57 results about "Pterin" patented technology

The invention describes a pharmaceutical composition and method for treating cancer comprised of A) 2,3-dimethoxy-5-methyl-1,4-benzoquinone and / or B) at least one of wild yam root, teasel root, balm of gilead bud, bakuchi seed, dichroa root, kochia seed, kanta kari, bushy knotweed rhizome, arjun, babul chall bark, opopanax and bhumy amalaki; optionally one or more of frankincense, garcinia fruit, vitex, dragons blood, mace, sage and red sandalwood with at least c) one compound capable of maximizing oxidative mitochondrial function preferably riboflavin or vitamin B2 derivatives, FAD, FMN, 5-amino-6-(5′-phosphoribitylamino)uracil, 6,7-Dimethyl-8-(1-D-ribityl)lumazine, ribitol, 5,6-dimethylbenzimidazole, tetrahydrobiopterin, vitamin B1, lipoic acid, biotin, vitamin B6, vitamin B12, folate, niacin, vitamin C and pantothenate and / or d) at least one lactic acid dehydrogenase inhibitor (preferably 2′,3,4′5,7-pentahydroxyflavone) and optionally f) an alkalizing agent (aloe vera, chlorella, wheat grass, sodium or potassium bicarbonate, potassium) g) an antiproliferative herb (speranskia or goldenseal) and h) a pharmaceutically acceptable carrier.

Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.

Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.

Guanosine triphosphate pathway tetrahydrobiopterin synthesis antagonist and / or pterin salvage pathway tetrahydrobiopterin synthesis antagonists are administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylactic or curative effect for endotoxin- or cytokine-induced hypotension or for restoration of vascular contractile sensitivity to pressor agents in the treatment of such hypotension). The tetrahydrobiopterin synthesis antagonist may be administered with alpha 1-adrenergic agonist or with nitric oxide synthase inhibitor. The tetrahydrobiopterin synthesis antagonists are also administered to attenuate inflammation caused by induced nitric oxide production in immune cells. Unwanted counterproductive or side effects can be eliminated or ameliorated by administration additionally of levodopa with or without carbidopa and L-5-hydroxytryptophane.

Ricin A-chain is an N-glycosidase that attacks ribosomal RNA at a highly conserved adenine residue. Crystallographic studies show that not only adenine and formycin, but also pterin-based rings can bind in the ricin active site. For a better understanding of the recognition mode between ricin, and adenine-like rings, the interaction energies and geometries were calculated for a number of complexes. Shiga toxin, a compound essentially identical to the protein originally isolated from Shigella dysenteriae, has an active protein chain that is a homologue of the ricin active chain, and catalyzes the same depurination reaction. The present invention is drawn to identifying inhibitors of ricin and Shiga toxin, using methods molecular mechanics and ab initio methods and using the identified inhibitors as antidotes to ricin or Shiga toxin, or to facilitate immunotoxin treatment by controlling non-specific cytotoxicity.

PCT No. PCT / JP97 / 02649 Sec. 371 Date Mar. 31, 1998 Sec. 102(e) Date Mar. 31, 1998 PCT Filed Jul. 30, 1997 PCT Pub. No. WO98 / 04558 PCT Pub. Date May 2, 1998An active oxygen scavenger comprising as an active ingredient a pterin derivative of the formula (I): wherein R1 and R2 are independently a hydrogen atom, an alkyl group of 1 to 4 carbon atoms, or an acyl group of the formula R3-CO-, R3 is an alkyl group of 1 to 4 carbon atoms, X is a formyl group or hydroxymethyl group, A is a group of the formula (Ia): and n is 0 or an integer of 1 or more, with the proviso that when X is a hydroxymethyl group, n is 0, or when n is an integer of 1 or more, each of R1 and R2 is a hydrogen atoms, and X is a formyl group, or a cyclic compound thereof, or a salt thereof is disclosed.

The present invention provides a transformed cell which is transformed by at least one gene of enzymes participating in biosynthesis of tetrahydrobiopterin and a process for the production of a biopterin compound using the same. In accordance with the present invention, the biopterin compound can be produced in large quantities in an industrial advantageous manner from less expensive materials.

Sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaaminopterin is assessed and patients are selected for treatment of cancer with 10-propargyl-10-deazaaminopterin, by determining the amount of a selected polypeptide expressed by the cancer and comparing the amount with the amount of the selected polypeptide expressed by a reference cancer. The polypeptide includes a member of a folate pathway polypeptide within a cell and may include at least one of reduced folate carrier-1 enzyme (RFC-1), dihydrofolate reductase (DHFR), folylpoly-gamma-glutamate synthetase (FPGS), thymidylate synthase (TS), γ-glutamyl hydrolase (GGH), and glycinamide ribonucleotide formyltransferase (GARFT).

