32 results about "Aldosterone Receptor Antagonist" patented technology

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.

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.

A method for treating or preventing ophthalmic disorders comprising the administration of one or more aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone is disclosed. The method results in a reduction of intraocular pressure which treats or prevents the ophthalmic disorders. Among the disorders are intraocular hypertension, glaucoma, low tension glaucoma, age-related macular degeneration (AMD), macular edema, and diabetic retinopathy.

As glucocorticoids and mineralocorticoids also cause the retention of ions, such as sodium and potassium, where aldosterone receptors are located, aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone, also can be administered to modulate the intraocular concentration of ions. Thus, aldosterone receptor antagonists can be administered to maintain an intraocular ionic environment that is beneficial to intraocular cell survival.

The present invention relates to novel compounds that are aldosterone receptor antagonists, to pharmaceutical compositions containing the aldosterone receptor antagonists, and to methods of treatment using the same.

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.

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.

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.

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 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.

Aldosterone receptor antagonists for the prevention and treatment of cognitive dysfunction are disclosed.

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 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.

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.

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).

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.

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.

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.