38 results about "Histamine Receptor Antagonists" patented technology

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.

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.

This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain non-imidazole tertiary amine derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.

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.

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.

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.

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.

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.

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.

The present invention includes methods for treating allergic conditions involving the airway by administering histamine receptor antagonists.

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.

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.

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

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.

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.

The present invention provides new method of treatment of Parkinson's disease, obstructive sleep apnea, narcolepsy, dementia with Lewy bodies, vascular dementia with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.

The invention relate to a liquid oral pharmaceutical dosage form, comprising a) pharmacologically effective amounts of at least one histamine H2-receptor antagonist in a hydrophobic / lipophilic liquidsubstantially free from water and b) pharmacologically effective amounts of at least one antacid, wherein a) and b) are physically separated from each other, a package comprising multiple liquid oraldosage forms as well as a method of treating a gastric disease or disorder by use of the liquid oral pharmaceutical dosage form.

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.

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).

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).

Provided are compositions and methods comprising a MAChR antagonist / inverse agonist / partial agonist and a histamine H3 receptor antagonist / inverse agonist / partial agonist for increasing proliferation Oligodendrocyte Progenitor Cells (OPCs) into mature, myelinating oligodendrocytes, and related methods of treating demyelination disorders.

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.

The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using 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. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently —(C1—C7) alkyl (optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence —H, -halogen, or —CH3.

The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.

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.

The present invention relates to physically and chemically stable salts of the selective histamine preceptor antagonist compound of l-[4-(4-{3-[(2R)-2-methyl-pyrrolidin-l-yl]-propoxy}-phenoxy)- piperidin-l-yl]-ethanone of formula (1) and / or polymorphs thereof and / or hydrates / solvates thereof, the process for the preparation thereof, pharmaceutical compositions comprising them, and for use in the treatment and / or prevention of conditions requiring the modulation of histamine H3 receptors (e.g. Alzheimer's disease, obesity, schizophrenia, miochardial ischaemia, migraine, autism spectrum disorder).

This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.

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.