Recombinant microbial cells and methods for producing 5HTP, melatonin and related compounds using such cells are described. More specifically, the recombinant microbial cell may comprise exogenous genes encoding one or more of an L-tryptophan hydroxylase, a 5-hydroxy-L-tryptophan decarboxylyase, a serotonin acetyltransferase, an acetylserotonin O-methyltransferase; and means for providing tetrahydrobiopterin (THB), and can be further genetically modified to enrich one or more of tryptophan, S-adenosyl-L-methinonine and acetyl coenzyme A. Related sequences and vectors for use in preparing such recombinant microbial cells are also described.

The inventive process for the reduction of pterins by means of an alkali metal boron hydride in water to the corresponding 5,6,7,8-tetrahydropterins is characterized in that the reduction is carried out in the presence of a catalytical amount of a water-soluble Pb(II)-salt.

The present invention relates to stable pharmaceutical compositions of tetrahydrobiopterin and processes for producing such compositions. Particularly the present invention relates to stable pharmaceutical compositions comprising tetrahydrobiopterin and at least one stabilizing agent.

Biopterins are useful compounds utilized in pharmaceutical agents or functional foods. The presence of sepiapterin reductase (SPR) involved in the biosynthesis of biopterins has not been confirmed so far in microorganisms except for a few microorganisms such as blue-green algae. For efficiently producing biopterins using microorganisms, it has been demanded to obtain and use SPR genes derived from microorganisms. The present inventors have found that when Saccharomyces cerevisiae or Escherichia coli is transformed with a YIR035C gene from Saccharomyces cerevisiae or a yueD gene from Bacillus subtilis, the transformed microorganism secretes biopterins into a culture solution. Based on this finding, the present invention provides a polypeptide, DNA encoding the polypeptide, a recombinant vector comprising the DNA, and a transformant obtained by transformation with the vector, which are useful in biopterin production using microorganisms. Moreover, the present invention provides a method for efficiently producing biopterins using the transformant.

Disclosed are crystalline forms of sepiapterin free base selected from polymorphs A, B, C, D, E, F, and G, and combinations thereof, as well as crystalline polymorphs of salts of sepiapterin. Also disclosed are pharmaceutical compositions containing one or more such polymorphs and methods for preparing such polymorphs. Sepiapterin is useful in the treatment of a number diseases associated with low cellular levels of BH4, for example, phenylketonuria.

The present invention features pharmaceutical compositions including sepiapterin, or a pharmaceutically acceptable salt and / or co-crystal thereof, and methods for the treatment of tetrahydrobiopterin-related disorders (e.g., tetrahydrobiopterin deficiency or phenylketonuria) with such compositions.

The present invention relates to new pharmaceutical salts and / or co-crystals of sepiapterin which exhibit improved properties. In particular, the invention relates to salts of sepiapterin with improved stability. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of one or more salts and / or co-crystals of sepiapterin, as well as methods of treating tetrahydrobiopterin-related disorders including administration of a sepiapterin salt and / or co-crystal of the invention to a subject in need thereof.

The present invention provides a transformed cell which is transformed by at least one gene of enzymes participating in biosynthesis of tetrahydrobiopterin and a process for the production of a biopterin compound using the same. In accordance with the present invention, the biopterin compound can be produced in large quantities in an industrial advantageous manner from less expensive materials.

The invention relates to a preparation method of an L-erythro biopterin compound, wherein the L-erythro biopterin compound has a structure as shown in a formula (I), and the L-erythro biopterin compound as shown in the formula (I) is mainly prepared from a compound with a structure as shown in a formula (II) or a formula (III) through a dihydroxylation reaction. The preparation method of the L-erythro biopterin compound is high in production efficiency, low in cost, green, environmentally friendly and suitable for industrial production.

The invention relates to an intermediate for preparing an L-red biopterincompound and a preparation method thereof, wherein the intermediate has a structure shown as a formula (IVa-1), a formula (IVa-2), a formula (IVa-3) or a formula (IVa-4), and the formulas (IVa-1), (IVa-2), (IVa-3) and (IVa-4) are defined in the specification. According to the invention, the intermediate and the preparation method thereof effectively realize the effects of one-pot resolution and purification, are simple and convenient to operate, can greatly reduce the production cost, and are particularly suitable for preparing L-red biopterin compounds.

This invention relates to methylaminopterin derivatives with 4-amino structure modified, which inhibit effect of nitrogen monoxide synthetase and growth of tumors. They have wide anti-cancer spectrum and little toxic side effect so as to be used in preparation of medicines for tumors, cancers, arthritis and intestinal diseases as well as chemicals for birth control.

