146 results about "Glutethimide" patented technology

PCT No. PCT / JP95 / 01994 Sec. 371 Date Sep. 8, 1997 Sec. 102(e) Date Sep. 8, 1997 PCT Filed Sep. 29, 1995 PCT Pub. No. WO96 / 10089 PCT Pub. Date Apr. 4, 1996A process for modifying a physiologically active peptide or a physiologically active protein which comprises reacting a physiologically active peptide or a physiologically active protein having at least a glutamine residue with a substance having an amino donor in the presence of a transglutaminase originating in a microorganism to thereby form an acid amide bond at the gamma -position acid amide group of the glutamine residue with the amino group of the amino donor; and the product of modification obtained thereby.

PCT No. PCT / JP96 / 02503 Sec. 371 Date Mar. 2, 1998 Sec. 102(e) Date Mar. 2, 1998 PCT Filed Sep. 4, 1996 PCT Pub. No. WO97 / 08946 PCT Pub. Date Mar. 13, 1997The present invention aims to provide a medium composition for in vitro fertilization, in particular, a composition usable in the culture of ova or early embryos which are fertilized eggs, the preparation or culture of sperm, and the pre-treatment of ova or sperm. The composition comprises, as its essential components, L-phenylalanine, L-tryptophan, L-lysine, L-threonine, L-valine, L-methionine, L-isoleucine, L-leucine, L-proline, glycine, L-alanine, L-tyrosine, L-histidine, L-arginine, L-taurine, L-aspartic acid, L-serine, L-asparagine, L-glutamic acid, L-glutamine and L-cystine, provided that at least a part of the L-cystine may be replaced by L-cysteine.

An inhibitor of a glutaminyl peptide cyclotransferase, and use thereof for the treatment and / or prevention of a disease or disorder selected from the group consisting of inflammatory diseases selected froma. neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, Familial Danish Dementia, multiple sclerosis,b. chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis,c. fibrosis, e.g. lung fibrosis, liver fibrosis, renal fibrosis,d. cancer, e.g. cancer / hemangioendothelioma proliferation, gastric carcinomas,e. metabolic diseases, e.g. hypertension,f. and other inflammatory diseases, e.g. neuropathic pain, graft rejection / graft failure / graft vasculopathy, HIV infections / AIDS, gestosis, tuberous sclerosis.Additionally disclosed are a respective diagnostic method, assay and kit.

The invention discloses a cultivated method of nervous stem cells, it includes following steps:1, Nervous stem cells substrate of human being is made up of base cultivate liquid which is compounded by mixing DMEM and F12 by rate of 1:1, and insulin, muriatic acid butyl amic, selenium natrium, ydrogen cortisone, L-glutamic acyl amic, man-turn iron albumen, flavone; 2, Noumenon serum of patient themselves is gathered immediately; 3. Noumenon serum of patient themselves is put into compounded Nervous stem cells substrate of human being, them, it is incubated by adding 3-7% CO2 warmer under conditino of 35C-38C. The method of the invention is simple, and invention has better repetition and its operation is simple and convenient; it plays an inestimable part in researching, teaching, clinic application, etc all of which relate to nervous stem cell and its application.

Novel site-specific mono-conjugates of Granulocyte Colony Stimulating Factor (G-CSF) are hereby described, with analogues and derivatives thereof, which stimulate proliferation and differentiation of progenitor cells to mature neutrophiles. These conjugates have been obtained using transglutaminase to covalently and site-specifically bind a hydrophilic, non-immunogenic polymer to a single glutamine residue of the human G-CSF native sequence and analogues thereof. These novel site-specific mono-conjugated derivatives are recommended for therapeutic use since they are stable in solution and exhibit significant biological activity in vitro and a longer bloodstream half-life, as compared to the non-conjugated protein, with a consequent prolonged pharmacological activity.

