Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.

Abstract: A method for reducing the symptoms of peripheral vascular disease and for improving peripheral circulation wherein a progestin is administered to a subject in need thereof.

Abstract: Compositions and methods of making the same for improving the bioavailability of a substantially water-insoluble pharmacologically active agent are described. The composition includes a substantially water-insoluble pharmacologically active agent, and a substantially water-insoluble matrix forming material comprising enzyme digestible or bile soluble nutrients, wherein the substantially water-insoluble pharmacologically active agent is dispersed in a solid matrix and wherein said pharmacologically active agent in said matrix is substantially free of the original crystalline form.

Abstract: Vaginal use compositions comprising pellets prepared from a debranched starch. Pellets may be conveniently prepared via extrusion/spheronization.

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: The disclosure provides methods of treating bipolar disorder by administering an antiestrogen to reduce the severity and frequency of mood episodes. The disclosure further provides methods of treating depression with an antiestrogen in a descending dose protocol.

Abstract: The invention relates to an drug delivery device and a method for delivering multiple drugs over a prolonged period of time. The drug delivery device has two or more unitary segments comprising a drug-permeable polymeric substance, wherein at least one of the segments further comprises a pharmaceutically active agent. The invention also relates to a method for the treatment of a benign ovarian secretory disorder in a female mammal, a method of contraception, and a method of relieving the symptoms associated with menopausal, perimenopausal and post-menopausal periods in a woman.

Abstract: Compositions and methods for inducing the deposition of elastin in skin by administering compositions including a mineralocorticoid, such as, for example, aldosterone and, optionally, a secondary active agent for enhancing or modulating the effect of the mineralocorticoid are described herein.

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 invention relates to novel monomers of Formula (I) useful for preparation of phase-separated biocompatible polymers or polymer compositions. These polymers or polymer compositions may be bioresorbable and/or biodegradable and have desirable mechanical properties, such as fracture and/or fatigue toughness, which have not been a primary design criteria for such polymers previously. The polymers or polymer compositions are useful in a variety of medical applications, such as in the fabrication of medical devices. Therefore, methods for preparing these polymers or polymer compositions and medical devices are also encompassed by this disclosure.

Abstract: A tablet comprising a core containing an active agent, and a coating, the core being disposed within the coating such that the coating has a thickness about a longitudinal axis (X-Y) of about 4.85 to 4.95 mm. The position of the core within the coating dictating that the active agent is released rapidly after a lag time during which time no active agent is released.

Abstract: Certain surfactants suitable for use alone to dissolve a water-insoluble component in compositions is described for providing VOC-free compressed gas aerosol compositions. The compositions include water-insoluble component(s), a surfactant and water. The water-insoluble component(s) can be active agent(s), such as fragrance(s) and/or an insecticide(s). The surfactant is present as a single surfactant which, in the absence of a solvent, dissolves or disperses the water-insoluble component(s) and provides a homogenous blend in water which provides a stable compressed gas emulsion.

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

Abstract: The invention provides a method for identifying whether a pregnant subject has an increased risk of preterm labour comprising measuring the progesterone concentration in a sample obtained from the subject, wherein a reduced progesterone concentration is indicative of an increased risk of preterm labour and delivery.

Abstract: Multi-layered vaginal rings 2 comprising silicone elastomers and pharmaceutically active ingredients are disclosed. The rings comprise a number of layers, at least one of which contains a pharmaceutically active ingredient, and each of which is a silicone elastomer. The multiple layers preferably are produced from these layers of different compositions, including an inner layer 4, a middle layer 5, and an outer layer 6. After extrusion and simultaneous curing, however, the ring 2 includes a contiguous body which comprises a continuous silicone body providing unimpeded diffusion of the pharmaceutically active ingredient from the inner layer (s) 4 to the outer layer (s) 6. Methods of producing these vaginal rings and of using them are also disclosed.

Abstract: The invention provides an analytical method for the determination of the susceptibility of a human patient suffering from breast cancer to anti-cancer treatment by providing an analytical method for determining the genetic predisposition of a patient in respect of susceptibility, e.g. responsiveness, to anti-cancer treatment, especially treatment using at least one chemotherapeutical agent and/or at least one anti-hormonal agent on the basis of analysis of a genetic marker.

