33 results about "Pteridine synthesis" patented technology

Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, being represented by the general formula (I). are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.

The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

Tri-substituted pteridines and tetra-substituted pteridines exhibit a significant and selective activity against certain types of viral infections, in particular they selectively inhibit the replication of the hepatitis C virus, and are useful for the prevention and treatment of such infections.

Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.

Use of 10H-benzo[g]pteridine-2,4-dione derivatives as photosensitizers in the inactivation of microorganisms.

The invention discloses a pteridine aqueous organic redox flow battery. According to the pteridine aqueous organic redox flow battery, organic molecules containing a pteridine structure is taken as a negative electrode; potassium ferrocyanide, TEMPO or benzoquinone potassium sulfonate is taken as a positive electrode; one or a mixture of more of an acid solution, an alkali solution and a salt water solution is taken as an electrolyte; a perfluorosulfonic acid-polytetrafluoroethylene copolymer membrane is taken as an ion exchange diaphragm; two copper plates serve as a current collector of the battery; a graphite plate with a flow channel is used as a flow field plate of the positive electrode and the negative electrode; a carbon paper, graphite felt or a metal electrode serves as an electrode of the battery; and the pteridine aqueous organic redox flow battery has the advantages of power energy design flexibility, low cost, large-scale assembly and application and the like, and is very suitable for large-scale energy storage application.

Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the formula I, and use of compound in preparing medicine for treating diseases mediated by EGFR, BLK, or FLT3 or inhibiting EGFR, BLK, and FLT3.

A method and apparatus for detection of pteridine levels in a biological sample using CE-LIF which is useful for early cancer screening involving fully oxidizing pteridine compounds in a sample such as a urine sample, subjecting to CE-LIF to assess compound concentration, and compare to expected levels in for healthy or cancer-bearing patients.

The invention discloses pteridine compounds and application of the same in pharmacy, belonging to the field of medicine. The pteridine compounds of the invention or stereoisomers thereof or pharmaceutically acceptable salts thereof have a structure as shown in a general formula (I) or (II), have CDK4 inhibiting activity of 47% or more (as high as 79%), show very good inhibitory activity against CDK4 / 6, and can be used as highly-effective inhibitors againast CDK4 / 6, and have broad application prospects.

The invention discloses a pralatrexate (I) preparation method, which comprises the following preparation steps: performing cyclization reaction on dialkyl N-[4-(1-(2-propinyl)-3,4-dioxo-n-butyl)benzoyl]-L-glutamate (II) and 2,4,5,6-tetraminopyrimidine (III) under oximation conditions to generate an intermediate compound alkyl N-[4-[1-(2,4-diamino-6-pteridine)methyl-3-butynyl]benzoyl]-L-glutamate (IV); and performing hydrolysis reaction on the intermediate compound (IV) to prepare pralatrexate (I). The preparation method is accessible in raw materials, simple in process, economic, environment-friendly and suitable for industrial production.

The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

The invention relates to a preparation method of L-erythro biopterin used as an import preparation intermediate body of a clinically used medicament (R)-2-amido-6-[(1R,2S)-1,2-dihydroxy propyl]-5,6,7,8-tetrahydro-4(3H)-pteridine ketone hydrochloride for treating atypical hyperphenylalaninemia, which belongs to the technical field of medicinal chemistry. The preparation method sequentially comprises the steps of: reacting L-(+)-arabinose 1 with alcohol by glycosidation; adding sulfonyl chloride for generating a sulfonation reaction; reducing and removing sulfonyl ester; removing reduced aldehyde protective groups; reacting with hydrazine for obtaining a hydrazine compound; reacting with estolide or the sulfonyl chloride; reacting with 2,4,5-3-amino-pyrimidine ketone; adding an oxidant; and removing acyl for obtaining L-erythro biopterin. The invention ensures deodorizing equipment is not installed on a reaction system by utilizing Odourless mercaptan thereby reducing production cost and optimizing a working environment; and the invention has mild reaction condition of each step and easy operation, and shortens a production period.

The invention discloses a lithium ion battery film forming additive composition, which comprises a pteridine compound and a sulfone, wherein the weight ratio of the sulfone to the pteridine compound is 0.035-100: 1, wherein that pteridine-type compound is selected from the group consisting of compound represented by formula I, and the sulfone is selected from the group consisting of compound represented by formula II and compounds represented by formula III. The invention also discloses a non-aqueous electrolyte containing the composition and a lithium ion battery using the non-aqueous electrolyte. A lithium ion battery employing a non-aqueous electrolyte containing the film forming additive composition according to the present invention exhibits a significantly improved service life, goodcycle performance and rate discharge performance even at high voltages.

The invention relates to a pralatrexate degradation impurity and a preparation method thereof. Specifically, the formula (I) of the pralatrexate degradation impurity is N-[4-1- [(2-amino-4-hydrox-6-pteridine) methyl]-3-butine-1-group] benzoyl]-L-glutamate. An N-[4-1- [(2-amino-4-diamido-6-pteridine) methyl]-3-butine-1-group] benzoic acid compound is subjected to substitution, condensation and hydrolysis, and a target compound is obtained, so that the pralatrexate degradation impurity is synthesized. According to the method, the compound of the formula (I) is chemically synthesized for the first time, and the obtained target compound can be separated efficiently and rapidly.

Engineering plastics, especially polyamide, are coloured with improved fastness and stability properties using pigment compositions comprising an organic pigment wholly overlaid with a crosslinked (meth)acrylic resin or copolymer thereof. Preference is given to the use of diketopyrrolopyrrole, azo, pteridine, isoindoline and isoindolinone pigments. The invention also relates to processes for the preparation of the pigment compositions.

