Abstract: 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.

Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

Abstract: Antimineralocorticoid compounds are disclosed for use in the prophylaxis and therapy of viral infections, especially the retroviral infection by HIV. These compounds can be administered alone or in combination with conventional anti-viral agents or anti-sense mineralocorticoid Steroid ReceptorNA or DNA mutants of heat shock proteins.

Abstract: An extract of the family Dioscoreaceae useful for preventing or treating the peripheral neuropathy; and a pharmaceutical composition or food composition comprising the extract are provided. In addition, a pharmaceutical composition or food composition useful for preventing or treating the peripheral neuropathy comprising a compound isolated from the extract of the family Dioscoreaceae is provided.

Abstract: This invention relates to certain sugar esters of phytosterols of formula (I).

Abstract: The invention relates to novel 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones of general formula (I), where Z=O, H2, ?NOR or ?NNHSO2R, where R=H, a straight- or branched-chain 1-4 or 3-4 C alkyl group, R4=H, halogen, methyl or trifluoromethyl, R6 and/or R7 can be ?- or ?-positioned and independently=branched- or straight-chain 1-4 or 3-4 alkyl, or R6=H and R7=a- or ?-positioned, straight- or branched-chain 1-4 or 3-4 C alkyl, or R6 and R7=H, or R6 and R7 together=a- or ?-positioned methylene or an additional bond. The novel compounds have gestagenic and antimineralocorticoid activity and are suitable for the production of pharmaceutical preparations, for example, for oral contraception and the treatment of pre-, peri- and post-menopausal pain.

Abstract: A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a ? receptor blocker; an imidazoline receptor antagonist; a centrally acting ? receptor antagonist; a peripherally acting ? receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

Abstract: The field of the invention is that of oral medicaments or pharmaceutical compositions, in particular of the type including one or more active principles. The aim of the invention is to provide an improved oral medicament to be administered in one or several daily doses and enabling the modified release of active principles (in particular of one active principle), whereby the prophylactic and therapeutic effectiveness of said medicament is improved. This aim is achieved by the oral multimicrocapsule galenic form according to the invention, in which the active principle release is controlled by a dual release trigger mechanism: “time-dependent trigger” and “pH-dependent trigger”.

Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

Abstract: The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.

Abstract: Provided are nanoparticles prepared by the aggregation of cucurbituril derivatives and having a particle size of 1 to 1,000 nm, a pharmaceutical composition in which a pharmaceutically active substance is loaded into the nanoparticles, and preparation methods thereof.

Abstract: Compounds and pharmaceutical compositions which include 2? oxo-voruscharin and derivatives are disclosed. The compounds and pharmaceutical compositions are useful in methods of treating cancer, particularly pancreatic cancer.

Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.

Abstract: A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action; comprising the oxidation of 17?-(3-hydroxypropyl)-6?,7?,15?,16?-dimethylene-5?-androstane-3?,5,17?-triol.

Abstract: A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the 10 method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a 13 receptor blocker; an imidazoline receptor antagonist; a centrally acting tx receptor antagonist; a peripherally acting ct receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduce SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

Abstract: This invention relates to a sealed container containing a powder formulation comprising a dehydroepiandrosterone, its analogue(s) or salt(s) by itself or with a pharmaceutically or veterinarily acceptable carrier or diluent, and having a particle size of about 0.1 ?m to about 100 ?m. The formulation can be used to treat or prevent asthma, chronic obstructive pulmonary disease, lung inflammation, and other respiratory diseases or conditions. The formulation may be prepared by jet milling, and may be delivered through the respiratory tract or other routes using a nebulizer. The sealed container is provided in a device and/or a therapeutic kit.

Abstract: The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which Z is an oxygen atom, two hydrogen atoms, a group ?NOR or ?NNHSO2R, where R is a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom or a trifluoromethyl group, and R6 and/or R7 may have a or a configuration, and R6 and R7 are independently of one another a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms or a straight- or branched-chain alkenyl group having 2 to 4 or 3 to 4 carbon atoms or a saturated cycloalkyl group having 3 to 5 carbon atoms or together are a methylene group or a double bond. The novel compounds have progestational and antimineralocorticoid activity.

Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.

Abstract: The present invention relates to platinum complexes containing bile acid derivatives having antitumor activity

Abstract: 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.

Abstract: A therapeutic method is described for treating cardiofibrosis or cardiac hypertrophy using a combination therapy comprising a therapeutically-effective amount of an angiotensin II receptor antagonist and a therapeutically-effective amount of expoxymexrenone.

