Abstract: Onapristone extended-release formulations and methods of administering onapristone extended-release formulations are provided. Onapristone extended-release formulations provide sufficient therapeutic activity as compared to immediate-release formulations with reduced potential for adverse side effects.

Abstract: Methods and systems for making onapristone (ONA) using acidic hydrolysis and dehydration with sulfuric acid in an alcoholic solution are provided.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Provided are a novel internal standard useful in the measurement of androgens, a method capable of measuring the androgen in a highly selective and highly sensitive (accurate) manner using liquid chromatography mass spectrometry with simplified pretreatments, and a method for diagnosis of a disease using the androgen measurement method. The novel stable isotope-labeled compound is synthesized by performing reduction reaction in a specific solvent. An androgen is measured using this novel stable isotope-labeled compound as an IS.

Abstract: This invention provides new methods for a) identifying Cushing's Syndrome patients at high risk of developing hypokalemia during glucocorticoid receptor modulator (GRM) treatment, and b) for prophylactically treating such patients to prevent, or reduce the severity of, hypokalemia. Patients at such high risk may be identified prior to their developing hypokalemia. Such a patient may be an adult patient with endogenous Cushing's Syndrome having type 2 diabetes mellitus or glucose intolerance to control hyperglycemia secondary to hypercortisolism. Patients may be identified by an above-threshold level of ACTH or cortisol in a patient sample taken post-GRM administration or pre-GRM administration, respectively. Upon identifying such a patient prior to the development of low potassium, the present methods provide for prophylactically treating the patient by administration of one or more hypokalemia treatments concurrently with an increased dose of GRM or with an initial dose of GRM to prevent hypokalemia.

Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.

Abstract: This invention provides new methods for a) identifying Cushing's Syndrome patients at high risk of developing hypokalemia during glucocorticoid receptor modulator (GRM) treatment, and b) for prophylactically treating such patients to prevent, or reduce the severity of, hypokalemia. Patients at such high risk may be identified prior to their developing hypokalemia. Such a patient may be an adult patient with endogenous Cushing's Syndrome having type 2 diabetes mellitus or glucose intolerance to control hyperglycemia secondary to hypercortisolism. Patients may be identified by an above-threshold level of ACTH or cortisol in a patient sample taken post-GRM administration or pre-GRM administration, respectively. Upon identifying such a patient prior to the development of low potassium, the present methods provide for prophylactically treating the patient by administration of one or more hypokalemia treatments concurrently with an increased dose of GRM or with an initial dose of GRM to prevent hypokalemia.

Abstract: This invention provides new methods for a) identifying Cushing's Syndrome patients at high risk of developing hypokalemia during glucocorticoid receptor modulator (GRM) treatment, and b) for prophylactically treating such patients to prevent, or reduce the severity of, hypokalemia. Patients at such high risk may be identified prior to their developing hypokalemia. Such a patient may be an adult patient with endogenous Cushing's Syndrome having type 2 diabetes mellitus or glucose intolerance to control hyperglycemia secondary to hypercortisolism. Patients may be identified by an above-threshold level of ACTH or cortisol in a patient sample taken post-GRM administration or pre-GRM administration, respectively. Upon identifying such a patient prior to the development of low potassium, the present methods provide for prophylactically treating the patient by administration of one or more hypokalemia treatments concurrently with an increased dose of GRM or with an initial dose of GRM to prevent hypokalemia.

Abstract: The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.

Abstract: A method for treating diastolic heart failure is provided including identifying a subject having diastolic heart failure and administering a therapeutically effective amount of a galectin-3 inhibitor to the subject to at least partially alleviate a symptom of diastolic heart failure.

Abstract: The present invention relates to novel neurosteroid derivatives with anti-apoptotic, neuroprotective and neurogenic properties that act on the nervous system as well as methods for making the same and their applications in the treatment and/or prevention or amelioration of neurodegenerative diseases related to neuronal apoptosis or neuronal injury, or conditions related to or resulting from apoptosis, including but not limited to Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis and amyotrophic lateral sclerosis (ALS), retinal degeneration and detachment, peripheral neuropathy caused by genetic abnormalities, diabetes, polio, herpes, AIDS and chemotherapy, brain trauma, or ischemia and stroke. The active compounds are represented by Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, B, X, Y and Z are defined in the description of the invention. The present invention also includes compositions which comprise one or more of the compounds of Formula (I).

Abstract: Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof, and a steroidal anti-inflammatory agent. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.

Abstract: The present invention concerns palatable veterinary compositions made from one or more pharmaceutical active ingredients having a smell and/or a taste that is repulsive to animals, and a preparation method for preparing said oral veterinary compositions.

