95 results about "Xanthine oxidase inhibitor" patented technology

A novel 1,2,4-triazole compound which is useful as a therapeutic agent for hyperuricemia and gout due to hyperuricemia is provided. A compound is represented by the following general formula (1):wherein R2 represents an unsubstituted or substituted pyridyl group, R1 represents a similar pyridyl group, a pyridine-N-oxide group corresponding to these pyridyl groups, or a phenyl group, and R3 represents hydrogen or a lower alkyl group substituted with pivaloyloxy group and R3 bonds to a nitrogen atom in the ring. A process for production of a compound by reacting a nitrile and a hydrazide, and a therapeutic agent, particularly a xanthine oxidase inhibitor are also provided.

A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the 10 method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a 13 receptor blocker; an imidazoline receptor antagonist; a centrally acting tx receptor antagonist; a peripherally acting ct receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduce SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

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

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%.

A novel 1,2,4-triazole compound which is useful as a therapeutic agent for hyperuricemia and gout due to hyperuricemia is provided. A compound is represented by the following general formula (1): wherein R2 represents an unsubstituted or substituted pyridyl group, R1 represents a similar pyridyl group, a pyridine-N-oxide group corresponding to these pyridyl groups, or a phenyl group, and R3 represents hydrogen or a lower alkyl group substituted with pivaloyloxy group and R3 bonds to a nitrogen atom in the ring. A process for production of a compound by reacting a nitrile and a hydrazide, and a therapeutic agent, particularly a xanthine oxidase inhibitor are also provided.

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.

The present invention relates to methods of preserving renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.

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 relates to a xanthine oxidase inhibitor for treating gout and a preparation method thereof. The preparation method for the xanthine oxidase inhibitor comprises the following steps of: 1) weighing 5.9 to 28.6 mass percent of hovenia dulcis thumb, 7.1 to 33.3 mass percent of lesser galangal root, 7.1 to 33.3 mass percent of fruit of princesplume ladysthumb, 7.1 to 33.3 mass percent ofliquoric root and 7.1 to 33.3 mass percent of pueraria flower; and 2) putting the medicinal materials weighed in the step 1) into a flask, adding 60 to 90 mass percent of ethanol in an amount which is 8 to 10 times the mass of the medicinal materials, refluxing and extracting for 30 to 50 minutes, filtering extracting solution for 3 times, mixing filtrate for 3 times, concentrating the filtrate and drying to form dry extract. The xanthine oxidase inhibitor has the advantages that: ethanol extract is an effective part of compound inhibitory xanthine oxidase, so a Chinese medicinal compound preparation prepared from the effective part has higher activity of the inhibitory xanthine oxidase, and is a competitive inhibitor.

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.

Disclosed are a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein R1 is selected from H, halogen, C1-2 alkyl, substituted C1-2 alkyl, and C1-2 alkoxy, and R1 is CH3 when ring A is pentabasic monocyclic heteroaryl; R2 is CN, I, C1, Br, -CF3, or -OCH3; R3 is H or D; ring A is thiazole, selenazole, oxazole, or pyridine; ring E is formula (A), (B), or (C); G1 is selected from O or NRa; G2, G3, and G4 are independently selected from -CRa or -CRbRc; Ra is selected from H, deuterium, halogen, C1-6 alkyl, or substituted C1-6 alkyl, and Ra does not comprise deuterium or halogen when Ra is connected to N; Rb and Rc are each independently selected from H, deuterium, halogen, C1-4 alkyl, or substituted C1-4 alkyl; and optionally Rb and Rc may cyclize to form C3-7 membered cycloalkyl or substituted C3-7 membered cycloalkyl. The compound or pharmaceutically acceptable salt thereof is used to prepare drugs for preventing or treating hyperuricemia, gout, diabetic nephropathy, inflammatory diseases, and neurological diseases.

A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a β receptor blocker; an imidazoline receptor antagonist; a centrally acting α receptor antagonist; a peripherally acting α receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

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.

The present invention relates to methods of preserving or increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. The present invention also relates to methods of increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.

The present invention relates to methods of preserving or increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. The present invention also relates to methods of increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.

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 B cell epitope for xanthine oxidase and an antigen peptide containing the epitope. The antigen peptide is prepared by the following steps: B cell epitope for xanthine oxidase is connected to a linear B cell epitope FEYQD which is at a membrane-proximal region of insulinoma-associated protein-2 by a flexible peptide in a series connection, and a terminal is connected to a N terminal of Th2 auxiliary epitope P2 of P277 by a flexible peptide in a series connection. Serum which is obtained by immunization of mice with the antigen peptide is detected by Western blot, results show that an antibody which is specifically combined with xanthine oxidase is generated, and the antigen peptide is used for detecting xanthine oxidase; serum of the mice which are immunized by the antigen peptide can be used for inhibiting exogenous activity of xanthine oxidase, the difference between the inhibition rate of xanthine oxidase and the inhibition rate of allopurinol is not substantial (P>0.5), and the serum can be used for preparing xanthine oxidase inhibitor; the antigen peptide is used for treating gout, hepatopathy, nephrosis, atherosclerotic, diabetes, senile dementia, eye diseases, cardiovascular diseases, and other diseases due to xanthine oxidase abnormity, uric acid abnormity and oxidative stress disorder with important theoretical values and wide application prospects.

