Abstract: Compositions and methods for providing hydrophobic active agents in a bioavailable form are disclosed and described. In one aspect of the invention, pharmaceutical composition containing a testosterone ester is provided. The composition includes a testosterone ester in both dissolved form and as undissolved particles and the dissolved form comprises at least 35 wt % of the testosterone ester present in the composition. The composition further includes a solubilizer and a stabilizer.

Abstract: A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.

Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: Described herein are bismethylene-17? carbolactone derivatives having progestational and/or antimineralocorticoid and/or aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.

Abstract: The invention concerns the use of ketoconazole and derivatives having a corresponding biological activity, and combinations thereof, in the treatment of abdominal obesity, hypertension, hyperinsulinemia, and elevated blood lipids.

Abstract: The present invention is directed to non-effervescent, orally disintegrating solid pharmaceutical dosage forms comprising progestin and methods of making and using the dosage forms to treat conditions in females in need thereof.

Abstract: The invention provides a method for providing emergency contraception in a female subject, comprising providing the subject with a therapeutically effective amount of ulipristal acetate in an oral dosage form before, during or after a meal. The invention further provides a kit comprising i) an oral dosage form comprising ulipristal acetate and ii) a printed matter stating that ulipristal acetate may be taken with or without food.

Abstract: Compositions particularly useful as coatings for solid dosage forms of therapeutic agents are provided, as are solid dosage forms comprising such coatings, processes for preparing such solid dosage forms, and the products of those processes. The coating compositions generally provide excellent strength and resistance to cracking, even when applied to flexible/swellable tablet cores such as hydrogel-type cores. The compositions also exhibit excellent odor-blocking characteristics.

Abstract: A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.

Abstract: Provided herein is a stable pharmaceutical product comprising a dry powder inhalation device, and a pharmaceutical composition that comprises R,R-Formoterol L-tartrate salt, in particular crystalline R,R-formoterol L-tartrate; and ciclesonide.

Abstract: To inhibit production of adipocytokines, in particular, adipocytokines that elicit insulin resistance and to prevent onset of pathosis caused by the insulin resistance, or improve the pathosis, the present invention provides an agent or a food or drink which contains a compound having a cyclolanostane skeleton, or an organic solvent extract, a hot water extract of a plant of the family Liliaceae or Gramineae, or a fraction thereof which contains the compound as an active ingredient.

Abstract: Compositions and methods for mucosal delivery of agents are provided. The compositions are intended for administration to mucosal surface, such as oral, gastrointestinal and nasal mucosa. The compositions provided contain one or more mucoadhesive proteins and an agent to be delivered. Methods for delivery of agents using the compositions provided herein are also provided.

Abstract: The present invention is related to a use of a steroid sulfatase inhibitor in the manufacture of a medicament for preventing or inhibiting premature uterine contractions. Specifically, the present invention is related to steroid sulfatase inhibitors useful for the preparation of a pharmaceutical formulation for the modulation, notably the inhibition of pre-term labor.

Abstract: The invention relates to pharmaceutical dosage units for oral, transmucosal or transdermal administration containing 15- or 16-substituted testosterone analogues, as well as to therapeutic methods that employ these testosterone analogues. More particularly, the invention is concerned with such pharmaceutical dosage units containing at least 10 ?g of an androgenic steroid selected from the group consisting of 15-hydroxytestosterones, 16-hydroxytestosterones, precursors thereof and mixtures of these hydroxytestosterones and/or their precursors; and a pharmaceutically acceptable excipient. The term “15-hydroxytestosterones” encompasses both 15?-hydroxytestosterone (15?, 17?-dihydroxy-4-androsten-3-one) and 15?-hydroxytestosterone (15?, 17?-dihydroxy-4-androsten-3-one). Similarly, the term “16-hydroxytestosterones” encompasses both 16?-hydroxytestosterone hydroxytestosterone (16?, 17?-dihydroxy-4-androsten-3-one) and 16?-hydroxytestosterone (16?, 17?-dihydroxy-4-androsten-3-one).

Abstract: The present invention relates to materials having therapeutic compositions releasably contained within the materials. The materials are configured to release therapeutic compositions at a desired rate. The present invention also relates to devices incorporating the materials.

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 provides compositions and methods for providing sustained release of an active agent through the skin of a subject, wherein a pharmaceutical percutaneous composition comprises at least one fatty acid ester and a therapeutically effective amount of active agent.

