Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a 19-nor cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: A pharmaceutical composition for the treatment of sexual dysfunction, particularly post-menopausal females, is provided. The composition includes a therapeutically effective amount of an estrogenic compound, androgenic compound, vasodilation compound, and a pharmaceutically acceptable carrier.

Abstract: SR-BI is present on the membranes of hepatocytes and steroidogenic tissues, including the adrenal gland, testes, and ovaries, where it mediates the uptake and transport of cholesteryl ester from high density lipoproteins. It has been demonstrated that transgenic animals which do not produce SR-BI are perfectly healthy, with the exception that the females are infertile. This provides evidence that inhibition of uptake, binding or transport of cholesteryl ester to SR-BI can be used to inhibit pregnancy. The same pathway can also be used to decrease production of steroids, and therefore be used as a therapy for disorders involving steroidal overproduction.

Abstract: The present invention relates to methods for regulating the condition of mammalian keratinous tissue wherein the methods comprise the step of topically applying to the keratinous tissue of a mammal needing such treatment, a safe and effective amount of a composition comprising:

Abstract: A combination therapy for the prophylaxis and/or treatment of benign prostatic hyperplasia in susceptible warm-blooded animals which comprises administering a combination of two or more compounds selected from the group consisting of an inhibitor of 5&agr;-reductase activity, an anti-estrogen, an inhibitor of aromatase activity, an inhibitor of 17&bgr;-hydroxysteroid dehydrogenase activity and, in some cases, an anti-androgen and/or an LHRH agonist. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such compositions are disclosed.

Abstract: This invention relates to a method of treating an immune-mediated disorder having one or more manifestations. The method comprises administering to a patient requiring such treatment a gold compound and at least one corticosteroid, wherein the at least one corticosteroid is selected to interact synergistically with the gold compound to exhibit preferential action towards one of the manifestations of said disorder or to exhibit equal action towards each manifestation of said disorder. The invention also relates to a pharmaceutical composition suitable for use in the method.

Abstract: The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds.

Abstract: Dietary compositions and methods employ a mammal food base and a component comprising estrogen, androgen or a mixture thereof in an amount sufficient to reduce weight gain normally incurred in the mammal type subsequent to neutering, castration, spaying, ovariectomy or ovariohysterectomy, or post menopause. Preferably, the component comprises phytoestrogen, phytoandrogen or a mixture thereof. The compositions are adapted for administration to the mammal on a regular, preferably daily, basis.

Abstract: A medicament for preventive and therapeutic treatment of obesity and a disease with abnormal lipid metabolism which comprises a 24-alkylcholest-5-en-3-one as an active ingredient.

Abstract: The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.

Abstract: A compound, process and method for increasing external auditory canal patency while simultaneously preventing the occurrence of otitis externa is disclosed wherein an aerosolized mixture of lipid crystals comprised of a mixture of one or more lipids surfactants and one or more spreading agents selected from the group consisting of sterols, lipids, fatty acids, cholesteryl esters, phospholipids, carbohydrates, nucleic acids and proteins, in powder form, and one or more fluorocarbon propellants is administered directly to the external auditory canal. Upon administration, the propellant(s) are evaporated from the mixture and the lipid crystals are deposited upon an air/liquid interface resident upon epithelial tissue lining the external auditory canal.

Abstract: The invention pertains to a pharmaceutical dosage unit, such as a tablet or a capsule, comprising an effective amount of tibolone (generally of from 0.1 to 10% by weight) and a starch-containing pharmaceutically acceptable carrier (also denoted as basic granulate), wherein the carrier contains of from 10 to 100% by weight of the starch. Thus a more stable tibolone formulation is obtained, allowing dry storage and lower doses of active ingredient.

Abstract: Human skin can be moisturized by the administration of &Dgr;5-androstene-3&bgr;-ol-7,17 dione and metabolizable precursors thereof, such as &Dgr;5-androstene-3&bgr;-acetoxy-7,17 dione.

Abstract: Wrinkles and fine lines occurring on human skin can be diminished by the administration of &Dgr;5-androstene-3&bgr;-ol-7,17 dione and metabolizable precursors thereof, such as &Dgr;5-androstene-3&bgr;-acetoxy-7,17 dione, to the skin.

Abstract: Methods for abating coronary artery blockage in human subjects include administering a combination of natural hormones including human growth hormone with sufficient T3 thyroid supplement to maintain the body temperature of the subject at or above 97.6° F. upon awakening and at 98.7° F. or higher during afternoon hours. Testosterone, if any, administered to male subjects is in natural, gel form.

Abstract: Low potency, preservative free sterile topical anti-inflammatory steroid compositions are to be applied to the area surrounding the eye. The compositions involve, for example, sterile gauze pads in a sterile package, as well as single-use capsules and tubes for dispensing the medicinal composition.

Abstract: The invention provides a process for the sterilization of a powdered form of a glucocorticosteroid, sterile glucocorticosteroids, sterile formulations containing glucocorticosteroids and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or lungs.