A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I with an alkylating agent of structure III in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

A ‘bioactive’ composition that has one or more oligogalacturonans ((1→4)-α-D-galacturonan) or any other oligosaccharides (oligoguluronans) that may present an ‘egg box’ conformation, this conformation being further stabilized by one or more polycationic saccharide(s), preferably either a chitosan oligosaccharide or a chitosan polysaccharide. A method prepares this composition and it is used, in medical, pharmaceutical, agricultural, nutraceutical, food, feed, textile, cosmetic, industrial and / or environmental applications.

The invention is methods and related kits for diagnosing a disease state of cachexia by measuring biomarker profiles from a biological sample. Rapid measurement of early onset or progression of the disease in a subject is determined by measuring biomarker levels from the subject and optionally comparing the biomarker levels to a standard biomarker profile or metabolome phase portrait for the disease. The biomarkers measured in the assay and related kit for cachexia progression include biomarkers selected from the group consisting of lactate, citrate, formate, acetoacetate, 3-hydroxy butrate, alanine, glutamine, glutamate, valine, isoleucine leucine, thrionine, lysine, arginine, tyrosine, phenyl alanine, histidine and tryptophan.

The present invention relates to methods and assays for identifying agents capable of inhibiting the mutant huntingtin protein, inhibiting or reducing cell death, in particular cell death associated with polyglutamine-induced protein aggregation, which inhibition is useful in the prevention, amelioration and / or treatment of neurodegenerative diseases, and Huntington's disease more generally. In particular, the present invention provides methods and assays for identifying agents for use in the prevention and / or treatment of Huntingtons disease. The invention provides polypeptide and nucleic acid TARGETs and siRNA sequences based on these TARGETS.

The invention discloses a novel orally-effective spirulina source antihypertensive peptide and a preparation method thereof. The antihypertensive peptide is a tripeptide with the sequence of isoleucine-glutamine-proline (Ile-Gln-Pro, IQP). An angiotensin converting enzyme (ACE) inhibitory peptide is prepared by the following steps of: performing enzymolysis on spirulina platensis by adopting alkali protease, and performing ultrafiltration, gel filtration chromatography and secondary reversed phase high-performance liquid chromatography purification. Tests prove that the IQP is a noncompetitive inhibitor of ACE, and can keep good ACE inhibitory activity under digestion of main gastrointestinal protease. The IQP has good antihypertensive effect on essential hypertension rat (SHR) and has great application prospects in medicaments and functional foods for preventing and treating hypertension.

Amino acid compositions which contain 10 to 40 parts by weight of L-arginine, 10 to 40 parts by weight of L-glutamine, 5 to 20 parts by weight of L-valine, 8 to 30 parts by weight of L-isoleucine, and 10 to 35 parts by weight of L-leucine may be taken orally and are effective for reducing body fat without dietary restrictions and exercise.

The invention relates to a composition with antialcoholism and hepatoprotective effect. The composition comprises flowers of kudzuvine, hovenia acerba, dandelion, licorice, dark plum, alanine, and glutamine in proportion, and can be processed to prepare various products with antialcoholism and hepatoprotective effect. The composition has the effects of improving human tolerance to alcohol, preventing acute alcoholism, assisting treatment of alcoholic hepatic injury, alcohol allergy, and the like. In addition, the invention also relates to a method for preparing various food and medicaments by the composition.

The present invention provides an antifungal agent which has excellent antifungal action, and which is also excellent in terms of its properties, and in particular its solubility in water and safety. The present invention discloses a compound represented by the following formula (I) or a salt thereof.(whereinR1 represents a hydrogen atom, a halogen atom, an amino group, R11—NH— (wherein R11 represents a C1-6 alkyl group, a hydroxy C1-6 alkyl group, a C1-6 alkoxy C1-6 alkyl group, or a C1-6 alkoxycarbonyl C1-6 alkyl group), R12—(CO)—NH— (wherein R12 represents a C1-6 alkyl group or a C1-6 alkoxy C1-6 alkyl group), a C1-6 alkyl group, a hydroxy C1-6 alkyl group, a cyano C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkoxy C1-6 alkyl group;R2 represents a group represented by the formula:one of X and Y is a nitrogen atom, and the other is a nitrogen atom or an oxygen atom;ring A represents a 5- or 6-member heteroaryl ring or benzene ring which may have 1 or 2 halogen atoms or C1 to C6 alkyl groups;Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—;R3 represents a hydrogen atom or a halogen atom, or represents a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or a 5- or 6-member non-aromatic heterocyclic group, each of which may have 1 or 2 substituents selected from substituent group a;R4 represents a hydrogen atom or a halogen atom; andR represents a hydrogen atom, or represents a C1-6 alkyl group which may be substituted with a dimethylamino group,[substituent group α]a halogen atom, a cyano group, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkoxycarbonyl group, a C3-8 cycloalkyl group, a C2-6 alkenyl group and a C2-6 alkynyl group).