Abstract: A preparation method for an ethanol extract of the fruiting body of Antrodia camphorata (EEAC) is provided. The preparation method includes steps of: (a) providing the fruiting body of A. camphorata (AC); (b) extracting the fruiting bodies with a first ethanol solution; and (c) obtaining EEAC. EEAC further can be sequentially extracted or fractioned by n-hexane, ethyl acetate and ethanol, and an n-hexane fraction (FC), an ethyl acetate fraction (FA) and an ethanol fraction (FB) respectively are generated. The growth inhibition and apoptosis induction of leukemia cell line HL 60 are effectively mediated by FA product, in which zhankuic acid A is the bioactive marker. The amount of triterpenoid in the fruiting body of AC can be determined by NMR and HPLC analysis.

Abstract: This present invention disclosed the use of mesoprogestins, a new class of progesterone receptor modulators (PRMs), for the treatment and prevention of benign hormone dependent gynecological disorders: a) for the treatment of gynecological disorder such as endometriosis, uterine fibroids, postoperative peritoneal adhesions, dysfunctional bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; b) for the prevention of gynecological disorders such as postoperative, peritoneal adhesions, dysfunctional uterine bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; and c) a method of treatment and prevention of the above mentioned disorders in a female, preferably in a human female, in need of treatment or prevention of one or more of these disorders, with an effective amount of a mesoprogestin. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo.

Abstract: A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).

Abstract: The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition.

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: Disclosed are methods that employ FKBPL as a marker for a subject's sensitivity to endocrine therapies in the treatment of cancers, and as a predictive marker of cancer progression and disease free survival in relation to hormone responsive cancers.

Abstract: Methods are disclosed for predicting a patient response to anti-Her2 therapy or anti-aromatase therapy. In certain embodiments, the methods involve the identification of low molecular weight cyclin E (LMW-E) in cancers, such as breast cancer cells, as a predictive and prognostic marker. In further embodiments, LMW-E expression by a cancerous or pre-cancerous cell may be used to predict response to an aromatase inhibitor and/or CDK2 inhibitor, and determination of LMW-E expression may be used in the personalization of cancer therapies.

Abstract: The invention relates to the use of compounds to treat a number of conditions, such as thrombocytopenia, neutropenia or the delayed effects of radiation therapy. Compounds that can be used in the invention include methyl-2,3,4-trihydroxy-1-O-(7,17-dioxoandrost-5-ene-3?-yl)-?-D-glucopyranosiduronate, 16?,3?-dihydroxy-5?-androstan-17-one or 3,7,16,17-tetrahydroxyandrost-5-ene, 3,7,16,17-tetrahydroxyandrost-4-ene, 3,7,16,17-tetrahydroxyandrost-1-ene or 3,7,16,17-tetrahydroxyandrostane that can be used in the treatment method.

Abstract: The invention involves methods and formulations for treating or preventing rhinosinusitis, including fungus-induced rhinosinusitis in mammals. In one embodiment, the formulation of the present invention comprises a steroidal anti-inflammatory agent having a specific particle size distribution profile. The formulation may also comprise an antifungal agent, antibiotic or antiviral agent.

Abstract: A multiphasic estrogenic/progestogenic contraceptive regimen that provides for the reduction or elimination of estrogen in the initial phase is disclosed. Also described is a contraceptive kit that may be used to practice the method of the invention.

Abstract: The present invention comprises novel methods for the use of compositions comprising 7-keto DHEA for treating psychiatric conditions. These methods include administering an effective amount of a composition comprising 7-keto DHEA in an acceptable carrier, alone or in combination with other psychiatric drugs, such as analgesic agents, anticonvulsants, anti-anxiety agents, antidepressants, anti-panic agents, antipsychotic agents, bipolar agents, psychostimulants to reduce or ameliorate symptoms of a psychiatric condition. This method may be used alone or as an adjunctive treatment for treating a wide variety of psychiatric conditions such as stress disorders, anxiety disorders and depressive disorders.

Abstract: There is provided a hemihydrate of (3?,5?,7?,12?)-7,12-dihydroxy-3-{2-[{4-[17?-hydroxy-3-oxo-17?-prop-1-ynylestra-4,9-dien-11?-yl]phenyl}(methyl)amino]ethoxy}cholan-24-oic acid in a crystalline form which is characterised by an X-ray diffraction pattern having major peaks at 2?=6.58±0.2, 8.54+0.2, 12.28±0.2, and 19.68±0.2. This crystalline material is useful in the treatment of conditions associated with an excess of hepatic glucocorticoid response.

