Abstract: The present invention relates to the field of chemistry and more particularly to that of therapeutic chemistry. The invention relates more particularly to novel contraceptive compositions formed from a progestative agent and an oestrogen. The invention relates specifically to novel pharmaceutical contraceptive compositions, characterized in that they contain, as active ingredients, a nomegestrol ester and oestradiol, in combination or admixture with an inert, non-toxic, pharmaceutically-acceptable vehicle or diluent which is suitable for oral administration.

Abstract: A method for enhancing the efficacy of chemotherapy in the treatment of cancer in animals, particularly humans, is provided wherein isocoumarin derivatives that exhibit unique chemopotentiation properties are employed in a combination treatment with chemotherapy.

Abstract: The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.

Abstract: Androgenic steroids having a (14?,17?-)-17-(hydroxymetheyl) configuration, useful for the preparation of male contraceptives and pharmaceutical formulations for the treatment of androgen insufficiency.

Abstract: In accordance with the present invention, there have been identified extracts from a tropical plant that initiate paclitaxel-like microtubule bundling. Bioassay-directed purification yields the steroid taccalonolide A. Taccalonolide, like paclitaxel, initiates the formation of abnormal interphaes and mitotic microtubules. Cells treated with taccalonolide exhibit thick bundles of microtubules that appear to nucleate independent of the microtubule organizing center. Abnormal mitotic spindles consisting of multi-polar spindles are initiated by taccalonolide and resemble abnormal mitotic spindles found in the presence of paclitaxel. Like paclitaxel, taccalonolide causes the breakdown of the nucleus into micronuclei. Taccalonolide causes G2/M arrest, Bc1-2 phosphorylation and initiates an apoptotic cascade that includes the activation of caspase 3. Taccalonolide is an effective inhibitor of proliferation against both SK-OV-3 and MDA-MB-435 cell with IC50 values of 2.3 ?M and 2.1 ?M respectively.

Abstract: The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds. The compounds according to the invention have a hybrid-type profile of action in the sense that they act as inhibitors of 5?-reductase and simultaneously as gestagens. They are therefore suitable for treating diseases that are the result of elevated androgen levels in certain organs and tissues in men and women. Together with other hormonal substances, such as an estrogen, testosterone or a strong androgen, the compounds according to the invention are suitable as contraceptive agents for women and for men.

Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI2-mimetic, a thromboxane (TXA2) inhibitor, a compound possessing TXA2-agonistic and TXA2-inhibiting properties, a compound possessing TXA2-antagonistic and PGI2-memetic activities, and a TXA2 antagonist.

Abstract: Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &agr;, &bgr;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &agr;, &bgr;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Abstract: Compositions and methods for alleviating the symptoms associated with muscle pain in general or muscle wasting are provided. The compositions are based on use of androgens, either alone or in combination with other hormones, including growth hormone.

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 method of treating estrogenic deficiencies in women while further avoiding the appearance of osteoporosis, withdrawal bleeding and cardiovascular diseases in post-menopausal women without any androgenic effect, and no deleterious effects on blood vessels comprising continuously without interruption administering to said women, a combination of 0.5 to 3 mg of an estrogenic compound and 1.5 to 3.75 mg of nomegestrol acetate.

Abstract: Processes for evaluating androgenic properties of various compounds and/or compositions are described, wherein the processes comprise: (a) providing a culture of at least one male fibroblast, the at least one male fibroblast having a metabolic activity; (b) contacting the culture with a potential active component; and (c) determining the metabolic activity of the fibroblast against a standard.

Abstract: Compounds are described which exhibit an inhibitory action towards the enzyme aromatase and which comprise at least one detectable group. Such compounds are excellently suitable for medical diagnosis and/or for therapy, particularly for tumor diseases and above all for breast cancer.

Abstract: A method of inducing ovulation in a female suffering from anovulatory infertility which comprises administering to said female two or more daily doses of at least one aromatase inhibitor. A method for augmenting ovulation in an ovulating female suffering from unexplained infertility or another type of ovulatory infertility which comprises administering to said female two or more daily doses of at least one aromatase inhibitor early in one or more menstrual cycles. A method of substantially reducing dosage levels of follicle stimulating hormone (FSH) for administration to a female undergoing infertility treatment which comprises administering a combination of two or more daily doses of at least one aromatase inhibitor (AI) with a plurality of daily doses of follicle stimulating hormone (FSH).

