Abstract: The present invention relates to a compound of formula (I) for its use for reversing or inhibiting multidrug resistance.

Abstract: Nuclear receptor LXR is an important member of 49 nuclear receptors in human bodies and has irreplaceable regulatory effects on cholesterol and fat metabolisms. The regulation of the biological activity of LXR may have therapeutic effects to the conditions such as cardiovascular and cerebrovascular obstructions, non-insulin dependent hyperglycemia, immune function disorders, and central nerve functional degeneration. We have developed a group of novel Chinese materia medica preparations targeting nuclear receptor LXR by using a computer-simulated docking technology and a process for determining biological activities of human cells cultured ex vivo. The group of preparations are featured by simple ingredients, low costs, easy to prepare, etc. No significant adverse effects were found in initial acute toxicology analysis which was carried out using mice.

Abstract: Methods of treatment of diseases that include or are characterized by inappropriate or pathological neovascularization are disclosed. These diseases include diseases of the eye, such as diabetic retinopathy, retinopathy of prematurity, and choroidal neovascularization which can occur in age-related macular degeneration (AMD). Disclosed methods include administering agents that cause directly or indirectly upregulation of the ABCA1 transporter protein in macrophages. These agents include, without limitation, LXR agonists. In some embodiments, inhibitors of CETP expression or activity can also be effective. Administration routes can include, without limitation, intraocular, periocular, or systemic administration.

Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X, and Y are as described herein. Compounds of the present invention are useful for the treatment of HIV-1.

Abstract: This invention relates to the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the prevention or treatment of stress induced hair loss.

Abstract: Disclosed is a cucurbitane-triterpenoid compound for activating estrogen receptor activity, and a pharmaceutical composition, use and preparation method thereof. The cucurbitane-triterpenoid compound is presented as formula (I): wherein a single bond or a double bond is formed between C5 and C10, and a single bond or a double bond is fromed between C8 and C9; when a single bond is formed between C5 and C10, the R1 is oxygen; while a single bond is formed between C8 and C9, R2 is carbonyl group (—C?O), methyl hydroxyl group (—CH(OH)), methyl ketone or methyl dimethoxy group (—CH(OCH3)2); and wherein while R1 is oxygen (—O—) and R2 is carbonyl group (—C?O) or methyl hydroxyl group (—CH(OH)), a single bond is formed between R1 (—O—) and C19 of R2 such that R1 and R2 are formed tetrahydro-2H-pyran-2-one or hemiacetal ring.

Abstract: The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present disclosure inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, enhances the cortical actin ring structure, and improves the stability of the tight junctions (TJs) between vascular cells, thereby inhibiting vascular leakage. The vascular leakage inhibitor of the present disclosure has the activity of not only reducing vascular permeability but also recovering the integrity of damaged blood vessels. Accordingly, the vascular leakage inhibitor of the present disclosure can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present disclosure is synthesized from commercially available or easily synthesizable cholesterols, it has remarkably superior feasibility of commercial synthesis.

Abstract: The application provides formulations for the topical administration of an active agent comprising at least one steroid, in the form of topical sprays that are propellant-free, and/or substantially non-foaming, and/or alcohol-free. The present application also provides processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.

Abstract: A cream base for the topical application of skin care therapeutics and a process for making the cream base. In one embodiment, the therapeutic is tretinoin, hydroquinone and fluocinolone acetonide for the treatment of hyperpigmented skin conditions, such as melasma.

Abstract: A ceramide production enhancer and a moisturizer containing, as an active ingredient, an extract of at least one plant selected from the group consisting of Chenopodium hybridum, Melia toosendan, Indigofera tinctoria, Cirsium japonicum, Catalpa ovate, and Tagetes erecta, or a compound represented by the following Formula (1): wherein, R represents an acyl group having 1 to 5 carbon atom(s).

Abstract: The present invention features novel withanolides, as well as analogs and salts thereof, for use in the treatment of proliferative disease, cardiovascular disease, neurodegenerative disease and inflammatory disease.

Abstract: The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70.

Abstract: The invention includes compositions and methods for regulating PI3K p110 delta as an anti-retroviral therapy. The invention includes inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-retroviral therapeutic approach for treating a retroviral infection, for example HIV. The invention includes a method of modulating PI3K p110 delta in a cell infected with a retrovirus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K p110 delta.

