- An improved synthesis of a b-blocker celiprolol hydrochloride
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Celiprolol hydrochloride, a β-blocker drug, has been synthesised from 4-chloronitrobenzene. The route involved hydrolysis of the chloride and acetylation of the phenol, reduction of the nitro group, and acylation of theamine. This was followed by Fries rearrangement of the acetyl group, Williamson etherification with epichlorohydrin, followed by opening of the epoxide ring and salt formation. The overall yield of celipropol was 39.1% on the basis of 4-chloronitrobenzene. The Fries rearrangement was substantially improved. The process is suitable for industrial application because of its convenient and environmentally friendly reaction conditions.
- Ji, Li,Qian, Chao,Chen, Xin-Zhi,Mao, Xiao-Yuan
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p. 640 - 643,4
(2020/07/30)
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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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- FLUORESCENCE BASED DETECTION OF SUBSTANCES
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A method for the fluorescent detection of a substance, the method comprising providing particles comprising a metal or a metal oxide core, wherein one or more optionally fluorescently tagged antibodies or human specific peptide nucleic acid (PNA) oligomers for binding to a substance is/are bound, directly or indirectly, to the surface of the metal or metal oxide; contacting a substrate, which may or may not have the substance on its surface, with the particles for a time sufficient to allow the antibody/PNA oligomer to bind with the substance; removing those particles which have not bound to the substrate; if the antibodies or PNA oligomers are not fluorescently tagged, contacting the substrate with one or more fluorophores that selectively bind with the antibody and/or substance, then optionally washing the substrate to remove unbound fluorophores; and illuminating the substrate with appropriate radiation to show the fluorophores on the substrate.
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- Method for treating resistant hypertension
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A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, 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.
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- A new and improved process for celiprolol hydrochloride
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Celiprolol hydrochloride, a β-blocker drug, has been synthesized by a new approach. How this new process offers distinctive advantages over the existing one will be described.
- Joshi, Ramesh A.,Gurjar, Mukund K.,Tripathy, Narendra K.,Chorghade, Mukund S.
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p. 176 - 178
(2013/09/07)
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- Novel crystalline salts of aryloxy-propanolamines, a process for their preparation and their use
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The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof.
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- On the Synthesis of Cardioselective β-Adrenergic Receptor Blocking Agent Celiprolol
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The synthesis of 3--1,1-diethyl-urea-hydrochloride (celiprolol-HCl, in the following briefly called celiprolol; ST 1396-HCl), as well as some physicochemical properties and spectroscopic data are reported. - Key words: β-Blockers; Celiprolol, cardioselectivity, synthesis; ST 1396-HCl
- Zoelss, G.
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