Abstract: The present invention relates to preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene (4) and 3-acetoxy2?-chloro-5-androsteno[17,16-b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole, a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC50 value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1 g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activity in vivo against indomethacin induced ulcer.

Abstract: Provided are methods for ameliorating a symptom of a neuropsychiatric disorder. Also provided are methods for ameliorating at least one symptom resulting from tobacco cessation; and for ameliorating a symptom of Alzheimer's disease or other cognitive disorder; of schizophrenia, schizoaffective disorder, or other psychotic disorder; of a depressive disorder; of bipolar disorder; of post-traumatic stress disorder or other anxiety disorder; of a pain disorder; or of traumatic brain injury. Also provided are methods for ameliorating a sleep disorder; for improving cognitive functioning; for predicting a predisposition to suicide, suicidal ideation, and/or suicidal behavior; and for ameliorating a neurodegenerative disorder. In some embodiments, the methods include administering to a subject in need thereof an effective amount of a neuroactive steroid composition, pharmaceutically acceptable salts thereof, derivatives thereof, or combinations thereof.

Abstract: A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): Also disclosed are methods, kits, combinations, and compositions for treating a disorder in a subject where an activator of liver X alpha is indicated, such as in, for example, treating a high cholesterol disease.

Abstract: The present invention relates to a method of reducing the incidence of nausea and vomiting associated with the administration of oral contraceptive formulation and a method of preparation of oral contraceptive formulation comprising progestin and/or estrogen and an antiemetic. The preferred oral contraceptive formulation comprises of levonorgestrel and an antiemetic.

Abstract: A transdermally absorbable preparation comprises a natural type sex hormone, a polyoxyethylene oleyl ether having a molar number of ethylene oxide units added of 20, at least two kinds of oily ingredients selected from the group consisting of diisopropyl adipate, cetyl alcohol, benzyl alcohol, and propylene glycol dicaprate, a polyhydric alcohol, and ethanol.

Abstract: The present invention relates to a compound of formula (I): for its use as progesterone receptor antagonist, in particular for its use for the prevention and/or the treatment of cancer or uterine pathologies.

Abstract: The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, including post-partum auto immune diseases) and more particularly. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of these Th1-mediated (cell-mediated) autoimmune diseases known to either have an initial onset following the birth of a child or which are exacerbated in patients in the post-partum period.

Abstract: The present invention generally relates to foams and, in particular, to foams for applications such as drug delivery, and particles that are made from such foams. One aspect relates to foams or particles containing pharmaceutically active agents. The foam may comprise a pharmaceutically acceptable polymeric carrier. In some cases, the foam or particle has an unexpectedly high specific surface area. A high specific surface area may, in some cases, facilitate delivery or release of the pharmaceutically active agent when the foam or particles made from the foam (e.g., by milling) are administered to a subject. The foam may also exhibit a relatively high loading of the pharmaceutically active agent. In some cases, the foam may be a microcellular foam. In one set of embodiments, the foam is created using a supercritical fluid, such as supercritical C02.

Abstract: The present invention relates to solubility improving preparation for enhancing the oral absorption of a poorly soluble drug, which is comprising (A) and (B); (A) a granulated substance which comprises (i) a poorly soluble drug having an acidic group in the molecule, (ii) an alkaline agent, (iii) a surfactant, and this granulated substance dose not substantially contain a disintegrator, (B) a disintegrator existing only in the external of the granulated substance.

Abstract: A postprandial hyperglycemia-improving agent, the agent is highly safe and exhibits excellent effects of inhibiting the postprandial increase of blood glucose. The postprandial hyperglycemia-improving agent comprises a cycloartenol or a derivative thereof as an active ingredient.

Abstract: Compositions and devices for transdermal hormone delivery are disclosed. The compositions and devices include desogestrel and enable delivery of effective amounts of progestin without the use of skin permeation enhancers.

Abstract: The present invention relates to a method for reducing cholesterol absorption and the occurrence of atherosclerotic lesions in an animal comprising administering to the animal a composition comprising an effective amount of at least one cholesterol ester.

