92 results about "Increased orotic acid" patented technology

The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.

The invention discloses a solid-phase synthesis method of degarelix. The solid-phase synthesis method of degarelix comprises the following steps: on the basis of taking Fmoc-amino resin as a solid-phase carrier, replacing orotic acid fragments connected with an alanine benzene ring in the fifth site and an amino in the fourth site with ivdde, and performing sequential condensation reaction from the end C to the end N so as to connect 10 protected amino acids, thereby obtaining a full-protective peptide resin; then removing the Fmoc protecting group of end N D-Nal, acetylating by using acetic anhydride and pyridine, replacing ivDde with Hor, cutting the peptide resin by using a splitting agent, and precipitating by using frozen diethyl ether to obtain crude peptide. Besides, the invention also relates to a method for synthesizing a raw material Fmoc-Aph(ivDde)-OH by use of ivDde-OH and Fmoc-Aph-OH. The solid-phase synthesis method of degarelix has the advantages that the ivDde is introduced to synthesize decapeptide firstly and then the Hor is used as a substitute to avoid a rearrangement side reaction; the solid-phase synthesis method is simple in process steps, easy to control, low in influence on a human body and the environment, high in yield, and suitable for large-scale production.

The invention relates to synthesis and a crystal form-transforming method of taltirelin. An intermediate S-1-methyl-4,5-dihydro-orotic acid is synthesized by using L-asparagine as a starting material and through Friedel-Crafts acylation, esterification, methylation and hydrogenation; His(Trt)-Pro-NH2 is prepared by reacting Fmoc-His(Trt)-OH with Pro-NH2 and deprotecting; a taltirelin salt crude product is obtained by carrying out condensation reaction on S-1-methyl-4,5-dihydro-orotic acid and His(Trt)-Pro-NH2, adding trifluoroacetic acid, stirring, adding a crystallization solvent, stirring, suction filtering and washing; taltirelin is obtained by purifying, desalting and freeze-drying; and beta-taltirelin is obtained by adding taltirelin into pure water for dissolution and crystallization, adding methanol, stirring, crystallizing and suction-filtering. Racemization of a final product in medium test amplification is effectively controlled in the reaction processes; product purity is high; production security is guaranteed; and the synthesis and crystal form-transforming method are suitable for large-scale amplified production.

The process of producing orotic acid includes the preparation of 5-bromo-2,6-dioxy-hexahydropyrimidine-4-carboxylic acid by using raw material including sodium bromide, chlorine and maleoyl carbamide, reaction of the obtained product with sodium hydroxide, acidification to obtain raw orotic acid and refining with concentrated ammonia water. The sodium bromide may be reused. The process has low cost, less corrosino of material to equipment and less environmental pollution and the prepared orotic acid may be used in production of cosmetics and medicine and research of biochemistry.

The invention relates to the field of foods, in particular to an alginate oligomer dairy capable of reducing cholesterol. The dairy disclosed by the invention contains alginate oligomers of which the mass percentage is 1-10%, and the molecular weight scope of the alginate oligomers is 2000-3000Da. The level of serum cholesterol can be obviously reduced by restraining the absorption of cholesterol by small intestines. After the alginate oligomers are prepared into the diary disclosed by the invention, the alginate oligomers are easier to absorb, and the diary has better effects of reducing the content of the cholesterol and the content of triglyceride in blood than a general dairy and initial alginate oligomer powder. Besides, the alginate oligomers interact with orotic acid in the dairy to restrain a reaction of synthesizing the cholesterol by livers and restrain the absorption of cholesterol by small intestines, so that the content of the cholesterol and the content of the triglyceride in the blood can be obviously reduced by the alginate oligomer dairy.

Pyrimidine nucleotide precursors including acyl derivatives of cytidine, uridine, and orotate, and uridine phosphorylase inhibitors, and their use in enhancing resistance to sepsis or systemic inflammation are disclosed.

New polymorphs of 5-amino or substituted amino 1,2,3-triazole and substituted derivatives thereof, of orotates of the carboxyamidotriazoles, of formulations of the triazoles and orotic acid in the ratio of 1:1 to 1:4 (base:acid) and of safer processes of the preparation of the same are disclosed. The compounds are useful in the control and treatment of diseases including, but not limited to solid cancers, macular degeneration, retinopathy, chronic myeloid leukemia, AIDS and diseases which rely on aberrant signal transduction. The improved processes to prepare the orotate formulations use stable, efficient and safer starting azide intermediate materials in the synthesis of new polymorphs of carboxyamidotriazole.

The invention discloses a method for combined production of chiral hydroxy ester and uridine phosphinylideyne compounds. In the method, orotic acid and beta-ketone ester compounds are used as substrates, glucose is used as an energy supplier, and yeast cells with permeability are used to prepare uridine phosphinylideyne compounds and chiral hydroxy ester at the same time. Based on the theory of full cell catalysis and metabolism engineering, the method uses the yeast cells with permeability to realize the combined production of the chiral hydroxy ester and the uridine phosphinylideyne compounds by establishing a metabolism network model and the metabolism flow rate analysis, so that the method has the advantages of improving yield, lowering production cost, shortening synthesis time and greatly improving the utilization ratio of the substrates.

