Abstract: The present invention provides Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and discloses methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides Compound (I): Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides an improved method of diagnosing a subject having received an organ transplant with Acute Cellular Rejection (ACR). The method comprises obtaining a biological sample from the subject, detecting an amount of at least one protein indicative of ACR in the sample, and comparing the amount of the protein in the sample to a control, wherein a difference between the amount of the protein in the sample relative to the control indicates the subject has or is developing ACR. The difference can be an increase or a decrease. In one version the biological sample comprises a serum sample, and the transplanted organ is selected from a heart, kidney, liver, bone marrow, pancreas, eye, lung or skin. Methods of treating a subject having an organ transplant for ACR are also provided.

Abstract: The present invention relates to a method of treating a life threatening condition in a critically ill human patient with a non-infectuous disorder, wherein the critically ill patient is a patient receiving enteral or parenteral nutrition, the method comprising the step of administering to said patient an autophagy inducing agent.

Abstract: The current invention relates to methods of forming a coating that involves the in-situ formation of drug microspheres. The coating may be applied to a medical device, such as a catheter balloon or a stent. Coated devices and methods of treatment therewith are also encompassed within the embodiments of the present invention.

Abstract: This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis.

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

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: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.

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: Described herein are methods of diagnosing lymphangioleiomyomatosis (LAM) that permits differentiating LAM from another lung disorder. Methods of treatment are also provided.

Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: Medical devices comprising nanobeads encapsulating one or more bioactive agents and methods of use thereof are provided.

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: Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such chemicals.

Abstract: The present invention relates to non-psychoactive derivatives of tetrahydrocannabinol, which are useful in treating interstitial cystitis and relieving symptoms thereof. The invention uses (6aR,10aR)-?8-tetrahydrocannabinol-11-oic acids (hereinafter referred to as (6aR,10aR)-?8-THC-11-oic acid), as well as pharmaceutical compositions containing the (6aR,10aR)-?8-THC-11-oic acids, for treatment of interstitial cystitis in a mammal. The invention further covers methods of formulating and administering the compounds and pharmaceutical compositions as therapeutic agents in the treatment of interstitial cystitis, with particularly preferred administration routes being oral and via intravesicular instillation.

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract: The present invention relates to inhalable particles comprising a stabilized amorphous form of tiotropium with a stabilizing agent. It also relates to inhalable particles comprising a stabilized amorphous form of tiotropium with a stabilizing agent mixed with one or more coarse excipients having a mean particle size of 15 to 250 ?m. It also relates to a pharmaceutical composition comprising the inhalable particles of the invention, to a process for their preparation, and to their use for the preparation of a medicament for the treatment of asthma or chronic obstructive pulmonary disease (COPD).

Abstract: The present invention is a substantially non-adhesive elastic gelatin matrix. The matrix is both non-adhesive to wounds, tissues and organs and is also elastic such that it is flexible. The matrix is a lyophilized mixture of protein(s), polymer(s), cross-linking agent(s) and optional plasticizer(s). The invention also provides methods for making the non-adhesive elastic gelatin matrix.

Abstract: Provided herein are coating designs for the tailored release of two therapeutic agents from polymer coatings and methods of making and using the same.

Abstract: The current invention relates to poly(amide) and poly(ester-amide) polymers, coatings including the polymers, and narrow polydispersity drug delivery particles including the polymers.

Abstract: A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight.

Abstract: A method for inhibiting formation of adhesions following abdominal surgery which involves application of an anti-static fatty acid ethoxylated amide (Cocamide DEA) in a matrix that is placed in the peritoneal cavity at the conclusion of an abdominal surgery and which releases this anti-adhesive chemical over a predetermined time in a range from about five to seven days. Tests conducted on laboratory rats established that the method reduced the incidences of adhesions from 100 percent (100%) in a test model to near zero percent (0%) in the treated animals. In an alternative embodiment, Andrographalide was delivered through a drug pump with similar results. In still another embodiment, an effective amount of Rapamune was delivered, via a pump, into the abdominal cavity, again with similar results.

Abstract: We have discovered that p63 inhibition results in increased cellular proliferation. We have also performed a screen for agents capable of increasing cellular proliferation, (e.g., of stem cells such as skin-derived precursors (SKPs)). The invention therefore invention provides compositions, methods, and kits for increasing proliferation of cells, using compounds that decrease p63 expression or activity or using the compounds described herein. The invention also features methods of using these compounds for increasing hair growth, improving skin health, or promoting skin repair in a subject.

Abstract: The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.

Abstract: A pharmaceutical combination comprising an mTOR inhibitor and a Raf kinase inhibitor and its use.

Abstract: A stable pharmaceutical compositions of Rapamycin Esters, in particular Rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid that is free of antioxidants and a process of preparing the same.

Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.

Abstract: 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.

Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.