Abstract: Disclosed herein are compositions and methods of identifying a subject at risk for preterm birth and selecting effective therapies for preventing preterm birth in the subject. The disclosed methods generally involve determining the identity of one or more nucleotides in the progesterone receptor (PR) gene of the subject.

Abstract: Methods for commercial production of transdermal formulations comprising a hormone compound are provided. In particular, methods for commercial scale production under an inert atmosphere of a transdermal formulation comprising a therapeutically effective amount of a hormone, preferably a testosterone compound, useful for the treatment of hypoactive sexual desire disorder (HSDD) in postmenopausal women are provided.

Abstract: The present invention comprises systems, methods and devices for the delivery of visualizable or treatment compositions or therapeutic agents comprising device elements for diagnosis and/or treatment of conduits. A delivery system comprising an introducer shaft having at least one exit port and at least one delivery catheter for placement of compositions into the conduit, such as a fallopian tube.

Abstract: Steroid compounds possessing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: A dosage form for hormonal contraception containing a specific number of gestagen-containing daily units A and a specific number of gestagen-containing daily units B for uninterrupted, daily, oral administration of daily units A and then immediately subsequently of daily units B, wherein the daily units A in each case contain at most 200 ?g of folic acid and the daily units B contain >200 ?g up to the maximum permissible amount of folic acid for women.

Abstract: The present invention relates to formulations of a pharmacological effective fat-soluble active ingredient with a high bioavailability of said fat-soluble active ingredient as well as to their manufacture and use as dietary supplement, food, feed, personal care product and/or pharmaceutical. Such formulations are those which when dissolved, dispersed or diluted in/with water have an extinction E1/1 at a wavelength in the range of from 200 to 800 nm, preferably in the range of from 250 to 600 nm, more preferably in the range of from 250 to 500 nm, more preferably in the range of from 370 to 485 nm, of ?380, preferably of ?600, most preferably ?900. In preferred embodiments of the formulations of the present invention such formulations show an extrusion loss of fat-soluble active ingredient of ?30% when pressed to tablets.

Abstract: Disclosed herein is a non-human animal model of protein aggregation cardiomyopathy. Also disclosed are compo-sitions and methods of treating or preventing a condition in a subject caused or exacerbated by reductive stress. Also disclosed are compositions and methods of predicting, detecting, or monitoring reductive stress in a subject.

Abstract: The present invention is directed to specific chromosomal rearrangements that are associated with prostate tumors that respond to compounds acting at estrogen receptors. Patients having the TMPRSS2-ERG fusion, may be treated with agonists of the estrogen beta receptor or antagonists of the estrogen alpha receptor.

Abstract: The present invention provides compositions comprising an effective amount of xanthohumol and honokiol. The present invention comprises compositions comprising an effective amount of xanthohumol and genistein. The present invention comprises compositions comprising an effective amount of xanthohumol and guggulsterone. The compositions of the present invention may be effective to decrease mature adipocytes viability, induce apoptosis of mature adipocytes, increase lipolysis in mature adipocytes, and/or reduce adipogenesis during the maturation of pre-adipocytes. The present invention further provides methods of treating obesity, diabetes, osteoporosis or bone disorders in a subject, which comprise administering to the subject compositions comprising an effective amount of xanthohumol and honokiol, guggulsterone, or genistein.

Abstract: A method for breeding bovines, especially a method for breeding dairy and beef cattle without use of heat detection prior to insemination or embryo implantation.

Abstract: The subject invention pertains to the treatment of tumors and cancerous tissues and the prevention of tumorigenesis and malignant transformation through the modulation of JAK/STAT3 intracellular signaling. The subject invention concerns pharmaceutical compositions containing cucurbitacin I, or a pharmaceutically acceptable salt or analog thereof. Another aspect of the invention concerns methods of inhibiting the growth of a tumor by administering a cucurbitacin I, or a pharmaceutically acceptable salt or analog thereof, to a patient, wherein the tumor is characterized by the constitutive activation of the JAK/STAT3 intracellular signaling pathway. The present invention further pertains to methods of moderating the JAK and/or STAT3 signaling pathways in vitro or in vivo using cucurbitacin I, or a pharmaceutically acceptable salt or analog thereof. Another aspect of the present invention concerns a method for screening candidate compounds for JAK and/or STAT3 inhibition and anti-tumor activity.

