US2007185070A1PendingUtilityA1

Novel PPAR ligands that do not cause fluid retention, edema or congestive heart failure

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Assignee: BETHESDA PHARMACEUTICALS INCPriority: Aug 10, 2002Filed: Apr 6, 2007Published: Aug 9, 2007
Est. expiryAug 10, 2022(expired)· nominal 20-yr term from priority
Inventors:Harrihar A. Pershadsingh
A61P 9/12A61P 7/02A61P 5/48A61P 43/00A61P 9/04A61P 3/10A61P 9/00A61P 9/10A61P 3/06A61P 3/00A61P 3/04A61P 29/00A61K 31/41A61P 13/12A61K 31/4184A61K 31/415A61P 1/16
63
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Claims

Abstract

Methods are provided for treating or prophylactically preventing metabolic disorders in humans without causing, promoting, or aggravating fluid retention, peripheral edema, pulmonary edema, or congestive heart failure, by administration of a therapeutically effective amount of a compound sufficient to partially or fully activate peroxisome proliferator activated receptors (PPARs) and partially or fully inhibit, antagonize or block the activity of angiotensin II type 1 receptors. Metabolic disorders that can be treated or prevented include but are not limited to type 2 diabetes, the metabolic syndrome, prediabetes, and other insulin resistance syndromes. Compounds are provided that antagonize or block the angiotensin II type 1 (AT1) receptor, function as partial or full activators of peroxisome proliferator activated receptors (PPARs), can be used to treat or prevent diseases known to be treatable or preventable by PPAR activators and were not previously recognized to be therapeutic targets for angiotensin II receptor antagonists.

Claims

exact text as granted — not AI-modified
1 - 17 . (canceled)  
     
     
         18 . A composition for treating hypertension, the composition comprising: 
 a therapeutically effective amount of a diuretic, wherein the therapeutically effective amount of the diuretic is sufficient to increase a risk for hyperglycemia and    a therapeutically effective amount of a compound sufficient to (a) at least partially activate peroxisome proliferator activated receptor-gamma (PPAR-γ), (b) at least partially inhibit, antagonize or block an activity of angiotensin II type 1 receptors and (c) reduce hyperglycemia.    
     
     
         19 . The composition of  claim 18 , wherein the therapeutically effective amount of the compound is sufficient to reduce a condition of dyslipidemia selected from the group consisting of hyperlipemia, hypercholesterolemia, and hypertriglyceridemia.  
     
     
         20 . The composition of  claim 18 , wherein the therapeutically effective amount of the compound is sufficient to reduce hyperinsulinemia.  
     
     
         21 . The composition of  claim 18 , wherein the diuretic is selected from the group consisting of a thiazide and a chlorbenzenesulfonamide.  
     
     
         22 . The composition of  claim 21 , wherein the diuretic is a thiazide and the thiazide is hydrochlorothiazide.  
     
     
         23 . The composition of  claim 21 , wherein the diuretic is a chlorbenzenesulfonamide and the chlorbenzenesulfonamide is chlorthalidone.  
     
     
         24 . The composition of  claim 18 , wherein the compound is selected from the group consisting of telmisartan, irbesartan, losartan, candesartan, candesartan cilexetil, olmesartan, and olmesartan medoximil, a tautomeric form thereof, a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable solvate thereof.  
     
     
         25 . The composition of  claim 18 , wherein the compound is telmisartan.  
     
     
         26 . The composition of  claim 25 , wherein the diuretic is hydrochlorothiazide.  
     
     
         27 . The composition of  claim 25 , wherein the diuretic is chlorthalidone.  
     
     
         28 . The composition of  claim 18 , wherein the compound is candesartan cilexetil.  
     
     
         29 . The composition of  claim 28 , wherein the diuretic is hydrochlorothiazide.  
     
     
         30 . The composition of  claim 18 , wherein the composition is suitable for administration in a pharmaceutically acceptable formulation.  
     
     
         31 . The composition of  claim 18 , formulated for oral administration.  
     
     
         32 . The composition of  claim 31 , comprising a solid or a fluid unit dosage form selected from the group consisting of tablets, hard gelatin capsules, soft gelatin capsules, suspensions, elixirs, and syrups.  
     
     
         33 . The composition of  claim 18 , formulated for parenteral administration.  
     
     
         34 . The composition of  claim 33  comprising an aqueous solution, wherein the compound is at a concentration of between about 1 to about 100 mg/ml.  
     
     
         35 . A unit dose comprising the composition of  claim 25 , containing a dose of telmisartan suitable for oral administration of telmisartan to a subject in need thereof, wherein the dose is between about 0.1 to about 10 mg/kg body weight of the subject.  
     
     
         36 . The composition of  claim 26 , wherein 1 part by weight of telmisartan is combined with 0.01 to 100 parts by weight of hydrochlorothiazide.  
     
     
         37 . The composition of  claim 36 , wherein the 1 part by weight of telmisartan is 80 mg.  
     
     
         38 . The composition of  claim 36 , wherein the 1 part by weight of telmisartan is 160 mg.  
     
     
         39 . A unit dose comprising the composition of  claim 36 .  
     
     
         40 . A unit dose comprising the composition of  claim 27  containing a dose of telmisartan suitable for oral administration of telmisartan to a subject in need thereof, wherein the dose is between about 0.1 to about 10 mg/kg body weight of the subject.  
     
     
         41 . The composition of  claim 27 , wherein 1 part by weight of telmisartan is combined with 0.01 to 100 parts by weight of chlorthalidone.  
     
     
         42 . The composition of  claim 41 , wherein the 1 part by weight of telmisartan is 80 mg.  
     
     
         43 . The composition of  claim 41 , wherein the 1 part by weight of telmisartan is 160 mg.  
     
     
         44 . A unit dose comprising the composition of  claim 41 .  
     
     
         45 . The composition of  claim 29 , wherein 1 part by weight of candesartan cilexetil is combined with 0.01 to 100 parts by weight of hydrochlorothiazide.  
     
     
         46 . A unit dose comprising the composition of  claim 45 .  
     
     
         47 . A method of treating hypertension comprising administering the composition of  claim 18  to a subject in need thereof.  
     
     
         48 . The method of  claim 47 , wherein the hypertension is insulin-resistant hypertension.  
     
     
         49 . A method of treating hypertension comprising administering the composition of  claim 26  to a subject in need thereof.  
     
     
         50 . The method of  claim 49 , wherein the hypertension is insulin-resistant hypertension.  
     
     
         51 . A method of treating hypertension comprising administering the composition of  claim 27  to a subject in need thereof.  
     
     
         52 . The method of  claim 51 , wherein the hypertension is insulin-resistant hypertension.  
     
     
         53 . A method of treating hypertension comprising administering the composition of  claim 29  to a subject in need thereof.  
     
     
         54 . The method of  claim 53 , wherein the hypertension is insulin-resistant hypertension.

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