Abstract: Disclosed is a novel mometasone furoate cream formulation for topical administration in a oleaginous base containing propylene glycol. This cream is a cosmetically elegant preparation of mometasone that is both stable and bioeffective.

Abstract: The present invention discloses an inhibitive effect of Na+-K+-ATPase caused by a compound selected from the group consisting of magnesium lithospermate B (MLB), isomer, prodrug, derivative, pharmaceutically acceptable salt, and a composition thereof. In this invention, the variations of Na+-K+-ATPase activity were monitored with increasing MLB concentrations, and the result shows the Na+-K+ ATPase activity is repressed by MLB. An outcome of the inhibitory effect, the function of cellular sodium/potassium lo exchanger is reduced and cellular calcium ion concentration is increased. That is, the MLB is useful for inhibiting the function of cellular Na+-K+ pump, and further brings the utility for cardiac stimulation, diuretic enhancement, heart failure curing, and so on.

Abstract: The present invention discloses an inhibitive effect of Na+—K+-ATPase caused by a compound selected from the group consisting of magnesium lithospermate B (MLB), isomer, prodrug, derivative, pharmaceutically acceptable salt, and a composition thereof. In this invention, the variations of Na+—K+-ATPase activity were monitored with increasing MLB concentrations, and the result shows the Na+—K+ ATPase activity is repressed by MLB. An outcome of the inhibitory effect, the function of cellular sodium/potassium exchanger is reduced and cellular calcium ion concentration is increased. The cerebral ischemia test exhibited MLB provides an effective repression of cell infarct. That is, the MLB is useful for inhibiting the function of cellular Na+—K+ pump, and further brings the utility for cardiac stimulation, diuretic enhancement, heart failure curing, anti-anoxia, neurocyte apoptosis protection, apoplexy prevention and treatment, and so on.

Abstract: The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula: for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-?B inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.

Abstract: A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.

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: According to one aspect of the invention, there is provided a compound of formula (I) and solvates thereof. There are also provided compositions containing the compound, processes for preparing it, and its use in therapy.

Abstract: A 19-norbufalin derivative compound of formula (I): wherein the R groups are as defined by the present specification. The compounds are Na+K?-ATPase inhibitors and can be used in the treatment of cardiac and/or vascular malfunction, renal malfunction, as digoxin antagonists, for treatment of CNS disorders and for the treatment of malignant and proliferative cell diseases.

Abstract: The present invention relates to a novel method for preparing 21-hydroxy-6,19-oxidopro-gesterone (21OH-6OP) and/or its 21-acetate, 21-propionate, 21-hemisuccinate, 21-phosphate, 21-oleate derivatives. 21OH-6OP and its ester derivatives are antiglucocorticoids for the treatment or prophyl axis of diseases associated to an excess of glucocorticoids, in particular for treating Cushing's syndrome, iatrogenic hypercortisolism or depression.

Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: The purpose of the present invention is to extract oil from the soybean material containing soybean germ as a main component, and to utilize it. The present invention relates to a method for producing a soybean material, comprising crudely crushing selected soybeans into a size of less than ½, and separating and concentrating a soybean germ fraction by means of sieving, sorting with air, separation based on the grain shape and the like, to the soybean germ fraction produced by said method, to oil prepared from the soybean material containing soybean germ as a main component, to oil containing 0.8% by weight or more of sterols' content, and to foods containing said oil.

Abstract: A method for treating or preventing ophthalmic disorders comprising the administration of one or more aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone is disclosed. The method results in a reduction of intraocular pressure which treats or prevents the ophthalmic disorders. Among the disorders are intraocular hypertension, glaucoma, low tension glaucoma, age-related macular degeneration (AMD), macular edema, and diabetic retinopathy. As glucocorticoids and mineralocorticoids also cause the retention of ions, such as sodium and potassium, where aldosterone receptors are located, aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone, also can be administered to modulate the intraocular concentration of ions. Thus, aldosterone receptor antagonists can be administered to maintain an intraocular ionic environment that is beneficial to intraocular cell survival.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: The invention is a method for balancing and maintaining Cortisol levels in humans by identifying the hormonal needs for a human, using blood tests or saliva tests to ascertain the current relationship between the DHEA, androstenedione, testosterone and androstenediol for that human, inserting the low values of each hormone level into a hormone tree, balancing the DHEA with the androstenediol and the testosterone and the androstenediol in a ratio which is normal for the particular person, modifying the inserted values individually forming modified values wherein the modified values account for a selected symptoms, changing the modified value to accommodate for sex type of an individual forming a gender accommodated value, and creating a morning and evening dose that priors an amount of bio-identical hormones to bring the gender accommodated value up to the normal ratio.

Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.

Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.

Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.

