Abstract: The application discloses a formulation and method for increasing bioavailability of an orally administered drug.

Abstract: This invention relates to a solution formulation containing a tiotropium salt, 12-20% ethanol, 0.1-1.5% of water, 0.05-0.10% citric acid (or other organic acid) and an HFA propellant, wherein the percentages are percentages by weight based on the total weight of the formulation. The invention also provides a pMDI comprising a canister containing the formulation.

Abstract: The instant invention provides a method of treating a cancer selected from the group consisting of non-small cell lung cancer and breast cancer with an mTOR inhibitor and an ?v62 3 integrin antagonist, wherein the mTOR inhibitor is ridaforolimus, everolimus, temsirolimus or a combination thereof.

Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.

Abstract: A method and device for local delivery of a water-insoluble therapeutic agent to the tissue of a normal or diseased body lumen is disclosed. An expandable structure of a medical disposable device, such as a balloon of a balloon catheter, is coated with a non-durable coating which comprises poly(HEMA) complexed with iodine and has a substantially water-insoluble therapeutic agent dispersed therein. The medical disposable device is inserted into a body lumen, and expanded to contact the non-durable coating against the body lumen and deliver the substantially water-insoluble therapeutic agent to the body lumen tissue.

Abstract: Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.

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 analyzes 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: A method of treating rhinitis and rhinorrhea includes taking a daytime oral dosage unit containing a non-sedating antihistamine for treating rhinitis and an anticholinergic agent having limited capacity to cross blood-brain barrier for treating rhinorrhea, and taking a nighttime oral dosage unit containing a non-sedating anticholinergic agent that has limited capacity to cross blood-brain barrier and that is in a lower amount than the amount in the daytime oral dosage unit for treating rhinorrhea or no anticholinergic agent.

Abstract: Disclosed are a polymeric drug carrier-containing pharmaceutical composition with enhanced stability in its solution state and a method for stabilizing the same. More particularly, disclosed are a pharmaceutical aqueous solution composition for storage under refrigeration containing a polymeric drug carrier comprising an amphiphilic block copolymer comprised of a hydrophilic block and a hydrophobic block, and a polylactic acid derivative fixed with a di- or tri-valent metal ion at its terminal carboxyl group and having preservation stability for at least 6 months, preferably at least 12 months when stored under refrigeration, and a method for stabilizing the same.

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The present invention provides compositions and methods for treating ocular disorders such as myopia.

Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, dermatitis.

Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.

Abstract: The present invention relates to methods of making a powder for inhalation comprising a first step of mixing particles of a force-controlling agent selected from the group consisting of phospholipids, titanium dioxide, aluminum dioxide, silicon dioxide, starch, and salts of fatty acids, with particles of one or more pharmacologically active materials, wherein the mixing is achieved by one or more of the processes of sieving, mixing or blending, and wherein the mixing results in the particles of the force-controlling agent being disposed on the surface of the particles of the one or more pharmacologically active materials as either a particulate coating or as a continuous or discontinuous film.

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: This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.

Abstract: Methods of treating or preventing cancer, or ameliorating a symptom thereof, by administering a muscarinic receptor inhibitor to inhibit cancer metastasis and/or a ? adrenergic receptor inhibitor to inhibit tumor initiation are provided. Also provided are pharmaceutical compositions for treating or preventing cancer comprising a muscarinic receptor inhibitor and/or a ? adrenergic receptor inhibitor.

Abstract: The present invention is related to a medical device carrying at least on a portion of its surface at least one drug or drug preparation and at least one lipophilic lubricant at a ratio of 0.1-500% by weight of the at least one lubricant in relation to 100% by weight of the drug, wherein the at least one drug is selected of paclitaxel, arsenic trioxide, and lipophilic derivatives of corticoids and selected Limus drugs, and the at least one lipophilic lubricant is a C6-C30-monocarboxylic acid salt.

Abstract: Biodegradable polymers useful for fabricating implantable medical devices and as coatings for medical devices are provided. The biodegradable polymers are biocompatible and can be tuned to provide optimum bioactive agent elution rates as well as degradation rates. Also provided are methods for making medical devices and medical device coatings using the biodegradable polymers.

Abstract: The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.

Abstract: The present invention is drawn to formulations for the transdermal delivery of rapamycin or other related compounds. Specifically, in one embodiment a formulation for transdermally delivering rapamycin includes an mTOR inhibitor, such as rapamycin, water, a polymer having surfactant properties, a polymer having thickening properties, a solvent for solubilizing the mTOR inhibitor, a glycol, a C10-C20 fatty acid; and a base.

Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.

Abstract: Implantable medical devices including a coating having a bioactive agent and a poly(ester amide) polymer. Methods of forming these coatings are also described.

Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.

Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.

Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.

Abstract: A coating material including a bio-absorbable cross-linked material and a cellular uptake inhibitor. The bio-absorbable cross-linked material includes two or more fatty acids cross-linked into a substantially random configuration by ester bonds. The coating material may be adhered to a medical device. A medical device system including a medical device and a coating is also included.

Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.

Abstract: Provided are methods and compositions for the treatment of depression and anxiety. The compositions contain scopolamine, or an analog thereof, and can optionally include one or more psychoactive agents. Further provided is an inhaler containing scopolamine, or an analog thereof, in a pharmaceutically acceptable carrier.

