Abstract: 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid crystal forms and a preparation method therefor are proposed. Crystal form I is a monoclinic crystal system, which has a Pc space group and can be obtained by slow cooling, evaporating the solvent at a constant temperature, evaporating the solvent at an increased temperature, or adding an anti-solvent. Crystal form II is a triclinic crystal system, which has a P1 space group and can be obtained by rapid cooling or freeze-drying. According to the method, the process is simple, costs are low, and the yield exceeds 90%; and the crystal forms of the crystal forms I and II have high purity, the crystal shapes thereof are intact, and have excellent fluidity, facilitating preparation, particularly the preparation of a pharmaceutical preparation for preventing and/or treating degenerative diseases of the central nervous system. Furthermore, the two crystal forms have a better apparent solubility than that of raw materials.

Abstract: A method for preparing 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid is proposed. The method may include protection, condensation, and hydrolysis. By means of the screening of a hydroxyl protecting reagent for a starting material, for example, 2-(4-trifluoromethyl)phenethylalcohol and the optimization of other process parameters, the contents of meta-isomer impurities and disubstituted impurities in a target product are effectively controlled. Accordingly, the quality of the product is significantly improved, the reaction yield is also greatly improved, and the improved product quality can satisfy related requirements of preparation research.

Abstract: The present invention relates to pharmaceutical compositions and methods for treating ischemic stroke in humans, using a tetrafluorobenzyl derivative of formula (I) or a pharmaceutically acceptable salt thereof conjointly with a thrombolytic drug, endovascular thrombectomy, or both (e.g., endovascular thrombectomy and a thrombolytic drug). Administration of a tetrafluorobenzyl derivative of formula (I) or its pharmaceutically acceptable salt can reduce reperfusion injury and other adverse events in patients conjointly receiving a thrombolytic drug, endovascular thrombectomy, or endovascular thrombectomy with a thrombolytic drug.

Abstract: The present invention relates to pharmaceutical compositions and methods for treating ischemic stroke in humans, using a tetrafluorobenzyl derivative of formula (I) or a pharmaceutically acceptable salt thereof conjointly with a thrombolytic drug, endovascular thrombectomy, or both (e.g., endovascular thrombectomy and a thrombolytic drug). Administration of a tetrafluorobenzyl derivative of formula (I) or its pharmaceutically acceptable salt can reduce reperfusion injury and other adverse events in patients conjointly receiving a thrombolytic drug, endovascular thrombectomy, or endovascular thrombectomy with a thrombolytic drug.

Abstract: The present invention relates to pharmaceutical compositions and methods for treating ischemic stroke in humans, using a tetrafluorobenzyl derivative of formula (I) or a pharmaceutically acceptable salt thereof conjointly with a thrombolytic drug, endovascular thrombectomy, or both (e.g., endovascular thrombectomy and a thrombolytic drug). Administration of a tetrafluorobenzyl derivative of formula (I) or its pharmaceutically acceptable salt can reduce reperfusion injury and other adverse events in patients conjointly receiving a thrombolytic drug, endovascular thrombectomy, or endovascular thrombectomy with a thrombolytic drug.