53684-49-4

Usage

Originator

Adobiol,Yoshitomi,Japan,1974

Uses

Bufetolol is a β-adrenergic blocking agent and it inhibits the activation of adenyl cyclase.

Manufacturing Process

The preparation of a similar compound in which a methoxyethoxy group replaces the tetrahydrofurfuryloxy group in Bufetrol is described in the following example. Nine grams of o-(2-methoxyethoxy)phenol is suspended in 50 milliliters of water containing 3.7 grams of potassium hydroxide, and 5.5 grams of epichlorhydrin is added thereto with stirring. The mixture is stirred at room temperature for 7 hours, and then extracted with two 50 milliliter portions of benzene. The extract is washed with water, dried over anhydrous magnesium sulfate and the benzene is distilled off to give 8.5 grams of oily 1- (2,3-epoxypropoxy)-2-(2-methoxyethoxy)benzene showing nD 20 = 1.5257. Bufetolol has the methoxyethoxy group in place of the 2- tetrahydrofurfuryloxy group in Bufetrol. To a solution of 1-(2,3-epoxypropoxy)-2-(2-tetrahydrofurfuryloxy)benzene in methanol are added tert-butylamine and water, the mixture is allowed to stand at 25°-30°C for 72 hours, and then the methanol is distilled off. The residue is dissolved in toluene and the solution is extracted twice with 5% oxalic acid. The aqueous extract is dried over potassium carbonate and concentrated to give Bufetrol.

Therapeutic Function

Antiarrhythmic

InChI:InChI=1/C18H29NO4/c1-18(2,3)19-11-14(20)12-22-16-8-4-5-9-17(16)23-13-15-7-6-10-21-15/h4-5,8-9,14-15,19-20H,6-7,10-13H2,1-3H3

Relevant academic research and scientific papers

THERAPY FOR COMPLICATIONS OF DIABETES

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.

ANTIHYPERTENSIVE THERAPY

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.

Method for treating resistant hypertension

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.

Enteric coated mixture of 4-(2-hydroxy-3-isopropylamino-propoxy) indole and sodium lauryl sulphate

The present invention provides a pharmaceutical composition for controlled release of 4-(2-hydroxy-3-isopropylamino-propoxy) indole in the intestinal tract, admixed with sodium lauryl sulphate, and enteric coated.