- 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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- 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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- Reduction of drug ketones by dihydrodiol dehydrogenases, carbonyl reductase and aldehyde reductase of human liver
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In this study, we compared the enzymatic reduction of 10 drugs with a ketone group by homogeneous carbonyl reductase, aldehyde reductase and three dihydrodiol dehydrogenases of human liver cytosol. At least one and in some cases all of the three dihydrodi
- Ohara, Hirotami,Miyabe, Yoshiyuki,Deyashiki, Yoshihiro,Matsuura, Kazuya,Hara, Akira
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p. 221 - 227
(2007/10/03)
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- Reaction of Epichlorohydrin with Hydroxybenzofuran
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Epichlorohydrin (4) was condensed with 2-acetyl-7-hydroxybenzofuran potassium salt (3) to give two radiochemical regio-isomeric 2-acetyl-7-glycidyloxybenzofurans (5a and 5b).The ratio, 5a/5b, was determined to be 5/7 by using 14C-radioisotopic tracer techniques.The present results showed that the reaction proceeds through two different paths in which the phenolate (3) attacks at C-1 of 4 to give 5a and at C-3 to give 5b, the latter path being more favorable than the former.Keywords - epichlorohydrin; nucleophilic substitution; 2-acetyl-7-glycidyloxybenzofuran; radiochemical regio-isomer; 14C-radioisotopic tracer technique; cleavage of carbon chain; reaction mechanism
- Ohishi, Yoshitaka,Nakanishi, Teruo
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p. 3418 - 3423
(2007/10/02)
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- PHARMACEUTICAL COMPOSITION CONTAINING BENZOFURAN DERIVATIVE
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A pharmaceutical composition containing as the essential active ingredient a benzofuran derivative of the formula: STR1 wherein A is--COR', STR2 or ethyl group; B is hydrogen atom when A is--COR' STR3 or--COR" substituted at the 3 or 4 position of the ben
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