52 results about "Triaziquone" patented technology

The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula Iwherein the variables are defined herein.

The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.

The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and / or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.

The invention belongs to the field of pharmaceutical chemicals, and particularly relates to pyrrolo-triazinone derivatives and the application thereof in drugs. More specifically, the related compounds can restrain the activity of poly(ADP-ribose)polymerase, and the poly ADP-ribose polymerase is also named poly(ADP-ribose)synthetase and poly ADP-ribosyltransferase and is generally called PARP. The compounds are characterized in that for the compound shown in the formula (1), X can be NRX or CRXRY; if X is NRX, n is 1 or 2; if X is CRXRY, n is 1; RX can be H, substitutional C1-20 alkyl, C5-20 aryl, C3-20 heterocyclic radical, acylamino, thioamide, ester, acyl or sulfonyl; RY can be H, hydroxyl or amino; or RX and RY can form spiro-C3-7-hydrocarbon radical or heterocyclic radical together; R2 and R3 are both H, or when X=CRXRY, R2, R3, RX and RY and carbon atoms connected with R2, R3, RX and RY form substitutional dense aromatic nucleus; R1 is H or halogen; R4 is H or halogen.

The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and / or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, A1, A2 and A3 are independent of each other and each represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X1, X2 and X3 are independent of each other and each represents a single bond, an optionally substituted C1-6 alkylene group, an optionally substituted C2-6 alkenylene group, an optionally substituted C2-6 alkynylene group, —NH—, —O—, —NHCO—, —CONH—, —SO0-2—, etc.; R1 and R2 are independent of each other and each represents a hydrogen atom or an optionally substituted C1-6 alkyl group, or R1 and R2 may be bound together such that CR2-ZR1 forms C═C; and R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group etc., or may be bound to any atom in A1 or A3 to form, together with the atom, an optionally substituted C5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

The invention discloses a polypeptide condensating agent 1-hydroxy-1,2,3-phentriazine-4(3H)-one and a preparation method thereof. According to the technical scheme, the polypeptide condensating agent 1-hydroxy-1,2,3-phentriazine-4(3H)-one has the structural formula shown in the specification. The invention also discloses a preparation method for the polypeptide condensating agent 1-hydroxy-1,2,3-phentriazine-4(3H)-one. The polypeptide condensating agent 1-hydroxy-1,2,3-phentriazine-4(3H)-one has the advantages of readily available raw material, simple line, few side reactions, high total yield and the like.

The invention discloses a synthesis method of a 1,2,3-phentriazine-4(3H)-one compound. 2-aminobenzamide and are used as raw materials and tert-butyl nitrite stirred at the room temperature in a reaction solvent, and the 1,2,3-phentriazine-4(3H)-one compound is obtained through an intramolecular diazotization reaction. The reaction equation is shown in the description, wherein R is H, fluorine, chlorine, bromine, trifluoromethyl, nitryl or methyl. The synthesis method has the benefits as follows: (1) the synthesis method is convenient in experiment operation, easy in posttreatment, mild in reaction condition and suitable of large-scale industrial production; (2) reaction substrate functional groups have high tolerance, and the substrate is wide in range and easy to obtain; (3) the reactionefficiency, yield and purity are higher.

The invention discloses a podophyllotoxin compound containing a 1,2,4-triazone structure, and an application thereof. The compound has a structure represented by general formula (I). Podophyllotoxin derivatives containing 1,2,4-triazone, represented by the general formula (I), and pharmaceutically acceptable salts thereof have antitumor effects. In-vitro cell activity experiments prove that the podophyllotoxin derivatives containing 1,2,4-triazone have a good inhibition effect on a human chronic myelocytic leukemia cell K562, a human cervical carcinoma cell Hela and a human breast cancer cellMCF-7. The compounds have a good antitumor medicine exploitation and application prospect.