Abstract: Novel pharmaceutical compositions of mometasone or a pharmaceutically acceptable derivate thereof in the form of an oil-in-water emulsion, notably a cream. The composition has excellent stability and therapeutic effect. The compositions contain mometasone in micronised form, propylene glycol and water and the weight ratio between the propylene glycol and water contained in the oil-in-water emulsion is from 1:1 to about 1:3.

Abstract: The invention provides methods for decreasing or inhibiting herpesviridae (HV) infection or pathogenesis of a cell in vitro, ex vivo or in vivo, a symptom or pathology associated with a herpesviridae (HV) infection or pathogenesis in vitro, ex vivo or in vivo, or an adverse side effect of herpesviridae (HV) infection or pathogenesis in vitro, ex vivo or in vivo. In one embodiment, a method of the invention includes treating a subject with an invention compound (e.g., cationic steroid antimicrobial or CSA).

Abstract: There is provided a method of treatment of allergic rhinitis which comprises administering to a patient a pharmaceutically acceptable amount of a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I) or a solvate thereof, wherein the administration is once-per-day and intranasal, and the total daily dose of the compound (I) is 50 to 100 ?g.

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: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.

Abstract: The potency of a topical corticosteroid in a pharmaceutical formulation is maintained even when the concentration of the corticosteroid is substantially reduced by providing the corticosteroid in a formulation containing a liquid oil component that includes a dicarboxylic acid ester and/or a monocarboxylic acid ester.

Abstract: Novel pharmaceutical compositions of mometasone or a pharmaceutically acceptable derivate thereof in the form of an oil-in-water emulsion, notably a cream. The composition has excellent stability and therapeutic effect. The compositions contain mometasone in micronised form, butylene glycol and water and the weight ratio between the butylene glycol and water contained in the oil-in-water emulsion is from 1:1 to about 1:3.

Abstract: The present invention is directed to mometasone furoate compositions comprising mometasone furoate and at least one surface stabilizer. The mometasone furoate particles of the composition preferably have an effective average particle size of less than about 2000 nm.

Abstract: A medicinal composition includes an active medicinal substance in therapeutic dose and a potentiated medicinal preparation produced from the substance by homeopathis methods.

Abstract: Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are ophthalmic formulations that deliver a variety of therapeutic agents, including but not limited to rapamycin (sirolimus), analogs thereof (rapalogs) or other mTOR inhibitors, to a subject for an extended period of time. The ophthalmic formulations may be placed in an aqueous medium of a subject, including but not limited to intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer a therapeutic agent to treat or prevent age-related macular degeneration, macular edema, diabetic retinopathy, uveitis, dry eye, or a hyperpermeability disease in a subject.

Abstract: 16?,17?-Epoxy-10?-hydroxyestr-4-en-3-one is useful in the treatment of hot flashes by vomeronasal administration.

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: Several embodiments of the present invention provide for an agglomerate useful for an agglomerate based dry powder inhaler comprising at least one active pharmaceutical agent, at least one additional functional excipient and at least one excipient, such as a binder. Useful at least one additional functional excipients include but are not limited to magnesium stearate, colloidal silica, silicon dioxide, sucrose stearate, L-leucine and combinations thereof.

Abstract: Provided are polymorphs of fluticasone furoate and processes for preparation thereof.

Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.

Abstract: Ophthalmically therapeutic materials, such as liquid-containing compositions and polymeric drug delivery systems, include a therapeutic component that includes an Glucocorticoid Derivative which, upon delivery to the posterior segment of a mammalian eye, does not significantly diffuse to the anterior segment of said eye. Methods of making and using the present materials are also described.

Abstract: The present invention relates to method for the treatment of allergic rhinitis comprising: administrating to a patient in need thereof a pharmaceutical formulation comprising a compound for formula (I) or a salt thereof, and an anti-inflammatory glucocorticoid compound of formula (II) or a solvate thereof.

Abstract: There are provided crystalline particles of unsolvated Form 1 polymorph of the compound of formula (I): characterised in that the particles are in the form of substantially triangular plates.

