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52 results about "Methylone" patented technology

Methylone (also known as "3,4-methylenedioxy-N-methylcathinone", "MDMC", "βk-MDMA" and by the slang term "M1") is an empathogen and stimulant psychoactive drug. It is a member of the substituted amphetamine, substituted cathinone and substituted methylenedioxyphenethylamine classes.

2-pyridinyl[7-(substituted-pyridin-4-yl) pyrazolo[1,5-a]pyrimidin-3-yl]methanones

InactiveUS20050245517A1BiocideOrganic active ingredientsNervous systemNeonatal cerebral hemorrhage
The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones with at least one substituent on both the 2- and 4-pyridinyl ring having the chemical structure of formula I: The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula I to modulate GABA and GABAA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and / or GABAA receptors.
Owner:SKOLNICK PHIL +1

Preparation method of (diphenylphosphine oxide)(mesitylene)ketone and (phenylphosphine oxide)bis(mesitylene ketone)

The invention relates to the technical field of optical radiation free-radical polymerized new materials, especially to a novel synthesis technological process of commercial photoinitiator compounds of (diphenylphosphine oxide)(mesitylene)ketone and (phenylphosphine oxide)bis(mesitylene ketone). According to the invention, 1,3,5-trimethyl-2-(trichloromethyl)-benzene is used as a key raw material and is respectively subjected to a condensation reaction with corresponding organic phosphine precursors so as to prepare the target compounds. In comparison with a known technological route, the technology disclosed in the application has significant advantages such as novelty of the chemical reaction process, economical cost, competitiveness and environmental friendliness.
Owner:SHENZHEN UV-CHEMTECH CO LTD

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

The present invention is directed to an indole benzylamine compound of formula I:useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
Owner:SANOFI SA

Preparation method of 2-p-chlorobenzyl pyridine

The invention relates to a preparation method of 2-p-chlorobenzyl pyridine, comprising the following steps of: firstly adding chlorobenzene and alchlor to 2-pyridine formyl chloride hydrochloride for reaction so as to obtain 1-(4-chlorphenyl)-1-(2-pyridyl) ketone; and then adding diglycol, hydrazine hydrate and potassium hydroxide to the prepared 1-(4-chlorphenyl)-1-(2-pyridyl) ketone for reaction so as to obtain the 2-p-chlorobenzyl pyridine. The 2-p-chlorobenzyl pyridine produced by the method is used as an intermediate for preparing chlorpheniramine and has high product purity and simple and convenient process, and the chlorpheniramine prepared by using the 2-p-chlorobenzyl pyridine accords with Chinese pharmacopoeia; in addition, the invention has low cost, easy industrialization and outstanding economic benefit and social benefit.
Owner:GUANGXI UNIV

Hydroxyalkyl benzophenone photocuring agent and its preparation and use

A novel hydroxyalkyl phenyl ketone: (1-hydroxycylohexyl)[4-(2- hydroxy ethoxy)phenyl] methanone, its preparing process and its application as the trigger for optical solidification are disclosed. Said trigger can effectively and optical trigger the polymerization between unsaturated compound and resin. Its special molecular structure can prevent migration, odoring and yellowing.
Owner:XIANGTAN UNIV

Asymmetric synthesis method for anti-allergy drug carbinoxamine

The invention relates to an asymmetric synthesis method for an anti-allergy drug carbinoxamine. The method specifically comprises the following steps: oxidizing (4-chlorophenyl)(2-pyridyl)ketone to obtain (4-chlorophenyl)(2-pyridyl)ketone-N-oxide; by taking monosulfonylated chiral diamine and metal ruthenium / rhodium / iridium complex as catalysts and sodium formate or a formic acid and triethylamine mixture or isopropanol as a hydrogen source, reducing the (4-chlorophenyl)(2-pyridyl)ketone-N-oxide through asymmetry transfer hydrogenation to prepare (S)-(4-chlorophenyl)(2-pyridyl)methanol-N-oxide; reducing the (S)-(4-chlorophenyl)(2-pyridyl)methanol-N-oxide to obtain (S)-(4-chlorophenyl)(2-pyridyl)methanol; and performing etherification reaction on the (S)-(4-chlorophenyl)(2-pyridyl)methanol and 2-chloro-N,N-dimethylethylamine to obtain the product, wherein the overall yield is 74.6%.
Owner:CHINA THREE GORGES UNIV