The invention discloses an esterified podophyllum derivative with antitumor activity and a preparation method and the usage of the esterified podophyllum derivative. The esterified podophyllum derivative with antitumor activity and shown as a formula (V) is obtained by means of esterification reaction of adamantine formic acid, orotic acid, 4-(pyrimidine sulfo) phenylacetic acid, cyclohexane carboxylic acid, 3,4-dimethoxy benzoic acid, 2-butoxycarbonyl-3-phenylalanine or 4-methoxy phenylacetic acid with podophyllotoxin or 4'-demethyl-epipodophyllotoxin. The esterified podophyllum derivative has multi-way multi-target actions on tumor cells to achieve better antitumor curative effects. According to in-vitro cell viability inhibition tests, the esterified podophyllum derivative has excellent antitumor activity and low toxic and side effects and can be prepared into antitumor drugs to be applied to antitumor treatment.

Food supplements comprising Tribulus terrestris extract, folic acid and an orotic acid or a derivative thereof. The food supplements optionally, but preferably, include effective amounts of nutrients selected from the group consisting of Vitamin A, Vitamin E, Vitamin C, Vitamin B1, Vitamin B2, Vitamin B6, Vitamin B12 and combinations thereof. The food supplements are suitable for supplementing the diet of an athlete, for decreasing body fat and increasing strength, lean muscle mass and endurance.

The invention belongs to the field of chemical synthesis, and relates to a preparation method for orotic acid. The preparation method for the orotic acid comprises the following steps: 1) synthesizing carbamyl aspartate; 2) synthesizing hydantoin ethanoic acid on the basis of the carbamyl aspartate obtained in the step 1); 3) synthesizing carboxyl methyl hydantoin on the basis of the hydantoin ethanoic acid obtained in the step 2); 4) synthesizing orotic acid on the basis of the carboxyl methyl hydantoin obtained in the step 3. The invention aims to provide the preparation method for the orotic acid with short process route, simple raw materials, good selectivity and high yield, and the reaction is performed in an opening system.

The invention discloses a nutrient composition and application thereof in preparation of medicines for treating aplastic anemia. The nutrient composition is prepared from the following components according to ratios: lysine, methionine, phenylalanine, threonine, tryptophan, arginine, histidine, glycine, aspartic acid, leucine, isoleucine, valine, serine, glutamine, taurine, orotic acid, nucleotide, vitamin A, vitamin D, vitamin B2, vitamin B6, vitamin B12, niacin, folic acid, vitamin C, iron, zinc, manganese, copper, selenium, chromium, potassium, calcium, magnesium, inositol and granulesten. Aplastic anemia body can be comprehensively repaired, so that an effect of treating aplastic anemia is achieved.

The present invention describes compounds produced from an orotic acid molecule and an amino acid molecule. The compounds being in the form of amino acid orotate compounds bound by an amide linkage and produced by one of two disclosed methods; 1) reacting orotic acid or derivatives thereof with a thionyl halide, and then combining the acyl halide with an amino acid in the presence of dichloromethane and a DMAP catalyst; or 2) protecting the carboxylic acid of an amino acid and then combining the amino acid with a DCC activated orotic acid, followed by removal of the carboxylic acid protecting group. The resulting amino acid orotate amide has an enhanced stability in solution as compared to a related ester. In addition, specific benefits are conferred by the particular amino acid used to form the compounds in addition to, and separate from, the orotate substituent.

L-arginine, citrulline and pyrimidine derivatives including orotic acid, uridine, uridine 5'-monophosphate (UMP), cytidine and cytidine 5'-monophosphate (CMP) are produced using a bacterium belonging to the genus Escherichia harboring a mutant carbamoylphosphate synthetase in which the amino acid sequence corresponding to positions from 947 to 951 in a wild type carbamoylphosphate synthetase is replaced with any one of amino acid sequences of SEQ ID NOS: 1 to 9, and feedback inhibition by uridine 5'-monophosphate in the bacterium is desensitized.

The invention provides a novel diabetic kidney lesion detection kit, which can identify early-stage patients more sensitively, accurately, simply, conveniently and noninvasively by being compared withtraditional indexes, and can be used as one of novel clinical auxiliary diagnosis means. According to the invention, a UPLC-ESI-MS/MS (ultra-high performance liquid chromatography-electrospray ionization tandem mass spectrometry) method is used; nine novel serum metabolic markers that are related to early diabetic nephropathy and include hexadecanoic acid, delinoleic acid, azoxystrobin acid, lysophosphatidylcholine (20:4), piperidine, 6-methylmercaptopurine, 6-aminocaproic acid, L-hydrogenated orotic acid and cumin are screened out. Preliminary research data show that the group of metabolitescan diagnose patients with or without early diabetic kidney lesion through single or combined detection, a basis is provided for early intervention treatment of clinicians, and the occurrence of nephropathy at the final stage is reduced to the greatest extent.