Abstract: Provided herein are methods for preventing or alleviating the symptoms of and inflammation associated with inflammatory diseases and conditions of the gastrointestinal tract, for example, those involving the esophagus. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.

Abstract: The preset invention relates to a new oral anti-diabetic compound prepared by synthesizing a steroid and a guanide or biguanide, which is eliminated via the hepatic route, instead of the renal route, to avoid adverse effects of Metformin, such as renal dysfunction. A pharmaceutical composition comprising the compound of the invention and the method for treating diabetes using the compound are also provided.

Abstract: The present application is directed to an aqueous pharmaceutical formulation comprising less than about 5% w/v sodium deoxycholate maintained at a pH sufficient to substantially inhibit precipitation of the sodium deoxycholate. Also disclosed herein, are methods for inhibiting precipitation of sodium deoxycholate in an aqueous solution comprising less than about 5% w/v of sodium deoxycholate, said method comprising maintaining pH of the solution of from at least about 8.0 to about 8.5.

Abstract: Provided herein are methods and compositions for treating metabolic diseases and conditions associated with metabolic diseases.

Abstract: An oral product includes a body that is wholly receivable in an oral cavity. The body includes a mouth-stable polymer matrix, cellulosic fibers embedded in the mouth-stable polymer matrix, and an additive dispersed in the mouth-stable polymer matrix. The oral product is adapted to release the additive from the body when the body is received within the oral cavity and exposed to saliva.

Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

Abstract: The present invention relates to a process for the preparation of branched biodegradable polymers comprising of the steps of: (a) preparing a macromonomer by ring-opening polymerization of at least one cyclic ester, cyclic carbonate, and/or cyclic carboxyanhydride in the presence of a branching agent and optionally a catalyst; and (b) subsequent polycondensation of the macromonomer, to a process for the preparation of a macromonomer by ring-opening polymerization of at least one cyclic ester, carbonate and/or N-carboxyanhydride in the presence of a defined branching agent and optionally a catalyst, according to step (a), and to the prepared macromonomer and branched biodegradable polymer and their uses.

Abstract: The invention is in the field of medical treatments of liver disease, in particular, non-alcoholic fatty liver diseases, such as non-alcoholic steatohepatitis. The invention provides a composition comprising an effective amount of a compound capable of increasing the intracellular level of 27-hydroxycholesterol for the treatment of liver inflammation in fatty liver disease. It also provides a method of reducing liver inflammation in a patient with non-alcoholic fatty liver disease by administering an effective amount of 27-hydroxycholesterol.

Abstract: Processes for preparing lanostane triterpenes from the medicinal mushroom Ganoderma lucidum, and related compounds are described. Compounds, compositions, and methods for treating cancer are also described.

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: The method of treating diabetes-related impaired wound healing includes the step of administering an effective amount of estrogen replacement therapy to a patient in need thereof to promote wound healing. Alternatively, the method of treating diabetes-related impaired wound healing includes the step of administering an effective amount of a TNF-? inhibitor to a patient in need thereof to promote wound healing. The method of treating diabetes-related impaired wound healing may also include both the step of administering an effective amount of estrogen replacement therapy and administering an effective amount of a TNF-? inhibitor to a patient in need thereof to promote wound healing.

Abstract: A 5?-androstane-3?,5,6?-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-?-cyclodextrin as a solubilizing agent and the active ingredient is present at a weight ratio of 1-20:40-500 to the hydroxypropyl-?-cyclodextrin. The injection may also comprise, by weight, 1-100 parts of at least one isotonic adjusting agent, 0-200 parts of at least one freeze drying filler, and 0-2000 parts of at least one solvent. The preparation method comprises dissolving hydroxypropyl-?-cyclodextrin solution, 5?-androstane-3?,5,6?-triol and at least one additional soluble excipient in water for injection in sequence to obtain a raw injection solution, and subjecting the raw injection solution to decolorization, depyrogenation, filtration and sterilization to obtain the injection, Drying the filtrate yields a solid for injection.