Abstract: The present invention cures hepatic cancer by MPA with the help of leptin. A therapeutic drug of MPA combined with leptin is applied to a liver cancer patient. Or, MPA can be directly applied to a patient having a high leptin expression. Or, if a patient has a low leptin expression, MPA is applied to the patient after leptin expression is increased. Hence, expression of leptin can be taken as a predictive factor and a prognostic factor of treatment effect on curing the patient with MPA.

Abstract: A method for the treatment and prophylaxis of conditions of aging due oxidative stress and as growth factors of stem cells. Such conditions due to oxidative stress are associated with a decreased presence of one or more cell-specific carbonic anhydrase enzymes in the tissue of a subject. Such conditions include but are not limited to alzheimer's disease, parkinson's disease, multiple sclerosis, autism, lou gehrig's disease, huntington's disease, diabetes mellitus, amyloid diseases, atherosclerosis, arthritis, osteoporosis, cystic fibrosis. The method comprises administering to the patient a pharmaceutically effective, non-toxic amount of one or more compounds that increases the presence of one or more Carbonic Anhydrase Isozymes whose levels have been reduced in the subject.

Abstract: An in-situ gel ophthalmic drug delivery system for estrogen containing an estrogen, a solubilizing and complexing agent, a humectant, a sorbic acid or sorbic acid based stabilizer, an optional chelating agent and gellan gum in the amount of about 0.1-0.5% w/v, optionally 0.1-0.3% w/v, of the composition.

Abstract: This invention relates to Huntington's disease and more specifically to methods for inhibiting the development of or treating Huntington's disease by administering estrogen, testosterone, precursors thereof or combinations thereof.

Abstract: This invention provides a system for compounding a pharmaceutical product for hormone replacement therapy. The system has a set of concentrated reagent compositions, each containing one or more steroid hormones dissolved in one or more solvents. The needs of each consumer are ascertained, and a pharmaceutical product is compounded for them using the concentrated reagent compositions. Each product has a custom tailored combination of steroid hormones at a concentration that is therapeutically effective for the consumer in accordance with their needs.

Abstract: The invention relates to a method of treating endometriosis using a combination of an aromatase inhibitor, a progestin and an oestrogen. The invention also relates to pharmaceutical formulations comprising said combination.

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: Certain diacylglycerol-polyethyleneglycol (DAG-PEG) lipids are especially useful for forming thermodynamically stable liposomes. Such liposomes are useful for a variety of purposes, including the delivery of therapeutic agents.

Abstract: Topical application of cholesterol has been found to be effective in preventing, treating or ameliorating the damage to the cornea caused by Streptococcus pneumoniae. Topical administration of cholesterol caused a significant decrease in the inflammation of the eye. In addition, cholesterol was surprisingly found to be a bactericide to Streptococcus pneumoniae outside the cornea. The effect of cholesterol can be enhanced by further administering a steroid or an antibiotic to the cornea.

Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.

Abstract: Compounds of formula (I): in which R1, R2, R3, R3?, R4, R5, R6, R6?, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, A, D, X, Y, and Z are defined in the specification. Also disclosed is a method of using one of the compounds to lower the blood cholesterol level and treat cancer, atherosclerosis, diabetes, Alzheimer's disease, and corneal arcus.

Abstract: A drug delivery system also intended as unit dosage form comprising a thin water-soluble film matrix, wherein said film matrix comprises a) a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer) as a water-soluble matrix polymer; an active ingredient being a steroid in which the positions 6 and 7 of the steroidal skeleton are both a —CH2— residue; and said film matrix has a thickness of less than 300 ?m.

Abstract: A topical formulation of an androstane steroid compound of improved solubility in combinations of the solvents propylene glycol and propylene carbonate.

Abstract: Intravaginal drug delivery devices, including intravaginal rings, are provided herein. The devices comprise a polyether urethane composition and a pharmaceutically effective amount of at least one vaginally administrable drug homogeneously distributed throughout the polyether urethane. The devices are capable of exhibiting a substantially zero order release profile of drug over extended periods of time. Also disclosed are methods for making the devices and methods of using the devices to prevent or treat a biological condition.

Abstract: The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.

Abstract: We describe lipid based pharmaceutical compositions adapted for oral delivery and optionally delivery in accordance with a circadian rhythm.

Abstract: Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed.

Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: The present invention relates to a method of treating asthma by raising the pH of the airways of an individual. The effect can be mediated directly by administering a pharmaceutically acceptable basic solution or alternatively, the effect can be mediated by enhancing the activity of glutaminase.

Abstract: Compositions which act synergistically to inhibit the growth of cancer cells and methods of use thereof are disclosed.

Abstract: The present invention relates to pharmaceutical compositions in the form of a gel for controlled- or sustained-release of a pharmaceutically active agent and to methods for treating or preventing a condition in an animal by administering to an animal in need thereof the pharmaceutical compositions. One particular type of condition for which the pharmaceutical compositions are useful is a microbial infection, e.g., of the skin, ear, or eye, especially for veterinary applications.

Abstract: A process for the syntheses of 17?-hydroxy-7?-methyl-19-nor-17?-pregn-5(10)-ene-20-yne-3-one (tibolone, 11) and intermediates useful for the synthesis thereof.

Abstract: The invention relates to a pharmaceutical composition in the form of a hydrogel that comprises a carboxylic acid diester, a C2-C4 alkyl alcohol, an active ingredient and a polymer matrix. The invention also relates to the use of a carboxylic acid diester as a transdermal permeation enhancer for an active ingredient in a pharmaceutical composition in the form of a hydrogel, whereby the composition comprises a polymer matrix and a C2-C4 alkyl alcohol. The invention also relates to a sweat-resistant composition in the form of a hydrogel, which comprises an acrylic polymer in combination with a cellulose derivative.

Abstract: Hormone compositions including bioidentical hormones dispersed in a lipid-based cream are provided in syringes for dispensation and self-administration by a user. The compositions, which are topically applied by the user, are percutaneously delivered to the vascular system of the user in accordance with a dosage protocol that causes a rhythmic and cyclic variation in the serum hormone levels that mimics the temporal variation in hormone levels present in the serum of a normal premenopausal woman.

Abstract: Disclosed are methods and materials for treating or preventing complications due to traumatic injuries using estrogen or derivatives thereof.

Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.

Abstract: The present invention is directed to a process for conferring cytoprotection on a population of cells which comprises administering to that population of cells a compound comprising a hydroxy-substituted aromatic ring structure and a non-fused polycyclic, hydrophobic substituent attached thereto. In particular, the present invention is directed to such a process wherein the administered compound is phenolic, such as a steriod (e.g., estrogen), and has a non-fused polycyclic, hydrophobic substituent attached to the hydroxy-substituted A-ring thereof.

Abstract: The present invention relates to a novel assay or screen for identifying compounds with potential therapeutic value for the treatment of protein trafficking diseases such as Cystic Fibrosis (CF) and nephrogenic diabetes insipidus (NDI). The usual approach involves expressing the mutant form of the gene in cells and assaying function in a multiwell format when cells are exposed to libraries of compounds. Although such functional assays are useful, they do not directly test the ability of a compound to correct defective trafficking of the protein. To address this a novel corrector screening assay for CF has been developed in which the appearance of the mutant protein at the cell surface is measured as the assay output. This assay was used to screen more than 3100 compounds. This novel screening approach to protein trafficking diseases is robust and general, and may enable the selection of molecules that can be translated rapidly to a clinical setting.

Abstract: This invention is directed to a novel method for the inhibition of ?-glucosidase enzyme and thus treating diabetes, viral infections, fungal infections, autoimmune function disorders and obesity using compounds derived as lichen metabolites; more specifically, this includes the therapeutic applications of methylorsellinate (2,4-dihydroxy-6-methylbenzoate, Compound I), methyl-?-orinolcarboxylate (2,4-dihydroxy-3,6-dimethylbenzoate, Compound II) and zeorin (6,22-hopanediol, Compound III).

Abstract: The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6 is H, ?CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1-3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being ? and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.

Abstract: The invention concerns a concentrated hormone pharmaceutical composition having from about 0.6 to about 80% of at least one hormone; from about 20 to about 90.4% of at least one solvent, and optionally a pharmaceutically acceptable carrier. The concentrated hormone pharmaceutical composition according to this invention provides a concentrated pharmaceutical composition that is easy to use and saves time and money to the pharmacies dealing with BHRT pharmaceutical products.

Abstract: The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, in the preparation of a medicament for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use a compound of formula (I) in an assay for detecting the phosphorylation state of cellular substrates. The present invention also relates to novel compounds of formula (I), and the chemical synthesis thereof.

Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.