32 results about "Aldosterone Receptor Antagonist" patented technology

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.

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.

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.

The present invention provides a novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone having relatively hich physical stability at normal temperatures of storage and use. The present invention provides Pharmaceutical compositionscomprising 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. The present invention a method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.

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.

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.

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.

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.

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.

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.

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.

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).

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 prognosisof patients of hypertension and the related complications, which is also the most meaningful clinical treatment problems which are solved by the invention.