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 greater than 30% by weight of the active agent, and may be formulated as solutions, solids, semisolids, microparticles, or crystals. Methods related to the implantation and use of the biodegradable drug delivery systems for treating nail unit conditions are also described.

Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

Abstract: The present invention provides compositions and methods for inhibiting protozoan growth comprising a synergistic combination of lipid synthesis inhibitors. In addition, the invention provides compositions and methods that are useful for the treatment of protozoan infections and the identification of potential new drugs for the treatment of protozoan infections.

Abstract: This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the treatment of central nervous system disorders, such as depression, bipolar disorder, and anxiety.

Abstract: The present invention relates to the compounds of formula (I), their preparation and use as antifungal and/or antibacterial agents. where the values for R1, R2, R3, R4, R5 and A are as defined herein.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

Abstract: The present invention relates to a novel nasal formulation for nasal hygiene and to improve nasal airflow of people suffering from nasal congestion.

Abstract: The present invention relates to a novel nasal formulation for the treatment and prophylaxis of nasal congestion. When an infant is born, its nasal passages are relatively sterile, in time the nasal passages are colonized by fungi, molds and other organisms which compromise the integrity of the nasal and paranasal mucosa. The presence of these organisms elicits a mild chronic inflammatory reaction of the nasal and paranasal mucosa, in some cases leading to congestion and excess production of mucus. This chronic inflammatory process compromises the integrity of the nasal and paranasal mucosa, making it more vulnerable to binding with allergens and other invading organisms such as the rhinovirus. The purpose of this invention is to establish a treatment and prophylaxis of nasal congestion, which will control the presence of the invading organisms in the nasal and paranasal mucosa, reducing congestion as well as mucus production.

Abstract: The present invention provides a polymorphic form of itraconazole.

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: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: The invention provides novel soluble conazole crystalline forms (e.g. itraconazole, posaconazole and saperconazole) that include salts, co-crystals and related solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, these conazole crystalline forms. Methods of using such compositions for the treatment or prevention of systemic and local fungal, yeast, and dermatophyte infections are also provided.

Abstract: Disclosed are topical compositions for the treatment of microbial infections on the skin or scalp which include a polyvalent metal salt of pyrithione and include a metal ion source. Also disclosed are methods for treating microbial infections of the skin or scalp using such compositions.

Abstract: The crystalline polymorph Form I of (?)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by the formula I pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.

Abstract: A method for the ultrafiltration of an antifungal agent using a zirconium-layered ceramic ultrafilter to reduce pyrogens is disclosed.

Abstract: The present invention relates to compositions containing itraconazole with a greatly increased bioavailability and their preparation methods. More specifically, the present invention relates to compositions containing itraconazole which is a sparingly-soluble drug, fatty acid or fatty alcohol and surfactant and their preparation methods. Compositions according to the present invention act as Self-MicroEmulsifying Drug Delivery System(SMEDDS) wherein itraconazole which is a sparingly-soluble drug is dissolved and dispersed to form a mocoidal phase, and the mocoidal phase is dissolved in water to form microemulsion. And because of increased dissolution property and increased bioavailability, compositions according to the present invention show equal efficacy using less amount than commercial pharmaceutical preparations such as sporanox capsule and are cheaper rather than the commercial pharmaceutical preparations such as sporanox capsule.

Abstract: The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of an integrin antagonist and an antineoplastic agent.

Abstract: Disclosed are pharmaceutical preparations for use in the therapeutical and prophylactic treatment of bacterial and parasitic infections, especially malaria. The preparations contain as active substances 3-N-formyl-hydroxylaminopropyl phosphonic acid derivatives or 3-N-acetylhydroxylaminopropyl phosphonic acid derivatives and may be combined with other pharmaceutical active agents and/or other pharmaceutically acceptable excipients. Also disclosed are methods of treatments using such preparations.

