Abstract: Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.

Abstract: Disclosed are compounds such as 5?-androstane-3,6,17-trione, formulations comprising said compounds, and methods of use thereof to stimulate endogenous testosterone production and improve athletic performance and libido.

Abstract: Stabilized dispersions are provided for the delivery of a bioactive agent to the respiratory tract of a patient. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a hydrofluoroalkane propellant. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as, by settling or flocculation. In particularly preferred embodiments, the stabilized dispersions may be administered to the lung of a patient using a metered dose inhaler.

Abstract: Anti-chemokine monoclonal antibody therapy is provided for the prevention, control or reversal of chronic rejection mediated vascular remodeling, including, e.g., but not limited to MCP-1/CCR2 antagonist antibody therapy for the modulation of cardiovascular pathologies associated with cardiac graft rejection including intimal thickening, arteritis, fibrosis, and necrosis.

Abstract: A method of improving cumulative embryo score may comprise administering an androgen to a human female, for example, DHEA, for at least about four consecutive months followed by harvesting and fertilizing oocytes and forming embryos. Between about 50 mg and about 100 mg of DHEA may be administered to a human female per day. Moreover, a method of increasing the quantity of fertilized oocytes in one cycle of in vitro fertilization may comprise administering an androgen to a human female for at least about four consecutive months, harvesting and fertilizing the oocytes. Furthermore, a method of increasing the quantity of day 3 embryos from one cycle of in vitro fertilization may comprise administering an androgen for at least about four consecutive months, harvesting and fertilizing the oocytes and forming day 3 embryos. A method of normalizing ovarian DHEA also may include administering an androgen for at least about four consecutive months.

Abstract: This invention provides a composition comprising a depolymerized glycosaminoglycan or derivative thereof covalently linked to a bile acid. This invention also provides a pharmaceutical composition comprising a depolymerized glycosaminoglycan or derivative thereof covalently linked to a bile acid and a pharmaceutically acceptable carrier. Finally, this invention provides a method for orally delivering heparin to a subject comprising administering to the subject a pharmaceutically effective amount of a pharmaceutical composition comprising a glycosaminoglycan or derivative thereof covalently linked to a bile acid and (b) a pharmaceutically acceptable carrier.

Abstract: A method for treating or preventing spontaneous preterm birth in pregnant women and improving neonatal morbidity and mortality. The method includes administering to a pregnant woman in need thereof an effective amount of progesterone sufficient to prolong gestation by minimizing the shortening or effacing of her cervix. Treatment and prophylaxis with progesterone in pregnant women having symptoms of short cervix has been clinically shown to increase neonatal health.

Abstract: The present invention relates to methods of determining inflammatory bowel disease status in a subject. The invention further relates to kits for determining inflammatory bowel disease status in a subject. The invention further related to methods of identifying biomarker for determining inflammatory bowel disease status in a subject.

Abstract: A medicament and a method of producing a medicament are disclosed. The medicament contains a soft steroid and is suitable for administration via a dry powder inhaler.

Abstract: The present invention provides methods for the treatment or the prevention of neuronal damage in the CNS. Specifically, the methods of the invention provide for the administration of a therapeutically effective amount of a progestin or progestin metabolite following a traumatic or ischemic injury to the CNS such that, prior to termination of administration of the progestin or progestin metabolite the administration is tapered to avoid withdrawal. The drug taper employed can involve a linear taper, an exponential taper, progressively dividing administered doses by 50%, or can be determined based on the treating physician's assessment of the patient's response to therapy. The tapered administration methods of the present invention may be used in combination with any therapeutic protocol or regimen for the administration of a therapeutically effective amount of a progestin or progestin metabolite to treat a traumatic or ischemic CNS injury.

Abstract: Disclosed is a is a treatment for the adverse psychological effects (including depression, low self esteem, guilt, increased stress, anhedonia, decreased cognition, sleep disturbances, general fatigue, agitation/motor dyskinesia and decreased appetite) resulting from androgens or GnRH analogue intake, by administering a compound which antagonizes estradiol or its receptors, or blocks and prevents estradiol binding to the estradiol receptors (including antiestrogens) and/or a compound which inhibits endogenous production of estradiol, including aromatase inhibitors. Suitable antiestrogens include clomiphene and its isomer enclomiphene, tamoxifen, 4-hydroxytamoxifen, and toremifene. Suitable cytochrome P450 (P450arom) aromatase inhibitors include formestane, exemestane, anastrozole, and letrozole.

Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.

Abstract: The present invention relates to monolithic intravaginal rings comprising progesterone, methods of making, and uses thereof. The intravaginal rings comprise progesterone, a polysiloxane elastomer, and a pharmaceutically acceptable hydrocarbon or glycerol esters of a fatty acid.

Abstract: The object of the invention is the use as a drug of a compound fitting formula I wherein X represents an oxygen atom or a ?N—OH group and R represents a group selected from or one of its esters and/or of its addition salts with pharmaceutically acceptable acids, particularly as a cytoprotective drug, preferentially a cardioprotective and/or neuroprotective drug, the compounds of formula I wherein R is R2, R3, R4, R5 or R6 as novel compounds as well as their preparation method and use.

Abstract: Provided herein provided herein are novel analogs and derivatives of betulinic acid. Also provided is a method for inhibiting an activity of one or more specificity protein (Sp) transcription factors cells associated with a neoplastic disease using betulinic acid, betulinic acid analog(s) and/or derivative(s) effective to decrease expression of a microRNA with concomitant increase in Sp suppressor gene expression. The betulinic acid analogs and derivatives also are effective in methods provided herein for inhibiting proliferation of cells associated with a neoplastic disease for treating a cancer or for reducing toxicity of a cancer therapy in a subject via administration of an analog or derivative of betulinic acid and, optionally, another anticancer drug.

Abstract: A method for reducing the symptoms of peripheral vascular disease wherein a chemical agent that reduces peripheral vascular hyperreactivity in response to a stimulus for contraction of peripheral vascular musculature is administered to a subject in need thereof. Kits for administering the chemical agent to reduce the symptoms of peripheral vascular disease.

Abstract: The present invention relates to new synthetic receptors. More particularly, the present invention relates to the use of the synthetic receptors for delivering a protein, peptide, drug, prodrug, lipid, nucleic acid, carbohydrate or small molecule into a target cell via receptor-mediated endocytosis. According to the invention, novel synthetic mimics of cell surface receptors have been designed and methods for use of the same are disclosed.

Abstract: The present invention relates to the use of cholest-4-en-3-one derivatives for obtaining a cytoprotective drug, with the exception of a neuroprotective drug.

Abstract: The present invention relates to methods of gene expression profiling for inflammatory bowel disease pathogenesis, in which the differential expression in a test sample from a mammalian subject of one or more IBD markers relative to a control is determined, wherein the differential expression in the test sample is indicative of an IBD in the mammalian subject from which the test sample was obtained.

Abstract: The present invention relates to a method of treating cancer selected from the group of cancers consisting of prostate cancer, renal cancer, breast cancer, ovarian cancer, CNS cancer, melanoma, lung cancer, and bladder cancer. This method involves administering to a patient in need of such treatment a therapeutically effective amount of a betulinol derivative compound of Formula (I). Also disclosed are conjugated and immunoconjugated derivatives of the compound of Formula (I) as well as methods of making and using them.

Abstract: A chronotherapeutic pharmaceutical formulation comprising a core containing an active agent (e.g., a drug) and a surfactant and a delayed release compression coating comprising a natural or synthetic gum applied onto the surface of the core.

Abstract: This invention relates to a method and pharmaceutical composition useful in treating a condition responsive to hormone replacement therapy. Specifically, the invention is related to the long term treatment of symptoms associated with atrophic vaginitis. The composition contains effective amounts of an estrogen, a progesterone compound and a pharmaceutically accepted vehicle, carrier and/or diluent.

Abstract: The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, neurodegenerative diseases or disorders, such as Alzheimer's disease, Parkinson's Disease, multiple sclerosis, stroke, ALS Pick's disease, prion disease and Huntington's disease. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of the diseases and disorders.