Abstract: The present invention relates to a method of treating asthma by raising the pH of the airways of an individual. The effect can be mediated directly by administering a pharmaceutically acceptable basic solution or alternatively, the effect can be mediated by enhancing the activity of glutaminase.

Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: A method for improving intracellular administration of a therapeutic agent is provided comprising: contacting cells with a compound comprising a charged derivative of a therapeutic agent having a therapeutic activity, the charged derivative being conjugated to a protein having a biological activity of being transported across a cell membrane into a cell; and having the cell transport the compound into the cell where the cell metabolizes at least a portion of the compound to form a charged metabolite product that possesses the therapeutic activity of the therapeutic agent, the charged metabolite product being less prone to being transported across the cell membrane out of the cell relative to the compound and less prone to being transported across the cell membrane out of the cell relative to the therapeutic agent.

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: According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof together with a long-acting ?2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of COPD over a period of 24 hours or more.

Abstract: The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I) as shown herein below Wherein X?OH or O or combination thereof and positioning of olefinic bonds are at 4(5); 5(6); 16(17); 17(20) or various combinations and said compounds containing at least one olefinic bond in or on their D-ring for the treatment of hyperlipidemic and hyperglycemic conditions in mammals, said method comprising administering an effective amount of the said compounds to the recipient mammals.

Abstract: There is provided a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I) or a solvate thereof.

Abstract: Disclosed is a novel mometasone furoate cream formulation for topical administration in a oleaginous base containing propylene glycol. This cream is a cosmetically elegant preparation of mometasone that is both stable and bioeffective.

Abstract: Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject.

Abstract: Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating a function of 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: There is provided a crystalline chemical composition comprising a compound of formula (I) 1

Abstract: The present invention relates to, for example, a compound of formula (X) 1

Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) 1

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The present invention relates to, for example, compounds of formula (VI) 1

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: Use of a compound of formula (I) or a 3-enol C1-4 alkanoate ester thereof in the manufacture of a medicament for the intermittent treatment of a condition of a human or non-human mammal in which sail mammal has a abnormally high serum concentration of an adrenal hormone: Wherein R1, R2, R5, and R6 are the same or different and each is hydrogen or C1 to 4? alkyl; R3 is hydrogen C1 to 4? alkyl, C1 to 4? alkenyl or C1 to 4? alkynyl; R4is hydroxy, C1 to 4? alkanoyloxy, a group of formula (II) or (III) Wherein R7 is (CH2)n, where n is an integer of from 0 to 4, R8 is hydrogen, C1 to 4? alkyl, hydroxy or NH2 and R9 and R10 are the same or different and each is hydrogen or C1 to 4? Alkyl; or R3 and R4 together are oxo, ethylenedioxy or propylenedioxy. The invention has practical benefits for the treatment of man and other animals with diseases associated with abnormal production of adrenal steroids.

Abstract: Compounds able to chelate paramagnetic metal ions and the use thereof as contrast agents in the technique known as “Magnetic Resonance Imaging” (M.R.I.).

Abstract: A method of contraception in mammalian females, which method comprises the parenteral or rectal 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) 1

Abstract: There is provided according to the invention a pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) an ester of fluticasone or a solvate thereof as medicament and (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid.

Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.

Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121 having unit cell dimensions of about 12.1±0.6 Å, 14.9±0.7 Å, and 16.2±0.8 Å when determined at either 120K or 150K.

Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P212121 having unit cell dimensions of about 7.6±0.6 Å, 12.7±0.7 Å, and 33±3 Å when determined at 120K.

Abstract: This invention provides novel compounds derived from a marine sponge, Adocia sp., that specifically modulat kinesin activity by targeting the kinesin motor domain and mimicking the activity a microtubule. The compounds act as potent anti-mitogens are useful in a wide variety of in vitro and in vivo applications.

Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.

Abstract: The present invention provides a pharmaceutical composition for application to the mucosa to be used in drug therapy comprising a water-insoluble and/or water-low soluble substance, ciclesonide, and an aqueous medium, and having an osmotic pressure of less than 290 mOsm. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to efficient and high ciclesonide retentivity and permeability to the submucosa or the blood at the mucosa.

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 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, 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 pathwaysin vitro or in vivo using cucurbitacin I, or a pharmaceutically acceptable salt or analog therof. Another aspect of the present invention concerns a method for screening candidate compoudns for JAK AND/or STAT3 inhibition and anti-tumor activity.

Abstract: According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), or a solvate thereof, together with a long-acting &bgr;2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.

Abstract: The method of treating narcotic withdrawal symptoms in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound having anti-mineralocorticoid activity sufficient to treat narcotic withdrawal symptoms.

Abstract: There is provided a pharmaceutical aerosol formulation comprising (i) a compound of formula (I) or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant; and characterized in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.