Abstract: A composition is disclosed for treating a patient suffering from abnormally high acidity in the vagina, wherein the vaginal pH value is lower than 4.0. The composition consists essentially of: (a) an effective amount of the following amino acids and/or physiologically acceptable salts thereof: glutamic acid, aspartic acid, isoleucine, phenylalanine and praline; (b) an effective amount of anti-fungi drugs; and (c) a sufficient amount of pharmaceutically acceptable acid or alkali, which results in a pH of the composition from 4.0-8.0; (d). One or more pharmaceutical carriers is used for the composition. The composition is particularly useful for treating vaginitis and fungal vaginitis associated with abnormally high vaginal acidity of a pH value less than 4.0.

Abstract: The crystalline polymorph Form I of (−)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by the formula I 1

Abstract: A method of treating and/or providing prophylaxis against a pulmonary fungal infection comprises delivering an aerosolized pharmaceutical formulation comprising an antifungal agent to the lungs. The method comprises determining the minimum inhibitory concentration of the antifungal agent for inhibiting pulmonary fungal growth. A sufficient amount of the pharmaceutical formulation is administered to maintain for a period of time a target antifungal agent lung concentration that is greater than the determined minimum inhibitory concentration. In one version, the antifungal agent is amphotericin B.

Abstract: The treatment of ungual and subungual diseases is disclosed.

Abstract: An improved method for using a NNRTI in the treatment of HIV-1 infection, comprising administering to a human, needing treatment for HIV-1 infection, a therapeutically effective amount of said NNRTI or a pharmaceutically acceptable salt thereof, and an amount of an inhibitor of the cytochromes P450 that is sufficient to elevate, enhance, or extend plasma concentrations of said NNRTI.

Abstract: The present invention relates to a pharmaceutical composition for reducing vaginal acidity, treating abnormal enhancement of vaginal acidity, and high acidity vaginitis associated with abnormal enhancement of vaginal acidity, especially for the treatment of fungal vaginitis, comprising of one or more ingredients defined as follows: amino acids, physiologically acceptable salts of amino acids, oligopeptides and polypeptides. Also, the present invention relates to the use of the said amino acids, physiologically acceptable salts of amino acids, oligopeptides and polypeptides, as active ingredients or auxiliaries in preparing drugs for reducing vaginal acidity, the treatment of abnormal enhancement of vaginal acidity, and high acidity vaginitis especially to their use in preparing drugs for the treatment of fungal vaginitis and the use thereof as nutrients for vaginal mucous membranes in preparing drugs that are locally applied in the vagina.

Abstract: A method of treating onychomycosis is described which includes administration of a topical formulation containing an effective amount of urea and an antioxidant to an infected area around a nail of a patient.

Abstract: Compounds of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.

Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:50).

Abstract: A method of manufacturing an itraconazole oral dosage from that is substantially free of residual methylene chloride comprises the steps of: (a) providing a working solution comprising an alcohol, a strong acid (preferably an inorganic acid or organic sulphonic acid), itraconazole, a water-soluble polymer, and water, with the itraconazole and the strong acid preferably present in the working solution in a ratio of 1 Mole itraconazole to 1-3 Moles acid; (b) providing particles formed from a pharmaceutically acceptable core material; (c) combining the working solution with the particles to produce itraconazole-coated particles; (d) drying the itraconazole-coated particles; and(e) forming the dried itraconazole-coated particles into an itraconazole oral dosage form that is substantially free of residual methylene chloride. The products of such methods and methods of use thereof are also disclosed.

Abstract: The present invention relates to a pharmaceutical formulation for stimulating the growth of gram-positive bacilli and increasing the acidity in the vagina which comprises sucrose and/to maltose, to the use of certain sucrose and/or maltose, in preparing the pharmaceutical formulation for stimulating the growth of gram-positive bacilli and increasing the acidity in the vagina, in particular to a method of stimulating the growth of gram-positive bacilli and increasing the acidity in the vagina, treating the reduction of gram-positive bacilli and the lowness of acidity in vagina as well as the vaginitis and the disturbance of vaginal bacterioflora accompanying the reduction of gram-positive bacilli, especially bacterial vaginal disease.