Abstract: The object of the invention is the use of 17-alpha-estradiol of formula (I) and its derivatives for the treatment and/or prevention of psychiatric clinical pictures. According to the invention, 17-alpha-estradiol and its derivatives can be used preferably as antidepressant drugs, especially preferably as quick-acting antidepressant drugs. According to the invention, 17-alpha-estradiol of formula (I) and its derivatives can also be used for the treatment and/or prevention of postpartum depression, post-menopausal depression, anxiety, schizophrenia, memory disturbance associated with depression or bipolar depression.

Abstract: Methods and compositions for the treatment of social phobia are provided, including administering a therapeutically effective amount of an androsta-4,16-dien-3-ol steroid to an individual in need of treatment and a pharmaceutical composition for the treatment of social phobia having a therapeutically effective amount of an androsta-4,16-dien-3-ol steroid. Therapeutically effective amounts may be, for example, between about 100 picograms and about 100 micrograms, or between about 1 nanogram and about 10 microgram, or between about 10 nanograms and about 1 microgram of an androsta-4,16-dien-3-ol steroid. Administration of the androsta-4,16-dien-3-ol compound is preferably intranasal administration to the nasal passages and the vomeronasal organ of the individual. A preferred androsta-4,16-dien-3-ol steroid is [3?]-androsta-4,16-dien-3-ol.

Abstract: Methods for the treatment of bacterial infections in the respiratory system of a subject, such as the lungs of a subject, using fusidic acid alone or in combination with a second bacterial agent such as tobramycin, amikacin, fosfomycin or levofloxacin are described.

Abstract: Polymeric micellar clusters formed from amphiphilic carbohydrate polymers and their uses in formulating drugs is disclosed, and in particular the finding that amphiphilic carbohydrate polymers are capable of self assembling to form micellar clusters in which the carbohydrate amphiphiles aggregate into hierarchically organized micellar clusters of individual aggregates. The micellar clusters may be transformed into stable nanoparticles with drugs, especially hydrophobic drugs that have poor aqueous solubility, and may improve the transfer of hydrophobic drugs across biological barriers.

Abstract: Provided is an antioxidant which is highly safe, inhibits oxidation of a biological component, in particular, a lipid, and may be used as a drug, food or drink, a food additive, an external preparation for skin, or the like. The antioxidant contains a compound selected from a cyclolanostane compound and a lophenol compound as an active ingredient.

Abstract: Described are transdermal drug delivery systems for the transdermal administration of estrogen, comprising a polymer matrix and estrogen. Methods of making and using such systems also are described.

Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

Abstract: Disclosed is the use of 5?-androstane(alkyl)-3?,5,6?-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord isehemia or hypoxia and has no obvious toxic reaction within effective dose thereof.

Abstract: A method is provided for early treatment of steatosis, which method is based on early detection of steatosis based on the detection of CD36. CD36 is determined in a body fluid, and CD36 levels above a predetermined value is indicative of steatosis.

Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).

Abstract: The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.

Abstract: Provided are methods and compositions for reducing superoxide anions such that a prophylactic or therapeutic effect against conditions associated with excess oxidative stress achieved. The compositions and methods provide for reducing inflammation and for enhancing lifespan of eukaryotic organisms. A screen for identifying compounds that can be used in these methods is also provided.

Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

Abstract: The present disclosure relates generally to methods and compositions for treating symptoms of Parkinson's disease and/or other movement disorders. More particularly, the present disclosure describes a method for treating symptoms of Parkinson's disease and related disorders by administering a composition comprising one or more of the following active agents; estradiol, estriol, testosterone, and 19-nortestosterone. In addition, the compositions of the present invention can be used for enhancing or optimizing the effectiveness of neural stimulation in treating the symptoms of movement disorders such as Parkinson's disease.

Abstract: The sulfated oxysterol 5-cholesten-3?, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.

Abstract: Methods of treating a subject with a traumatic central nervous system injury, more particularly, a traumatic brain injury, are provided. The methods comprise a therapy comprising a constant or a two-level dosing regime of progesterone. In one method, a subject in need thereof is administered at least one cycle of therapy, wherein the cycle of therapy comprises administering a therapeutically effective two-level intravenous dosing regime of progesterone. The two-level dosing regime comprises a first time period, wherein a higher hourly dose of progesterone is administered to the subject, followed by a second time period, wherein a lower hourly dose of progesterone is administered to the subject.

