- A process for preparing went horizontal method
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The invention discloses a method for synthesizing aranidipine. The method comprises the following steps: performing addition on propargyl alcohol and ethylene glycol, performing reaction on propargyl alcohol and ethylene glycol which are subjected to addition and ketene dimer to obtain acetoacetic acid 2,2-ethylenedioxy propyl ester, then performing amination and performing condensation and hydrolysis on acetoacetic acid 2,2-ethylenedioxy propyl ester and 2-(2-nitro benzal)-3-oxo-methyl butyrate to obtain aranidipine serving as an anti-hypertension medicine. According to the preparation method for aranidipine, NiCl2 replaces mercury bichloride, is used as a promoter for preparing 2,2-ethylenedioxy propyl alcohol, non-toxic and is good in catalysis effect; ethanediamine is used as a catalyst for preparing acetoacetic acid 2,2-ethylenedioxy propyl ester and is high in catalytic yield; moreover, a product can be put into the next reaction step without being purified; by the use of NiCl2 and ethanediamine, the speed of the whole reaction process is increased, and the method is environment-friendly and is high in economical benefit.
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Paragraph 0033; 0034
(2017/08/25)
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- THERAPY FOR COMPLICATIONS OF DIABETES
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A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
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- ANTIHYPERTENSIVE THERAPY
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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.
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- 1,4-Dihydropyridine compounds
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1,4-Dihydropyridine compounds having excellent coronary and vertebral vasodilation, blood pressure depression and anti-hypertensive activities are disclosed. These compounds are low toxic and stable to light, and are very useful for pharmaceutical agents.
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