Abstract: Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the following structure: 1

Abstract: Disclosed herein are novel compositions and/or formulations containing minoxidil as an active ingredient in combination with other active agents and/or enhancer agents (e.g., saw palmetto extract and nettle root extract) which increase the hair growth capability of the composition. Also disclosed are methods of using the novel compositions to treat male patterned baldness and to stimulate hair growth on the scalp, including both the apex and frontal regions of the scalp.

Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I: 1

Abstract: A composition comprising itraconazole and an organic acid and the use of such composition in the production of pharmaceutical compositions comprising itryconazole as an active ingredient.

Abstract: The invention provides an itraconazole composition comprising itraconazole dispersed in a hydrophilic polymer, and, optionally, a surfactant, having a dissolution at 30 minutes between 10 and 40%, at 45 minutes between 25 and 80%, at 60 minutes between 60 and 95%, at 90 minutes at least 80%, as measured using the type II paddle method at 100 rpm according to the US Pharmacopoeia, in a dissolution medium comprised of 1000 ml HCl 0.1N. The invention also provides a process for manufacturing this composition.

Abstract: The present invention is concerned with pellets comprising a 710-1180 &mgr;m (16-25 mesh) sugar core, a coating film of a water-soluble polymer and an antifungal agent, and a seal coating layer wherein the residual concentration of dichloromethane is below 600 ppm; pharmaceutical dosage forms comprising said pellets and a method of preparing said pellets.

Abstract: The present invention provides a topical drug delivery system which comprises: a therapeutically effective amount of an antifungal agent; at least one dermal penetration enhancer, which is a safe skin-tolerant ester sunscreen ester; and a volatile liquid. The invention also provides a method for administering at least one systemic acting antifungal agent to an animal which comprises applying an effective amount of the antifungal agent in the form of the drug delivery system of the present invention.

Abstract: The present invention provides therapeutic targets for antifungal treatment, especially CIK1.

Abstract: The invention concerns the use of ketoconazole and derivatives having a corresponding biological activity, and combinations thereof, in the treatment of abdominal obesity, hypertension, hyperinsulinemia, and elevated blood lipids.

Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.

Abstract: A pharmaceutical composition suitable for topical application comprising ketoconazole in a solutio9n which comprises: (i) 13 to 50 wt % water; (ii) 45 to 85 wt % of an alcohol having a boiling point of less than 100° C.; and (iii) 2 to 30 wt % fo a non-volatile, water miscible, non-ionic surface active agent; the ketoconazole being present in an amount of 0.5 to 3 st % relative to components (i), (ii) and (iii).

Abstract: The crystalline polymorph Form I of (−)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by the formula I pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

Abstract: Methods of treating or preventing fungal infections in humans of 12 years and older in need of such treating or preventing which comprises orally administering an effective amount of posaconazole in divided doses two to four times a day to produce an arithmetic mean steady state average maximum plasma concentration of posaconazole of at least about 300 ng/mL to at least about 500.

Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.

Abstract: The present invention relates to the use of agents active againstcandida for the prevention and/or treatment of some specific disorders of the oral and intestinal mucosa, in particular the use ofLactobacilli active and/or activated against Candida for the prevention and/or treatment of ulcerative colitis, Crohn's disease and oral aphthas; the invention also relates to pharmaceutical compositions and kits for the sequential administration of the activeagents.

Abstract: This invention relates to compositions and methods for treating vaginal infections whereby the patient administers, intravaginally, a volume of semisolid treatment composition, this volume being not greater than 4.7 milliliters, preferably not greater than 4.4 milliliters and more preferably not great than 4 milliliters.

Abstract: This invention relates to a method of treating mucositis, and in particular fungal sinusitis in mammals, using oral medication, including azole antifungal agents such as, for example fluconazole and voriconazole, and with proton pump inhibitors such as esomeprazole.

Abstract: A solid dosage form for application in the oral cavity, comprising a poorly bioavailable pharmaceutical active ingredient dispersed in a pharmaceutically acceptable matrix.

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. The compounds precipitate in aqueous environments. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a period of up to 15 days or even longer.

Abstract: The present application is directed to compounds having the general formula: and to the use of these compounds in therapeutic methods.