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

Abstract: A method of treating preeclampsia including administering a therapeutically effective dose of resibufagenin to a patient having preeclampsia. Effecting the determination of the presence of preeclampsia may be by determining whether there has been a substantial elevation in marinobufagenin which may be blood-derived or urine-derived and if such elevation does exist, concluding that preeclampsia does exist. The method may advantageously be practiced by employing urine, blood serum or blood plasma as the body specimen containing the protein in determining whether a patient has preeclampsia. In another embodiment, bufodienolide derivatives other than resibufagenin may be employed in lieu of thereof or in combination therewith. In another embodiment, resibufagenin analogues may be employed in the treatment of preeclampsia.

Abstract: The invention relates to compounds and methods for inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin, by way of fructosamine-3-kinase inhibition, thereby treating or prevention various diseases, disorders or conditions. Additionally, the invention relates to treatment of various diseases, disorders or conditions associated with or mediated by oxidative stress since 3DG induces ROS and AGEs, which are associated with the inflammatory response caused by oxidative stress.

Abstract: This invention relates to a method of preventing pregnancy and treating PMS including PMDD. More particularly, the invention relates to a method, which involves administering one of several combination oral contraceptive regimens in combination with an antidepressant and a kit containing the same.

Abstract: A transdermal delivery system comprising a composition comprising a physiologically active agent and a penetration enhancer wherein the penetration enhancer comprises a combination of (i) an ester of salicylic acid, preferably selected from the C6 to C30 aliphatic ester of salicylic acid and (ii) polyethylene glycol (PEG) of average molecular weight no more than 300.

Abstract: The 17?-cyano-19-androst-4-ene derivatives of the present invention possess gestagenic activity.

Abstract: The present invention provides a process for extracting sterols from a high solids, thermochemically hydrolyzed corn fiber using ethanol as the extractant. The process includes obtaining a corn fiber slurry having a moisture content from about 20 weight percent to about 50 weight percent solids (high solids content), thermochemically processing the corn fiber slurry having high solids content of 20 to 50% to produce a hydrolyzed corn fiber slurry, dewatering the hydrolyzed corn fiber slurry to achieve a residual corn fiber having a moisture content from about 30 to 80 weight percent solids, washing the residual corn fiber, dewatering the washed, hydrolyzed corn fiber slurry to achieve a residual corn fiber having a moisture content from about 30 to 80 weight percent solids, and extracting the residual corn fiber with ethanol and separating at least one sterol.

Abstract: The present invention is related to an intravaginal delivery system for the controlled release of drospirenone and an estrogen, optionally also comprising one or more therapeutically active or a health-promoting substance capable of giving and/or enhancing protection against bacterial and fungal infections, and/or enhancing protection against sexually transmitted diseases. The delivery system consists of one or more compartments, one of each comprising a core and a membrane encasing the core, said core and membrane essentially consisting of a same or different polymer composition, wherein at least one compartment comprises drospirenone ant at least one compartment which may be the same or different from the one comprising drospirenone, comprises an estrogen or a mixture of drospirenone and an estrogen, and wherein the membrane or the surface of the membrane or at least one of the cores comprises said therapeutically active or a health-promoting substance.

Abstract: A process for preparing particles of a substance, such as a protein or polypeptide, comprising: (a) preparing a first liquid comprising water, the substance and a modulator, wherein the modulator has a solubility in water which decreases with increasing temperature; and (b) contacting the first liquid with a second liquid comprising a fluid gas and an organic solvent using an anti-solvent fluid gas technique under conditions of temperature and pressure which result in the precipitation of particles comprising the substance, wherein the temperature of the first liquid is at or above the cloud point temperature of the first liquid when the first liquid contacts the second liquid. Also claimed are particles obtained according to the process and compositions containing the particles.

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: The invention relates to a method for contraception comprising the administration of trimegestone to a woman of child-bearing age on at least 21 successive days, beginning on day 1 of the menstrual cycle, wherein on at least one of the at least 21 successive days the daily dose of trimegestone is more than 500 ?g.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: The present invention relates to topical pharmaceutical compositions comprising fusidic acid and a corticosteroid. More particularly, the present invention relates to topical pharmaceutical compositions comprising fusidic acid and mometasone or halobetasol or their esters, processes for preparing the same, and the use of such compositions for prevention and treatment of dermal infections.

Abstract: Compositions and methods for alleviating the symptoms associated with chronic fatigue syndrome and fibromyalgia syndrome are provided. The compositions are based on use of a transdermal gel formulation delivery system for androgens, either alone or in combination with other hormones.

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 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: 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: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.

