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: A transdermal delivery system is provided for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric and/or adhesive coating that is applied to either the transdermal system's backing or release liner. The transdermal delivery device is manufactured to optimize drug loading while providing desirable adhesion to skin or mucosa as well as providing modulation of the drug delivery and profile.

Abstract: Fertility problems affect (1 in 10) couples in Western society, making it one of the most common serious health issues. Despite this, little is known about the causes of infertility, and thus patient counseling and treatment are suboptimal. With infertility being such a common problem, identification of any cause would impact on a large number of patients, allowing better counseling, clearer diagnoses and the possibility of making more informed choices (e.g. adoption vs. IVF treatment). The present invention provides methods to identify a cause of infertility in a subject based on the genotype of the subject, in particular, by evaluating the status of the gene encoding FK506 binding protein-like (FKBPL). In particular, the present invention relates to use of the status of the gene encoding FK506 binding protein-like for identification of a cause of an infertile phenotype in a subject.

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 present invention concerns aqueous-alcoholic, single-phase transcutaneous pharmaceutical compositions with an amount of alcohol of greater than 30% containing a steroid hormone combined with at least one penetrating agent selected from propylene glycol fatty acid esters, terpene derivatives, and mixtures thereof.

Abstract: A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.

Abstract: Treating and/or preventing prostate problems and/or metastases, by selectively occluding various groin vessels and tools for selective occluding of various groin veins, including, for example, the deferential vein. Optionally providing anti-androgen treatment after such occluding.

Abstract: Compositions and methods for treating hyperandrogenism and conditions associated therewith, including polycystic ovary syndrome are disclosed. The invention is directed to methods for treating hyperandrogenism and conditions associated therewith, in a subject comprising administering a fatty acid ester of an estrogen or an estrogen derivative. Furthermore the invention is directed to compositions for treating hyperandrogenism and conditions associated with hyperandrogenism, including polycystic ovary syndrome, comprising a fatty acid ester of an estrogen or an estrogen derivative.

Abstract: A transdermal delivery system comprising a composition comprising a pharmacological agent and a penetration enhancer wherein the penetration enhancer comprises polyethylene glycol (PEG) of average molecular weight no more than 300.

Abstract: Method of manufacture of compressed pharmaceutical formulation with the active substance tibolone by direct compression into tablets, whereas during the manufacturing process the formulation is subjected to the action of a protic solvent, either by addition of 0.1 to 3% by weight of said solvent in the liquid state and/or in the vapor form by ensuring the ambient atmosphere with the contents of solvent vapors above 50% relative.

Abstract: The present invention relates to novel uses of C-19 steroid compounds, in particular C-19 steroids having an androsten-17-(OR4)-3-one structure for cosmetic and further uses, wherein R4 is hydrogen or an unsubstituted or substituted alkyl, aryl, acyl or any group leading to hydroxyl upon biological metabolization or chemical deprotection. The present invention particularly relates to selected C-19 steroids displaying properties of high binding affinity to androgen receptor to block dihydrotestosterone from binding, while at the same time providing anabolic effects, which is useful for certain applications, particularly for influencing or controlling problems of the skin and its skin-associated body structures like cellulite, wrinkles, adipose fat tissues, hair follikles or hair growth; for influencing or controlling gland function and activity such as the sebaceous gland and other glands affecting the skin and/or perspiration.

Abstract: Effective treatments of pain and/or inflammation are provided. Through the administration of a biodegradable drug depot film, patch, strip or sponge being implantable at or near a cardiac tissue or within a nasal or sinus cavity, one can reduce, prevent or treat pain and/or inflammation.

Abstract: Compositions with synergistic anti-inflammatory effects in inflammatory diseases resulting from activation and consequent degranulation of mast cells and followed by secretion of inflammatory biomolecules from the activated mast cells, composed of a heavily sulfated, non-bovine proteoglycan such as shark cartilage chondroitin sulfate C, an unrefined olive kernel oil/extract that increases absorption of these compositions in various routes of administration, and one or more of a hexosamine sulfate such as D-glucosamine sulfate, a flavone such as quercetin, S-adenosylmethionine, a histamine-1 receptor antagonist, a histamine-3 receptor agonist, an antagonist of the actions of CRH, caffeine, and a polyamine.

Abstract: A pharmaceutical dosage unit for oral administration to a human female comprising a therapeutically effective amount of 17?-estradiol-3-lower alkanoate, most preferably 17?-estradiol-3-acetate, and a pharmaceutically acceptable carrier is disclosed. Also disclosed is a method for treating a human female in need of 17?-estradiol and a contraceptive method by oral administration of the pharmaceutical dosage unit and a method of preparing a pharmaceutical composition that may be used to form the pharmaceutical dosage unit of the invention.