Abstract: The subject invention provides for cancer therapy.

Abstract: A medical assembly is disclosed comprises a stent and a catheter having a balloon, wherein the coefficient of friction and/or the adhesion at the stent/balloon interface are reduced.

Abstract: Ophthalmic compositions containing norketotifen and methods of making the same and the use thereof are disclosed. The methods also comprise administering to the eyes of a mammal in need thereof topical ophthalmic compositions containing norketotifen.

Abstract: Methods for diagnosing and treating Alzheimer's disease are provided. In particular, methods of restoring blood-brain barrier integrity and/or promoting vascular reversion in a person suffering from Alzheimer's disease by administering an anti-angiogenic agent or an agent that is capable of restoring tight junction integrity. Methods of preventing or delaying the onset of Alzheimer's disease in a subject are also provided.

Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.

Abstract: The present invention provides methods of delivering a composition comprising nanoparticles that comprise a macrolide and an albumin by directly injecting the nanoparticle composition into the blood vessel wall or the tissue surrounding the blood vessel wall. The methods can be used for inhibiting negative remodeling or vascular fibrosis in the blood vessel and are useful for treating various diseases.

Abstract: Implantable devices formed of or coated with a material that includes an amorphous poly(D,L-lactide) formed of a starting material such as meso-D,L-lactide are provided. The implantable device can be used for the treatment, mitigation, prevention, or inhibition of a disorder such as atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, patent foramen ovale, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, or combinations thereof.

Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.

Abstract: This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.

Abstract: It is discovered that noscapine is effective in treating temozolomide (TMZ)-resistant brain cancer. Provided are compositions and methods of treating brain cancer patients, in particular those that are TMZ-resistant. The patients are treated by administration of a therapeutically effective amount of noscapine or an analog thereof. In certain aspects, TMZ is also administered to the patients. Examples of brain cancers include glioma such as glioblastoma multiforme.

Abstract: The present invention provides methods of identifying an agent or drug candidate molecule, validating a target, and identifying normalizing therapeutics that modulates translation, such as in an oncogenic signaling pathway, in a biological sample as determined by translational profiling of one or more genes in the biological sample. The present invention also provides diagnostic and therapeutic methods using the translational profiling methods described herein.

Abstract: The invention relates to the innate immune pathway and anti-inflammatory molecules with therapeutic properties. In some embodiments, the invention relates to compounds and pharmaceutical compositions and methods of using the compounds and compositions to treat inflammatory diseases including inflammation associated with auto-immune diseases.

Abstract: Disclosed are pharmaceutical combinations comprising at least one S1P receptor agonist, as well as a method for treating demyelinating diseases, e.g. multiple sclerosis or disorders associated therewith or Guillain-Barré syndrome, comprising co-administration, e.g. concomitantly or in sequence, of a therapeutically effective amount of a) an S1P receptor agonist, and b) at least one co-agent shown to have clinical activity against at least one symptom of a demyelinating disease.

Abstract: The present invention provides methods for the treatment of denervation-induced skeletal muscle atrophy, and generally, denervation-induced skeletal muscle degeneration diseases using agents that decrease the activity of mammalian target of rapamycin and/or the activity of at least one of the Forkhead Box Transcription Factors 1, 3 and 4.

Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying pulmonary hypertension by administering nanoparticles that comprise rapamycin or a derivative thereof and/or nanoparticles that comprise a taxane (e.g., paclitaxel) or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof and/or nanoparticles that comprise a carrier protein and a taxane (e.g., paclitaxel) or a derivative4 thereof.

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 invention is related to a dry powder formulation containing tiotropium to be administered via inhalation, the use of said formulation in the treatment of respiratory diseases especially asthma and COPD (Chronic obstructive pulmonary disease), and the production process of said formulation.

Abstract: This invention relates to an method of manufacture of an implantable medical device comprising an oxygen-sensitive rapamycin derivative that is protected by addition of an antioxidant during the manufacturing process where the amount of antioxidant added at the outset of the processing is such that when the device is fully fabricated, sterilized and packaged the amount of antioxidant has reduced to a minimal, preferably non-detect, amount.

Abstract: The present invention relates to an oxygen-sensitive macrocyclic triene lactone that is protected by addition of an appropriate amount of an antioxidant stabilizer during fabrication of an implantable medical device comprising the macrocyclic triene lactone, wherein the amount of the antioxidant stabilizer has been reduced to a minimal, preferably, non-detect, level in the final packaged product.

Abstract: Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.

Abstract: The disclosure relates to compounds and compositions for bone formation, fracture treatment, bone grafting, bone fusion, cartilage maintenance and repair and methods related thereto. In certain embodiments, the disclosure relates to compositions comprising one or more compound(s) disclosed herein, such as clotrimazole, honokiol, magnolol, tacrolimus, pimecrolimus, sirolimus, everolimus, temsirolimus, spironolactone, fluticasone, fluticasone propionate, fluticasone furoate, linezolid, telmisartan, chlorambucil, retinol, isotretinoin, acitretin, etretinate, retinoic acid (tretinoin), teniposide, mitomycin C, cytarabine, decitabine, vinblastine, vincristine, vindesine, vinorelbine, valrubicin, doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxantrone, pixantrone, plicamycin, pazopanib, topotecan, camptothecin, irinotecan, sunitinib, derivatives, or salt thereof, for use in bone growth processes.