The invention discloses an application of astragalus mongholicus polysaccharide as the medicine prepared for treating neurodegenerative diseases.Proven by the mammal cell and caenorhadits elegans disease model test, the astragalus polysaccharides has the following functions: effectively inhibiting abnormal aggregation of mammal cell and caenorhadits elegans disease model polyglutamine, effectively relieving neurotoxicity triggered by the abnormal aggregation of polyglutamine and noticeably lengthening life span of the caenorhadits elegans model. With the functions of the astragalus polysaccharides, minor ingredients can be added to the astragalus polysaccharides according to pharmaceutical principles to serve as the medicine for treating neurodegenerative diseases or to be prepared into various dosage forms such as capsule, tablet or granule and the like.

A composition of probiotics, vitamins and minerals, electrolytes with glutamine and glucose along with medium chain triglycerides are provided as a supplement to animals. This is administered to cattle, calves, sheep, pigs, horses, dogs, and cats that are experiencing stress and or are undergoing medical drug therapy to treat conditions of diseases along with pre and post operative surgical conditions. The composition helps correct imbalances in beneficial bacteria, provides energy and helps in rehydration to reduce recovery time from stress or in disease treatment in these animals.

The present invention relates to compositions for supplementing the diet of subjects suffering from cardiovascular or peripheral vascular disease or those at risk for such conditions. Ribose is given alone or in combination with one or a combination of vasodilators, nutrients and vitamins. Preferred vitamins include Vitamins C, B6, B12 and folic acid. Preferred nutrients include glutamine and glucose.

A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I: with an alkylating agent of structure III: in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

The invention discloses a nutriment for improving the immunity of patients suffering from tumors after operation, radiotherapy and chemotherapy and a preparation method of the nutriment, and belongs to the technical field of medical foods. The nutriment comprises 45-98g / L of protein, 22-48g / L of fat, 98-245g / L of carbohydrate, 0-18g / L of dietary fibers, 0.35-0.75g / L of vitamins, 3.6-7.2g / L of trace elements, 1.0-2.2g / L of nucleotide, 0.2-20g / L of arginine, 0-0.2g / L of taurine, and an appropriate amount of water. The nutriment has various nutrient components, is rich in glutamine, arginine, nucleotide, omega-stability fatty acid and the like, is scientific in proportion, improves the nutritional status of patients, improves the resistance power of patients during operation, and after operation, radiotherapy and chemotherapy, improves the immunity of organisms of the patients, controls the acute inflammation, protects the function of intestinal mucosal barrier, reduces complication, shortens hospital days and reduces treatment price.

To provide a prophylactic / therapeutic agent for neurodegenerative diseases (such as polyglutamine diseases), the agent containing an HMGB family protein or a derivative thereof, such as a protein according any one of (a) and (b) below:(a) a protein having the amino acid sequence of SEQ ID NO: 2, 4, 6 or 8; and(b) a protein having an amino acid sequence resulting from deletion, substitution, addition or insertion of one or more amino acids in the amino acid sequence of SEQ ID NO: 2, 4, 6 or 8 and having binding activity to an abnormal polyglutamine protein produced in a neurodegenerative disease.