The invention relates to a 4-phenoxy pyridine derivative containing a 3-pyridazinone structure, a 4-pyridazinone structure and a 1,2,4-triazinone structure, and applications thereof. According to theinvention, the 4-phenoxy pyridine derivative has a structure represented by a general formula (I), and the compound has strong inhibiting effect on c-Met kinase. The invention further relates to applications of the compound, the pharmaceutically acceptable salt, the hydrate, the solvate or the prodrug thereof in preparation of drugs for treating and / or preventing diseases caused by abnormal high expression of c-Met kinase, especially in preparation of drugs for treating and / or preventing cancers.

The present invention concerns a topical, cosmetic or pharmaceutical preparation containing a combination of 3 or 4 solar filters comprising: -one or two UVA filters to obtain a critical wavelength >370 nm, chosen from among: ( i) - 5, 6, 5, 6-tetraphenyl-3, 3'-(1,4-phenylene)-bis[1, 2, 4]triazine; (ii) 1,1'-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl]phenyl]-methanone; (iii)- Butyl Methoxydibenzoylmethane (BMDBM), in a quantity less than 2% by weight with regard to the total weight of said composition; (iv) - Hexyl -[4-(diethylamino)-2- hydroxybenzoyl]benzoate, -2,4-Bis[4-(2-ethylhexyloxy)-2-hydroxyphenyl]-6- (4-methoxyphenyl)-1, 3, 5-triazine = (BEMT), - one or two selected from the group consisting of diethylhexyl butamido triazone, ethylhexyl triazone, and filtersof tris-biphenyl triazine, ethylhexyl salicylate, phenylbenzimidazole sulfonic acid and TiO2 in an amount of from 3% by weight to 7% by weight relative to the total weight of the composition.

Compounds of the formula (I) in which X, R1 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase and PARP-1 and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of imflamination.

The present invention relates to salt forms and derivatives of 2-methylthio-6-nitro-1,2,4-triazoio[5,1-c]1,2,4-triazine -7-one, dehydrate and pharmaceutical compositions thereof. These salt forms and derivatives exhibit improved antiviral activity. The present invention also relates to processes for preparing the compounds, and intermediates used in their preparation.

The invention discloses a preparation method of 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazine 5 (4H)-ketone. The method comprises steps of: reacting 4-amino-6-tert-butyl-3-sulfydryl-1,2,4-triazine-5 (4H)-ketone, dimethyl sulfate and anhydrous sodium carbonate in a molar ratio of 1:1.1-1.4:1.5-2 in a solvent acetone and in the presence of a catalyst potassium iodide at 15-45 DEG C for 2-4 h; and finally recovering acetone, adding water to dilute the material, separating and drying to obtain the 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazine 5 (4H)-ketone. The raw materials used in the method are easily available, and cheap; and the method provided by the invention has advantages of moderate reaction and easily controlled reaction parameters, and can guarantee the safety of the production process. Potassium iodide is used as a catalyst, so as to realize rapid complete reaction at room temperature, reduce the production cycle and effectively reduce production cost; the product yield reaches more than 90%, and products with content of more than 96% can be directly obtained. The preparation method satisfies requirements of industrial production, and has a good application prospect.

Peptide analogs in which one or more amino acids is replaced by a diaza- or triazacyclohexenone, or by an aza-, diaza-, or triazacyclohexenone that is substituted at the α-position with a side chain of an amino acid, display an improved ability to assume a β-strand conformation and to enter into β-sheet-like interactions with peptides in an affinity-specific manner. The peptide analogs of this invention therefore have utility as β-strand mimics offering advantages over both native peptides and β-strand mimics of the prior art.

The invention discloses a preparation method of 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one. The molar ratio is 1:1.1~1.4 : 1.5-2 4-amino-6-tert-butyl-3-mercapto-1,2,4-triazin-5(4H)-one, dimethyl sulfate and anhydrous sodium carbonate, solvent acetone, catalyst potassium iodide , keep warm at 15-45°C for 2-4 hours, finally recover acetone, add water to precipitate, separate and dry to obtain 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazine -5(4H)-one. The raw materials used in the method of the present invention are easy to get, and the price is low; The method of the present invention has mild reaction, easy control of reaction parameters, and can ensure the safety of the production process; Potassium iodide is used as the catalyst, which makes the rapid reaction complete at normal temperature, greatly reducing the Its production cycle effectively reduces the production cost; the product yield is high, reaching over 90%, and products with a content of over 96% can be directly obtained, which meets the requirements of industrial production and has a good application prospect.