Abstract: The present invention relates to novel oral suspension formulation comprising prednisolone acetate, a pharmaceutically acceptable vehicle and a thickening agent. The present invention further provides a method of treating patients in need of prednisolone with the novel formulation.

Abstract: The present invention provides a method of manufacturing tablets. An example of the method involves preparing a placebo blend containing only excipients. This placebo blend is compressed into tablets having concavities such as pinholes or indentations. Separately, a dispersion containing an active pharmaceutical ingredient, a drug, or a drug substance is prepared. A predetermined amount of this dispersion is placed into those concavities, and the tablets are dried. In this method, an active ingredient is handled in the form of a dispersion rather than as a solid. In addition, once the tablets are dried, the active ingredient is trapped inside the concavities and remains unexposed to external physical friction. As a result, human contact with powders or dust of active ingredient during the manufacturing and shipping processes may be minimized in a cost-effective manner. The present invention is also directed to the tablets prepared by this method.

Abstract: The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70.

Abstract: A respiratory dispersion is provided for the pulmonary delivery of at least two bioactive agents. The dispersion comprises a propellant suspension medium having dispersed therein a plurality of perforated microstructures, wherein the two bioactive agents are incorporated into individual perforated microstructures.

Abstract: The present invention relates to the modulation of glucocorticoid metabolism. In particular the invention relates to the modulation of the functional activity of the glucocorticoid receptor by 5? reduced metabolic breakdown products of glucocorticoids.

Abstract: Methods for forming porous stent coatings are disclosed.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: In accordance with certain embodiments of the present disclosure, A method for intracellular delivery of cytotoxin in combination with cyoablation is provided. The method includes encapsulation of one or more cytotoxins in a thermally responsive nanocapsule by decreasing the temperature of the nanocapsule to increase the permeability of the nanocapsule whereby the one or more cytotoxins are sucked into or diffuse into the nanocapsule. The temperature of the nanocapsule is increased and the nanocapsule is delivered into a cell. Cryoablation is performed in proximity to the cell resulting in the release of the one or more cytotoxins from the nanocapsule into the cell.

Abstract: A method of filling a drug capsule (2) for a dry powder inhaler comprising introducing a dose of powdered active substance (4) into the capsule and introducing a separate quantity of filler particles (6) into the capsule (2), said filler particles being of different composition and having a larger average particle size than the active substance.

Abstract: The subject of the present invention is the use, in particular the cosmetic and/or therapeutic use, of the apolipoprotein D, of polypeptides derived from this protein or of analogues thereof, of a nucleic sequence encoding such a polypeptide or of an agent modulating the activity or of the expression of such a polypeptide, in particular for stimulating terminal epithelial differentiation. The invention also relates to the use of the protein apolipoprotein D, of polypeptides derived from this protein or of analogues thereof, or of a nucleic sequence encoding such a polypeptide as a marker for evaluating the state of the epidermis.

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 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: Described herein are nitrated lipids and methods of making and using the nitrated lipids.

Abstract: Disclosed are methods and agents for detecting the presence or diagnosing the risk of ankylosing spondylitis (AS) in mammals. These methods are based on the detection of polymorphisms within any one or more of the ARTS-1 gene, the IL-23R gene, the TNFR1 gene locus, the TRADD gene locus and the chromosome loci 2P15 and 21Q22. The present invention also features methods for the treatment or prevention of AS based on the diagnosis.

Abstract: Novel etiology underlying certain types of seizures is presented, whereby changes in endocrine levels result in changes in osteoclast activity levels which in turn result in elevated extracellular Ca2+ levels which in turn result in systemic alterations in nerves, including increased membrane depolarization and enhanced neurotransmitter release, which in turn result in increased seizure risk in people with low seizure thresholds. Treatment methods are provided that modulate the bone microenvironment to provide an etiology based seizure treatment method based on the novel disclosures. The treatment methods include use of compounds such as calcitonin, SERMs such as raloxifene, testosterone, estrogen, calcimimetics such as cinacalcet, RANKL inhibitors such as denosumab, and bisphosphonates such as risedronate.

Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.

Abstract: The present invention provides extended cycle contraceptive regimens in which a female is administered a combined dosage form of estrogen and progestin. The disclosed extended cycle contraceptive regimens can be administered to a female as a method of providing non-contraceptive benefits.

Abstract: Syntheses of steroids such as 3-hydroxy-7?-methyl-21-[2?-methoxy-4?-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.