The tripeptide glycine-proline-glutamine (GPE) may be administered before, or usually after, injury to reduce damage to the central nervous system. GPE appears useful for neuronal rescue particularly but not exclusively within the hippocampus. Advantages of GPE include: (a) that it crosses the blood-brain barrier, so is effective by injected peripheral administration, (b) it is unlikely to challenge the immune system, (c) it is cheap, and (d) its therapeutic ratio is high. GPE may also be infused into the CSF. It may be administered prior to parturition or elective brain or cardiac surgery. Transdermal routes may be useful for chronic neural disorders. The CNS of mammals (including foetal mammals) after trauma including hypoxic / ischaemic experimental insults showed reduced damage under GPE protection as measured by histological assessment of cell damage or death and regional shrinkage.

The invention discloses a rapid hemostatic product for war wounds, as well as a preparation method and application thereof. The rapid hemostatic product comprises a substrate with added microbial transglutaminase (mTG), wherein the amino acid sequence of the transglutaminase is the protein sequence coded by the gene shown in SEQ ID NO.: 3, or a protein sequence shown in SEQ ID NO.: 4. More specifically, the rapid hemostatic product is selected from a hemostatic agent, a hemostatic device, a hemostatic first-aid kit or a common hemostatic product, the substrate is in a fluid or semi-solid form, which can be absorbed by a human body, or in a malleable gel or colloid form, and the rapid hemostatic product contains the microbial transglutaminase and gelatin. The rapid hemostatic product has the advantages of rapid hemostasis, convenience for use, organ adhesion prevention, wound healing promotion, low toxic and side effects, complete absorption and the like; except for hemostasis in a war, the rapid hemostatic product can also be widely applied to rapid hemostasis for wounds in fire control, accidents and other wild environments.

The invention discloses application of regulatory T cells in preparing a drug for treating autoimmune diabetes and an expanding cultivation solution and method thereof. The expanding cultivation solution of the regulatory T cells is prepared from, by volume, 35.274-42.69 parts of serum-free cultivation solutions, 1.25-2.5 parts of 4-(2-hydroxyerhyl)piperazine-1-erhanesulfonic acid buffer solution, 0.5-1 part of penicillin-streptomycin solution, 0.5-1 part of L-glutamine, 0.05-0.1 part of 2-mercaptoethanol, 0.00769-0.01154 part of recombinant interleukin-2, 0.001-0.01 part of rapamycin and 5-10 parts of AB serum. According to the application of the regulatory T cells in preparing the drug for treating the autoimmune diabetes, through targeted research on the regulatory T cells and the pathogenesis of the autoimmune diabetes, applicants find that the regulatory T cells has relatively good therapeutic effects at the aspect of treating the autoimmune diabetes.

The invention relates to application of GMFB (glia maturation factor beta) as a biomarker for early diagnosis of diabetic retinopathy and for diabetes progression, application of GMFB as a therapeutic target of diabetic retinopathy, a GMFB disrupter and application of the GMFB disrupter. Compared with the prior art, the invention proves that the GMFB content in vitreous body is significantly improved in early period of diabetes in rats of STZ-induced I type diabetes (TIDM). The invention is the first to prove that GMFB content gradually drops with the development of DR (diabetic retinopathy), therefore the GMFB is applicable to dynamic detection of DR progress; the invention is the first to prove that by interfering GMFB expression in rats of DR, visual function can be protected; and the invention is the first to prove that GMFB mediates retinopathy mechanism, including causing decrease of glutamine synthetase of Muller cell, death of ganglion cells and inducing autophagy of photoreceptor cells.

The invention relates to a tilapia immune potentiator and a preparation method thereof, and belongs to the technical field of an aquatic compound feed additive. The preparation method is characterized by comprising the following steps: fully mixing curcumin, glutamine, betaine and a carrier; and crushing the components into dry powder. The tilapia immune potentiator has the advantages of stable raw material source, simple preparation process, wide material selection range and low cost; starting from an immune mechanism of fish, Chinese herbal medicines and a western medicine-glutamine dipeptide are supplemented in the immune potentiator; and by means of combination of the traditional Chinese medicines and the western medicine, immunity of the fish is improved. By utilizing the tilapia immune potentiator, the immunity and oxidation resistance of the fish are improved, the capability of tilapia on resisting pathogenic streptococcus infection is strengthened, and growth of the tilapia is promoted.