Abstract: The present invention provides for progesterone containing pharmaceutical oral dosage forms and related methods. The oral dosage forms can each include an amount of progesterone as well as a pharmaceutically acceptable carrier. The oral dosage forms can be formulated to have at least one of the following characteristics: the oral dosage form produces an pregnane metabolite mean blood plasma level of less than about 1000 nmol/L; the oral dosage form produces an pregnane metabolites mean blood plasma level, after administration of single dose of progesterone composition, such that the ratio of pregnane metabolite level to parent progesterone level of less than 10:1; has a dissolution rate in vitro, when measure using a USP Type-1 dissolution apparatus in 900 mL of deionized water with 2.

Abstract: The present invention provides for progesterone containing pharmaceutical oral dosage forms and related methods. The oral dosage forms can each include an amount of progesterone as well as a pharmaceutically acceptable carrier. The oral dosage forms can be formulated to have at least one of the following characteristics: the oral dosage form produces an pregnane metabolite mean blood plasma level of less than about 1000 nmol/L; the oral dosage form produces an pregnane metabolites mean blood plasma level, after administration of single dose of progesterone composition, such that the ratio of pregnane metabolite level to parent progesterone level of less than 10:1; has a dissolution rate in vitro, when measure using a USP Type-1 dissolution apparatus in 900 mL of deionized water with 2.

Abstract: The present invention relates to a method of preventing or treating benign estrogen sensitive gynecological disorders in a female mammal, wherein the method comprises the administration to said female mammal of a combination of progestogen and androgen in an amount that is therapeutically effective to prevent or reduce the symptoms of these disorders. The present method is particularly suitable for preventing or treating disorders selected from the group consisting of endrometriosis, adenomyosis, uterine fibroids, dysmenorrhoea, menorrhagia and metrorrhagia. Another aspect of the invention relates to a pharmaceutical kit comprising a plurality of oral dosage units which comprise a progestogen in an amount equivalent to 3-500 ?g levonorgestrel and either 5 to 250 mg dehydroepiandrosterone or 1 to 50 mg testosterone undecanoate.

Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, R1?, R2?, R3?, and R4? are defined the same as the specification.

Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.

Abstract: The present invention relates to a antisolvent solidification process wherein a liquid medium comprising at least one organic or inorganic compound which is to be solidified is forced through a membrane into one or more antisolvents, or wherein one or more antisolvents are forced through a membrane into a liquid medium comprising at least one organic or inorganic compound which is to be solidified, yielding a composition comprising solid particles comprising said organic and/or inorganic compound(s).

Abstract: A solid pharmaceutical composition of exemestane, in particular for oral use and treatment of cancer, comprises micronized exemestane and anti-oxidant in a film-coated tablet.

Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.

Abstract: Described are sterile, ready-to-use, pharmaceutical oil-in-water emulsion compositions for parenteral administration comprising: 0.015 to 0.5% wt/vol progesterone; 0.5 to 10% wt/vol oil, wherein the oil comprises at least 85% wt./wt. triglyceride; 0.0425 to 4.1% wt/vol phospholipid; 80-99.4% wt/vol aqueous medium; wherein the composition has an osmolality in the range of 200-1000 mOsm/kg. Also described are methods of making such compositions and method of using such compositions in therapeutic or prophylactic treatment, such as treatments comprising intravenous administration of the pharmaceutical composition.

Abstract: Provided are methods of diagnosing a medical condition associated with hypersensitivity to a female reproductive hormone in a subject, with the proviso that the medical condition is not estrogen dermatitis. The method is effected by administering into a skin of the subject at least one female reproductive hormone such as estriol or estrone, and monitoring a reaction to the female reproductive hormone on the skin, wherein a presence of the reaction above a predetermined threshold is indicative of the presence of the medical condition in the subject. Also provided are methods and computing platforms for treating the medical conditions associated with the hypersensitivity to the female reproductive hormone by desensitization.

Abstract: Described are a sterile, ready-to-use, pharmaceutical oil-in water emulsion compositions for parenteral administration comprising: 0.015 to 1.2% wt/vol of progestogen; 0.5-30% wt/vol oil, wherein the oil comprises at least 85% wt/wt triglyceride; 0.0425-12.5% wt/vol phospholipid; 61.4-99.4% wt/vol aqueous medium; wherein the phospholipid is present in an amount of 6.8%-43% of the oil (wt/wt), and wherein the progestogen is present in an amount greater than or equal to 2.1 wt % of the oil. Also described are methods of making such compositions and method of using such compositions in therapeutic or prophylactic treatment, such as treatments comprising intravenous administration of the pharmaceutical composition.