Abstract: The present invention relates to a pharmaceutical composition comprising micronized progesterone, soya bean lecithin, and at least one oil selected from the group consisting of sunflower oil, olive oil, sesame seed oil, colza oil, almond oil, to the method for the preparation thereof and to the uses thereof for treating a physiological condition linked to insufficiency of progesterone secretion.

Abstract: A medicament delivery device and method of delivering a medicament is provided wherein the device is insertable into the uterine myometrium for the delivery of medicaments to the pelvic area and organs thereof, for example, the bladder, peritoneum, the vulva, vagina, fallopian tubes, ovaries, and uterus, and then to the bloodstream.

Abstract: A liposome contains an active agent and has a gel-phase lipid bilayer membrane comprising phospholipid and a surface active agent. The phospholipids are the primary lipid source for the lipid bilayer membrane and the surface active agent is contained in the bilayer membrane in an amount sufficient to increase the percentage of active agent released at the phase transition temperature of the lipid bilayer, compared to that which would occur in the absence of the surface active agent. The surface active agent is present in the lipid bilayer membrane so as to not destabilize the membrane in the gel phase.

Abstract: The invention relates to a novel combination of a soft steroid, in particular loteprednol, and at least one ?2 adrenoceptor agonist for the simultaneous, sequential or separate treatment of allergies and/or airway disorders, medicaments comprising the combination, processes for the production of such medicaments and the use of the novel combination for the production of medicaments for the simultaneous, sequential or separate treatment of allergies and/or airway disorders.

Abstract: The invention provides methods and compositions for maintaining a state of sexual wellness in a healthy human by providing a dietary supplement comprising one or more sexual steroid prohormones.

Abstract: The invention relates to compounds of the general formula (I) to a method for the production thereof, to pharmaceutical, cosmetic compositions or dosage forms which contain these compounds, and to a method for contraception by administration of these compounds.

Abstract: A liposome contains an active agent and has a gel-phase lipid bilayer membrane comprising phospholipid and a surface active agent. The phospholipids are the primary lipid source for the lipid bilayer membrane and the surface active agent is contained in the bilayer membrane in an amount sufficient to increase the percentage of active agent released at the phase transition temperature of the lipid bilayer, compared to that which would occur in the absence of the surface active agent. The surface active agent is present in the lipid bilayer membrane so as to not destabilize the membrane in the gel phase.

Abstract: Mucoadhesive and controlled release formulations consisting of aqueous solutions containing 0.05% to 5% by weight of a natural purified polymer having xyloglucan structure and 10% to 70% by weight of glycerol. These formulations are suitable for the application on human mucous membranes, such as nasal, oral and vaginal mucous membranes, as moisturizing and softening agents or as pharmaceutical release system. Further objects of the invention are pharmaceutical formulations and medical devices suitable for the application to human mucous membranes, containing the mucoadhesive and controlled release formulations together with active ingredients and excipients.

Abstract: Pharmaceutical composition comprising compounds and/or compositions useful to inhibit viral replication are disclosed.

Abstract: This invention provides a dermatological preparation to improve skin cosmesis or conditioning by using different formulations in a sequence that suits the needs of the skin at different points of the hormonal cycle. In its simplest implementation, this would be a two-phase skin treatment, such as a cosmetic, lotion or soap whose formulation changes to balance the differing states of hydration and reactivity of the skin during the early and late phases of the cycle. The formulations would be made in a way to be easily identified and delivered conveniently for use at different times of a hormonal cycle. The preparation would be packaged to permit the convenient purchase and dispensing of the different formulations in a manner that could be easily sequenced with the hormonal cycle.

Abstract: Methods for modulating hormonal pathways involving the progesterone receptor in a subject with a neurodegenerative disorder, are provided. Progesterone receptor activity is modulated by administering an effective amount of an progesterone receptor modulating pharmacological agent to a subject such that the progesterone receptor modulating pharmacological agent interacts with the progesterone receptor and alters the expression of a protein associated with the neurodegenerative disease.

Abstract: The present invention comprises lupine-type triterpenoids that inhibit cell proliferations, in particular cancer and conditions associated with cancer. For example, associated malignancies include ovarian cancer, cervical cancer, breast cancer, colorectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit cancer and treat, prevent, or inhibit the foregoing diseases.