The invention provides methods and compositions for treating asthma and / or COPD. For example, provided herein are compositions that include a kinase inhibiting agent such as 6,7-bis(3-hydroxyphenyl)-pteridine-2,4-diamine or pharmaceutically acceptable salts thereof; and a surfactant.

The invention provides methods for determining and evaluating the in vitro-in vivo activity relationship of the efficacy of families of compounds for infectious diseases such as tuberculosis. The validity of the methods can be confirmed by evaluation of the compounds in animal models, for example, in murine models of tuberculosis. Examples of families of antibacterial compounds that can be evaluated for in vivo efficacy using the in vitro methods described herein include benzimidazoles, pyridopyrazines, pteridines, diphenyl ethers, beta-lactams, PBP inhibitors, and compounds that are non-ribonucleic acid and protein synthesis inhibitors. The methods can be used to evaluate classes of small molecule compounds and inhibitors that may be effective against any bacterial pathogen. The methods aid the identification of compounds, such as various benzimidazoles, with modes of action having activity against clinical isolates, as well as non-replicating persistent bacilli, which can therefore enhance current clinical therapeutic regimens.

The invention relates to a preparation method and application of pteridine folic acid. The preparation method has the advantages that by using p-aminobenzoyl glutamic acid, triamino pyrimidine sulfate and trichloroacetone as raw materials, and adopting the chemical synthesizing method, the content of crude product of pteridine folic acid is obviously increased; by using preparation chromatography to separate, the pteridine folic acid with purity more than 95% is obtained; the production mechanism and control method of the pteridine folic acid are favorably further studied, and the quality control level of the folic acid is effectively increased.

The invention relates to a preparation method of L-erythro biopterin used as a preparation intermediate body of a clinically used medicament (R)-2-amido-6-[(1R, 2S)-1,2-dihydroxy propyl]-5,6,7,8-tetrahydro-4(3H)-pteridine ketone hydrochloride for treating atypical hyperphenylalaninemia, which belongs to the technical field of medicinal chemistry. The preparation method sequentially comprises the steps of: reacting L-(+)-arabinose 1 with alkyl hydrosulfide by acetalization; adding sulfonyl chloride for generating a sulfonation reaction; reducing and removing sulfonyl ester; removing reduced sulfur aldehyde protective groups; reacting with hydrazine for obtaining a hydrazine compound; reacting with estolide or the sulfonyl chloride; reacting with 2,4,5-3-amino-pyrimidine ketone; adding an oxidant; and removing acyl for obtaining the L-erythro biopterin. The invention ensures deodorizing equipment is not installed on a reaction system by utilizing Odourless mercaptan, thereby saving costand optimizing a working environment; and the invention has mild reaction condition of each step, short period and easy operation.

A process for mass colouring high molecular weight organic material by using a pyrimidopteridine of formula (I) and / or (II) or a mixture thereof, wherein A, B, C and D are each independently of one another -NH2, -OH, hydrogen, C1-C4-alkyl; phenyl, biphenyl or naphthyl which are unsubstituted or substituted by halogen, -OH, -NH2, C1-C4alkyl or C1-C4alkoxy; -NHR1, -N(R1)2 or formula (1), wherein R1 is C1-C4alkyl; phenyl which is unsubstituted or substituted by halogen, C1-C4alkyl or C1-C4alkoxy, or -COXR2, X is a direct bond, -O- or -NH-, and R2 is C1-C4alkyl; phenyl which is unsubstituted or substituted by halogen, C1-C4alkyl or C1-C4alkoxy, with the proviso that at least two of the radicals A, B, C and D are -NH2 or -OH.

The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.

Compounds as immune system modulators bearing a pteridine core are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing autoimmunity disease using the same are described.

The invention provides methods for determining and evaluating the in vitro-in vivo activity relationship of the efficacy of families of compounds for infectious diseases such as tuberculosis. The validity of the methods can be confirmed by evaluation of the compounds in animal models, for example, in murine models of tuberculosis. Examples of families of antibacterial compounds that can be evaluated for in vivo efficacy using the in vitro methods described herein include benzimidazoles, pyridopyrazines, pteridines, diphenyl ethers, beta-lactams, PBP inhibitors, and compounds that are non-ribonucleic acid and protein synthesis inhibitors. The methods can be used to evaluate classes of small molecule compounds and inhibitors that may be effective against any bacterial pathogen. The methods aid the identification of compounds, such as various benzimidazoles, with modes of action having activity against clinical isolates, as well as non-replicating persistent bacilli, which can therefore enhance current clinical therapeutic regimens.

A method and apparatus for detection of pteridine levels in a biological sample using CE-LIF which is useful for early cancer screening involving fully oxidizing pteridine compounds in a sample such as a urine sample, subjecting to CE-LIF to assess compound concentration, and compare to expected levels in for healthy or cancer-bearing patients.

The invention relates to a method for designing and synthesizing N2-fragrant formyl-4-amido / amido-pteridines derivation with Nitric Oxide Synthase, which has the structure of (I), wherein R1 and R2 at least has one fragrant formyl. The pteridines compound can adjust the activity of NOS and can prepare for the drug.

The invention discloses seven N-[(4-(2, 4-diamido-6-pteridine methyl-methylamino)-benzoyl]-Glu-Lys-Glu-R and a preparation thereof, inhibition effect of the N-[(4-(2, 4-diamido-6-pteridine methyl-methylamino)-benzoyl]-Glu-Lys-Glu-R on tumor growth and tumor transfer, and application of the N-[(4-(2, 4-diamido-6-pteridine methyl-methylamino)-benzoyl]-Glu-Lys-Glu-R in preparation of antitumor drugs.