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32 results about "Aldosterone Receptor Antagonist" patented technology
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A class of agents that act by selectively inhibiting aldosterone receptor activation with diuretic activity. Aldosterone receptor antagonists bind to and block the activation of aldosterone (mineralocorticoid) receptors on the epithelial cells in the late distal tubule and collecting duct of the kidney, thus preventing the synthesis of aldosterone-induced proteins which enhance Na+ retention and K+ and H+ secretion. The enhanced excretion of Na+ produces diuresis ultimately resulting in a reduction in blood pressure without the loss of K+.
Combination of an aldosterone receptor antagonist and an anti-diabetic agent
A combination therapy comprising a therapeutically-effective amount of an aldosterone receptor antagonist and a therapeutically-effective amount of an anti-diabetic agent is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred antidiabetic agents are those compounds having high potency and oral or parenteral bioavailability. Preferred aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9α,11α-substituted epoxy moiety.
Owner:PHARMACIA CORP
Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of congestive heart failure
InactiveUS20020042405A1Reduce pathogenicityImprove the level ofMetabolism disorderBlood disorderCalcium channel blockerAldosterone
A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9alpha,11alpha-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HCl (Benzenacetonitrile, (±)-alpha[3[[2-(3,4-dimethoxyphenyl) ethyl]methylamino]propyl]-3,4-dimethoxy-alpha-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.
Owner:SCHUH JOSEPH R
Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of congestive heart failure
A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 2O-spiroxane steroidal compounds characterized by the presence of a 9alpha,11alpha-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HC1 (Benzenacetonitrile, (±) -alpha[3[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-alpha-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.
Owner:GD SEARLE & CO
Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of cardiovascular disorders
InactiveUS20030220312A1Reduce pathogenicityImprove the level ofOrganic active ingredientsCapsule deliveryAnginaCongestive heart failure chf
A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, angina and congestive heart failure. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9alpha,11alpha-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker amlodipine and the aldosterone receptor antagonist eplerenone.
Owner:GD SEARLE & CO
Eplerenone crystalline form exhibiting enhanced dissolution rate
A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
Owner:GD SEARLE & CO
Methods of treating ophthalmic disorders with epoxy-steroidal aldosterone receptor antagonists
Owner:PHARMACIA CORP
Eplerenone crystalline form
InactiveCN1433427AHigh chemical purityOrganic active ingredientsNervous disorderDiseaseIncreased aldosterone
Owner:PHARMACIA CORP
Novel aldosterone antagonists and uses thereof
InactiveUS20070066580A1Inhibiting aldosterone receptor activityOrganic active ingredientsLactone steroidsIncreased aldosteroneTreatment use
Owner:RECORDATIE IRELAND LTD
New method for preparing eplerenone
InactiveCN102617697ASources are cheap and readily availableControllableSteroidsMicrobial transformationDouble bond
The invention provides a method for preparing a novel steroid aldosterone acceptor antagonist eplerenone. The method comprises the following steps: producing 9alpha-hydroxyandrostenedione (9alpha-OH-AD) through carrying out microbial conversion on a raw material androstenedione (4-AD), carrying out 17-keto epoxidation, condensation and carboxyl removal, introducing double bonds to 9(11) and 6(7), and carrying out 6(7) furanization, oxidation and esterification, and carrying out 9, 11 double bond epoxidation to generate eplerenone. The method which utilizes the cheap and easily available raw material and adopts a semisynthetic technology of microbial fermentation has the advantages of environmental protection, easy control of the operation, high yield, and low cost, and is suitable for industrialized production.
Owner:SHANGHAI SCIENPHARM CO LTD
Epoxy-steroidal aldosterone antagonist and beta-adrenergic antagonist combination therapy for treatment of congestive heart failure
InactiveUS20050215537A1Reduce high blood pressureImprove heart functionBiocideSteroidsAldosteroneCombination therapy
A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a beta-adrenergic antagonist is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred beta-adrenergic antagonists are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9α,11α-substituted epoxy moiety. A preferred combination therapy includes the beta-adrenergic antagonist metoprolol ((±)1-(isopropylamino)-3-[p-(2-methoxyethyl)phenoxyl]-2-propanolol succinate) and the aldosterone receptor antagonist epoxymexrenone.
Owner:PHARMACIA CORP
Combination therapy of angiotensin converting enzyme inhibitor and eplerenone for treatment of cardiovascular disease
Combinations of an ACE inhibitor and an epoxy-steroidal aldosterone receptor antagonist are described for use in treatment of circulatory disorders. Of particular interest are therapies using epoxy-steroidal-type aldosterone receptor antagonist compounds, such as eplerenone, in combination with an angiotensin converting enzyme inhibitor. This co-therapy would be particularly useful to treat congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects such as hyperkalemia.
