US2016206593A1PendingUtilityA1

Pharmaceutical for prophylaxis or treatment of hypertension

Assignee: DAIICHI SANKYO CO LTDPriority: Jul 23, 2013Filed: Jan 14, 2016Published: Jul 21, 2016
Est. expiryJul 23, 2033(~7 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 9/10A61P 9/00A61P 9/06A61P 9/04A61P 9/12A61P 3/10A61K 9/2054A61K 31/4422A61K 31/40A61K 31/4178A61K 45/00A61P 25/00A61P 13/02A61P 13/12A61K 31/549
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Claims

Abstract

A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by comprising (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (A) to (C), for administration simultaneously or separately at a time interval: (A) an angiotensin II receptor antagonist, (B) a calcium antagonist, and (C) a diuretic.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension, characterized by comprising
 (i) a mineralocorticoid receptor antagonist which comprises a substance selected from the group consisting of a compound represented by the following formula (I):   
       
         
           
           
               
               
           
         
         and an atropisomer thereof, and a pharmacologically acceptable salt thereof, and 
         (ii) one or more components selected from the following components (A) to (C), for administration simultaneously or separately at a time interval:
 (A) one or more angiotensin II receptor antagonists; 
 (B) one or more calcium antagonists comprising a substance selected from the group consisting of a 1,4-dihydropyridine-based compound and a pharmacologically acceptable salt thereof; and 
 (C) one or more diuretics. 
 
       
     
     
         2 . A pharmaceutical for the prophylaxis or treatment of a disease selected from the group consisting of hypertension, a heart disease, angina pectoris, myocardial infarction, arrhythmia, sudden death, heart failure, cardiac hypertrophy, a kidney disease, diabetic nephropathy, glomerulonephritis, nephrosclerosis, a cerebrovascular disease, cerebral infarction, intracerebral hemorrhage, and a vascular disorder (arteriosclerosis, restenosis after PTCA, or peripheral circulatory disturbance), comprising one or more components selected from component (A), component (B), and component (C), and the mineralocorticoid receptor antagonist according to  claim 1  as active ingredients. 
     
     
         3 . The pharmaceutical according to  claim 1 , wherein the pharmaceutical is in the form of a pharmaceutical composition. 
     
     
         4 . The pharmaceutical according to  claim 1 , wherein the angiotensin II receptor antagonist is (5-methyl-2-oxo-1,3-dioxolan-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[2′-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]imidazole-5-carboxylate. 
     
     
         5 . The pharmaceutical according to  claim 1 , wherein the calcium antagonist is a calcium antagonist selected from the group consisting of azelnidipine, amlodipine, benidipine, nitrendipine, manidipine, nicardipine, nifedipine, nisoldipine, cilnidipine, lercanidipine, niguldipine, nimodipine, aranidipine, efonidipine, barnidipine, felodipine, clevidipine, lacidipine, and nilvadipine. 
     
     
         6 . The pharmaceutical according to  claim 1 , wherein the calcium antagonist is amlodipine. 
     
     
         7 . The pharmaceutical according to  claim 1 , wherein the diuretic is a diuretic selected from the group consisting of hydrochlorothiazide, methyclothiazide, benzylhydrochlorothiazide, trichloromethiazide, cyclopenthiazide, polythiazide, ethiazide, cyclothiazide, bendroflumethiazide, and hydroflumethiazide. 
     
     
         8 . The pharmaceutical according to  claim 1 , wherein the diuretic is hydrochlorothiazide. 
     
     
         9 . The pharmaceutical according to  claim 1 , wherein the mineralocorticoid receptor antagonist is (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide represented by the following formula (Ia): 
       
         
           
           
               
               
           
         
         and the calcium antagonist is amlodipine. 
       
     
     
         10 . The pharmaceutical according to  claim 1 , wherein the pharmaceutical is formulated as a single preparation.

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