99368-66-8Relevant articles and documents
Novel micro-channel preparation process of 2-hydroxy-3-trifluoromethyl-5-nitropyridine
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Paragraph 0031-0071; 0081-0082, (2021/08/14)
The invention discloses a novel micro-channel preparation process of 2-hydroxy-3-trifluoromethyl-5-nitropyridine, and belongs to the technical field of pharmaceutical chemicals. The novel micro-channel preparation process comprises the following steps of: (1) stirring 2-hydroxy-3-trifluoromethylpyridine and a solvent sulfuric acid for 10-30 minutes; (2) stirring nitric acid and sulfuric acid for 30-60 minutes to obtain nitro-sulfur mixed acid; (3) filling a micro-channel pipeline with the mixed solution obtained in the step (1) at a low speed; (4) introducing the nitro-sulfur mixed acid obtained in the step (2) into the micro-channel, controlling the material flow rate to be 9-15mL/min and the reaction time to be 10-40s, and introducing a nitryl positive ion group on 2-hydroxy-3-trifluoromethylpyridine; (5) introducing the reaction liquid obtained in the step (4) into ice water from the outlet end of a reactor for quenching; and (6) carrying out suction filtration on the solid-liquid mixed solution obtained in the step (5), and repeatedly washing with water to obtain the 2-hydroxy-3-trifluoromethyl-5-nitropyridine. The method has the advantages of excellent production safety, high yield, high product purity, simple steps and production cost saving.
Solid dispersions containing an apoptosis-inducing agent
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Page/Page column 208-209, (2019/03/15)
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
ANDROGEN RECEPTOR MODULATOR FOR TREATMENT OF PROSTATE CANCER AND ANDROGEN RECEPTOR-ASSOCIATED DISEASES
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, (2016/11/14)
PROBLEM TO BE SOLVED: To provide a series of compounds that modulate the function of the nuclear hormone receptors, especially the androgen receptor. SOLUTION: The present invention relates to hydantoin compounds, methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example, prostate cancer, and to pharmaceutical compositions containing such compounds. In an embodiment, a pharmaceutical composition includes a therapeutically effective amount of a compound according to the formula II, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or adjuvant. The present invention provides a series of compounds that modulate the function of the nuclear hormone receptors, especially the androgen receptor. These compounds can cause disappearance of prostate cancer cells and tumors. COPYRIGHT: (C)2016,JPOandINPIT