Abstract: This invention involves the administration of the natural androgen metabolite 5-alpha-androst-1-en-3,17-dione(1-androstenedione) to produce an androgenic and anabolic response in humans. 1-Androstenedione behaves as a prohormone in vivo, and converts to the active hormone 17-beta-hydroxy-5-alpha-androst-1-en-3-one.

Abstract: Lupus erythematosus can be treated by administering therapeutic amounts of delta-5-androstene-3-beta-ol-7,17-dione and its metabolizable precursors, which are not appreciably metabolized in vivo to androgens, estrogens or dehydroepiandrosterone. Such treatment can be prophylactic, ameliorative or curative in nature.

Abstract: A dry powder formulation for treatment of pulmonary conditions, via inhalation, includes an effective amount of formoterol or a salt or solvate thereof, in a dry powder form, an effective amount of fluticasone, in a dry powder form, and an excipient. A method for preparing a physically stable dry powder formulation for inhalation includes the steps of micronizing a first active polar drug, a second active non-polar drug, and a polar excipient. The second non-polar active drug is first blended with the excipient to form an intermediate mixture. The intermediate mixture is then blended with the first active polar drug. The increased separation of the polar drug and polar excipient stabilizes the formulation.

Abstract: An oral pharmaceutical composition in the form of a stable suspension in water, said composition comprising:

Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.

Abstract: A compound having the general formula: 1

Abstract: A bioadhesive composition for use as a skin adhesive, the composition formed by polymerising with cross-linking and/or entanglement an aqueous reaction mixture comprising effective amounts of at least one monomer dissolved or suspended therein and capable of forming a hydrogel on polymerisation, optionally at least one cross-linking agent for the monomer, and water, said composition having an elastic modulus (G′) and a viscous modulus (G″), wherein the degree of polymerisation and/or the degree of cross-linking and/or entanglement are selected to control the skin adhesion properties of the bioadhesive composition having regard to the rate of change of tan delta (G″÷G″) against frequency in a diagnostic portion of the frequency range 0.01 to 300 rad/s, typically the lower end of the said frequency range below about 100 rad/s.

Abstract: The invention related to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-4,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17(20)-dien-3-one, 20&xgr;-fluoropregna-4,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.

Abstract: A method is provided for enhancing a female individual's sexual desire and responsiveness. The method involves administration of a pharmaceutical formulation containing an effective amount of an androgenic agent, wherein administration is on an as-needed basis rather than involving chronic pharmacotherapy. Local delivery may be accomplished via administration to the vagina, vulvar area or urethra of the individual, although oral administration is preferred for those androgenic agents that are orally active. Formulations and kits for carrying out the method are provided as well.

Abstract: The subject of the invention is the products of formula (I): 1

Abstract: This invention describes the use of antiestrogens (aromatase inhibitors, estrogen receptor antagonists) for the production of pharmaceutical agents for male birth control.

Abstract: The invention relates to a method of alleviating pain. The method comprises nasally administering a steroid which is a human vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.

Abstract: Methods for improving the efficiency of electroporation protocols as well as methods to enhance the permeabilized state, in order to improve the intracellular delivery of therapeutic substances, involve the use of at least one agent which is capable of prolonging the permeability of the cell membranes in the tissue exposed to an electroporation-inducing electrical field.

Abstract: This invention involves the administration of the natural androgen metabolite 5alpha-androst-1-en-3,17-dione(1-androstenedione) to produce an androgenic and anabolic response in humans. 1-androstenedione behaves as a prohormone in vivo, and converts to the active hormone 17beta-hydroxy-5alpha-androst-1-en-3-one.

Abstract: This invention relates to the use of an aromatase inhibitor in the treatment of decreased androgen to estrogen ration (DATER) as well as to a method for the treatment of detrusor urethral sphincter dyssnergia (DUSD) in men.

Abstract: Syntheses of steroids such as 3-hydroxy-7&agr;-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: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating to consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: According to the present invention, a process for producing a practical cholesterol-reduced substance by converting cholesterol contained in foods and feeds to coprostanol having very low intestinal tract absorbability by utilizing enzymatic action is provided. Cholesterol in a cholesterol-containing substance such as meat, egg, milk, seafood and cooked processed foods containing the same, or feeds for animals, poultry and pisciculture, and the like, can be treated with three kinds of enzymes which are a cholesterol dehydrogenase having an optimum pH in a neutral pH range and 4-cholesten-3-one dehydrogenase and coprostan-3-one dehydrogenase each having an optimum pH in a weak acidic range, or microbial cells containing the enzymes, for converting the cholesterol to coprostanol to reduce the amount of the cholesterol.

Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and medroxyprogesterone acetate.

Abstract: The present invention teaches that daily, cyclical vaginal delivery of progestin may be used to provide regular, predictable withdrawal bleeding during hormone replacement therapy. The present invention also teaches that constant administration of progestin in a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer may be used to maintain amenorrhea. Either regimen is accompanied by a significant decrease in adverse side effects.

