139332-61-9Relevant articles and documents
Preparation method of arotinolol hydrochloride
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, (2021/07/09)
The invention relates to the technical field of medicines, particularly provides a preparation method of arotinolol hydrochloride, and relates to the technical field of medicines. The preparation method of the arotinolol hydrochloride, provided by the invention, comprises the following steps: (1) enabling tetrahydrofuran, 2-formamide-5-(2-sulfydryl-1, 3-thiazole-4-yl)-thiophene, water, sodium bicarbonate and epoxy chloropropane to react to generate an intermediate product C181101170-I03; (2) carrying out a reaction on absolute ethyl alcohol, C181101170-I03 and tert-butylamine, so as to obtain an intermediate product C181101170-I02; (3) subjecting methanol, ethyl acetate, C181101170-I02 and concentrated hydrochloric acid to a reaction, and obtaining an arotinolol hydrochloride crude product; and (4) treating the arotinolol hydrochloride crude product with DMSO and acetone to obtain arotinolol hydrochloride. The product arotinolol hydrochloride obtained by the method is high in yield, high in purity and small in impurity, the purity of the product can be well controlled, and the method is suitable for industrial production.
Refinement method of arotinolol hydrochloride
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Paragraph 0018; 0020; 0022; 0024, (2018/02/04)
The invention relates to a refinement method of arotinolol hydrochloride and belongs to the field of chemical medicines. The refinement method is characterized in that crude arotinolol hydrochloride is added to a system containing ethyl acetate, methanol and pure water, subjected to an alkali recovery operation under a weak alkaline condition, then pulped and purified, and free alkaline arotinolol with higher purity is obtained; arotinolol forms salt in an alcoholic solution, and refined arotinolol hydrochloride is obtained. The method is simple to operate, the yield is relatively high, and industrial production is facilitated.
ANTIHYPERTENSIVE THERAPY
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, (2009/09/08)
A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.