The invention discloses a synthesis method of trinitrobenzo [4, 5] imidazo [2, 1-c] [1, 2, 4] triazine-4-one, and the method comprises the following steps: adding concentrated sulfuric acid into a reaction flask at low temperature, adding 3-nitro-4-amino-benzo [4, 5] imidazo [2, 1-c] [1, 2, 4] triazine in batches, and stirring; dropwise adding fuming nitric acid, heating to obtain a first reactionsystem after the reaction is finished, pouring the first reaction system into ice water, extracting a water phase by using ethyl acetate, combining organic phases, drying with anhydrous sodium sulfate, concentrating the organic phases to obtain a crude product, and further purifying the crude product through column chromatography to obtain 3, 7, 9-trinitrobenzo [4, 5] imidazo [2, 1-C] [1, 2, 4] triazine-4 (3H)-one and 3, 9-dinitrobenzo [4, 5] imidazo [2, 1-C] [1, 2, 4] triazine-4 (3H)-one. The raw material 2-aminobenzimidazole used in the reaction is a commercialized product in the market, and is low in price and easy to obtain.

The invention relates to the field of pesticides, and discloses a preparation method of 3, 3-dimethyl-2-oxobutyric acid and triazinone. The preparation method of the 3, 3-dimethyl-2-oxobutyric acid provided by the invention comprises the step of oxidizing the 3, 3-dimethyl-2-oxobutyric acid and / or a salt thereof by taking oxygen-containing gas as an oxidizing agent in the presence of a catalyst under the condition that the pH value is 7-13. According to the method disclosed by the invention, the 3, 3-dimethyl-2-hydroxybutyric acid and / or the salt thereof is taken as the raw material, and oxygen or air is used for replacing other oxidants, so that high-salinity wastewater and solid waste are avoided, the cost of the raw material is reduced, and the method is simple to operate and suitable for industrial production.

The invention relates to a coupling complexing extraction agent composition and a method for treating triazinone production wastewater. The composition comprises a first composition and a second composition, the first composition comprises a first complexing agent and a first diluent; the second composition comprises a second complexing agent and a second diluent; the first complexing agent comprises at least one of N503, butyl dibutyl phosphate, quaternary ammonium chloride and tertiary amine; and the second complexing agent comprises at least one of naphthenic acid and 2-ethylhexyl phosphoric acid. The method comprises the following steps: adjusting the pH value of triazinone production wastewater to 2-4, adding a first composition, reacting, and layering to obtain an upper-layer first extraction phase and a lower-layer first water phase; and adjusting the pH value of the first water phase to 6-8, adding a second composition, reacting, and layering to obtain an upper-layer second extraction phase and a lower-layer second water phase. According to the method, organic acid, organic alkali and other toxic organic pollutants in the wastewater can be extracted and separated, the COD removal rate is higher than that in the prior art, and water obtained after complexing extraction can be reused in the production process.

The invention relates to a bactericidal and insecticidal composition and a method for preventing and controlling crop diseases and pests. The bactericidal and insecticidal composition comprises a first active ingredient and a second active ingredient, wherein the first active ingredient is (E)-4,5-dihydro-6-methyl-4-((3-pyridinylmethylene)amino)-1,2,4-triazin-3(2H)-one; the second active ingredient is 5-(4-chlorphenyl)-2,2-dimethyl-1-(1,2,4-triazole-1-methyl)cyclopentanol; the weight percentage of the first active ingredient and the second active ingredient is (1:100)-(100:1). The bactericidal and insecticidal composition has insect and disease prevention functions and also has an enhancement effect but not simple addition of two medicines.