Abstract: TRPC ion channels are non-selective channels widely expressed in human tissues. These channels are involved in numerous physiological functions and are putative targets for the development of novel medicines. There is a need to gain a better understanding of TRPC ion channels in cells and beyond. The present invention provides a pharmacological tool compound that allows to study TRPC ion channels due to its discriminating inhibition of TRPC subfamilies. In the present invention, norgestimate is shown to selectively inhibit TRPC3, TRPC6 and TRPC7.

Abstract: The present invention provides ascending-dose extended cycle regimens in which a female is administered an estrogen and a progestin for a period of greater than 30 or 31 consecutive days, optionally followed by a hormone-free period or by a period of administration of estrogen. The disclosed regimens can be administered to a female to provide contraceptive and non-contraceptive benefits.

Abstract: Novel dosing regimens for the treatment and prevention of bacterial infections using fusidic acid are described. The use of a high loading dose of fusidic acid, followed by moderate maintenance doses of the drug, have been found to prevent development of drug-resistant strains of bacteria, to increase the effective spectrum of the drug, and to avoid nausea and vomiting associated with a prolonged course of therapy of high amounts of the drug.

Abstract: A neutral-fat-level-regulating agent, a cholesterol-level-regulating agent, a free-fatty-acid-level-regulating agent or an anti-obesity agent, including: at least one of protopanaxatriol, panaxatriol, protopanaxadiol and panaxadiol which are aglycons of dammarane-type saponins and a hyperlipemia-ameliorating agent including: at least one of the neutral-fat-level-regulating agent, the cholesterol-level-regulating agent, the free-fatty-acid-level-regulating agent and the anti-obesity agent.

Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

Abstract: Methods for treating neurodegeneration and/or myelination in patients are disclosed comprising treating the patient with a progestin compound which exerts binding to progesterone receptors and elicits progesterone-receptor-induced biological responses without interacting with the androgen receptor and without inducing androgen or glucocorticoid biological responses at a dosage sufficient to prevent or reduce neurodegeneration. The progestin compound preferably comprises 16-methylene-17?-acetoxy-19-norpregn-4-ene-3,20-dione, and the methods include combining the progestin compound with an estrogen compound to provide both contraception and treatment for myelin repair and neurodegeneration, and include effects on stroke and TBI.

Abstract: The subject invention provides a drug delivery system comprising at least one compartment consisting of (i) a drug-loaded thermoplastic polymer core, (ii) a drug-loaded thermoplastic polymer intermediate layer and (iii) a non-medicated thermoplastic polymer skin covering the intermediate layer, wherein said intermediate layer is loaded with (a) crystals of a first pharmaceutically active compound and with (b) a second pharmaceutically active compound in dissolved form and wherein said core is loaded with said second compound in dissolved form.

Abstract: Methods and compositions are provided for treating metabolic disorders by modulating bile acid levels. Generally, the methods and compositions can modulate bile acid levels, such as serum bile acid levels, to treat a metabolic disorder. In one embodiment, a method of modulating a bile acid level includes measuring a bile acid level and delivering a composition effective to modulate the bile acid level. A method for modulating a bile acid profile includes comparing a bile acid profile to a target profile and delivering a bile acid cocktail to increase bile acid levels. In another embodiment, a pharmaceutical composition for increasing bile acid levels includes a bile acid cocktail effective to increase bile acid levels. The composition is further useful as part of an implantable system.

Abstract: The present invention relates to steroidal esters of 17-oximino-5-androsten-3-ol, of compound of general formula (A) wherein R is selected from a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from Dehydroandrosterone acetate. The compounds were tested for their antiproliferative activity and 5?-reductase inhibitory activity in comparison to Finasteride. Decreased androgen level have been found in serum of animal treated with newly synthesized compounds. These compounds have also shown better cytotoxicity in comparison to reference drug Finasteride. Thus such compounds can be useful in treatment of androgen dependent disorder of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferative activity.

Abstract: Described are estradiol-containing pharmaceutical compositions and, and methods using the same to alleviate menopause-related symptoms, such as hot flushes, by topically administering estradiol at low effective doses.