68 results about "Pteridine" patented technology

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

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.

This invention relates to a group of substituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro-derivatives, and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and / or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system, TNF-α related disorders, viral diseases, inflammatory bowel diseases and cell proliferative disorders.

The present invention relates to a crystalline form a dihydropteridione derivative, namely a crystalline form of the free base N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

This invention relates to the use of a group of pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, for the manufacture of a medicament for the prevention or treatment of TNF-α related disorders.

This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and / or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).

The invention relates to pteridinone derivatives as BLK and FLT3 inhibitors and applications thereof. Particularly, the invention relates to a compound shown in the following formula I, a pharmaceutical composition containing the compound shown in the following formula I, and use of the compound in preparation of a drug for treating BLK and FLT3-mediated diseases or inhibiting BLK and FLT3.

The invention relates to a crosslinkable organic molecule having a structure of the formula (1) and to the use thereof, wherein Ar is independently of one another, an unsaturated or aromatic carbo- or heterocyclic unit with 5 to 30 ring atoms, selected from the group consisting of naphthalene, anthracene, phenanthrene, pyrene, dihydropyrene, chrysene, perylene, fluoranthene, benzanthracene, tetracene, pentacene, benzpyrene, furan, benzofuran, isobenzofuran, thiophene, benzothiophene, isobenzothiophene, dibenzothiophene, pyrrole, indole, isoindole, carbazole, pyridine, quinoline, isoquinoline, acridine, phenanthridine, benzo-5,6-quinoline, benzo-6,7-quinoline, benzo-7,8-quinoline, phenothiazine, phenoxazine, pyrazole, indazole, imidazole, benzimidazol, naphthimidazole, phenanthrimidazole, pyridimidazole, pyrazine-imidazole, quinoxalinimidazole, oxazole, benzoxazole, naphthoxazole, anthroxazole, phenanthroxazole, isoxazole, isothiazole, 1,3-thiazole, benzothiazole, pyridazine, benzopyridazine, pyrimidine, benzpyrimidine, quinoxaline, pyrazine, phenazine, naphthyridine, azacarbazole, benzocarboline, phenanthroline, 1,2,3-triazole, 1,2,4-triazole, benzotriazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,3,5-triazine, 1,2,4-triazine, 1,2,3-triazine, tetrazole, 1,2,3,4- oxatriazole, 1,2,3,4-oxatriazole, 1,2,4,5-tetrazine, 1,2,3,4-tetrazine, 1,2,3,5-tetrazin, purine, pteridine, indolizine, benzothiadiazole, indenocarbazole, indenofluorene, spirobifluorene, and indolocarbazole; D1 is a donor group having a structure of the formula (1a); and D2 is a donor group having a structure of the formula (1b).

The present invention relates to the use of pteridine derivatives as nitric oxide synthase activators. In particular, the derivatives find use in the treatment of diseases associated with endothelial dysfunction such as cardiovascular diseases.

The invention relates to an environment-friendly preparation method of synthetic folic acid. The method comprises the steps of forming 2-amino-4-hydroxyl-6-chloromethyl pteridine with 2,4-diamido-5-nitroso-6-hydroxyl pyrimidine and glycerol by the action of composite catalysis, and further allowing aminobenzene formyl-L-glutamic acid to react to prepare folic acid. The method reduces reduction of nitroso, and avoids acetone chlorination, and high-purity glycerol provides guarantee for preparing a high-purity intermediate. The raw materials used by the method are cheap and easy to obtain, a technological flow is short, the reaction operation is easy and simple, in addition, the reaction selectivity is high, and the product cost is low.

The invention provides a meter panel surface shield composition, a meter panel surface shield, and a preparation method of the surface shield. The meter panel surface shield comprises a polymer resin and an organic dye, wherein the polymer resin is selected from one or more of polymethyl methacrylate, polycarbonate or a cycloolefin copolymer; the organic dye is selected from one or more of a phthalocyanine dye, a halogenated phthalocyanine dye, a perylene dye, a qinacridone (qinacrididone) dye, a diketopyrrolopyrrole dye, a dioxazine dye, a quinophthalone dye, a benzidine dye, an isoindole dye, a benzimidazolone dye, an anthraquinone dye, a pteridine dye and a condensed azo dye. The haze of the meter panel surface shield prepared from the composition is small, so it is convenient for clearly reading the indication of a meter panel.

The invention relates a novel pteridine derivative with formula (I), which is a NO synthetase, in particular the suppressant for evoked type NO synthetase, which can be used in the prevention and treatment of diseases caused by NO level rise.