Owner:GD SEARLE & CO
Formulations comprising aldosterone receptor antagonists and treatments using same
ActiveUS20200171054A1Organic active ingredientsGranular deliveryAntagonistAldosterone Receptor Antagonist
Disclosed herein are oral dose formulations of aldosterone receptor antagonists, such as eplerenone and spironolactone, for the treatment of heart failure with preserved ejection fraction and uncontrolled hypertension.
Owner:SHAH SALIM
Eplerenone crystalline form exhibiting enhanced dissolution rate
InactiveCN1891209AHigh chemical purityOrganic active ingredientsNervous disorderEnhanced dissolutionSolvation
A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
Owner:PHARMACIA CORP
Medicine compounds used for cardiovascular disorders
ActiveCN101229156AGood effectEffective blood pressure reductionPill deliveryGranular deliveryTreatment effectTreatment hypertension
The invention relates to a drug composition for curing cardiovascular system diseases and the key point is that the invention which combines sartans, aldosterone receptor antagonist and isosorbide mononitrate according to certain proportions becomes a novel drug which cures the cardiovascular system diseases such as hypertension and heart failures and achieves ideal treatment effects comprehensively considered. The invention has the advantages that 1. The invention has a good effect in anti-myocardial fibrosis anti-ventricular hypertrophy as well as effective antihypertensive. 2. The invention is good in treating simple systolic hypertension of the elderly, exact in hypertensive effect, stable in operation and has no drug resistance. 3. The invention has active influences on the prognosis of patients of hypertension and the related complications, which is also the most meaningful clinical treatment problems which are solved by the invention.
Owner:LUNAN PHARMA GROUP CORPORATION
Use of an aldosterone receptor antagonist to improve cognitive function
InactiveUS20060058274A1Preventing and treating cognitive dysfunctionImprove cognitive functionOrganic active ingredientsNervous disorderIncreased aldosteronePsychiatry
Aldosterone receptor antagonists for the prevention and treatment of cognitive dysfunction are disclosed.
Owner:PHARMACIA CORP
Compound medicine containing antihypertensive peptide and aldosterone receptor antagonist for curing hypertension
ActiveCN101987200ASignificant blood pressure lowering effectThe incidence of adverse reactions is excellentDipeptide ingredientsTripeptide ingredientsAngiotensin-converting enzymeActive component
The invention provides a compound medicine containing antihypertensive peptide and aldosterone receptor antagonist for curing hypertension, which is composed of aldosterone receptor antagonist as an active component, peptide for reducing blood pressure and one or more pharmaceutic adjuvants, wherein the peptide for reducing blood pressure is peptide which has angiotensin converting enzyme inhibition.
Owner:TIANJIN JINYAO GRP
Formulations comprising aldosterone receptor antagonists and treatments using same
ActiveUS11007203B2Organic active ingredientsGranular deliveryAntagonistAldosterone Receptor Antagonist
Owner:SHAH SALIM
Combination of an aldosterone receptor antagonist and an HMG CoA reductase inhibitor
InactiveUS20060003975A1Reduce impactHigh levelAntibacterial agentsBiocideIncreased aldosteroneAldosterone
Novel methods and combinations for the treatment and / or prophylaxis of a pathologic condition in a subject, wherein the methods comprise the administration of one or more HMG Co-A reductase inhibitors and one or more aldosterone receptor antagonists, and the combinations comprise one or more HMG Co-A reductase inhibitors and one or more of said aldosterone receptor antagonists.
Owner:PHARMACIA CORP
Compound antihypertensive medicine composition
InactiveCN106267147AImprove the quality of lifeReduce mortalityOrganic active ingredientsDipeptide ingredientsAngiotensin-converting enzymeCombined use
The invention provides a compound antihypertensive medicine composition. Per unit preparation of the compound antihypertensive medicine composition contains perindopril tert-butylamine salt and eplerenone. Damage caused by aldosterone can still happen though ACEI and ARB treatment is fully conducted. Thus, it is necessary to adopt an aldosterone receptor antagonist to treat hypertension. Perindopril tert-butylamine salt and eplerenone are compounded according to the mechanism, animal test observation proves that combined use of the angiotensin converting enzyme inhibitor, namely perindopril tert-butylamine salt, and eplerenone influences nitric oxide bioavailability and spontaneous atherosclerosis of experimental rabbits; bioavailability of nitric oxide can be effectively improved. Perindopril tert-butylamine salt and eplerenone are used together so as to improve living quality and reduce the death rate of patients suffering from severe heart failures and myocardial infarction.