Substituted (e)-n'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors

Substituted (E)-N-(1-phenylethylidene)benzohydrazide analogs or (3-(5-chloro-2-hydroxyphenyl)-4-METHYL-1 H-pyrazol-1-YL)(3- (morpholinosulfonyl)phenyl)methanone, derivatives thereof, and related compounds are useful as inhibitors of lysine-specific histone demethylase, including LSD1. Synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1 (lysine-specific demethylase). A pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof, and one or more of: (a) at least one agent known to increase histone demethylase activity; (b) at least one agent known to decrease histone demethylase activity; (c) at least one agent known to treat a disorder of uncontrolled cellular proliferation; (d) at least one agent known to treat a neurodegenerative disorder; (e) instructions for treating a neurodegenerative disorder; or (f) instructions for treating a disorder associated with uncontrolled cellular proliferation.
Owner:UNIV OF UTAH RES FOUND

Method for preparing SGLT2 (Sodium-Dependent Glucose Transporters 2) inhibitor intermittent

The invention discloses a method for preparing an SGLT2 (Sodium-Dependent Glucose Transporters 2) inhibitor intermittent. The method comprises the following steps: (1) carrying out a Friedel-Crafts reaction on 5-halogen-2-chlorobenzoic acid and fluorobenzene so as to obtain (5-halogen-2-chlorphenyl) (4-fluorophenyl) ketone; (2) under the action of an organic alkali, carrying out a substitution reaction on (5-halogen-2-chlorphenyl) (4-fluorophenyl) ketone and ethanol, and after the reaction is completed, treating so as to obtain (5-halogen-2-chlorphenyl) (4-ethyoxyl phenyl) ketone; (3) carryingout a carbonyl reduction reaction on the (5-halogen-2-chlorphenyl) (4-ethyoxyl phenyl) ketone under the action of a reducing agent, thereby obtaining the SGLT2 inhibitor intermittent. By adopting themethod, an ethoxy metal reagent and DMSO (Dimethyl Sulfoxide) (or DMF (Dimethyl Formamide)) are replaced by the inorganic alkali and ethanol, so that not only is the cost effectively reduced, but also the environment can be protected.
Owner:杭州科耀医药科技有限公司

(4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and their use

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Owner:THE UNIV OF EDINBURGH

Photoprotective system

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.
Owner:PIERRE FABRE DERMO COSMETIQUE CORP

Production method of 4-(4-chlorophenoxy)-2-chloro phenyl-methyl ketone

A process for preparing 4-(4-chlorophenoxy)-2-chlorophenyl-methylone as the intermediate of difenoconazole includes reacting between p-chlorophenol and 2,4-dichloro phenyl ethanone at 100 deg.C under catalysis of copper match, and separating. Its advantages are low reaction temp, and high output rate up to more than 95%.
Owner:JIANGSU CHANGQING AGROCHEMICAL CO LTD

New method for preparing 1-(6-methylpyridine-3-yl)-2-[4-(methylsulfanyl)phenyl]acetone

ActiveCN103664754AIncrease hydroxylamine lengthAvoid it happening againOrganic chemistryGrignard reagentKetone
The invention relates to a new method for preparing 1-(6-methylpyridine-3-yl)-2-[4-(methylsulfanyl)phenyl]acetone. The method comprises the step of reacting Grignard reagent of formula (II) with isoxazole-2-yl-(6-methylpyridine-3-yl)-ketone of formula (III) at minus 20 to 0 DEG C to obtain the 1-(6-methylpyridine-3-yl)-2-[4-(methylsulfanyl)phenyl]acetone of formula (I). Compared with the prior art, the method has the advantage of lowering the explosive risk of the reaction system.
Owner:SHANGHAI JIAO TONG UNIV +1

Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament

Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
Owner:BOEHRINGER INGELHEIM INT GMBH