Abstract: A topical testosterone formulation is disclosed. In one aspect, the formulation may include a therapeutically effective amount of micronized testosterone, an arginine ingredient, and a tocopherol ingredient admixed with a poloxamer lecithin organogel. Additional ingredients may be included, such as melatonin, oxytocin, DHEA, and progesterone.

Abstract: Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue.

Abstract: A topical testosterone formulation is disclosed. In one aspect, the formulation may include a therapeutically effective amount of micronized testosterone, an arginine ingredient, and a tocopherol ingredient admixed with a poloxamer lecithin organogel. Additional ingredients may be included, such as melatonin, oxytocin, DHEA, and progesterone.

Abstract: A novel process for making estra-4,9(10)-diene-3,17-dione steroids from readily available 19-nor-androst-4-ene-3-one steroids by a straightforward three-step process. Products of this process are important intermediates in the preparation of biologically active substances.

Abstract: There is provided a natural composition for boosting the libido of an individual, the composition including an effective amount of an aphrodisiac and a compound to increase blood flow to the pelvic area in a pharmaceutically acceptable carrier. A natural composition for boosting the libido of an individual, including an effective amount of a compound for driving blood flow to the penis and an aphrodisiac in a pharmaceutically acceptable carrier is also provided. Also provided is a method of increasing the libido by administering an effective amount of composition including an aphrodisiac and a compound to increase blood flow to the pelvic area in a pharmaceutically acceptable carrier.

Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.

Abstract: The present invention discloses the use of methyltestosterone as a novel pharmaceutical for treatment of anti-HPV infections, especially for treatment of verruca planae, condyloma acuminatum, and the relapse of these disorders. The therapeutic efficacy of the aforementioned indications proves satisfactory.

Abstract: Compositions comprising a sterol component and a glycerol fatty acid ester component, wherein the glycerol fatty acid ester component has a hydroxyl value of from 20 to 120, and wherein at least 40% of acyl groups present in the glycerol fatty acid ester component are saturated and contain no more than 12 carbon atoms; are described along with methods of dissolving sterols and improving the solubility of sterols using such glycerol fatty acid esters.

Abstract: The present invention relates to the use of progesterone or a progesterone receptor agonist for the inhibition of steroid synthesis, in particular for inhibiting the expression of the steroidogenic acute regulatory protein (StAR protein).

Abstract: The present invention is directed to a composition and method for enhancing the appearance of skin or tissue. The invention is preferably a combination of elastin-derived peptides and steroidal compounds useful in the treatment of problems associated with deficient elastin or conditions that would benefit from increased elastin.

Abstract: The invention relates to the use of progesterone receptor inhibitors for inhibition of growth-factor-dependency of tumor cells.

Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: 1

Abstract: The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7&agr;-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17&bgr;-diol, more particularly to a formulation adapted for administration by injection containing the compound 7&agr;-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17&bgr;-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: A method of inhibiting the occurrence of advanced endometrium maturation in a female mammal undergoing fertility treatment is disclosed. The method comprises the administration at least one 17&agr;-fluoralkylated progesterone receptor antagonist to the female mammal.

Abstract: The invention relates to new 7&agr;, 17&agr;, 17&bgr;-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma.

Abstract: The present invention relates to compositions and methods for preventing the development of epithelial ovarian cancer by administering compounds in an amount capable of increasing TGF-&bgr; expression in the ovarian epithelium. HRT and OCP regimens comprising such compositions and methods are disclosed.

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 a cosmetic process for treating dry skin or a dry scalp by the topical application to the skin or the scalp of a composition containing, in a physiologically acceptable medium, at least one of 5-cholesten-3&bgr;,25-diol-7-one and esters and ethers thereof.

Abstract: The invention concerns a progestin co-micronized with a surfactant and a pharmaccutical composition comprising said gestagenic. The invention also concerns methods for preparing same.

Abstract: Certain compounds, structurally related to natural compounds which can be extracted i.a. from bull testes and from human follicular fluid, can be used for regulating the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives. These compounds have the structural formula wherein the substituents are as defined in the specification.

Abstract: The present invention relates to transdermal dosage forms for delivery of androgens.

