145 results about "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 present invention relates generally to the method of increasing the oral bioavailability, reducing chemotherapy induced toxicity and side effects, and improving the effectiveness of pharmaceutical agents that are poorly absorbed from the gastrointestinal tract. Specifically, the invention relates to poorly absorbed pharmaceutical drugs and converting them to orotate salts. The orotate salts of the drugs can be dosed at lower doses to provide the efficacy benefits of a higher dose, while reducing the drugs' toxic effects at lower doses. Additionally, the orotate salts of pharmaceutical agents have better clearance and reduce the potential for drug-induced hepatic toxicity. Therefore, an especially useful formulation of the orotate salt of the pharmaceutical agent can provide rapid and consistent action using a lower dose while reducing drug interactions and side-effects.

Provided herein are methods and compositions for use in the treatment of depression, anxiety or a depressive or anxiety-related disorder. Embodiments describe the administration of orotic acid or a salt thereof, or the administration of one or more probiotic microorganisms, or administration of a combination of orotic acid or a salt thereof and one or more probiotic microorganisms.

An L-amino acid is produced by culturing a microorganism which belongs to the family Enterobacteriaceae and is able to produce an L-amino acid, wherein the bacterium has been modified to enhance orotate phosphoribosyltransferase activity is enhanced, in a medium to produce and cause accumulation of an L-amino acid in the medium or cells, and collecting the L-amino acid from the medium or the cells.

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.

Pharmaceutical compositions comprising compounds of the formula where R1, R2, and R3 are described here, have therapeutic utility in selectively inhibiting P. falciparum dihydroorotate dehydrogenase. Accordingly, such compositions have use in the treatment and prevention of malaria.

The invention discloses a 5-aminoorotic acid dinuclear cadmium complex. The 5-aminoorotic acid dinuclear cadmium complex is characterized in that the complex is prepared from a cadmium salt, an orotic acid derivative and 2,2'-bipyridine through a hydrothermal method; the complex has a definite space structure and an accurate molecular formula; and synthesis steps are simple. The constitutional unit of the complex comprises two metallic cadmium ions, two 5-aminoorotic acids, one oxalate ions, two 2,2'-bipyridines, two coordination water molecules and four object water molecules; the molecular formula of the complex is C32H36N10O18Cd2; the complex belongs to a triclinic system; the space group of the complex is P-1; and cell parameters are that a is equal to 8.8941 angstrom, b is equal to 9.2338 angstrom, c is equal to 13.759 angstrom, alpha is equal to 97.978 DEG, beta is equal to 97.975 DEG and gamma is equal to 116.416 DEG. The prepared complex is a purple fluorescent material, has excellent physicochemical performance and shows wide application prospects in the field of photoelectric materials or catalytic materials.

The present disclosure relates generally to compositions and methods to provide probiotic supplements useful for the therapeutic and / or prophylactic treatment, amelioration and / or regulation of disease states or pathological conditions. More specifically the present disclosure relates to compositions comprising at least one probiotic microorganism, optionally in combination with one or more of orotic acid or a salt thereof, carnitine and / or coenzyme Q10, and to uses of such compositions for the treatment or prevention of fatigue, for promoting synthesis of adenosine triphosphate (ATP), for muscle repair and the treatment of muscle degeneration, muscle aches and inflammation, and / or for boosting energy levels, by improving mitochondrial function.

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.

The invention relates to a thiazole derivative used as a DHODH restrainer and an application thereof. Specifically, the invention relates to a compound shown as formula I, a drug compound containing the compound shown as formula I and the application of the compound in preparing the drug for treating DHODH mediated diseases or restraining DHODH.

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 discloses a method for preparing citicoline through biological enzyme catalysis. The method is characterized by comprising the steps that a single artificially-transformed gene engineering strain is used as an enzyme source, an ammonium chloride catalyst, orotic acid, choline phosphate and other chemical substances are subjected to a reaction to generate citicoline, and then the citicoline is extracted from the reaction solution. Compared with the prior art, single strain is adopted for fermentation, the production technology is simple, the production period is short, the production cost is low, and the method for preparing citicoline through biological enzyme catalysis can be widely applied to industrial production of citicoline.

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.