The invention relates to a method for synthesizing a persantine intermediate 2,4,6,8-tetrahydroxy pyrimido[5,4-d] pyrimidine, comprising the following steps of: (1) adding nitro orotic acid in an alkali liquid, then hydrogenating with Ni/H2, and filtering to obtain an amino orotic acid solution which is directly used for next reaction without separation; (2) adjusting pH of the amino orotic acid solution with concentrated hydrochloric acid to 3, adding sodium cyanate for temperature control reaction to obtain the urea derivatives of the amino orotic acid; then dropping a 30% sodium hydroxide solution to adjust pH to 13, heating for cyclization, dropping a 50-60% sulfuric acid solution to adjust pH to 3; (3) cooling to room temperature, filtering, washing to neutrality and drying to obtain the product. The intermediate of step (1) is not needed to separate, thereby saving a lot of time and labor, reducing about 50% of total reaction time with mild reaction condition and maximum reaction temperature reduced to 95 DEG C so that the device is less required and more durable.

The invention discloses an improved synthesis method of orotic acid and belongs to the field of organic chemical synthesis. The improved synthesis method comprises the following steps: heating a watersolution of hydantoin, glyoxylic acid and sodium hydroxide in a specific micro-channel reactor and reacting to obtain an orotic acid crude product; after refining the crude product, obtaining an orotic acid pure product. According to the improved synthesis method, a whole production process is carried out in the micro-channel reactor, so that the reaction conversion rate and the yield are improved and the reaction yield reaches 90 percent or above.

The invention discloses a novel technology with an introduced catalyst to optimize the synthesis of dipyridamole, and belongs to the technical field of medical intermediates. According to the technology, in the step of oxidizing a methyl group of 6-methyl uracil into formic acid, a Co(OAc)2/HOAc/AIBN/O2 catalytic system is introduced, and the reaction yield is increased to 90 to 95%. In the step of reducing a nitro group of nitro-orotic acid into an amino group, activated copper powder is taken as the catalyst, the yield is more than 85%; and moreover, the environmental pollution and danger caused by sodium hydrosulfite are avoided. In the step of converting substituted hydroxyl group into substituted chlorine, SOCl12 and N,N-dimethyl formamide are introduced into the reaction system so as to reduce the environment pollution and the difficulty of post treatment. In the reactions of preparing 2,6-dichloro-4,8-bis(piperidine-1-yl)pyrimido[5,4-d]pyrimidine from perchloro pyrimido[5,4-d]pyrimidine, a CuI/PhNO2 catalytic system is introduced into the reaction system, the reaction yield reaches 95%, moreover, the operation is easy, and the treatment is simple. The provided technology increases the yield, reduces the cost, guarantees the safety, saves the energy, and meets the requirements of green reactions and modern chemical production.

The invention discloses a nutrition compound and application in preparing a drug for promoting stem cell proliferation. The nutrition compound is prepared from the following materials in proportion: lysine, methionine, phenylalanine, threonine, tryptophan, arginine, histidine, glycine, aspartic acid, leucine, isoleucine, valine, serine, glutamine, taurine, orotic acid, nucleotide, Vitamin A, Vitamin D, Vitamin B2, Vitamin B6, Vitamin B12, niacin, folic acid, Vitamin C, iron, zinc, manganese, copper, selenium, chromium, potassium, calcium, magnesium, inositol and granulesten. The nutrition compound has the effects of boosting the proliferation of hematopoietic stem cells, liver stem cells, mesenchymal stem cells, kidney stem cells and gastric mucosa stem cells. The nutrition compound can be used for preparing the drug for promoting stem cell proliferation, is free from toxic and side effect and can avoid various problems caused by introduction of exogenous stem cells for treating diseases.

The invention comprises a composition of inosine and orotic acid or a salt thereof, and its methods of use in treating, maintaining and enhancing the health of the heart, and specifically the integrity of the myocardium. The effective combination of inosine and orotic acid/orotate effectively improves various medical parameters that are widely used to assess cardiac function and structure. These include EKG and VCG recordings, quantitative assessments of work capacity and athletic performance, clinically relevant observations, and direct biochemical, histological and ultrastructural analyses. The observations and controlled studies in mice, rats, rabbits, cardiology patients and high performance human athletes (cyclists) consistently support the effectiveness of the combination of inosine and orotic acid/orotate in both preventing and reversing damage to the myocardium resulting from physical stress.

The invention provides a plurality of recombinant microorganisms for producing orotic acid and a method thereof. The recombinant microbial strains have one or more or all of the following characteristics: (1) the synthesis of phosphoribosyltransferase or orotic acid nucleoside monophosphate decarboxylase in an orotic acid metabolic pathway is weakened or completely lost; (2) a corresponding enzymeamount is increased through overexpression of five genes of enzymes participating in the orotic acid synthesis route; and (3) the corresponding transport protein is increased by overexpression of a transport protein coding gene for intracellular transport of orotic acid.