Abstract: An oral testosterone delivery system with sustained release properties where the micronized testosterone is present as a tablet, bolus, capsule, powder, liquid or suspension and, optionally, at least part of the testosterone is microencapsulated; in a preferred embodiment, the testosterone is present in a solid lipid suspension, wherein the suspension exhibits pseudotropic and/or thixotropic flow properties when melted.

Abstract: The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

Abstract: The present invention relates to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a testosterone deficient disorder, or the symptoms associated with, or related to a testosterone deficient disorder in a subject in need thereof. The present invention also relates to a method of administering a steroid in the testosterone synthetic pathway to a subject in need thereof. In addition, the methods, kits, combinations and compositions may be used in conjunction with other pharmaceutical agents effective at treating, preventing, or reducing the risk of developing a testosterone deficient disorder. The present invention also can also be used in conjunction with a pharmacologically effective amount of an estrogenic hormone. Furthermore, the methods, kits, combinations and compositions can be used in conjunction with a pharmacologically effective amount of another steroid or pharmaceutical agent that increases serum testosterone levels in a mammal.

Abstract: The present invention relates to methods of treating aldosterone-mediated diseases such as cardiovascular diseases in peri-menopausal or post-menopausal women by administering an agent with antimineralocorticoid and progestational activity, in particular drospirenone.

Abstract: The invention also relates to the use of active modulators of LXR&agr; activity or expression in stimulation of pre-adipocyte differentiation and hence also in the treatment of insulin resistance syndrome, or dyslipidemia, or type 2 diabetes.

Abstract: A solvent comprising a combination of water and organic solvent(s) capable of dissolving a therapeutically effective amount of medicament(s) not readily soluble in aqueous solvents, said organic solvents including alcohol and glycol, and said medicaments including hydrocortisone.

Abstract: The present invention relates to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a disorder or disease related to, or the symptoms associated with, neurotoxicity in a subject, particularly to beta-amyloid-induced neurotoxicity and Alzheimer's disease. The compounds of the present invention are biologically active 22R-hydroxycholesterol derivatives containing a common spirost-5-en-3-ol structure.

Abstract: There is provided a parenterally deliverable pharmaceutical composition comprising eplerenone and a solvent liquid having the eplerenone in solution therein. Compositions of the invention are storage stable.

Abstract: The present invention relates to a pharmaceutical composition in the form of a hydro-alcoholic gel or a solution for transdermal application, comprising:

Abstract: The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14&bgr;,15&bgr;-cyclopropane ring and a 17&agr; hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.

Abstract: Lupus erythematosus can be treated by administering therapeutic amounts of &Dgr;5-androstene-3&bgr;-ol-7,17-dione and metabolizable precursors thereof, such as &Dgr;5-androstene-3b-acetoxy-7,17-dione, which are readily metabolized in vivo to &Dgr;5-androstene-3&bgr;-ol-7,17-dione but are not appreciably metabolizable in vivo to androgens, estrogens or dehydroepiandrosterone. Such treatment can be prophylactic, ameliorative or curative in nature.

Abstract: The present invention is directed to a method for preventing an increase in matrix metalloproteinase (MMP) activity or reducing MMP activity in a subject in need thereof by administering to the subject a therapeutically effective amount of a selective aldosterone blocker. More particularly, the present invention is directed to attenuating or preventing an increase in MMP activity comprising administering eplerenone, or derivatives thereof.

Abstract: The present invention provides methods for treating inflammatory conditions, including but not limited to, inflammatory bowel disease (ulcerative colitis, Crohn's disease, and proctitis), other noninfectious, inflammatory conditions of the GI tract (microscopic colitis, allergic eosinophilic gastroenteritis, food allergies, pill induced esophagitis, celiac disease, recurrent polyps, and hemorrhoids), and psoriasis, using progesterone or progesterone analogs such as medroxyprogesterone acetate.

Abstract: The present invention concerns the combination of dehydroepiandrosterone (DHEA) and at least one aromatase inhibitor and the use of such a combination to produce a medicament for treating relative and/or absolute androgen deficiency in men. Selective aromatase inhibitors such as atamestan, formestan, pentrozol, aramidex, fadrozol, CGS 20267 and/or vorozol, are preferred for producing the medicament according to the invention.