The invention relates to the technical field of chemical engineering, in particular to a triazinone production line. The triazinone production line comprises a hydrolysis kettle, wherein an oxidationkettle is arranged on and communicates with the hydrolysis kettle through a first connecting pipe; a cyclization kettle is arranged on and communicates with the oxidation kettle through a second connecting pipe; a middle kettle is arranged on and communicates with the cyclization kettle through a third connecting pipe; the first connecting pipe, the second connecting pipe and the third connectingpipe are each provided with a first pump body and a first valve; the middle kettle is connected with a centrifugal machine through a fourth connecting pipe in a communicating mode; a solid material discharging port of the centrifugal machine is provided with a material guiding pipe in a communicating mode; the material guiding pipe is provided with an air pump; a shell is arranged on the materialguiding pipe in a communicating mode; the lower end of the shell is fixedly connected with a supporting base; the bottom wall of the shell is rotationally connected with a connecting cylinder througha sealing bearing; a plurality of connecting pipes are arranged on the connecting cylinder in a communicating mode; and the lower end of the connecting cylinder is rotationally connected with a connecting cover through the sealing bearing. The invention also provides a preparation method of triazinone. According to the invention, particulate matters are prevented from adhering to each other and becoming lumps, so product quality is not influenced.

The invention discloses a synthesis method of 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one, which comprises a molar ratio of 1:1.05 ~1.5:1.5~2 of 4-amino-6-tert-butyl-3-mercapto-1,2,4-triazin-5(4H)-one, dimethyl sulfate and anhydrous sodium carbonate, solvent acetone, Catalyst potassium iodide, heat preservation reaction at 15-45°C for 2-5 hours, finally recover acetone, add water to precipitate, separate and dry to obtain 4-amino-6-tert-butyl-3-methylthio-1,2,4- Triazin-5(4H)-one. The raw materials used in the method of the present invention are easy to get, and the price is low; The method of the present invention has mild reaction, easy control of reaction parameters, and can ensure the safety of the production process; Potassium iodide is used as the catalyst, which makes the rapid reaction complete at normal temperature, greatly reducing the Its production cycle effectively reduces the production cost; the product yield is high, reaching over 90%, and products with a content of over 96% can be directly obtained, which meets the requirements of industrial production and has a good application prospect.

The invention relates to a recycling method of waste acid water from metribuzin production, which comprises the following steps: (1) extracting the waste acid water from metribuzin production to recover part of triazinone and metribuzin and reduce organic matters in the waste acid water; (2) carrying out aeration stripping on the extracted waste acid water to remove low-boiling-point substances such as methanol; (3) removing insoluble substances in the waste acid water subjected to aeration stripping; (4) performing resin adsorption on the waste acid water treated in the step (3) to remove residual organic matters, reducing the COD of the waste acid water from 4000-5000mg / L to 1000mg / L or below, changing the original wastewater color from yellow to faint yellow, and basically eliminating the odor of the waste acid water; and (5) concentrating the waste acid water subjected to resin adsorption to obtain concentrated sulfuric acid. According to the method, the waste acid water can be treated into the concentrated sulfuric acid capable of being recycled, treatment equipment is simple, energy consumption is low, and under the increasingly severe environment-friendly situation, high practicability and economical efficiency are achieved.

The invention discloses a podophyllotoxin compound containing a 1,2,4-triazone structure, and an application thereof. The compound has a structure represented by general formula (I). Podophyllotoxin derivatives containing 1,2,4-triazone, represented by the general formula (I), and pharmaceutically acceptable salts thereof have antitumor effects. In-vitro cell activity experiments prove that the podophyllotoxin derivatives containing 1,2,4-triazone have a good inhibition effect on a human chronic myelocytic leukemia cell K562, a human cervical carcinoma cell Hela and a human breast cancer cellMCF-7. The compounds have a good antitumor medicine exploitation and application prospect.

The invention relates to a preparation method of metribuzin and a treatment method of waste liquid. The preparation method comprises the following steps: carrying out heat-insulation reaction on triazinone and dimethyl sulfate at 75 to 80 DEG C in the presence of p-xylene and concentrated sulfuric acid; after the reaction is finished, cooling to 60 DEG C or below; adding water and quenching the reaction; washing a p-xylene layer, distillating under the reduced pressure and drying to obtain the metribuzin. According to the preparation method provided by the invention, the triazinone, which is convenient to purchase in the market, is used as a raw material, the p-xylene is used as a solvent and the concentrated sulfuric acid is used as a catalyst; the metribuzin is prepared through a methodof dropwise adding the dimethyl sulfate; in the reaction process, few byproducts are produced and the treatment method is simple. In a wastewater treatment link, the p-xylene and water can be recycledand utilized and unreacted triazinone is easy to recycle and reutilize. The method provided by the invention has the advantages of high recycling rate, low cost and short production period and the prepared metribuzin has high purity and meets safety and environment protection requirements.