This invention is in the field of chemical restructuring of pharmaceutical agents known to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the anthracyclines, doxorubicin and daunorubicin, that are found to reduce levels of the pharmaceutical agent in noncancerous tissues. These orotate derivatives are equally efficacious in inhibiting the SCCAKI-1 kidney tumor in animals and the reduction in the heart tissue of doxorubicin compared with doxorubicin HCl suggests a reduction in toxicity induced by free radical generation by the anthracyclines.

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.

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 present invention is related to a method for the fermentative production of glycolic acid, its derivatives or precursors, comprising the culture of an Escherichia coli strain in an appropriate culture medium comprising a carbon source, and the recovery of glycolic acid in the medium, wherein said E. coli strain is modified to improve the conversion of orotate into orotidine 5′-P.The invention is also related to the modified E. coli strain, showing an improved conversion of orotate into orotidine 5′-P, and optionally that was furthermore modified for an improved glycolic acid production.

This invention is in the field of chemical restructuring of pharmaceutical agents known to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the anthracyclines, doxorubicin and daunorubicin, that are found to reduce levels of the pharmaceutical agent in noncancerous tissues. There orotate derivatives are equally efficacious in inhibiting the SCCAKI-1 kidney tumor in animals and the reduction in the heart tissue of doxorubicin compared with doxorubicin HCl suggests a reduction in toxicity induced by free radical generation by the anthrracyclines.

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.

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 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.

The invention discloses a method for catalyzing and synthesizing uridine phosphinylidyne compound in an oriented way; the method takes uridine or saratin and phosphate radical ion as substrate as well as glucose as ribose radical donor and energy donor, utilizes microbial cells with permeability as enzyme source, and promotes the reaction system to biologically catalyzing and synthesizing the uridine phosphinylidyne compound in an oriented way by means of changing reaction temperature and dissolved oxygen periodically. According to the demand, the method can be used for producing any of three matters, and the reaction system is simple, nontoxic, production cost is low and control method is easy, so that the production control in industrialization is facilitated. When the uridine is used as substrate, the yields of UMP, UTP and UDPG are respectively 77%, 67% and 61%; when the saratin is used as substrate, the yields of UMP, UTP and UDPG are respectively 70%, 61% and 53%.

The invention discloses a one-step fermentation method for producing gamatine through microorganism. A non-pathogenic microorganism is adopted to directly convert a carbon source and a nitrogen source to the gamatine through fermentation, and the produced gamatine can be further prepared into salt, such as sulfate, hydrochloride, phosphate, nitrate and orotic acid salt which are used as nutritious supplements, so that the method has a wide industrial application prospect. The microorganism used in the method comprises corynebacterium glutamicum constructed through gene engineering and preserved with the preservation number of CGMCC (China General Microbiological Culture Collection Center) No. 12601 in General Microbiology Center of China Committee for Culture Collection of Microorganisms.

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 discloses a preparation method of citicoline. The method comprises the following steps: the culture of a single gene engineering bacterium or the treatment material of the culture is used as enzyme source to catalyze the reaction of a substrate comprising ammonium chloride, orotic acid and phosphocholine and ensure that citicoline is generated and accumulated in the reaction solution, and citicoline is extracted from the reaction solution. The invention has the following beneficial effects: (1) the single microorganism is utilized to catalyze the reaction, reaction conditions are easy to control; (2) the cost of the substrate is lower so that the production cost of citicoline is lower; and (3) the reaction is fast and the conversion rate is higher. The method can be widely used in the preparation of citicoline.

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 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.

New salts of Meldonium, the method of their preparation, and pharmaceutical formulation on their basis have been described. The general formula of these salts is X−(CH3)3N+NHCH2CH2COOH where X− is an acid anion selected from the group of pharmaceutically acceptable acids. Practically non-hygroscopic and / or increased thermal stability and / or lasting action Meldonium hydrogen salts of fumaric acid, phosphoric acid, oxalic acid, maleic acid, and pamoic acid as well as Meldonium orotate and galactarate are especially suitable. Novel pharmaceutical formulations containing non-hygroscopic and / or increased thermal stability and / or and / or lasting action 3-(2,2,2-trimethylhydrazinium) propionate salts for oral parenteral, rectal, and transdermal introduction are concurrently described.