Abstract: This invention relates to devices, systems and methods for delivering preprogrammed quantities of an active ingredient to a biological system over time without the need for external power or electronics.

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 and determining whether the 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.

Abstract: Disclosed and claimed are compounds suitable for use as an inhibitor of oestrone sulphatase in a subject in need thereof, as well as compositions containing such compounds and methods for using such compounds.

Abstract: A process for preparing an emulsion or a dispersion comprising crystalline particles of at least one active principal that comprises contacting a solution of at least one solute in a solvent or mixture of solvents in a first flowing stream with a non-solvent in a second flowing stream wherein the non-solvent and solvent are not miscible with each other, so as to form an emulsion or a dispersion. Super saturation is brought about by suitable means, and the emulsion or dispersion is subjected to ultrasonic irradiation to mediate crystal nucleation.

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: One aspect of the present invention relates to the use of an estrogen in the treatment of Meconium Aspiration Syndrome (MAS) in a newborn infant, said treatment comprising administering an effective amount of estrogen to said newborn infant within 7 days after birth. The present treatment offers the advantage that estrogens can be administered using non-invasive modes of administration, e.g. oral or rectal administration. Other aspects of the present invention relate to a suppository for use in newborn infants comprising at least 1 ?g of estrogen and to an oral applicator comprising a container holding an aqueous liquid containing micronised estetrol and a metering dispenser for metering the liquid into the oral cavity of a newborn infant.

Abstract: Described herein are methods of treating a tumor by contacting the tumor with a therapeutic agent encapsulated in a first nanoemulsion and exposing the tumor to a first ultrasonic radiation of less than 300 kHz to the tumor. In some aspects, the tumor can be contacted with a second nanoemulsion. In some aspects, the second emulsion can be injected directly into the tumor via intratumoral injection before exposing the tumor to the first ultrasonic radiation. In some aspects, the tumor is exposed to a second ultrasonic radiation from about 1 to 5 MHz after the first ultrasonic radiation. The methods described herein can be used to treat numerous tumors including, but not limited to, multidrug resistant tumors and inoperable tumors. These tumors may include, but are not limited to, breast cancers, ovarian cancers, pancreatic cancers, or any combination thereof.

Abstract: The invention pertains to the discovery that type II glucocorticoid receptor antagonists can be used in methods for reversing or inhibiting the symptoms of depression in patients receiving interleukin-2 treatment.

Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.

Abstract: 3-Hydroxy-7?-hydroxy steroids and 3-oxo-7?-hydroxy steroids and pharmaceutically acceptable esters thereof are useful for protection against neuronal damage.

Abstract: The present invention discloses compositions having particles comprising, inorganic element; one or more active ingredient and optionally a release rate modulating agent, suitable for the delivery of active ingredients to human and animal tissues. The particles are nanoparticles or microparticles or mixtures thereof, made preferably by sol-gel method. The compositions are useful for application to the topical or mucosal surfaces preferably in the form of creams, gels, lotions, dry powders, spray, foam and other suitable forms.

Abstract: Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.

Abstract: A method of achieving contraception in a woman which comprises administering orally to said woman an estroprogestative composition comprising nomegestrol acetate and an estrogen is provided.

Abstract: Novel estrogenic compounds of Formula I are provided. wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an ? or a ? orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

Abstract: An anhydrous multiphase gel system consisting of an outer lipid matrix and an inner phase gelled by means of a polymer is described, which can be obtained by a) Melting the lipid phase with the formation of a liquid lipid phase, b) Mixing and homogenizing polymers or polymer blends capable of swelling with the formation of a polymer phase to be dispersed, c) Combining the polymer phase with the liquid lipid phase and homogenizing the phases, and d) Cold stirring the phase mixture until a solid gel-like mixed structure of the entire system is formed. The anhydrous multiphase gel system is particularly suitable for taking up difficultly soluble active substances in high concentration and for providing topical and transdermal applications. The described system is called an EDRS, “Entrapped Drug Reservoir System”.

Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

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 organised 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: The present invention relates to the use of 3-acetyl-7-oxo-dehydroepiandrosterone (7-keto DHEA) in the preparation of a medicament to treat or ameliorate psychiatric conditions. The present invention relates to methods of using compositions comprising 7-keto DHEA to treat or ameliorate psychiatric conditions. These methods include administering an effective amount of a composition comprising 7-keto DHEA in an acceptable carrier, alone or in combination with other psychiatric drugs to reduce or ameliorate symptoms of a psychiatric condition. This method may be used alone or as an adjunctive treatment for treating a wide variety of psychiatric conditions.