The invention discloses a method for preparing 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one, which comprises a molar ratio of 1:1.2 ~1.5:1.6~2.1 of 4-amino-6-tert-butyl-3-mercapto-1,2,4-triazin-5(4H)-one, dimethyl sulfate and anhydrous sodium carbonate, solvent acetone, Catalyst potassium iodide, heat preservation reaction at 20-30°C for 4-5 hours, finally recover acetone, add water to precipitate, separate and dry to obtain 4-amino-6-tert-butyl-3-methylthio-1,2,4- Triazin-5(4H)-one. The raw materials used in the method of the present invention are easy to get, and the price is low; The reaction of the present invention is mild, easy to control the reaction parameters, and can ensure the safety of the production process; Potassium iodide is used as the catalyst, so that the rapid reaction is complete at normal temperature, greatly reducing the Its production cycle effectively reduces the production cost; the product yield is high, reaching over 90%, and products with a content of over 96% can be directly obtained, which meets the requirements of industrial production and has a good application prospect.

The invention discloses a preparation method of a sun-screening agent octyl triazinone, octyl triazinone prepared by the preparation method and an application of octyl triazinone, and the method comprises the following steps: step 1, carrying out esterification reaction on p-nitrobenzoic acid and isooctyl alcohol to obtain a product I, 2, carrying out a hydrogenation reaction on the product I in the presence of a catalyst, filtering after the reaction is completed, and carrying out reduced pressure distillation to obtain a product II, and step 3, adding a solvent into the product II, heating to reflux, adding the solution A, carrying out a reaction, and carrying out post-treatment to obtain octyltriazinone. Cheap and easily available p-nitrobenzoic acid is used as a raw material, the sun-screening agent octyl triazinone is efficiently prepared through esterification, hydrogenation and coupling, meanwhile, iso-octyl p-aminobenzoate is obtained, the obtained octyl triazinone is high in chromatographic purity and yield, and the method has the advantages of being few in three wastes, low in cost, green, environmentally friendly, easy to operate, easy to control and the like.Easy realization of industrial production.

The invention relates to a preparation method of a stable triazinone anticoccidial drug dry suspension. The triazinone anticoccidial drug is uniformly dispersed in a drug auxiliary material and a carrier through optimization of a suspending aid, a surfactant and a dispersing agent, the dry suspension is prepared through an extrusion spheronization process, and the preparation can be uniformly suspended in water according to a certain proportion for animals to drink. All auxiliary materials involved in the invention are easy to obtain, the cost is low, the preparation process is simple, the product quality is stable, the suspension effect in water is good and the like, and compared with a premix and a solution, the clinical application advantages are more obvious.

The invention provides a novel metribuzin synthesis method which comprises the following steps: (1) adding 6-tert-butyl-4-amino-3-sulfydryl-1, 2, 4-triazine-5 (4H)-ketone into a certain amount of sulfuric acid in batches, and heating until the 6-tert-butyl-4-amino-3-sulfydryl-1, 2, 4-triazine-5 (4H)-ketone is completely dissolved and clarified; 2) cooling to a certain feeding temperature, adding acertain amount of methanol, controlling the temperature to a certain temperature, carrying out a heat preservation reaction for a period of time, and cooling the reaction material to a certain temperature for post-treatment; 3) dropwise adding a certain amount of water into the reaction material, and separating out a large amount of material, namely metribuzin sulfate; and 4) suspending the precipitated metribuzin sulfate in a certain amount of solvent, then adding alkali for neutralization, standing for layering, slowly cooling an organic phase for crystallization, and filtering to obtain high-purity metribuzin. The method is smooth in process, mild in condition and environmentally friendly, metribuzin with the purity of 98% or above can be directly obtained, and the yield can reach 85%or above.