Preparation method of (4,6-diaryl-tetrahydropyridine-3-yl)(aryl) ketone

The invention relates to a preparation method of (4,6-diaryl-tetrahydropyridine-3-yl)(aryl)ketone. The method includes the following steps that (1) aryl propargyl alcohol, chalcone derivatives, acid and a solvent are mixed and heated for reaction under reflux conditions; (2) amine compounds are added into a reaction system where the reaction is completed for reaction for 9-17 hours under reflux conditions, and the (4,6-diaryl-tetrahydropyridine-3-yl)(aryl)ketone is obtained. Compared with the prior art, the synthesis method has the advantages that the method is simple, the condition is mild, the yield is relatively high, and the atom utilization rate can reach 100%. The synthesis method greatly optimizes synthesis of the compound and provides a new synthesis idea for the synthesis of compounds with similar structures.
Owner:SHANGHAI INST OF TECH

2-substituted-3-arylketone-6-(5-methyl-2-phenyl-4-ehtyoxyloxazole)benzofuran compound

InactiveCN103588763AEstablish and optimize preparation methodsEasy to prepareAntibacterial agentsOrganic active ingredientsKetoneAntibacterial activity
The invention relates to a 2-substituted-3-arylketone-6-(5-methyl-2-phenyl-4-ehtyoxyloxazole)benzofuran compound with the structural formula as shown in the specification. Compared with the prior art, the novel compound is prepared by introducing (5-methyl-2-phenyloxaole-4-yl)ethyoxyl to the 6 site of benzofuran by taking 3-ketone substituent benzofuran as the center of an aromatic ring; a preparation method of the compound is established and optimized; the prepared novel compound is subjected to an antibacterial screening experiment; the primary in-vitro antibacterial experiment confirms that the prepared novel compound has excellent broad-spectrum antibacterial activity and can be used for preparing novel antibacterial drugs.
Owner:SHANGHAI JIAO TONG UNIV

Preparation method of (3-amino-azetidine-1-yl)-cyclopropyl-ketone

The invention discloses a preparation method of (3-amino-azetidine-1-yl)-cyclopropyl-ketone. The preparation method comprises the following steps: dissolving azetidine-3-ketone hydrochloride in a solvent under an alkaline condition, adding an acylation reagent for reaction to obtain 1-cyclopropanecarbonyl-azetidine-3-ketone; dissolving the 1-cyclopropanecarbonyl-azetidine-3-ketone in a solvent, adding benzylamine, stirring and dissolving the benzylamine, and adding a reducing agent for reaction at-5-5 DEG C to obtain (3-benzylamino-azetidine-1-yl)-cyclopropyl-ketone; dissolving 3-boroamino-azetidine-1-yl)-cyclopropyl-ketone in a solvent to react with a reducing agent in the presence of a catalyst to obtain (3-amino-azetidine-1-yl)-cyclopropyl-ketone. The raw materials used in the preparation method provided by the invention are low in price and wide in source, six steps of reaction of an original synthesis method are reduced to three steps of reaction, dangerous reagents are not used,reaction steps are shortened, and reaction efficiency is improved.
Owner:南京合巨药业有限公司

Synthesis method of phenyl(quinolin-8-yl)-one derivative

A synthesis method of a phenyl(quinolin-8-yl)-one derivative comprises the following steps: by taking 8-methylquinoline or substituted 8-methylquinoline and aryl iodide as raw materials, Ag2CO3 as an additive, KOAc as alkali and Pd(OAc)2 as a catalyst, reacting the raw materials in a solution formed by mixing hexafluoroisopropanol and glacial acetic acid according to a volume ratio of 3: 7, sealing a tube at 130 DEG C, and reacting for 24 hours to generate the target product. The synthesis process route is simple, and the highest yield reaches 87%.
Owner:XUZHOU NORMAL UNIVERSITY

3,4-methylenedioxy methcathinone detection methods

InactiveCN110346470AFast waySimple methodComponent separationGas chromatography flame ionization detectorDischarge ionization detector
The invention discloses 3,4-methylenedioxy methcathinone detection methods. One method in the invention performs organic solvent extraction on Methylone in a suspected drug sample, performs qualitative analysis by using gas chromatography-mass spectrography (GC-MS), and performs quantitative analysis on Methylone by using a gas chromatography-flame ionization detector (GC-FID). The other method inthe method performs organic solvent extraction on Methylone in the suspected drug sample, performs qualitative analysis in a multi-reaction monitoring (MRM) mode by using a liquid chromatography-tandem mass spectrometry (LC-MS / MS), and performs quantitative analysis on Methylone by using a liquid chromatography-diode array or ultraviolet detector (LC-DVD) or LC-UV).
Owner:INST OF FORENSIC SCI OF MIN OF PUBLIC SECURITY

Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives

The present invention relates to a process for the preparation of particular 2-(2H-[1,2,3]triazol-2-yl)-benzoic acid derivatives of formula (I), to certain crystalline forms of potassium salts of said2-(2H-[1,2,3]triazol-2-yl)-benzoic acid derivatives of formula (IK), to certain crystalline forms of said 2-(2H-[1,2,3]triazol-2-yl)-benzoic acid derivatives of formula (I), and to their use in the preparation of pharmaceuticals such as (S)-(2-(5-chloro-4-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)-(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone.
Owner:IDORSIA PHARM LTD

Application of substituted piperazine compound in preparation of medicament for resisting fungal infection

The invention relates to the application of a substituted piperazine compound in the preparation of a medicament for resisting fungal infection and particularly discloses a compound which is (4-chlorophenyl)-(piperazin-1-yl)-methanone or pharmaceutically acceptable salt thereof as well as a preparation method and medicinal application of the (4-chlorophenyl)-(piperazin-1-yl)-methanone or medicinally acceptable salt thereof. The steps for synthesizing the compound are simple, the method for preparing the compound is simple and practical, the sources of raw materials are easy to obtain, the cost is low, and less pollution is caused. The compound has an obvious activity of inhibiting the growth of fungi and has the MIC value of 62.5mcg / ml. The pharmacodynamic results show that the substituted piperazine compound or medicinally acceptable salt is expected to be used to prepare the medicament for preventing and treating the diseases caused by fungal infection.
Owner:DALI UNIV

Synthesis method of (3,4-dimethoxyphenyl)(4-p henyl fluoride) ketone

The invention relates to a synthesis method of (3,4-dimethoxyphenyl)(4-p henyl fluoride) ketone, and solves the problem that in the prior art, the synthesis method brings large amout of pollution and the cost is high. According to the method, acidic ionic liquid is applied as the catalyst which is polymerized by an ionic liquid precursor containing positive electricity and metal halides with negative electricity, wherein, the ionic liquid precursor is [Bmim] C1 or [Bmim] Br, the metal halide is AlCl3, FeC13, ZnCl2 or CuCl2. The synthesis method of (3,4-dimethoxyphenyl)(4-p henyl fluoride) ketone has the advantages of largely reducing the use amout of catalysts, lowering the emission of the waste water, saving the neutralization process of sulfuric acid, eliminating the waste water generated in the step, avoiding the corrosion caused by strong acid. Compared with the original reaction, the emission of slag is omitted. The reaction product is easy to be separated. The post-treatment is simpler. The reaction temperature is low. The energy cost is low. The product yield rate can reach as high as 97% or higher.
Owner:BEIJING UNIV OF CHEM TECH

2-Substituted-3-arylmethanone-6-(5-methyl-2-phenyl-4-ethoxyoxazole)benzofuran compound

InactiveCN103588763BEstablish and optimize preparation methodsEasy to prepareAntibacterial agentsOrganic active ingredientsAntibacterial activityKetone
The invention relates to a 2-substituted-3-arylketone-6-(5-methyl-2-phenyl-4-ehtyoxyloxazole)benzofuran compound with the structural formula as shown in the specification. Compared with the prior art, the novel compound is prepared by introducing (5-methyl-2-phenyloxaole-4-yl)ethyoxyl to the 6 site of benzofuran by taking 3-ketone substituent benzofuran as the center of an aromatic ring; a preparation method of the compound is established and optimized; the prepared novel compound is subjected to an antibacterial screening experiment; the primary in-vitro antibacterial experiment confirms that the prepared novel compound has excellent broad-spectrum antibacterial activity and can be used for preparing novel antibacterial drugs.
Owner:SHANGHAI JIAO TONG UNIV
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