Abstract: Compositions useful for inducing bone growth or inhibiting bone loss in an animal comprising one or more isoflavones or isoflavone metabolites and methods for inducing bone growth or inhibiting bone loss in an animal utilizing such compositions. The compositions and methods are particularly useful for post-menopause, post-andropause, gonadectomized, spayed, or neutered animals.

Abstract: Compounds having a cyclolanostane skeleton such as 9,19-cyclolanostan-3-ol and 24-methylene-9,19-cyclolanostan-3-ol are used as an active ingredient of a drug and food or drink for improving pancreatic functions.

Abstract: The 17?-cyano-18a-homo-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity.

Abstract: The 17?-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity.

Abstract: A biodegradable and thermosensitive poly(organophosphazene) with a functional group, a preparation method thereof, and a use thereof for delivery of bioactive substances are provided.

Abstract: A container suitable for the preparation, storage and dispensing of compounded suppositories is provided. Methods of preparing, storing and dispensing compounded suppositories utilizing such a container and related kits are also provided.

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

Abstract: The present invention relates to the use of C3-C10 17?-esters of 9,11-dehydrocortexolone as agents for inhibiting gonadotrophin secretion. The present invention therefore relates to the use of C3-C10 17 ?-esters of 9,11-dehydrocortexolone for the preparation of a medicine for the treatment of disorders associated with the secretion of gonadotrophin and with the corresponding pharmaceutical compounds. The present invention relates specifically to the use of 9,11-dehydrocortexolone 17?-butyrate.

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: 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: A compound having the structure: wherein R1 and Z are as described above, X is selected from the group consisting of: C1-C6 alkyl, a substituted alkyl, a halogen, a halogenated alkyl, a glucuronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3—CH(CH2)nCOOCH3, —(CH2)n—O—CH3, —CH2OH, —(CH2)n—O—NH2, —NH(CH2)nCH3, NH(CH2)nOCH3, —NH(CH2)nCHOH—COOH, —N(CH3)2, —(CH2)n(NH)CH2OH, —NHCOOH, —(CH2)nNHCOOH, —NO2, —SCN, —SO2alkyl, —B(OH)2, —(CH2)nN(CH3)—SO2—NH3, —(CH2)nNH—SO2—NH2, —NHC(?S)CH3, and —NHNH2; R3 is selected from the group consisting of: H, a C1-C6 alkyl, a substituted alkyl, a halogen, and a halogenated alkyl; R4 and Y are independently selected from a group consisting of: O, —OH, —H, a —C1-C6 alkyl, a substituted alkyl, a halogen, a halogenated alkyl, a sulfate, a glucuronide, a bulky group, a phenyl or a substituted phenyl group, a cyclo- or heterocyclo group, piperidine, piperazine, morpholine, pyrimidine, —NH2, —N(CH2)nCH3; a phosphate group, a phosphinate group, whe

Abstract: The present invention provides a method of reducing or inhibiting osteoclast development induced by the receptor for activation of nuclear factor kappa B ligand (RANKL), comprising the step of contacting said osteoclast, or a precursor of the osteoclast, with a pharmacologically effective dose of compounds such as diferuloylmethane, guggulsterone, 1?-Acetoxychavicol or analogues thereof.

Abstract: The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7?-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17?-diol, more particularly to a formulation adapted for administration by injection containing the compound 7?-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17?-diol in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.

Abstract: The present disclosure provides methods for preventing or treating illness, improving responsiveness to immunization, and improving the efficacy of gene therapy in a patient by disrupting sex steroid signalling in the patient, wherein the bone marrow and other immune cell functionality is improved without, prior to, or concurrently with, thymic regeneration. In some embodiments, sex steroid signalling is interrupted or ablated in the patient by the administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines, anti-androgens, anti-estrogens, selective estrogen receptor modulators (SERMs), selective androgen receptor modulators (SARMs), selective progesterone response modulators (SPRMs), ERDs, aromatase inhibitors, or various combinations thereof.

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