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: 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 and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.

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: The present invention relates to pregnancy hormone combinations and methods of treatment for autoimmune diseases having at least two hormonal components, a pregnancy hormone (such as estriol), and a gestagen (such as levonorgestrel or norethindrone) thereby providing for the continuous, uninterrupted administration of pregnancy hormones for the treatment for autoimmune disorders, such as multiple sclerosis.

Abstract: The present invention relates to a method for treating and/or preventing ovarian cycle disturbance, prolonged un-opposed secretion of estrogens, and/or ovarian follicular cyst formation in pre-menopausal women with functional ovaries when treated with steroid sulfatase inhibitors (STS-I) for an estrogen-dependant condition.

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: The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.

Abstract: The multiphase combination preparation for oral therapy of dysfunctional uterine bleeding and for oral contraception contains a first phase consisting of 2 daily dosage units, each containing 3 mg of estradiol valerate or <3 mg of estradiol; a second phase consisting of a first group of 5 daily dosage units, each consisting of a combination of 2 mg of dienogest with 2 mg of estradiol valerate or <2 mg of estradiol, and a second group consisting of 17 daily dosage units, each consisting of a combination of 3 mg of dienogest with 2 mg of estradiol valerate or <2 mg of estradiol; a third phase consisting of 2 daily dosage units, each containing 1 mg of estradiol valerate or <1 mg of estradiol; and another phase consisting of 2 daily dosage units of a pharmaceutically harmless placebos.

Abstract: A method of long-term therapy using corticosteroids to treat tissue damage associated with graft-versus-host disease in a patient having undergone hematopoietic cell transplantation, and host-versus-graft disease in a patient having undergone organ allograft transplantation. The method includes orally administering to the patient a therapeutically effective amount of a topically active corticosteroids, such as beclomethasone dipropionate, from the 29th day until the 56th day following hematopoietic cell or organ allograft transplantation. Representative tissues include tissue of the intestine and liver, while representative tissue damage includes inflammation thereof.

Abstract: A method of treating preeclampsia including administering a therapeutically effective dose of resibufagenin to a patient having preeclampsia. Effecting the determination of the presence of preeclampsia may be by determining whether there has been a substantial elevation in marinobufagenin which may be blood-derived or urine-derived and if such elevation does exist, concluding that preeclampsia does exist. The method may advantageously be practiced by employing urine, blood serum or blood plasma as the body specimen containing the protein in determining whether a patient has preeclampsia. In another embodiment, bufodienolide derivatives other than resibufagenin may be employed in lieu of thereof or in combination therewith. In another embodiment, resibufagenin analogues may be employed in the treatment of preeclampsia.

Abstract: A stanol composition containing in addition to sitostanol as the main component, also a substantial amount of at least 10% campestanol has been found to effectively lower serum cholesterol levels when incorporated in edible commodities. Upon esterification the composition is especially useful in edible fats and oils and in fat-containing foods.

Abstract: A transdermal drug delivery device is disclosed. Over an extended wear period, the device causes cumulative moderate irritation plus significant irritation of less than 5% and/or achieves a meaningful degree of detachment over a seven day period of less than 20%.

Abstract: Compositions and methods useful in the reduction of localized fat deposits in patients in need thereof using pharmacologically active detergents are disclosed. The pharmacologically active detergent compositions can additionally include anti-inflammatory agents, analgesics, dispersion or anti-dispersion agents and pharmaceutically acceptable excipients. The pharmacologically active detergent compositions are useful for treating localized accumulations of fat including, for example, lower eyelid fat herniation, lipodystrophy and fat deposits associated with cellulite and do not require surgical procedures such as liposuction.

Abstract: The multiphase preparation having higher contraceptive safety and reduced side effects is based on a combination of a natural oestrogen with dienogest or drospirenon. The multiphase prepration is characterized by a first phase consisting of 2 daily dose dose units of 3 mg of oestradiol valerate, a second phase consisting of 2 groups of daily dose units, wherein a first group is formed by 5 daily dose units each containing a combination of 2 mg of oestradiol valerate and at least two or three times an ovulation-inhibitory dose of dienogest or drospirenon and a second group is formed by 17 daily dose units each containing a combination of 2 mg of oestradiol valerate and at least three or four times the ovulation-inhibitory dose of dienogest or drospirenon, a third phase consisting of 2 daily dose units of 1 mg of oestradiol valerate, and a further phase consisting of 2 daily dose units of pharmaceutically acceptable placebo.

