35 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.

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.

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.

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 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.

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).

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 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 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.

Histamine receptor antagonists are administered to delay the onset of or prevent heat stroke in mammals. H2 receptor antagonists including cimetidine, famotidine, nizatidine, and ranitidine are administered to the mammals prior to the exposure of the mammal to stress conditions, such as temperature, environmental, drug, exercise, or combinations thereof. The explosive temperature rise and precipitous mean arterial pressure crash seen in untreated subjects were delayed 2.6 fold (p<0.05) in H2 receptor antagonist-treated animals. The results teach that these antihistamines and acid reducers can increase tolerance to heat stress and may potentially increase survival to heat stress induced by environmental, drug related, or exercise and heat induced stress in athletes, military, and workers required to work in extreme temperature environments.

The present invention relates to the selective histamine H3 receptor antagonists/inverse agonists 1-[4-(4-{3-[(2R)-2-methylpyrrolidin-1-yl]-propoxy}-phenoxy)-piperidin-1-yl]-ethan-1-on, its pharmaceutically acceptable salts, derivatives, pharmaceutical compositions, active metabolites and combinations for use in the treatment of symptoms of autism spectrum disorder (ASD).