Abstract: The present invention relates to a composition for treating skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and a corticosteroid. It discloses a composition for treating skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) an active pharmaceutical ingredient (API) composition in the form of mometasone furoate, used in treating skin inflammation c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, and a corticosteroid in the form of mometasone furoate, are incorporated in cream base for use in treating skin inflammation due to allergy & itching & wounds on human skin involving contacting human skin with the above identified composition.

Abstract: Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure.

Abstract: This invention relates to steroidal solutions for the preparation of medicaments and drug products useful for treating diseases of the upper and lower airway passages. Various embodiments of the present invention provide compositions, compositions and dosage forms with mometasone furoate in a dissolved state that are suitable for inhalation and can be used for the treatment of diseases of the upper and/or lower airway passages.

Abstract: A method of treating an ophthalmic condition or disease by administering a compound disclosed herein is provided. The compound can be administered systemically or locally and in a variety of ways, such as via a temporary device, an implant, an injection or an eye drop. The compound can also be administered with an additional therapeutic agent.

Abstract: Known or suspected traumatic brain injuries may be treated therapeutically by administering a therapeutically effective dose of resibufogenin. A preferred method for determining if a patient has a traumatic brain injury includes obtaining a body specimen from the patient, determining the concentration of marinobufagenin in the body specimen, comparing the concentration of marinobufagenin to the concentration in such body specimens in normal patients, and if the marinobufagenin concentration is substantially above the concentration of a normal patient, concluding traumatic brain injury exists. In a preferred embodiment, a substantial elevation is deemed to be an increase of about 30 percent above the marinobufagenin concentration of a normal patient. The body specimen may be blood, urine, or cerebrospinal fluid.

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

Abstract: Method and compositions for reducing the inflammation after cytokine exposure of an islet cell transplant without affecting the viability and potency are disclosed herein. The present invention describes a composition comprising Withaferin A (WA), a steroidal lactone derived from Withania somnifera to effectively block NF-kB activation in beta cells, minimize cytokine-induced cell death and improve survival of transplanted islets. The method of the present invention involves identifying a subject having islet cells in need of treatment; and providing a effective amount of a Withaferin A composition disposed in a pharmaceutically acceptable carrier in an amount sufficient to reduce the inflammation after cytokine exposure without affecting the viability and potency of the islet cell population.

Abstract: The present disclosure relates generally to compositions for cosmetic or pharmaceutical application. The compositions include a carrier and rheology modulators.

Abstract: A medication or combination of medications for the treatment of a disease involving the sinuses is incorporated into a sterile medical gel. The viscosity of the gel or the adhesion of the gel to the patient's sinus cavity allows the gel to be maintained in the cavity for a sufficient length of time for treatment of the affected area. This reduces the amount of wasted medication that would otherwise result from other topical methods.

Abstract: A method of preventing preeclampsia including administering to a patient during an early stage of pregnancy a prophylactically-effective amount of resibufogenin. The administration of resibufogenin is periodically repeated. The method serves to prevent hypertension, proteinuria, and intrauterine growth restriction.

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v 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?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.

Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.

Abstract: The present invention relates to novel chemical compounds, in particular cholest-4-en-3-one oxime derivatives and to the use thereof as medicaments, especially as cytoprotective medicaments, in particular neuroprotective, cardioprotective and/or hepatoprotective medicaments.

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: Methods of inhibiting osteoclastogenesis and the activity of osteoclasts are disclosed. Methods of treating patients who have diseases characterized bone loss are disclosed. According to the methods, an amount of a TRANCE/RANK inhibitor effective to inhibit osteoclastogenesis is administered to the patient. Pharmaceutical compositions which comprise TRANCE/RANK inhibitor in an amount effective to inhibit osteoclastogenesis. Methods of modulating dendritic cell maturation, T cell proliferation, and/or CD40 receptor systems in an individual are disclosed. The methods comprise the step of administering to the individual an amount of a TRANCE/RANK inhibitor effective to modulating dendritic cell maturation, T cell proliferation, and/or CD40 receptor systems.

Abstract: The invention relates to treating chronic obstructive pulmonary disease, involving the administration by inhalation of mometasone furoate particles in daily doses where at least about 250 ?g of the inhaled particles have sizes equal to or less than 6.5 ?m.

Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.