The invention discloses a preparation method of Volasertib (I). The preparation method comprises the following step: carrying out a nucleophilic substitution reaction on an intermediate 2-amido-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) and an intermediate N-[trans-4-[4-( cyclopropyl methyl)-1-piperazinyl]cyclohexyl]-4-halogen-3-methoxybenzamide (III) to prepare the Volasertib (I). The preparation method disclosed by the invention is simple in process, moderate in condition, less in side reaction and suitable for the requirement on industrialized amplification. Besides, the invention also discloses the intermediate 2-amido-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) and intermediate N-[trans-4-[4-( cyclopropyl methyl)-1-piperazinyl]cyclohexyl]-4-halogen-3-methoxybenzamide (III) of the volasertib (I) and a preparation method thereof.

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 discloses a preparation method of an ultrahigh-voltage flame-retardant cable material. The preparation method comprises the following steps: S1, polycondensation of 3,3'-(2,4-diamino-6,7-pteridinediyl)bisphenol and carboxyl-terminated polyurethane; S2, preparation of an intermediate; S3, modification of a polyurethane-based polycondensate; and S4, forming of the cable material. The invention also discloses the ultrahigh-voltage flame-retardant cable material prepared by the preparation method. The ultrahigh-voltage flame-retardant cable material disclosed by the invention is excellent in comprehensive performance, good in flame retardance and insulativity, good in performance stability, long in service life, and safe and environment-friendly in production and use processes.

The invention discloses an iridium complex, a preparation method, and an application thereof. The iridium complex has the structure as the specification, wherein the coordinated group in the section Cis selected from: phenyl, pyridyl, thienyl and pyrimidinyl; the coordinated group in the section N is selected from: pyridyl, pyrimidinyl, pyridazinyl, triazinyl, thiazolyl, imidazolyl, quinolyl, isoquinolyl, quinazolinyl or pteridinyl; the R1 is selected from: alkane derivatives, ether derivatives, halogenated hydrocarbon derivatives, ketone derivatives, benzene derivatives, pyridine derivativesand naphthalene derivatives; R2 is selected from: alcohol derivatives, amine derivatives, benzene derivatives, pyridine derivatives, pyrimidine derivatives, diphenylamine derivatives, carbazole derivatives, carboline derivatives, 9,10-dihydroacridine derivatives, phenoxazine derivatives, phenothiazine derivatives, and azole derivatives. The iridium complex has high carrier transport capability, is easy to synthesize, has stable chemical properties, and is easy to sublimate and purify.

The invention relates to a compound hypotensive tablet and a preparation method thereof. Particularly, the invention relates to a pharmaceutical composition. The pharmaceutical composition comprises the following raw materials in parts by weight: 0.1 part of reserpine, 10-15 parts of hydrochlorothiazide, 10-15 parts of triamterene and 10-15 parts of dihydralazine sulfate. The invention further relates to a method for preparing the pharmaceutical composition. Furthermore, the invention further relates to a method for stabilizing the pharmaceutical composition in a tablet form. The method comprises a step of adding saccharides and starch additives to the pharmaceutical composition. The pharmaceutical composition comprises the reserpine, the hydrochlorothiazide, the triamterene and the dihydralazine sulfate. The compound hypotensive tablet is generally called Beijing hypotensive No.0 or No.0 in the field, is an excellent hypotensive drug which is accurate in curative effect, low in bad reaction and low in price, and has excellent pharmaceutical properties.

The invention discloses a preparation method of 2,4-diamino-6-bromomethyl pteridine, wherein the preparation method comprises: on the basis of utilizing 2,4,5,6-tetraaminopyrimidine hydrochloride as a raw material and acidic 4A molecular sieve as a catalyst, reacting the raw material with 1,3-dioxyacetone in the presence of oxygen to generate 2,4-diamino-6-bromomethyl pteridine, and performing bromination under the action of NBS (N-bromosuccinimide) and triphenylphosphine to obtain the product 2,4-diamino-6-bromomethyl pteridine. The technique is simple to operate, the yield is high, and large scale industrial production is easier to realize.

The invention relates to the technical field of chemical synthesis, and particularly provides a 6, 7-disubstituted 2-(ethylthio)-pteridine-4-amine derivative and a preparation method and application thereof. According to the method, 2-(ethylthio) pyrimidine-4, 5, 6-triamine and a 1, 2-diketone derivative are used as raw materials, the pteridine derivative with the ethylthio at the second position, the amino at the fourth position and the same substituent at the sixth and seventh positions is synthesized through a one-step reaction, the synthesis method does not need to add a catalyst, and the method has the advantages of being simple in process route, easy to purify, high in product yield and the like. Through activity screening, the derivatives are found to be capable of effectively inhibiting growth of tumor cells, and a thought and a method are provided for development and application of pteridine antitumor drugs.

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.

The invention relates to compositions comprising 3,6,7-trimethyllumazine, methods and uses thereof in preventing, ameliorating or treating inflammation and / or preventing, ameliorating or treating conditions associated with inflammation. More particularly, though not solely, the invention relates to compositions comprising 3,6,7-trimethyllumazine and methods of use thereof in preventing, ameliorating or treating MMP-9 associated conditions, such as inflammation of the gastrointestinal tract and / or inflammatory conditions associated with the gastrointestinal tract.

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.