151 results about "Monoamine oxidase inhibitor" patented technology

The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

The present disclosure relates to novel dosage forms of xanthine oxidoreductase inhibitors.

The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

The invention provides a method for screening a xanthine oxidase inhibitor by ultra performance liquid chromatography and mass spectrometry. The method is used for analyzing the in-vitro inhibition rate of the extract or monomer of a natural product on the xanthine oxidase and the catalytic activity of the xanthine oxidase. By using the ultra performance liquid chromatography-mass spectrometry in the xanthine oxidase inhibitor screening, the method is rapid and accurate in sample detection, and the correlation coefficients of the linear equation reaches 0.998. The mass spectrometry has high accuracy and good specificity in detecting the mass electron ratio of a compound, and can be used for screening the xanthine oxidase inhibitor and for the kinetic study of the xanthine oxidase inhibitor without false positive and false negative results which occur in the spectrometry. The results showed that the inhibition rate I of 20 mumol/L allopurinol is 80%; the inhibition rate of 20 mumol/L isorhamnetin is 73%; the inhibition rate of 20 mumol/L genistein is 50%; and the inhibition rate of 0.1 mg/mL aqueous extract of Ginkgo biloba is 27%.

The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

The invention relates to application of arachidonic acid as a xanthine oxidase inhibitor and in the preparation of medicines for treating hyperuricemia or gout. Xanthine oxidase is a key enzyme for the generation and the development of the hyperuricemia or the gout, most substrates of the xanthine oxidase are cyclic small molecules, and the arachidonic acid is long chain polyunsaturated fatty acid; a three dimensional structure of the xanthine oxidase is downloaded from a protein data bank (PDB) of a website; a three dimensional structure of the arachidonic acid is downloaded from a pubchem; molecular docking between the arachidonic acid and the xanthine oxidase is performed by iGEMDOCK software and docking energy is computed; and in-vitro enzyme activity tests prove that the arachidonic acid has an inhibition effect on the xanthine oxidase. By the application, another important physiological function of the arachidonic acid is discovered, and a wider way is provided for screening the xanthine oxidase inhibitor from a natural product to treat the hyperuricemia or the gout simultaneously.

A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.

Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.

The invention discloses a method for fast screening a xanthine oxidase inhibitor or a superoxide anion scavenging agent by utilizing a coupling technique of thin-layer chromatography and bioautography. According to the method, the thin-layer chromatography is combined with biological activity assay, a superoxide anion free radical (O2<.->) generated by an enzymatic reaction reacts with nitroblue tetrazolium (NBT) to generate formazan which is a bluish violet insoluble substance, and substances capable of inhibiting xanthine oxidase or scavenging superoxide anion inhibit the reaction so yellow and/or white spots under a purple background show on a thin layer plate. The method is suitable for analyzing the in-vitro inhibition activity to the the xanthine oxidase or the scavenging activity to the superoxide anion of natural drugs and/or traditional Chinese medicine extracts or monomeric compounds.

The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A_2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, a monoamine oxidase inhibitor, a 5-HT₂ antagonist or the like), and the like.

The invention belongs to the technical field of medicine and relates to 2-(3-cyano/nitro-4-substituted phenyl)-4-methyl-2(i)H(/i)-1,2,3-triazole-4-methane acid and formyl hydrazine compounds shown in the formula I, medicinal salt and medicinal solvate and a preparation method thereof. The substituent definition of the compounds is defined as claim books and manuals. The invention further relates to application of the compounds in preparation of medicine for treatment of hyperuricemia and gout diseases.

Compositions containing monoamine oxidase inhibitors prepared by removal of alcohol from agave-derived beverages are disclosed.

8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.

The invention discloses a stilbene coumarin derivative as well as a preparation method and an application thereof, and relates to the technical field of medicine synthesis. The structure general formula of the stilbene coumarin derivative is shown in formula (1) which is specified in the description. The synthesis process disclosed by the invention has the characteristics of being simple and practicable in reaction, and high in product yield; moreover, the synthesised stilbene coumarin derivative is good in inhibitory activity and selectivity on anthropogenic monoamine oxidases (hMAO-A and hMAO-B), and therefore can be used for preparing a monoamine oxidase inhibitor.

Methods for preventing or treating bruxism, including alleviating or eliminating one or more symptoms, diseases or conditions associated with or resulting from bruxism, using dopaminergic agents such as monoamine oxidase inhibitors that increase dopaminergic activity and dopamine agonists, are disclosed.

The invention discloses a xanthine oxidase inhibitor and application thereof. The xanthine oxidase inhibitor is a compound shown as a general formula (I) and is a pharmaceutically acceptable salt. The xanthine oxidase inhibitor, which is the compound and the pharmaceutically acceptable salt, can be applied to preparation of the xanthine oxidase inhibitor and particularly applied to preparation of medicines for preventing or treating hypeluricemia diseases, gout or diabetic nephropathy.

The invention discloses an xanthine oxidase inhibitor containing phenylalanine and application thereof to preparation of drugs for preventing and treating hyperuricemia and gout diseases. The inhibitor contains one or more of polypeptide FH, FK, FVR or LFW; the four kinds of polypeptide can be obtained by being separated from skipjack proteolytic liquid, ethyl alcohol is added into skipjack zymolyte and subjected to centrifugal separation, the supernatant liquid is taken, concentrated and subjected to spray drying, and a skipjack zymolyte alcohol soluble component is obtained; the alcohol soluble component is separated through Sephadex G-15, and finally separated through UPLC (ultra performance liquid chromatography), and the four kinds of polypeptide is obtained. The four kinds of polypeptide can be chemically synthesized, and also can be prepared directionally from the skipjack enzymatic product. The four polypeptide has the very good xanthine oxidase inhibiting activity, therefore can directly serve as a lead compound to conduct modification treatment and be applied to health-caring food or drugs for preventing and curing hyperuricemia and gout diseases.