Owner:SHANGHAI PHARMA DONGYING JIANGSU PHARMA CO LTD
Eplerenone crystalline form exhibiting enhanced dissolution rate
InactiveCN1557833AHigh chemical purityOrganic active ingredientsNervous disorderPharmaceutical drugEnhanced dissolution
A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
Owner:PHARMACIA CORP
Combined combination drug for resisting heart failure and application of combined combination drug in preparation of drug for resisting heart failure
ActiveCN112089843AImprove the anti-heart failure effectImprove survival rateOrganic active ingredientsCardiovascular disorderAntioxidantNebivolol
The invention discloses a combined combination drug for resisting heart failure and application of a steroid aldosterone receptor antagonist and beta-cyclodextrin in preparation of a drug for resisting heart failure. The combined drug contains a diluent, an adhesive, a disintegrating agent, an antioxidant, an emulsifier, a solubilizer, the steroid aldosterone receptor antagonist and beta-cyclodextrin. According to the combined combination drug for resisting heart failure, compared with drugs such as spirolactone, beta-cyclodextrin, nebivolol and amlodipine which are independently used, the combined combination drug of the steroid aldosterone receptor antagonist and beta-cyclodextrin can significantly increase the cell survival rate, can reduce the ROS content in cells treated by adriamycin, can significantly improve the antioxidant ability of the cells, and can further greatly improve the anti-heart failure effect of the drug.
Owner:HEFEI UNIV OF TECH
Application of finerenone in preparation of drugs for treatment of senile calcific valvular heart diseases
InactiveCN110327334ALower the targetGood conditionDipeptide ingredientsHeterocyclic compound active ingredientsDegenerative changeLife quality
The present invention relates to a novel use of drugs and particularly discloses an application of finerenone in preparation of drugs for treatment of senile calcific valvular heart diseases. Studiesshow that finerenone is a third-generation aldosterone receptor antagonist with strong affinity for mineralocorticoids, antagonizes a series of pathological processes caused by excessive activation ofthe mineralocorticoids by aldosterone by competitively binding mineralocorticoid receptor (MR), thus regulates cell proliferation, differentiation and apoptosis, significantly improves degenerative changes of heart valve connective tissues, fibrosis, thickening and calcification, and protects cardiomyocytes. Compared with the prior art, the finerenone can reduce various indexes of senile patientswith the calcific valvular heart diseases, improves disease conditions, and improves life quality of the senile patients with the calcific valvular heart diseases.
Owner:HUISHENG MEDICAL TECH XUZHOU CO LTD
Mineralocorticoid receptor antagonists
The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
Owner:MERCK SHARP & DOHME LLC
Eplerenone drug substance having high phase purity
InactiveUS20050261261A1Improve physical stabilityUnique propertyOrganic active ingredientsSteroidsIncreased aldosteroneExcipient
A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
Owner:PHARMACIA CORP
Eplerenone crystalline form exhibiting enhanced dissolution rate
InactiveCN1152886CHigh chemical purityOrganic active ingredientsNervous disorderEnhanced dissolutionSolvation
A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having relatively hich physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
Owner:PHARMACIA CORP
Eplerenone crystalline form
InactiveCN101317848AHigh chemical purityOrganic active ingredientsSteroidsDiseaseIncreased aldosterone
A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively hich physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
Owner:PHARMACIA CORP
Compound medicine containing antihypertensive peptide and aldosterone receptor antagonist for curing hypertension
ActiveCN101987200BDipeptide ingredientsTripeptide ingredientsAngiotensin-converting enzymeActive component
The invention provides a compound medicine containing antihypertensive peptide and aldosterone receptor antagonist for curing hypertension, which is composed of aldosterone receptor antagonist as an active component, peptide for reducing blood pressure and one or more pharmaceutic adjuvants, wherein the peptide for reducing blood pressure is peptide which has angiotensin converting enzyme inhibition.
Owner:TIANJIN JINYAO GRP
Eplerenone Drug Substance Having High Phase Purity
InactiveUS20090149431A1Improve physical stabilityUnique propertyOrganic active ingredientsNervous disorderIncreased aldosteroneExcipient
A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
Owner:BARTON KATHLEEN P +14
Mineralocorticoid receptor antagonists
The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
Owner:MERCK SHARP & DOHME LLC
Medicine composition used for cardiovascular disorders
ActiveCN101229156BEffective blood pressure reductionDefinitely reduce blood pressurePill deliveryCapsule deliveryTherapeutic effectVentricular hypertrophy
Owner:LUNAN PHARMA GROUP CORPORATION
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