The invention relates to compounds of the following formula (I) or their salts: in which R1 is a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, carboxyl, halogen, hydroxyl, nitro, or cyano; R2 is cyano, nitro, or the like; R3 is hydroxyl or the like; X is oxygen, sulfur, or the like; and Y is oxygen or sulfur, and a xanthine oxidase inhibitor containing the compound.

The invention discloses application of a digallate derivative which has a formula (I) and a pharmaceutically acceptable salt thereof to preparation of a medicine for treating hyperuricemia. The digallate derivative has a strong effect of inhibiting xanthine oxidase in vitro, can be used for reducing the level of serum uric acid of a mouse with hyperuricemia significantly, is dose dependent and can be used for treating hyperuricemia and gout or gout complications caused by hyperuricemia as a potential xanthine oxidase inhibitor and a potential uric acid lowering medicine.

The invention provides a topiroxostat tablet and a preparation method thereof, and belongs to the technical field of medicines. The topiroxostat tablet is mainly prepared from a main drug, filler, a disintegrating agent, an adhesive and a lubricant. Topiroxostat is a non-purine selective xanthine oxidase inhibitor, and is used for treating gout and hyperuricemia. The topiroxostat tablet is safe and effective, has the advantages of quick disintegration, good solubility, stable quality, high bioavailability and low cost, is convenient to take, and can be used for improving the compliance of patients.

The invention belongs to the technical field of pharmaceutical and chemical industry and discloses nitrogen-substituted phenyl pyrazole xanthine oxidoreductase inhibitor and preparation and application thereof. The nitrogen-substituted phenyl pyrazole xanthine oxidoreductase inhibitor has a structural formula shown as in formula (I), wherein each of R1 and R2 independently represents hydrogen or C1-C6 alkyl, or R1, R2 and nitrogen atoms connecting R1 and R2 together form monocyclic nitrogen-bearing heterocyclic group having 3-6 carbon atoms, R3 is nitryl or cyano, and R4 is hydrogen, methyl or trifluoromethyl. The compound of formula (I) prepared herein has a chemical structure different from that of known xanthine oxidoreductase inhibitors, and a new route to prepare anti-hyperuricemia or gout drugs is provided.

The invention discloses novel application of artemisia selengensis leaf extract, raspberry extract and compositions thereof to preparation of xanthine oxidase inhibitors. The invention further provides a composition with the xanthine oxidase inhibitory activity. In the composition, a mass ratio of the artemisia selengensis leaf extract to raspberry extract is (1-10):1, preferably 8:1. According tothe application in the invention, a feasible novel pathway is provided for clinic treatment of hyperuricemia, the artemisia selengensis leaf extract and the raspberry extract serving as food sourceshave high safety, the application range of the artemisia selengensis and raspberry is widened, intensive processing and utilization are promoted, and additional values of the raw materials are increased.

The invention discloses application of caulis polygoni multiflori aqueous extracts or extracting paste or amylase to the preparation of medicine for treating glucose tolerance lack, diabetes, adiposity, hyperuricemia or uarthritis. The invention also discloses the application of aqueous extracts or extracting paste prepared from caulis polygoni multiflori and sargentg loryvine according to a weight ratio of 1 / 1 to the preparation of medicine for treating glucose tolerance lack, diabetes, adiposity, hyperuricemia or uarthritis. The invention is obtained through sieving from 70 kinds of traditional Chinese medicine and 16 kinds of compositions which do not have the hyperglycemic, blood uric acid reduction, alpha-glucosaccharase inhabiting agents and xanthine oxidase inhabiting agents till now, and consists of the caulis polygoni multiflori or the caulis polygoni multiflori and the sargentg loryvine. The invention discovers the inhabiting effects on the alpha-glucosaccharase and the xanthine oxidase for the first time.

The invention discloses combined application of gallnut catechin or catechin gallate or gallnut catechin gallate and salt capable of being pharmaceutically accepted and gallic acid to treating hyperuricemia. A catechin compound has the strong in-vitro inhibition effect on xanthine oxidase, the serum uric acid level of a mouse suffering from hyperuricemia can be obviously reduced, and the catechin compound can serve as a potential xanthine oxidase inhibitor and a uric acid reduction medicine to be used for treating hyperuricemia and gout or gout complications caused by hyperuricemia.

The invention relates to the field of drug screening, particularly a method for simultaneously screening a superoxide anion remover and a xanthine oxidase inhibitor. The method comprises the following steps: adding a fluorescent probe into a reaction system composed of a compound to be detected, a substrate and a target protein, reacting the probe with the superoxide anion for some time to generate a specific product 2-OH-E+, terminating the reaction by a proper process, carrying out quantitative analysis on uric acid and the 2-OH-E+ generated in the reaction system by using a high-performance liquid phase-mass spectrometer coupling technique, and identifying the structure of the compound. The changes of the contents of the uric acid and 2-OH-E+ before and after the reaction between the xanthine oxidase or superoxide anion are detected to analyze the inhibition rate of the natural product extract or monomeric compound xanthine oxidase or the clearance rate of the superoxide anion.

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 present invention provides a new apigenin derivative having a selective xanthine oxidase inhibition effect and represented by a formula I, or a pharmaceutically acceptable salt thereof, wherein R is H or C1-C5 straight or branched chain alkyl, and n is an integer from 1-10. The formula I is defined in the specification.