Abstract: The present invention relates to the fields of chemistry and pharmacy and, in particular, to the production of novel molecular entities: esterane derivatives fused with spirostanes rings, acting upon the Central Nervous Systems (CNS). From diosgenin, a naturally occurring sapogenin, with some subsequent transformations thereof, spirosteroid derivatives of the I-IV general formula can be obtained, with a cyclopentaneperhydrophenantrene nucleus fused to a 25R-spirostanes nucleus. Such molecular entities have an anti-inflammatory and anti-glutamatergic actions that can be used to treat inflammatory, cerebrovascular, neurodegenerative, neuropsychiatric, and neurologic diseases.

Abstract: The invention relates to 17-(1?-propenyl)-17-3?-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.

Abstract: Compositions, and methods of using such compositions, useful for placement, for example injection, into the interior of human or animal eyes are provided. Such compositions include a therapeutic component, such as one or more corticosteroids, a biocompatible polymeric component, and a solvent component. The composition is in a fluid form before placement in the interior of an eye, and becomes less fluid after the composition is placed in the eye to form an extended or delayed release drug delivery element or system. The drug delivery element is formed by the dissipation of the solvent from the composition when the composition is placed in the interior of an eye. One example of a composition includes triamcinolone acetonide as a therapeutic agent. A method of treating an ophthalmic condition, or otherwise improving or enhancing vision of a patient, comprises placing the fluid composition in the interior of the eye. The method may be practiced by injecting the fluid composition into the interior of the eye.

Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.

Abstract: The present invention describes intrauterine use of 18-methyl-15?,16?-methylene-19-nor-20-spirox-4-en-3-ones of the general formula (1) wherein R6 and R7 are hydrogen or a methylene group, in the treatment of menorrhagia, of uterine haemorrhages in general, and an intrauterine system for said use, comprising a compound of formula 1.

Abstract: The 15?,16?-methylene-17-hydroxy-19-nor-17-pregna-4-en-3-one-21-carboxylic acid ?-lactone derivatives of the present invention possess progestational efficacy. They have the general chemical formula I, in which Z is selected from the group comprising an oxygen atom, two hydrogen atoms, NOR and NNHSO2R, where R is hydrogen, C1-C10-alkyl, aryl or C7-C20-aralkyl, R4 is hydrogen or halogen, and moreover either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, C1-C10-alkyl, C2-C10-alkenyl or C2-C10-alkynyl, and R7 is selected from the group comprising hydrogen, C1-C10-alkyl, C3-C6-cycloalkyl, C2-C10-alkenyl or C2-C10-alkynyl, or: R6a is hydrogen and R6b and R7, together, denote a bond, an oxygen or form methylene, R18 represents hydrogen or C1-C3-alkyl and in addition include their solvates, hydrates, stereoisomers and salts.

Abstract: The present invention describes intrauterine use of 18-methyl-15?,16?-methylene-19-nor-20-spirox-4-en-3-ones of the general formula (1) in contraception and gynaecological treatment, and an intrauterine system comprising compounds of formula 1.

Abstract: Provided herein are timosaponin compounds of Formula I, II, III, I?, II? and III?, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.

Abstract: The invention relates to 17-hydroxy-19-nor-21-carboxylic acid-steroid ?-lactone derivatives with the chemical formula I, where R4, R6a, R6b, R7, R15, R16a, R16b, R18 and Z have the meanings stated in claim 1, and their solvates, hydrates, stereoisomers and salts. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.

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

Abstract: The present invention discloses the preparation method of drospirenone. 3?,5-dyhydroxy-6?,7?,15?, 16?-dimethylene- 5?-androstane-17,20-epoxy is taken as the raw material. It is subject to oxidization of the hydroxyl at the 3rd position, ketalization of 3-ketone group, condensation reaction and deesterification to obtain carboxylic acid lactone, sulfonation of the hydroxyl at the 5th position, and deketalization and desulphonation in the reaction system of glacial acetic acid and sodium acetate to produce the 3-keto-4-alkenyl compound, thus obtaining drospirenone. The preparation method of the invention has high intensification, reaction specificity, less by-products and high yield of products in each step, thus overcoming the disadvantages of low yield and unstable quality.

Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:

Abstract: The present invention relates to 18-methyl-6,7-methylene-17-pregn-4-ene-21,17?-carbolactones of general formula I wherein the 6,7-methylene group can be in ?- or ? position, pharmaceutical preparations containing at least one isomer of formula I and use thereof in the treatment of endometriosis.

Abstract: The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wherein the steps of oxidation and lactonization are performed with 1,3,5-trichloro1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (trichloroisocyanuric acid, TCCA) or 1,3-dichloro-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (dichloroisocyanuric acid, DCCA) or an alkaline metal salt thereof such as the sodium salt dihydrate (DCCA sodium salt) or 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX). New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too.

Abstract: The present relates to a method for detecting cardiac remodeling in a subject without clinical signs of heart failure comprising determining the level of the NGAL-MMP9 complex in a blood sample obtained from the patient.

