- NOVEL TETRAZOLES
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This invention relates to tetrazoles and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune
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Page/Page column 26-27
(2021/04/23)
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- Growth Factor Receptor antagonists. Preparation method and application thereof
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The invention relates to a small molecule antagonist for transforming growth factor β receptors, a method for preparing the small molecule antagonist, and application of the small molecule antagonist in preparation of drugs. The small molecule antagonist for transforming the growth factor β receptor has the application of treating and/or preventing various diseases mediated by ALK5, and has great clinical application potential.
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Paragraph 0093-0094; 0103-0106
(2021/11/10)
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- Synthetic method of 4-aminothiazole-5-carboxylic acid ethyl ester
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The invention belongs to the technical field of medical intermediates, and relates to a synthetic method of 4-aminothiazole-5-carboxylic acid ethyl ester. The synthetic method comprises the steps that4-amino-2-(methylthio)thiazol-5-carboxylic acid ethyl ester is dissolved in anhydrous ethanol, concentrated hydrochloric acid is added, zinc powder is added in batches under agitation, and a refluxing reaction is conducted for 4 hours to obtain a neutralization solution; the neutralization solution is filtered, a filter cake is washed with ethanol for 2-3 times, filter liquor is combined, vacuumconcentration is conducted, and a concentrated solution is obtained; dichloromethane and water are added into the concentrated solution and agitated to separate an organic phase; and the organic phaseis washed by a saturated sodium chloride solution, and is dried and concentrated by anhydrous sodium sulfate, and isopropanol is used for crystallizing to obtain the 4-aminothiazole-5-carboxylic acidethyl ester. According to the synthetic method, a novel method for removing methylthio group from an aromatic ring, the cost of raw materials is low, the yield is high, and the synthetic method is suitable for scale-up production.
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Paragraph 0026-0030
(2019/11/12)
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