52 results about "Methylone" patented technology

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.

The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of Claim 1. The present invention is directed also to the preparation of a compound of formula I.

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%.

Substituted (E)‑N'‑(1‑phenylethylidene)phenylhydrazide analogs or (3‑(5‑chloro‑2‑hydroxyphenyl)‑4‑methyl‑1H‑pyrazole -1-yl)(3-(morpholinosulfonyl)phenyl)methanone, derivatives thereof, and related compounds are useful as inhibitors of lysine-specific histone demethylases including LSD1 of. Synthetic methods of making the compounds; pharmaceutical compositions comprising the compounds; methods of using the compounds and compositions to treat disorders associated with LSD1 (lysine specific demethylase) dysfunction. A pharmaceutically acceptable salt, hydrate, solvate or polymorph thereof, and one or more of the following: (a) at least one agent known to increase the activity of histone demethylase; ( b) at least one agent known to reduce the activity of histone demethylases; (c) at least one agent known to treat disorders of uncontrolled cell proliferation; (d) at least one agent known to treat neurodegeneration (e) instructions for treating neurodegenerative disorders; or (f) instructions for treating disorders associated with uncontrolled cell proliferation.

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.

Provided are novel crystals of [2-(1-methyl-1H-pyrazol-4-yl)-6-(morpholin-4-yl)-9H-purin-8-yl][4-(morpholin-4-yl)piperidin-1-yl]methanone and a pharmaceutically acceptable salt thereof having advantageous characteristics. [2-(1-Methyl-1H-pyrazol-4-yl)-6-(morpholin-4-yl)-9H-purin-8-yl][4-(morpholin-4-yl)piperidin-1-yl]methanone and a pharmaceutically acceptable salt thereof provided by the present invention are excellent in stability and have satisfactory physical properties as a drug substance of a pharmaceutical product.

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%.

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.

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.

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.

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.

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.