Abstract: The present disclosure is generally directed to neuroactive 13,17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: Provided herein is technology relating to theranostic agents and particularly, but not exclusively, to compositions comprising cell-specific theranostic agents and associated methods and systems for using the cell-specific theranostic agents to treat subjects.

Abstract: The invention relates to compositions, methods, and kits for treating subjects infected by or at risk of infection with a DNA virus (e.g., a JC Virus or a BK virus). Aspects of the invention are useful to prevent or treat DNA virus associated conditions (e.g., PML) in subjects that are immunocompromised. Compositions are provided that inhibit intracellular replication of DNA viruses.

Abstract: Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the ?-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.

Abstract: The present invention is based in part on the discovery of a panel of miRs whose levels are increased or decreased in the circulation of chronic systolic HF patients. Accordingly, an extensive panel of miRs was screened in the sera of stable chronic systolic HF patients and the results were compared to an age, gender and ethnically matched control group.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.

Abstract: Improved medical devices and methods are provided comprising an anabolic agent for healing an injury. These improved medical devices and methods can enhance healing in injuries from traumatic soft tissue injury, surgical injuries, burn, traumatic brain injuries, musculotendinous injuries, musculoskeletal conditions, bone injury or other injuries or maladies, which can be chronic or non-chronic in origin. In some embodiments, the medical device comprises a drug depot that releases the anabolic agent over at least 2 days to enhance healing of an injury.

Abstract: The present invention relates to the use of spironolactone for the preparation of a pharmaceutical composition intended for preventing and/or treating multiple sclerosis. Alternatively, the invention relates to the use of spironolactone directly in T-lymphocytes or dendritic cells obtained from a blood sample taken from a patient and then injected back into the circulation. Therefore, the present invention relates to the use of a composition comprising spironolactone that can be used in the treatment of multiple sclerosis, which covers the administration of spironolactone directly or lymphocytes pre-treated with spironolactone, or dendritic cells to individuals requiring such treatment. Spironolactone is an orally administered drug that is less expensive than many of the treatments available for MS and, furthermore, has the advantage of being a known compound already used in humans for extended periods and therefore the adverse effects thereof have been described in clinical studies.

Abstract: The present application discloses 17? hydroxy steroid dehydrogenase (17? HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17? HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17? HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17? HSD1 and 17? HSD3 that have a spiro-morpholine substituent at C20.

Abstract: The present invention relates to steroid-derived cyclopamine analogs and methods for using the same for inhibiting sonic hedgehog signaling and preventing or treating cancer. A method for synthesizing the analogs of the present invention from a steroid is also provided.

Abstract: The present invention includes novel compounds based on the tomatidine skeleton as well as composition comprising these compounds alone and in combination with known compounds, which exhibit antimicrobial activity against extracellular or intracellular electron transport-deficient microbes and/or increase the antimicrobial activity of aminoglycoside antibiotics against their targets, and which are useful as antibacterial agents for treatment or prophylaxis of monomicrobiotic or polymicrobic bacterial infections or for the reduction of antibiotic resistance development in animals or in humans, or for use as antiseptics or agents for sterilization or disinfection.

Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient.

Abstract: Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof, and a steroidal anti-inflammatory agent. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.

Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.

Abstract: Disclosed are methods for the treatment of chronic heart failure, comprising administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said chronic heart failure. The chronic heart failure maybe non-ischaemic or ischaemic. Also disclosed is the use of perhexiline in the manufacture of a medicament to treat chronic heart failure, including chronic heart failure of a non-ischaemic origin and chronic heart failure of an ischaemic origin.

Abstract: The present invention provides methods of preventing or delaying the development of cancer (e.g., breast cancer) in BRCA1 mutation positive patients by beginning progesterone receptor antagonist treatment at an early age (e.g., by age 35, 30, or 25). In certain embodiment, such early treatment is long-term treatment, which may substitute or delay a preventative ovariectomy, single or double mastectomy (e.g., in patients wishing to delay or avoid a mastectomy, or patients that cannot afford a mastectomy).

Abstract: The present invention relates to a biomarker for characterizing prostate cancer and method of using the same. More particularly, the invention relates to method of using a membrane-associated C family G protein-coupled receptor GPRC6A as biomarker of characterizing prostate cancer progression. The present invention also provides a kit for detecting prostate cancer in a subject.

Abstract: A dermal, transdermal and/or mucosal formulation for topical application on skin, comprising an active pharmaceutical ingredient and a pharmaceutically acceptable solvent, and an anti-solvent; wherein the active pharmaceutical ingredient is soluble in the solvent in the absence of the anti-solvent, and wherein the active pharmaceutical ingredient is substantially in the solid state in the presence of the anti-solvent. A method for increasing the stability of an active pharmaceutical ingredient.