The invention relates to process for in vitro prediction of a potentially allergenic substance wherein monocytes and / or macrophages and / or myelomonocytic cell lines are cultivated in the presence of the substance and interferon-γ, whereby productions of cytokines and / or neopterin are increased and measured. The allergic reaction may be estimated by measuring up regulated or down-regulated genes chosen from G1P2, OASL, IFIT1, TRIM22, IFI44L, MXI, RSAD2, IFIT3, IFITM1, IFIT2, C 33.28 HERV-H protein mRNA, IFITM3, XK, GPR15, MT1G, MT1B; MT1A, ADFP, IL8, MT1E, MT1F, MT1H, SLC30A1, SERPINB2, CD83, TncRNA or expression products from them are measured. The invention also relates to a reagent kit for use in the process comprising interferon-γ and reagents which recognise cytokines preferably each of IL-8 and neopterin and / or reagents such as probes recognising up-regulated or down-regulated genes.

Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.

The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.

Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.

The invention provides an application of an exosome metabolite as a bipolar affective disorder marker. Specifically, the invention provides application of a reagent material and / or instrument equipment for detecting the exosome metabolite level in a sample from an individual to be detected in preparation of a detection system for diagnosing the bipolar affective disorder disease risk, and the exosome metabolite comprises phosphoric acid, chenodeoxycholic acid, lysophosphatidylethanolamine 14:0, N-acetyl methionine, 13-oxo-9Z,11E-octadecadienoic acid, glycine, 1-naphthylacetic acid, 2-aminoethanesulfonic acid / taurine, D-2-aminobutyric acid, biopterin, glucosamine, lysophosphatidylcholine 18:0, lysophosphatidylethanolamine 18:0, lysophosphatidylcholine 20:1, and PAF C-16. According to the invention, positive help can be provided for pathogenesis of bipolar affective disorder and research of new targeted therapy means.

The present invention relates to a biomarker and a method for determining an oxidative stress level in a biological sample, which employs co-factor-dependent oxidative stress parameters, as well as a kit adapted for carrying out such a method. In one aspect the co-factor is tetrahydrobiopterin.

The invention provides a method for detecting the content of an impurity 6-formylpterin in folic acid. According to the method, Agi 1 entSB-CN is taken as a chromatographic column, after high performance liquid chromatography (HPLC) separation, a fluorescence detector is adopted to carry out qualitative and quantitative detection on the impurity 6-formylpterin in folic acid, and methodological verification is carried out. Experiments prove that the method can realize synchronous quantitative detection of trace photosensitive impurities 6-formylpterin and pterin 6-carboxylic acid in folic acid, and has the advantages of strong specificity, rapidness, high sensitivity, high accuracy and the like. The method for synchronously and quantitatively detecting the trace photosensitive impurities 6-formylpterin and pterin 6-carboxylic acid in the folic acid is established for the first time, and the quality control on the folic acid is facilitated, so that the quality and the medication safety of the folic acid bulk drug are improved.

The present invention relates to a method for assessing the sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaminopterin and a method for selecting a patient for treatment of cancer with 10-propargyl-10-deazaminopterin, by determining the amount of a selected polypeptide expressed by the cancer and comparing the amount with the amount of the selected polypeptide expressed by a reference cancer, wherein the polypeptide includes a member of folate pathways within cells and may include at least one of reduced folate carrier-1 enzyme (RFC-1), dihydrofolate reductase (DHFR), folylpoly-gamma-glutamate synthetase (FPGS), thymidylate synthase (TS), γ-glutamyl hydrolase (GGH), and glycinamide ribonucleotide formyltransferase (GARFT). The present invention also relates to the use of 10-propargyl-10-deazaminopterin in the treatment of multiple myeloma.

The invention relates to a metabolic marker of medulloblastoma in urine and an application thereof. Specifically, the invention relates to an application of a reagent in preparing kits and / or chips for diagnosis and / or prognostic of medulloblastoma for detecting metabolites levels in urine of a subject. Metabolites are selected from one or more of the following matters: Uropterin, 20-oxo-leukotriene E4, Cortolone, Tetrahydrocortisone, [6]-Gingerdiol 3,5-diacetate, Pteroside Z, 12-oxo-2,3-dinor-10,15-phytodienoic acid, Melleolide M, Ethyl 7-epi-12-hydroxyjasmonate glucoside, Piperdial, Epishyobunone, 4R,5S,7R,11S)-11,12-Dihydroxy-1(10)-spirovetiven-2-one11-glucoside, PC-M5 and Acuminoside.