Abstract: This invention relates to an oramucosal pharmaceutical dosage form in the form of a wafer. The wafer comprises a porous, hydroscopic, muco-adhesive polymeric matrix with at least one desired pharmaceutically active compound added thereto. The polymer is selected from a number of polymers having different dissolution rates and, in use when taken orally, the matrix adheres to an oramucosal surface to dissolve over a predetermined period of time to release the pharmaceutically active compound. The invention also extends to a method of manufacturing an oramucosal pharmaceutical dosage form in the form of a wafer which involves freeze drying or lyophilisation.

Abstract: The instant invention describes an anti-biofouling structure for placement onto structures or surfaces that are exposed to aquatic environments. Embedded within the anti-biofouling structure are agents that can diffuse out of the structure and prevent the formation and/or accumulation of plant and animal species build-up that creates biofouling. The instant invention also describes a system for preventing biofouling of an object stored in an aquatic environment which includes the anti-biofouling structure, and a protective cover element constructed and arranged to fit various structures, such as boat propellers.

Abstract: The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent.

Abstract: The instant invention relates to the use of tiotropium salts for the manufacture of a medicament for the treatment of patients suffering from severe persistent asthma.

Abstract: The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. He human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The inventor also provides methods for reducing on or more side effects of administration of the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.

Abstract: The invention relates to respirable dry particles that contain one or more divalent metal cations, such as calcium, in an amount of less than 3% by weight, and to dry powders that contain the respirable particles. The dry particles can further contain an active agent, or can be used as carrier particles to deliver an active agent.

Abstract: Embodiments described herein concern medical products, which come into contact with the organism, such as short-term implants and long-term implants, coated with at least one layer, containing a molecular-disperse distributed or dissolved active substance in at least one carrier and optionally one or more adjuvants, wherein the at least one layer forms a stably spreadable solution, methods for making this coating of stably spreadable solution and use of the medical products coated with the stably spreadable solution.

Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract: A biodegradable in vivo supporting device is disclosed. The in vivo supporting device comprises a biodegradable metal scaffold and a biodegradable polymer coating covering at least a portion of the biodegradable metal scaffold, wherein the biodegradable polymer coating has a degradation rate that is faster than the degradation rate of the biodegradable metal scaffold.

Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

Abstract: The invention provides active agents, such as paclitaxel, rapamycin, or 17-DMAG, encapsulated by safe poly(ethylene glycol)-block-poly(lactic acid) (“PEG-b-PLA”) micelles. The compositions provide effective solubilization of drug combinations, such as paclitaxel, rapamycin, and 17-DMAG, as well as others described herein. A significant advantage of PEG-b-PLA as a carrier is that it is less toxic than Cremophor® EL or DMSO, which are used in currently known compositions. Additionally, PEG-b-PLA micelles are easier to handle than DMSO and they do not possess a foul odor, which is a problem with formulations currently in clinical trials. Accordingly, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity. It was also found that larger doses of individual drugs in micelle formulations can be administered compared to non-micelle formulations.

Abstract: Methods for treating a human with cancer comprise administering a therapeutically effective amount of at least one MEK inhibitor and at least one mTOR inhibitor to said patient, wherein said patient has at least one mutation in at least one Ras protein or gene encoding at least one Ras protein and/or wherein said patient has at least one mutation, deletion or insertion in LKB1/STK11.

Abstract: The present invention relates to novel tacrolimus analogues, a composition for the prevention or treatment of neurological diseases or immune hypersensitivity disorders comprising the same, a method for preventing or treating neurological diseases or immune hypersensitivity disorders comprising administering the analogues to a subject, a method for preparing the analogues using an isolated modified Streptomyces sp. strain wherein the activity of one or more enzymes selected from the group consisting of TcsA, TcsB, TcsC and TcsD is reduced; and the isolated modified Streptomyces sp. strain for prepare the analogues.

Abstract: The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing obesity.

Abstract: The present invention provides a coating comprising a semi-crystalline polymer on an implantable device and methods of making and using the same.

Abstract: The present disclosure provides a device for intracorporeal use which comprises an implant or a temporary device and at least one source of myolimus or a derivative thereof. The present disclosure also provides a method of inhibiting cell proliferation, inflammation or cytokine production by systemic or local administration of a therapeutically effective amount of myolimus or a derivative thereof. Further included in the present disclosure is a method of treating an ophthalmic condition or disease by administering a therapeutically effective amount of myolimus or a derivative thereof.

Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 i

Abstract: The present invention provides an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors.

Abstract: The present invention provides isolated or substantially purified polypeptides, nucleic acids, and virus-like particles (VLPs) derived from a Merkel cell carcinoma virus (MCV), which is a newly-discovered virus. The invention further provides monoclonal antibody molecules that bind to MCV polypeptides. The invention further provides diagnostic, prophylactic, and therapeutic methods relating to the identification, prevention, and treatment of MCV-related diseases.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumors.

Abstract: The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes.

Abstract: The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area.

Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.

Abstract: The presently disclosed subject matter generally relates to methods and compositions for treating enteritis. More particularly, the presently disclosed subject matter relates to methods and compositions for modulating a component of a PI3K/mTOR pathway. In some embodiments, the methods and compositions of the presently disclosed subject matter generally relates to the treatment of campylobacteriosis. More particularly, the methods and compositions of the presently disclosed subject matter relate to the treatment of campylobacteriosis by modulating a component of a PI3K/mTOR pathway.

Abstract: The present invention provides inhibitors of kinases, specifically I?B kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-?B-mediated diseases.

