Abstract: The invention describes a method of preparing lipid compositions by associating pH sensitive compounds which maybe weak acids, bases or amphoteric compounds with at least one ionisable or pH sensitive group and low water solubility into preformed and standardised lipid particles by pH manipulation. Drug association is carried out in situ by changing the pH of the aqueous medium to pH 6-8 wherein the compound spontaneously partitions into the lipid particles. Drug association may also be carried out by exploiting pH changes in the GI tract. The lipophilic compound is solubilised by the lipid particles and may be used as such for in-vitro and pharmacokinetic assessments or processed for oral, parenteral or topical therapy.

Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.

Abstract: The present invention is directed to solvates and various polymorphic forms of (E)-1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione dihydrochloride and pharmaceutical compositions thereof.

Abstract: We disclose a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such as SCS in the presence of an adrenal incidentaloma.

Abstract: Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Abstract: A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death.

Abstract: A tissue adhesive including cyanoacrylate and polyethylene glycol (PEG), wherein the PEG remains a polyether and wherein the tissue adhesive is bioabsorbable. A tissue adhesive including cyanoacrylate bulk monomer and cyanoacrylate nanoparticles containing a therapeutic therein. A kit for applying a tissue adhesive, including the tissue adhesive described above and an applicator. Methods of accelerating degradation of a cyanoacrylate tissue adhesive applying a tissue adhesive, closing an internal wound, administering a therapeutic to tissue, treating cancer, and preventing infection in a wound. Methods of method of making a bioabsorbable tissue adhesive and making a therapeutic tissue adhesive.

Abstract: Formulations of sparingly water-soluble active ingredientscomprising carrier particles provided with active ingredient-containing coatings, the sparingly soluble active ingredients being embedded in coatings composed of amphiphilic copolymers, and the coatings being applied in the form of a solvent-free melt.

Abstract: The present invention has as its objective to provide mucoadherent compositions with enhanced properties of bioadhesivity, consistency, stability and vaginal pH regulation. It can also be the carrier of an active principle for the treatment or prophylaxis of disturbances or diseases caused in mucosa, particularly in the vaginal tract, as well as their use.

Abstract: Disclosed are a method for preparing a powder containing a nanoparticulated sparingly soluble drug, a powder prepared thereby, and a pharmaceutical composition containing the same. The disclosed method includes: providing a uniformly dispersed solution of a sparingly soluble drug which is formed into nanoparticles in the presence of a surface stabilizer; mixing the uniformly dispersed solution with a water-soluble dispersant solution; and drying the mixed solution to obtain the powder. When the powder containing the nanoparticulated sparingly soluble drug obtained by the disclosed method is redispersed in an aqueous solution, the sparingly soluble drug retains a particle size in the nano scale while the solubility and the dissolution rate of the drug are increased, thereby providing enhanced bioavailability. Consequently, the present disclosure can be useful in the development of preparations of a sparingly soluble drug for oral or parenteral administration.

Abstract: The present invention relates to a novel technology for forming fine particles with a size of 0.02˜3 microns from a solid that can be dissolved in a liquid solvent and is not decomposed by heat. The particle preparation technology according to the present invention may be applicable to the fields of food, cosmetics, biopolymer, polymer compositions, and pharmaceuticals.

Abstract: The present invention is directed to new nanosuspensions of antifungal azole derivatives, particularly itraconazole, with with improved impurity profile optimized for inhaled administration for the prevention, reversal and medical treatment of fungal infections of the respiratory tract including adjacent lymph nodes. The new formulation which is devoid of particulate inorganic contamination can be safely administered by inhalation. This administration route results in an improved therapeutic effect and reduced side effect profile as compared to the previously used clinical administration route, i.e. oral or parenteral (intravenous) administration.