The present invention is a glutamine analogue which enters the mitochondrion and is subsequently exposed to ionizing radiation. When exposed to ionizing radiation, the present invention damages mitochondrial (as well as other) substructures such as mtDNA, the outer membrane, the inner membrane, cristae, ribosomes, etc., and causes the effective destruction of such mitochondrion. Tumorigenic cells without mitochondria cannot produce the energy they need to subsist and replicate, effectively starving them of energy and causing their destruction.

Sodium N-(N'-oleoylglycyl)-chitosan sulfonate and a preparation method thereof relate to the technical field of chemical and medicine; N-hydroxysuccinimide and dicyclohexylcarbodiimide are mixed with DMF (dimethyl formamide) solution of oleic acid to obtain filtrate; glycine and potassium carbonate are dissolved in water, the filtrate is dropwise added under ice water bath, and reacting is allowed at room temperature to obtain n-hydroxysuccinimide; N-oleoylglycyl solution is adjusted to neutrality and is mixed with chitosan, 1-(3-dimethylaminopropyl)-3-ethyl-carbodiimide hydrochloride and N-hydroxysuccinimide for reacting to obtain N-(N'-oleoylglycyl)-chitosan, swelling with DMF for sulfonation reaction, supernate is collected and dialyzed to obtain filtrate, and the filtrate is lyophilized to obtain sodium N-(N'-oleoylglycyl)-chitosan sulfonate. The finished sodium N-(N'-oleoylglycyl)-chitosan sulfonate is a green surfactant having good biocompatibility, high performance, zero toxify and adjustable surface activity.

An extract of animal's brain is prepared by use of composite enzyme and can play the role of increasing the adaptive capacity to mental stress. A food for increasing the adptive capacity to mental stress contains said extract and 20 other components including VA, VE, folic acid, glutamine, etc.

The invention relates to a constructing method of a human amniotic membrane epithelial stem cell library. The method comprises the following steps: digesting a human amniotic membrane through trypsin, and carrying out filtering to prepare single-cell suspension; adding human epidermal growth factors, human transferrins, human insulin, sodium selenite, alanyl-L-glutamine dipeptide, alanine, asparaginate, aspartic acid, glutamic acid, glycine, proline and serine into a DMEM / F12 culture medium, putting cells into a CO2 incubator at temperature of 37 DEG C, saturated humidity and volume percentage of 5 percent for culturing, liquid change and passage under a serum-free condition; and putting cells obtained through in-vitro culture and amplification into liquid nitrogen for cryopreservation, and constructing a cell information file for retrieval, namely building the human amniotic membrane epithelial stem cell library. The human amniotic membrane epithelial stem cell library is used for storing human amniotic membrane epithelial stem cells and has the characteristics of wide source and no ethical restriction, and a cell culture and storage medium is animal origin-free. The human amniotic membrane epithelial stem cell library can supply the epithelial stem cells for cell treatment and other applications.

The invention provides a derivatization separation and detection method of a glycyl-L-glutamine chiral isomer, and belongs to the field of analytical chemistry. The method comprises the steps that before the glycyl-L-glutamine chiral isomer enters a liquid chromatographic column, derivatization is conducted through a derivatization reagent, and the derivatization reagent adopts an N<alpha>-(5-fluorine-2,4-dinitrophenyl)-L-amino acid compound. The separation determination method is high efficiency liquid chromatography. The used chromatographic column is a chromatographic column which takes base octadecyl bonded silica as filler. The separation and detection method mainly comprises the steps of preparing a sample solution and a derivative solution, conducting a derivative reaction, conducting derivative reaction aftertreatment and conducting separation determination through a high performance liquid chromatographic instrument. The pre-column derivatization method has the advantages that the reaction condition is mild, derived products are stable, the reaction velocity is high, the side reactions are few, determination is not disturbed by the excess derivatization reagent, and separation between glycyl-L-glutamine and the chiral isomer of the glycyl-L-glutamine can be achieved by using an ordinary chromatographic column.