Abstract: The present invention relates to sustained-release pellets containing tacrolimus as an active ingredient. The sustained-release pellets of the present invention have multiple layers of hydroxypropyl methylcellulose, and may control the release of drugs by specific contents of hydroxypropyl methylcellulose and Surelease™, thus rendering the dissolution rate thereof uniform and stable, and enabling the dissolution rate to be adjusted as desired. The entire process for preparing the pellets of the present invention is carried out in a single fluidized-bed granulator, and therefore the preparation process is simplified and the time required for preparation is shortened while obtaining sustained-release pellets having uniform particle size distribution and contents. The sustained-release pellets of the present invention may have medicinal effects that last up to 24 hours, and therefore may be administered just once a day, thus improving patient compliance.

Abstract: The present invention relates to the compound of formula (I) for use in the treatment of a nonsense-mutation-mediated genetic disease.

Abstract: A pharmaceutical composition is provided. The pharmaceutical composition comprises as an active ingredient a tropane alkaloid drug or a muscarinic receptor antagonist and stinging cells or capsules.

Abstract: The present invention is directed toward respirable dry particles for delivery of divalent metal cation salts and/or monovalent cation salts to the respiratory tract and methods for treating a subject having a respiratory disease and/or infection.

Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).

Abstract: Methods of treating renal cancers and other kidney-related inflammatory disorders with a bioabsorbable polymer scaffold (such as a stent) are described. The treatments are provided as alternative to complete or partial surgical removal of a diseased kidney.

Abstract: This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of mantle cell lymphoma.

Abstract: Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the prevention of thrombosis. The drugs, agents, and/or compounds may also be utilized to treat specific disorders, including vulnerable plaque. Implantable coated medical devices may be processed through annealing to better control the elution characteristics of the therapeutic agents.

Abstract: A cancer therapy sensitizer is disclosed. The cancer therapy sensitizer includes rapamycin and substituted quinoline. The present invention discloses a cancer therapy sensitization kit containing the two aforementioned compounds and a use of a combination of the two aforementioned compounds as a cancer therapy sensitizer as well. The application of the cancer therapy sensitizer, the kit and the use of the present invention is advantageous for improving the treatment effect of cancer therapies.

Abstract: A solid pharmaceutical composition containing AP23573 suitable for oral administration is disclosed.

Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).

Abstract: Methods for targeting adaptive responses to chemotherapy are described. In various embodiments, a method comprises administering at least one compound that inhibits S6K1, mTORC, or upstream or downstream pathway components of S6K1 or mTORC, in association with administration of at least one antagonist of PPAR?, PPAR?, or PGC1?. In various embodiments, the compound that inhibits S6K1, mTORC, or upstream or downstream pathway components of S6K1 or mTORC is rapamycin, everolimus, temsirolimus, or imatinib. The antagonist of PPAR?, PPAR?, or PGC1? can be GW7647, GW6471, GW501516, GSK3787, or GSK0660.

Abstract: A process for reducing the particle size of an active pharmaceutical ingredient (API) while maintaining its polymorphic form, comprises the step of processing the active pharmaceutical ingredient by cavitation at elevated pressure. The process preferably comprises the step of isolating the processed active ingredient in the form of powder, wherein the isolation step comprises filtration or spray drying. Particles produced by the process of the invention typically have a span value of less than 2.5.

Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.

Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

Abstract: The present invention relates to a pharmaceutical formulation and process for preparing the same comprising an oral dosage formulation, such as a capsule formulation, of a macrolide compound, such as tacrolimus, wherein the capsule formulation contains both a solid dispersion of the macrolide along with a non-dispersed form of the macrolide. The pharmaceutical formulation according to the invention is bioequivalent to the FDA approved product according to a bioavailability study conducted in humans.

Abstract: The present invention relates to substituted cellulose acetates and methods of use thereof. One embodiment of the present invention provides a coating having a substituted cellulose acetate having a polar substituent that has an oxygen atom covalently bonded to a nonmetal selected from the group of sulfur, phosphorus, and boron; wherein the nonmetal is present in at least about 0.01% by weight of the substituted cellulose acetate.

Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents, or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.

Abstract: The invention relates to a medical device for delivering a therapeutic agent to a tissue. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent, an antioxidant, and an additive. In certain embodiments, the additive has a hydrophilic part and a drug affinity part, wherein the drug affinity part is at least one of a hydrophobic part, a part that has an affinity to the therapeutic agent by hydrogen bonding, and a part that has an affinity to the therapeutic agent by van der Waals interactions. In some embodiments, the additive is a liquid. In other embodiments, the additive is at least one of a surfactant and a chemical compound, and the chemical compound has one or more hydroxyl, amino, carbonyl, carboxyl, acid, amide or ester groups.

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 liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations.

Abstract: Medical device are provided for delivering a therapeutic agent to a tissue. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent and an additive. In certain embodiments, the additive has a hydrophilic part and a drug affinity part, wherein the drug affinity part is at least one of a hydrophobic part, a part that has an affinity to the therapeutic agent by hydrogen bonding, and a part that has an affinity to the therapeutic agent by van der Waals interactions. In embodiments, the additive is water-soluble. In further embodiments, the additive is at least one of a surfactant and a chemical compound, and the chemical compound has a molecular weight of from 80 to 750 or has more than four hydroxyl groups.

Abstract: A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.

Abstract: Described herein are formulations comprising therapeutic agents, including but not limited to formulations comprising rapamycin, pharmaceutical formulations, unit dose forms, kits, methods of preparing formulations, and methods of using formulations. Such formulations and methods have increased stability.