Abstract: The present invention provides a composition and method of forming an amorphous drug-loaded particle by forming one or more amorphous drug-loaded nanoparticles comprising one or more active agents stabilized by one or more polymers, desolvating the one or more amorphous drug-loaded nanoparticles to form one or more flocculated amorphous drug-loaded nanoparticles, filtering the one or more flocculated amorphous drug-loaded nanoparticles and drying the one or more flocculated amorphous drug-loaded nanoparticles to form amorphous drug-loaded particles.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: The present invention relates to therapeutic combinations and kits useful in treating CFTR-related diseases, such as cystic fibrosis.

Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.

Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.

Abstract: The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a base anti-inflammatory agent, such as indometacin; one or more optional active ingredients selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol™, L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR-?) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g.

Abstract: The present application provides novel compositions comprising posaconazole and a polymer wherein the composition has a glass transition temperature (Tg) of less than about 1100 C. The application also describes compositions comprising posaconazole and a polymer having a bulk density of greater than about 0.4 mg/mL. The application also describes compositions comprising posaconazole and a polymer which provide an exposure (AUCtf) of at least about 10,000 ng·hr/mL when administered to a patient in a fasted state. The application also describes a novel process for preparing these compositions. The preff erred polymer is HPMCAS. Preferably the composition is an extruded material.

Abstract: The present invention relates to a pharmaceutical composition comprising crystalline form Y of posaconazole. The pharmaceutical composition can be used to treat or prevent fungal infections.

Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.

Abstract: There is provided a pharmaceutical composition comprising an antimycotic agent and an antiviral agent, useful for prophylaxis and/or treatment of an associated infection and/or disease and a method of manufacturing thereof.

Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: The present invention provides methods and compositions for increasing the rate of nail growth in mammals, especially humans, using thyromimetic compounds.

Abstract: The invention describes a new class of crystalline silica material having two levels of porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners, edges or faces following patterns imposed by interaction with cationic surfactant or triblock copolymer molecules. After evacuation of these molecules, microporosity is obtained inside the nanoslabs, and a precise mesoporosity between the nanoslabs depending on the tiling pattern of the zeolite nanoslabs, as evidenced by X-ray diffraction. These materials are useful for the fixation of biologically active species, such as poorly soluble drugs.

Abstract: A topical treatment for onychomycosis and Tinea pedis comprising a delivery system further comprising at least one hydroxy acid agent having a pH-pKa value of 0.5 or greater and at least one antifungal agent formulated into creams, lotions, gels, sprays, foams, pads, films, patches, and solutions.

Abstract: The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.

Abstract: A topical treatment for skin disorders and diseases comprising a combination of at least one antifungal agent and at least one hydroxy acid agent having a pH?pKa value of 0.5 or more formulated into shampoos, creams, lotions, gels, sprays, foams, pads, films, patches, and solutions for treatment of skin disorders and diseases in both humans and animals.

Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

Abstract: An antifungal product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antifungal product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: Disclosed herein are methods of using metaxalone. In one embodiment, the method comprises determining that a patient in need metaxalone therapy is taking a substance that is a n inhibitor or an inducer of a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4, and adjusting administration to the patient of metaxalone or the substance to avoid an adverse event associated with metaxalone. In another embodiment, the method comprises informing a user that metaxalone is metabolized by a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4. Also included are articles of manufacture comprising a container containing a dosage form of metaxalone, wherein the container is associated with published material informing that metaxalone affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a metaxalone product.

Abstract: The present invention relates to crystalline form IV of posaconazole and pharmaceutical compositions comprising the same. The pharmaceutical composition can be used to treat or prevent fungal infections.

Abstract: The present invention relates generally to use of a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer), such as Kollicoat IR, in the formulation of solid dispersions of low aqueous solubility and dissolution rate bioactive compound and, more particularly to a system and method for improving the solubility and dissolution rate of such low aqueous solubility and dissolution rate bioactive compound, in particular the drug of low aqueous solubility, such as a BCS Class II or Class IV drug compounds.