Abstract: 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 9&agr;, 11&agr;-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.

Abstract: The present invention provides 5-androsten-3&bgr;-ol steroid intermediates and processes for their preparation.

Abstract: The invention relates to nanoparticles comprising spironolactone. The nanoparticles have a mean diameter, measured by photon corrrelation spectroscopy, in the range of from about 300 nm to about 900 nm.

Abstract: The invention discloses certain steroidal sapogenins and derivatives thereof, and their use in the treatment of cognitive dysfunction, non-cognitive neurodegeneration, non-cognitive neuromuscular degeneration, and receptor loss in the absence of cognitive, neural and neuromuscular impairment. Methods of synthesis, treatment and pharmaceutical compositions are also disclosed.

Abstract: The method of treating narcotic withdrawal symptoms in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound having anti-mineralocorticoid activity sufficient to treat narcotic withdrawal symptoms.

Abstract: The present invention involves a novel crystal form of 17&bgr;-hydroxy-7&agr;-(5′-methyl-2′-furyl)-pregna-4,9(11)-dien-3-one-21-carboxylic acid, &ggr;-lactone, having the formula 1

Abstract: Described herein are diuretic condensation aerosols and methods of making and using them. Kits for delivering a condensation aerosol are also described. The diuretic aerosols typically comprise diuretic condensation aerosol particles that comprise a diuretic compound. In some variations the diuretic compound is selected from the group consisting of bumetanide, ethacrynic acid, furosemide, muzolimine, spironolactone, torsemide, triamterene, tripamide, BG 9928, and BG 9719. Methods of treating edema using the described aerosols are also provided. In general, the methods typically comprise the step of administering a therapeutically effective amount of diuretic condensation aerosol to a person with edema. The diuretic condensation aerosol may be administered in a single inhalation, or may be administered in more than one inhalation. Methods of forming a diuretic condensation aerosol are also described.

Abstract: This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein R=NH2, NHR1, NHOR2, NHNHR2, NHCOR2, and R1=C(1-4)alkyl, C(3-6)cycloalkyl, Cn, where n=1-3, R2=methyl, ethyl, R3=alkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetreoaryl; wherein R4, R5=C(1-4)alkyl. Novel compounds according to Formula (III), wherein R6 and R7 are any of H, CH3CO, CH3CH2CO, CH3CH2CH2CO provided that R6 and R7 are not both H, or Formula (IV), wherein R8 and R9 are any of H, CH3CO, CH3CH2CO or CH3CH2CH2CO, having use in such methods, are also described.

Abstract: A combination therapy comprising a therapeutically-effective amount of an epoxy-free spirolactone-type aldosterone receptor antagonist and a therapeutically-effective amount of an angiotensin II receptor antagonist is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred angiotensin II receptor antagonists are those compounds having high potency and bioavailability and which are characterized in having an imidazole or triazole moiety attached to a biphenylmethyl or pyridinyl/phenylmethyl moiety. A preferred epoxy-free spirolactone-type aldosterone receptor antagonist is spironolactone. A preferred combination therapy includes the angiotensin II receptor antagonist 5-[2-[5-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-pyridinyl]phenyl-1H-tetrazole and the aldosterone receptor antagonist spironolactone.

Abstract: Use of low dosages of an aldosterone receptor antagonist, such as spironolactone, is described for use in treatment of circulatory disorders. This therapy would be particularly useful to treat congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.

Abstract: This invention relates to processes for the preparation of novel 7-carboxy substituted steroid compounds of Formula I, 1

Abstract: This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I, 1

Abstract: Combinations of aldosterone blockers and Cyclooxygenase-2 inhibitors useful in the treatment of inflammation are disclosed.

Abstract: The invention concerns a 3-methylene steroid derivative selected from the group consisting of (7&agr;,17&bgr;)-7-methyl-3-methyleneestr-5(10)-en-17-ol, (5&bgr;,7&agr;,17&agr;)-5,10-epoxy-7-methyl-3-methylene-19-norpregn-20-yn-17-ol, (5&bgr;,7&agr;,17&bgr;)-5,10-epoxy-7-methyl-3-methyleneestran-17-ol, (5&agr;,7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregn-20-en-17-ol, (5&agr;,7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregn-20-yn-17-ol, (5&bgr;,7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregnan-17-ol, (7&agr;)-7-methyl-3,17-dimethyleneestr-5(10)ene, (7&agr;,16&agr;,17&bgr;)-7,16-dimethyl-3-methylene-17-(1-propynyl)estr-5(10)-en-17-ol, (7&agr;,16&agr;,17&bgr;)-16-ethyl-7-methyl-3-methylene-17-(1-propynyl)estr-5(10)-en-17-ol, (7&agr;,17&bgr;)-7-methyl-3-methylene-17-(1 -propynyl)estr-5(10)-en-17-ol, (7&agr;,16&bgr;,17&bgr;)-16-ethyl-7-methyl-3-methylene-19-norpregn-5(10)-en-20-yn-17-ol, (7&agr;)-3-methylene-7-methylestr-5(10)-ene, (7&agr;)-3-methylene-7-methylestr-5(10)-en-17-one O-methyloxime and (7&agr;)-3-m