Abstract: The present invention teaches that daily, cyclical vaginal delivery of progestin may be used to provide regular, predictable withdrawal bleeding during hormone replacement therapy. The present invention also teaches that constant administration of progestin in a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer may be used to maintain amenorrhea. Either regimen is accompanied by a significant decrease in adverse side effects.

Abstract: Plant sterols and plant sterol esters have been shown to be cholesterol-reducing agents in human serum. In the present invention, plant sterols, plant stanols, plant sterol esters, and plant stanol esters are incorporated into mouthfeel-enhancing, texture-building and composition-stabilizing compositions which are mesophase-stabilized compositions for use in low-fat, fat-free and triglyceride-free food products. Such compositions may be incorporated into food products resulting in low-fat, fat-free and triglyceride-free food products which may be used to deliver a recommended daily dosage of the cholesterol-reducing compounds to segments of the population which must limit it's cholesterol intake.

Abstract: Methods for treating ocular neovascularization using photodynamic therapy in combination with an angiostatic steriod are disclosed.

Abstract: The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their topical use in the ocular bacterial infections, more preferably in the treatment of conjunctivitis, keratitis and blepharitis.

Abstract: The subject of the invention is the products of formula (I): in which either R1 represents halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen, or R1 and R2 form together a double bond, Z is chosen from optionally substituted (C1-C8) alkylthio, optionally substituted arylthio, (C1-C8) alkyloxy, halogen, cyano, mercapto, thiocyanato and (CH2)0-1—CO2H, optionally esterified, Y represents hydrogen or methyl, the dotted line in position 1-2 or 5-6 optionally representing a second bond, as well as their addition salts, their preparation process, the intermediates of this process and the pharmaceutical compositions containing them.

Abstract: The application discloses methods of treating mammalian diseases characterized by undesirable angiogenesis by administering compounds including those having the general formulae wherein A is a fused tropone having a general formula: wherein X is selected from the group consisting of hydrogen, hydroxy, carboxy, halogen, nitro, C1 to C12 alkenyl, C1 to C12 alkyl, C1 to C12 alkoxy, SR, NR2, OSO3−, OSO2NR2, HNSO3−, NHSO2NR2, SSO3−, SSO2NR2, wherein R is hydrogen or a C1 to C6 alkyl and the 17-ester and keto derivatives thereof, in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the method of the invention.

Abstract: The present invention relates to an oral dosage delivery form which is effective in increasing the testosterone levels in humans. In a preferred embodiment, the composition comprises a mixture of four (4) prohormones, three (3) anti-estrogen agents and at least one (1) enteric coating. The inventive prohormone/anti-estrogen time-release dosage form allows the prohormone/anti-estrogen ingredients to be released over an extended period of time so as to provide for a sustained elevated blood serum testosterone level.

Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

Abstract: The invention is accomplished by preventing and/or reversing inner ear damage due to noise or toxins. In part, this is accomplished by upregulating antioxidant enzyme activity by applying agents such as R-N6-Phenylisopropyl adenosine (R-PIA) to the round window membrane of the inner ear or systemically, and/or by also applying agents such as 1-2-oxothiazolidine-4-carboxylic acid (Procysteine) to the round window membrane. Also, the invention is accomplished by giving the compounds systemically. Selective auditory hair cell protection in the face of gentamicin exposure by concomitant delivery of an NMDA antagonist or glial dervied neurtrophic factor (GDNF) with the gentamicin. These and additional agents are also accomplished by curtailing activated programmed cell death pathways and/or inducing/enhancing cell repair mechanisms in the inner ear. The agent(s) may be applied before, during or after the noise trauma or toxin exposure.

Abstract: A pharmaceutical composition contains an acid addition salt of a basic drug and a fatty acid or bile acid. The acid addition salts thus formed exhibit enhanced transmucosal and transdermal penetration of the basic drug. The acid addition salts, an inclusion complex containing said salts and a use of said salts are also disclosed.

Abstract: The invention pertains to a pharmaceutical dosage unit, such as a tablet or a capsule, comprising an effective amount of tibolone (generally of from 0.1 to 10% by weight) and a starch-containing pharmaceutically acceptable carrier (also denoted as basic granulate), wherein the carrier contains of from 10 to 100% by weight of the starch. Thus a more stable tibolone formulation is obtained, allowing dry storage and lower doses of active ingredient.

Abstract: A method for the treatment of ischemic damage, such as damage due to stroke or myocardial infarction, is provided, comprising administering to a mammal afflicted with stroke, an effective amount of a progestin in a suitable vehicle.

Abstract: This invention discloses a method of administering direct precursors of the hormone dihydrotestosterone as a means of increasing androgen levels in humans. As men age, a decline in androgenic hormone levels is typically noted, possibly resulting in muscle mass, bone density and energy loss. Various methods have therefore been developed to supplement androgens for men with declining levels. This invention teaches using precursors to testosterone, in that DHT and its precursors cannot be converted to estrogens in the human body. This may be a very advantageous trait for aging men at risk for benign prostatic hypertrophy, as estrogenic and androgenic action are both needed to induce this condition. As testosterone is the primary substrate for the synthesis of estradiol in men, its use as a target for androgen replacement may pose a greater health risk.