Abstract: The present invention concerns an intermittent dosing regimen for the treatment of obesity or the reduction of body weight wherein a pharmaceutical composition containing an apoB secretion/MTP inhibitor is administered to a subject in need thereof for a period of time, then withheld for a period of time, and again administered for a period of time. The intermittent regimen may be repeated depending on the response in the subject that is being sought.

Abstract: The present invention relates to a pharmaceutical formulation comprising a pharmaceutically activeagent; water; a polyethylene glycol or a poloxamer; and a polyethylene glycol mono- or di-ether. Preferably the pharmaceutically active agent is an anti-fungal or anti-mycotic agent. Preferably the pharmaceutically active agent is lipophilic and/or keratinophilic. The present invention also relates to the use of the formulation in treating diseases, disorders or pathological conditions of the nail or skin, such as onychomycosis, dermatomycosis and other mycoses. The present invention also relates to a method of administering a pharmaceutically active agent to a subject by applying the formulation comprising the pharmaceutically active agent to a nail or skin of the subject. The present invention further relates to a method of preparing the formulation.

Abstract: Methods for diagnosing, treating, and preventing catabolism-related vitamin D deficiency and related disorders; related compositions, apparatus and kits, are disclosed. A method involves measuring CYP24 expression and/or activity, or a proxy thereof such as FGF23 level, in a patient and correlating abnormally elevated CYP24 expression and/or activity with catabolism-related vitamin D deficiency or with susceptibility for catabolism-related vitamin D deficiency. In response to abnormally elevated CYP24 expression and/or activity, the method further includes administering a CYP24 inhibitor to the vitamin D deficient or at-risk patient, and preferably avoiding activation of the vitamin D binding receptor, such as by avoiding administration of active vitamin D compounds to such patients. Optionally, a vitamin D prohormone or prohormone can be administered.

Abstract: Several diterpene glycosides (e.g., rubusoside, rebaudioside, steviol monoside and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, and celecoxib. The use of the diterpene glycoside rubusoside increased solubility in all tested compounds. The diterpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries. Aqueous solutions by using rubusoside to increase the solubility of otherwise insoluble drugs will have several new routes of administration. In addition, aqueous solutions of therapeutic compounds with rubusoside were shown to retain the known pharmacological activity of the compounds.

Abstract: The present invention provides a solid molecularly dispersed composition comprising a poorly water soluble and weakly basic azole antifungal compound and a pH sensitive polymer, pharmaceutical compositions, comprising the solid molecularly dispersed composition of the invention and methods of treating and/or preventing a fungal infection in a patient in need thereof comprising orally administering a pharmaceutical composition comprising a composition of the invention to a patient in need thereof. Preferably the antifungal, compound is posaconazole, and the pH sensitive polymer is HPMCAS.

Abstract: Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: Described herein are methods of inhibiting IMPDH type 1, and treating or preventing a disease or disorder (or symptoms thereof) associated with IMPDH type 1, wherein an IMPDH type 1 inhibitor compound is administered to a subject.

Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.

Abstract: The invention provides a compound of formula I: wherein R1-R6, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of MAO-B enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

Abstract: The present invention provides methods of increasing an amount of a treatment agent in the body, a cancer or tumor. The methods include administering an inhibitor of the metabolic degradation or conversion of the treatment agent to a subject undergoing treatment for a hyperproliferative disorder with said treatment agent. Methods of treating hyperproliferative disorders, tumors and cancers are also provided.

Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R , such as obesity, and diabetes.

Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: Pharmaceutical compositions comprising the 2S,4R ketoconazole enantiomer or its pharmaceutically acceptable salts, hydrates, and solvates, that are substantially free of the 2R,4S ketoconazole enantiomer are useful to reduce testosterone synthesis and for the treatment of prostate cancer, benign prostatic hyperplasia, seborrhea, hirsutism, alopecia, polycystic ovary syndrome, and other diseases and conditions, including but not limited to systemic hyperandrogenism.

Abstract: [Object] It is to provide a novel LXR? agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C?O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.

Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R6, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.