Abstract: 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 9&agr;,11&agr;-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker amlodipine and the aldosterone receptor antagonist eplerenone.

Abstract: 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 aldosterone receptor antagonists and one or more, bile acid sequestering agents and the combinations comprise one or more of said aldosterone receptor antagonists and one or more of said bile acid sequestering agents.

Abstract: 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 9&agr;,11&agr;-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HCl (Benzenacetonitrile, (±)-&agr;[3[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-&agr;-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.

Abstract: A combination comprising therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of an angiotensin II receptor antagonist is described for treatment of circulatory disorders.

Abstract: The present invention provides methods for the treatment or prophylaxis of one or more aldosterone-mediated pathogenic effects in a subject suffering from or susceptible to the pathogenic effect or effects wherein the subject has one or more conditions selected from the group consisting of a sub-normal endogenous aldosterone level, salt sensitivity and an elevated dietary sodium intake. The methods comprise administering to the subject a therapeutically-effective amount of one or more epoxy-steroidal compounds that are aldosterone antagonists.

Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

Abstract: Aldosterone blockers used for the treatment and prevention of inflammation are disclosed

Abstract: The invention discloses substituted sapogenins and their use in the treatment of cognitive disfunction and similar conditions.

Abstract: The invention concerns a compound of formula (I) wherein: n is equal to 0 or 1; R1, R2, R3, R4 represent a hydrogen or an alkyl group, or R1 and R3 together form a cycloalkyl group; R5 represents a hydrogen, an alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, hetereoalkylalkyl, hetereocycloalkyl, hetereocycloalkylalkyl group (all optionally substituted), or a —CO—R6 group; and R6 represents R7 or OR7 or NR7R8, with R7 representing an aryl, arylalkyl, heteroaryl or heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl group (all optionally substituted), and R8 representing an alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl (all optionally substituted); or R5 and R6 form with the nitrogen atom and the Z group bearing them a saturated monocyclic, bicyclic or tricyclic group, partially unsaturated or unsaturated, with 5 to 16 chain links containing 1 to 7 heteroatoms and optionally substituted; R10 represents a hydrogen atom or a hydroxy group, and in the latter case R1, R2, R

Abstract: 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.

Abstract: Combinations of an ACE inhibitor, an aldosterone receptor antagonist and a diuretic are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril or enalapril co-administered with a low-dose of spironolactone and furosemide. This co-therapy would be particularly useful to treat congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects such as hyperkalemia.

Abstract: The invention discloses the use of smilagenin and anzurogenin D in the treatment of cognitive dysfunction and similar conditions. Methods of treatment, and pharmaceutical compositions are also disclosed.

Abstract: Steroidal sapogenins and pharmaceutically acceptable salts thereof, useful in the prevention of coccidiosis in animals and methods of administering an effective amount of steroidal sapogenin or pharmaceutically acceptable salts thereof in the diet or drinking water of the animal.

Abstract: Use of low dosages of an aldosterone receptor antagonist, spironolactone, is described for treatment of circulatory disorders. This therapy would be particularly useful to treat or retard the development of congestive heart failure, while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.

Abstract: The invention relates to the use of compounds to treat a number of conditions, such as thrombocytopenia, neutropenia or the delayed effects of radiation therapy. Compounds that can be used in the invention include methyl-2,3,4-trihydroxy-1-O-(7,17-dioxoandrost-5-ene-3&bgr;-yl)-&bgr;-D-glucopyranosiduronate, 16&agr;,3&agr;-dihydroxy-5&agr;-androstan-17-one or 3,7,16,17-tetrahydroxyandrost-5-ene, 3,7,16,17-tetrahydroxyandrost-4-ene,3,7,16,17-tetrahydroxyandrost-1-ene or 3,7,16,17-tetrahydroxyandrostane that can be used in the treatment method.