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: A contraceptive kit comprising a package containing daily dosages of: (a) a first composition containing a progestin in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol for about 22 to about 26 days; (b) a second composition containing an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol for about 2 to about 3 days and an optional third composition that is a placebo provided that (i) if estrogen administration is continuous then the first composition is administered for 25 to 26 days, the second composition is administered for 2 to 3 days and no third composition is administered and (ii) if estrogen administration is not continuous then the first composition is administered for 22 to 24 days, the second composition is administered for 2 to 3 days and the third composition is administered for 1 to 4 days.

Abstract: A method for preventing or treating vascular hyperreactivity in which a chemical compound that is an estrogen beta receptor agonist is administered to a subject suffering from or at risk of vascular hyperreactivity. Preferably, the administration is topically to the skin.

Abstract: An agent having progesterone antagonist properties may be used to treat eye conditions associated with pathological blood vessel formation, for example age-related macular degeneration, choroidal neovascularisation, retinal neovascularisation or corneal neovascularisation. The agent may be mifepristone.

Abstract: The invention concerns a pharmaceutical composition comprises trimegestone optionally associated with an oestrogen, characterized in that it comprises a buffer solution whereof the pH, when it is introduced in the composition, ranging essentially between 2 and 5.5. The invention also concerns the methods for making such a composition and the primary package containing them.

Abstract: A method of contraception in mammalian females, which method comprises the oral administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1) in which R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and/or a progestogenic component.

Abstract: Described herein are 3-(6,6-ethylene-17?-hydroxy-3-oxo-17?-pregna-4-ene-17?-yl)propionic acid ?-lactone derivatives having progestational and aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.

Abstract: The present invention relates to new steroid modulators of progesterone receptor activity and/or glucocorticoid receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention includes methods for preventing endometrial hyperplasia associated with estrogen therapy through the administration of a progestin agent. The methods presented may include starting the administration of a progestin agent at a high dose, and then lowering the dose.

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 present invention is a product comprising a ?2 agonist and a progestin, as a combined preparation for separate, simultaneous or sequential use in the treatment or prevention of muscle loss. The present invention is also a ?2 agonist selected from R,R-formoterol, indacaterol or ritodrine, for use in the treatment or prevention of muscle loss.

Abstract: A dosage comprising an antibiotic, an estrogen, and a progestagen is provided. The dosage can be oral, or administered in other methods, such as intravaginally with a tampon. The dosage can be used for menstrual suppression, contraception, and/or hormone replacement therapy. A method of treating a patient with the dosage comprises administering the dosage to the patient over a course of treatment, in amounts or frequencies that can remain constant, or be varied.

Abstract: Cosmetic substances having 1x×10?7 to 1×10?2 percent by weight of at least one steroid chosen from among certain 16-androstene and estrene steroids, and 0.1 to 30.0 percent by weight of at least one film-forming and/or solidifying polymers. Also disclosed is the use of those cosmetic substances for treating keratin fibers, particularly for temporarily deforming such fibers.

Abstract: Use of a mixture of phytosterols, selected from the group comprising: brassicasterol (Delta 5-C22 unsaturated); campesterol; campestanol; stigmasterol (Delta 5-C22 unsaturated); Delta 5-C23-stigmastadienol; clerosterol (Delta 8-C25 unsaturated); Beta-sitosterol; sitostanol; Delta 5-venasterol (Delta 5-C24 unsaturated); Delta 5-C24-stigmastadienol (Delta 5-C24 diene unsaturated); Delta 7-stigmastenol; 24-methylene-cycloartenol; gramisterol; 24-methylcholest-7-enol; isofucosterol; Delta 7-avenasterol (Delta 7-C24 unsaturated); Delta 5-avenastenol, for the manufacture of a medicament to induce into the adult organism proliferation and differentiation of the stem cells which are present in the organism.

Abstract: The present invention provides methods and related compositions for treating or preventing cardiovascular diseases, including, e.g., atherosclerosis, using an oxysterol. In addition, the present invention provides novel methods and related compositions for treating or preventing cardiovascular diseases, including, e.g., atherosclerosis, using a hedgehog protein, or a biologically active fragment or variant thereof.

Abstract: There is disclosed an emergency contraceptive preparation which comprises at least one aromatase inhibitor wherein the preparation comprises at least one dose for administration on one or more days to a female patient following an unprotected sexual encounter until the establishment or continuation of pregnancy of the patient is prevented. Also disclosed is a method of emergency contraception.

Abstract: The subject invention provides a liquid contraceptive formulation for oral transmucosal administration. The formulation comprises etonogestrel, optionally together with ethinyl estradiol but does not contain a matrix former or a percutaneous absorption promoter, which is a hydroxy acid or a salt thereof.