDigestive systemNausea sicknessSide effect
Disclosed is a novel use of rice, rice bran or rice hull extract as a histamine receptor antagonist. The rice, rice bran or rice hull extract may be used as a natural antihistamine to prevent or treat allergic rhinitis, inflammatory bowel disease, asthma, bronchitis, nausea, gastric and duodenal ulcer, gastroesophageal reflux disease, sleep disorder, anxiety and depression. It provides comparable or better effect of decreasing sleep latency, increasing sleep duration and increasing non-REM sleep as compared to diazepam, which is currently used as sleeping drug. Derived from the natural product rice, rice bran or rice hull, it has no side effect such as cognitive impairment, resistance or dependency even after long-term use.
Owner:KOREA FOOD RES INST

Histamine-3 receptor ligands for diabetic conditions

The invention relates to a method of treating a diabetic condition by administering a therapeutically effective amount of a histamine-3 receptor antagonist, including benzofuran and benzopyran derivatives of formula (I), aminoalkoxybiphenylcarboxamide compounds of formula (III), and aminoetherbiphenyl compounds of formula (IV) as described herein.
Owner:HANCOCK ARTHUR A +5

Novel oxidation method for preparing alcaftadine

The invention relates to a novel oxidation method for preparing a histamine H1 receptor antagonist--alcaftadine. The method comprises the step of using a Dess-Martin periodinane as an oxidation reagent to oxidize an intermediate--6,11-dihydro-11-(1-methyl-4-piperidylidene)-5H-imidazo[2,1-b][3]benzazepine-3- methanol so as to obtain the alcaftadine. The novel oxidation method for preparing the alcaftadine is simplified and has the advantages of simple operation, environment-friendly process, cheap and easily-available raw materials and reagents, high yield and more applicability to industrial production.
Owner:WUHAN WUYAO SCI & TECH

Histamine h3 receptor agents, preparation and therapeutic uses

InactiveUS20070208024A1Selective and high affinity bindingHigh affinityBiocideNervous disorderHistamine Receptor AntagonistsTreatment use
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
Owner:ELI LILLY & CO

Ophthalmic compositions and methods of use

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.
Owner:OCUGEN INC

Antiflatulents in combination with histamine H1-receptor antagonists for treating gastrointestinal disorders

InactiveCN1761460ABacteria material medical ingredientsDigestive systemDiseaseHistamine H1 Receptor Antagonists
Compositions and methods for providing relief from pain and / or discomfort associated with gastrointestinal disorders, including, for example, bloating, crying, gas, cramping, regurgitation, diarrhea and gastrointestinal pain, associated with colic comprising, at least one antiflatulent, at least one histamine H1-receptor antagonist, and optionally,one or more prebiotic and / or one or more probiotic.
Owner:LIFESCAPE BIOSCIENCE INC

Methods of preventing and treating hypoglycemia in type 1 and type 2 diabetes patients

Disclosed are methods for increasing glucagon secretion in response to exogenous insulin-induced hypoglycemia in patients with type 1 or type 2 diabetes. Also disclosed are methods of increasing glucagon secretion, and thus preventing or treating hypoglycemia, in patients with insulin producing tumors. The methods include administering a therapeutic amount of a histamine 1 receptor antagonist, a histamine 3 receptor antagonist, and / or a combination histamine 1 / 3 receptor antagonist. It may also be further advantageous to administer a therapeutic amount of a serotonin receptor antagonist in the methods disclosed herein.
Owner:FEROX THERAPEUTICS LLC

A substituted fused imidazole ring compound and its pharmaceutical composition

The invention relates to a substituted condensed imidazole ring compound, a composition containing the compound and applications thereof. Specifically, the invention discloses a fused imidazole ring compound represented by formula (), or a pharmaceutical composition of its crystal form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate or solvate. The compound of the present invention can be used as a histamine H1-receptor antagonist and a mast cell stabilizer, which can inhibit the release of histamine from mast cells and prevent the action of histamine, thereby alleviating allergic reactions. Formula (I).
Owner:SHENZHEN TARGETRX INC

Use of anti-histaminics for acute reduction of elevated intracranial pressure

The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and / or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. The novel compounds comprise compounds according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. Also claimed is the novel use of commercially available histamine H1-and H2-receptor antagonists for the reduction of intracranial pressure (ICP).
Owner:JANSSEN PHARMA NV

L-setastine hydrochloride and preparation method thereof

The present invention relates to the field of medicine, and disclosed are an L-setastine hydrochloride and a preparation method therefor. The compound of the present invention has the advantages of stronger histamine Hi receptor antagonism and small side effect; the yield of the preparation method is more than 80%, and the product purity is high. The present invention also provides an application of the compound as an H1 histamine receptor antagonist.
Owner:ANHUI QINGYUN PHARMA & CHEM

2-(1H-4(5)-imidazoyl cyclopropyl derivatives

The present invention provides compounds having H3 histamine receptor antagonist activity of formula (1.0) wherein R2 is a hydrogen or a methyl or ethyl group; R3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) phenyl or substituted pneyly; (c) alkyl; (d) heterocyclic; (e) decahydronaphthalene; and (f) octahydroindene; with the proviso that when X is H, A can be -CH2CH2, -COCH2-CON(CH3)-, -CH=CH-, alpha , -CH2-NH-, -CH3-N(CH3)-, -CH(OH)CH2-, -NH-CH2-, -N(CH3)-CH2-, -CH2O-, -CH2S-, and -NHCOO-; when X is NH2, HN(CH3), N(CH3)2, OH, OCH3, CH3, SH and SCH3; A can be -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=XH-, -COCH2-, -CH2CH2-, -CH( )H)CH2-, or beta ; and when R1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure, X can be NH, O, or S. The pharmaceutically acceptable salts, hydrates, and individual stereoisomers of compounds of structural formula (1.0), as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of said formula and a method of treating conditions in which antagonism of histamine H3 receptors may be of therapeutic importance.
Owner:GLIATECH

Roxatidine acetate hydrochloride tablets and preparation method thereof

InactiveCN105616366AImprove toleranceNo anti-androgenic effectOrganic active ingredientsDigestive systemAspiration PneumonitisReflux esophagitis
The invention relates to roxatidine acetate hydrochloride tablets and a preparation method thereof. A main material comprises roxatidine acetate hydrochloride, and an auxiliary material comprises a filler, a disintegrating agent, an adhesive and a lubricant, wherein the raw materials in weight percentage are 20-50% of the main material, 15-60% of the filler, 5-30% of the disintegrating agent, 0.1-20% of the adhesive, and 0.01-3% of the lubricant. A roxatidine acetate hydrochloride tablets histamine H2 acceptor antagonist has the advantages of long-acting, good tolerance, and no anti-male hormone effect, has no harm to drug metabolism for liver, can be used for treating gastric ulcer, duodenal ulcer, marginal ulcer, zollinger-ellison syndrome, and reflux esophagitis, and can be used for administration before anaesthesia so as to prevent aspiration pneumonia, the tablets are prepared, the preparation method is easy and simple to be carried out, and is suitable for industrial production.
Owner:HEILONGJIANG ZHICHENG MEDICAL TECH
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