Abstract: The invention in some aspects relates to methods, devices and compositions for evaluating material properties, such as mechanical and rheological properties of substances, particularly biological substances, such as cells, tissues, and biological fluids. In some aspects, the invention relates to methods, devices and compositions for evaluating material properties of deformable objects, such as cells. In further aspects, the invention relates to methods, devices and compositions for diagnosing and/or characterizing disease based on material properties of biological cells.

Abstract: There is provided a composition comprising microspheres which comprise a water-insoluble, water-swellable polymer and associated with the polymer, in releasable form, a chemotherapeutic agent, for use in the treatment of a pancreatic tumour or cyst, wherein the microspheres, when equilibrated in water at 37° C., comprise at least 40 wt % water based on weight of polymer plus water, wherein the polymer is anionically charged at pH7 and the chemotherapeutic agent is cationically charged and electrostatically associated with the polymer. Also provided are methods of treating pancreatic tumours or cysts using this composition.

Abstract: The present invention provides a film-form base having one or more sugars or sugar alcohols dispersed as fine particles therein, and also provides a film-form preparation containing the base and a drug. The base is produced by dispersing, in an organic solvent having a solubility parameter of 9.7 or higher, an edible polymer soluble in water and the organic solvent, and particles of one or two or more compounds selected from the group consisting of mono- to hexasaccharide sugars and sugar alcohols thereof which have an average particle size of 0.1 ?m to 60 ?m and are insoluble in an organic solvent. The present invention can therefore provide oral film-form base and preparation which have a rapid dissolution profile in the mouth and sufficient film strength, and provide a reduced sticky sensation attributed to the water-soluble polymer in the mouth and an improved feel when handled with the fingers.

Abstract: The present invention relates to a method for enhancing the activity of kinase inhibitors in target cells, and more specifically for enhancing the activity of tyrosine kinase inhibitors (TKIs), said method comprising contacting a cell with a kinase inhibitor and a photosensitizing agent and irradiating said cell with light of a wavelength effective to activate the photosensitizing agent, and to the use of this method for enhancing the effects of kinase inhibitors or kinase inhibitor-based drugs in particular to achieve cell death, for example, in cancer treatment and other diseases or conditions in which kinase inhibitors, such as TKIs, have a beneficial effect.

Abstract: A process is described for loading hydrophilic polymer particles with a water-insoluble solvent-soluble drug. The particles are preferably embolic agents. The method provides particles having little or no drug at the surface and in a surface layer, whereby the burst effect is minimised. The drug is precipitated in the core of the particle, leading to extended release. The drug is, for instance, paclitaxel, rapamycin, dexamethasone or ibuprofen.

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: A method of treating a fibrotic disease or condition in a patient comprising administering noscapine and a pharmaceutical carrier to said patient.

Abstract: The invention relates to a coating composition for an implantable medical device, a method of coating a medical device and a device coated with the composition.

Abstract: A sustained release pharmaceutical composition for tacrolimus, comprising a solid dispersion containing tacrolimus or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of tacrolimus after 4 hours from the beginning of a dissolution test is less than 35%, is disclosed.

Abstract: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

Abstract: Systems and compositions comprising paclitaxel and a second drug, such as rapamycin, analogs, derivatives, salts and esters thereof are disclosed, as well as methods of delivery wherein the drugs have effects that complement each other. Medical devices comprising supporting structures capable of including or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient can contain one or more therapeutic agents or substances, with the carrier preferably including a coating on the surface thereof, and the coating including the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature.

Abstract: An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.

Abstract: The present invention relates to targeted drug delivery of a drug or therapeutic agent through medical devices coated with formulations comprising of therapeutic agent. The coating on medical devices comprises of therapeutic agent(s), affinity vehicle(s) and additives for targeted drug delivery of biologically active material(s). The invention provides a method of manufacturing the formulation, method of coating the medical devices with such formulations to achieve controlled delivery of optimum drug dose at the target site within the body, desirable drug retention on the medical devices in vivo and in vitro and desirable drug release at the target tissue in-vivo. The invention this provides a mechanism to enhance the bioavailability of the therapeutic agent at the target tissue in the treatment of restenosis thereby reduces the actual dose of the therapeutic agent and provides a very thin layer of coating on the surface of the medical device.

Abstract: Provided herein are methods for functionalizing a polymer for forming a coating and coatings and devices formed thereof or for functionalizing a coating or device surface including an polymer.

Abstract: Compositions and methods for treating or preventing infectious diseases, and inhibiting the ability of microbes to travel within mammalian cells, and inhibiting microbial replication, are disclosed. The compositions include various noscapine analogs, which are capable of blocking the movement of viruses and other microbes within mammalian and other cells by inhibiting the cytoplasmic transport mechanisms within the cells. The compositions described herein include an effective amount of the noscapine analogues described herein, along with a pharmaceutically acceptable carrier or excipient. The compositions can also include one or more additional antimicrobial compounds.

Abstract: The present invention relates to a stable pharmaceutical composition that includes sirolimus. The pharmaceutical composition includes sirolimus in the amorphous form, a fatty acid ester, such as glyceryl behenate, and a pharmaceutically acceptable polymer wherein the fatty acid ester is present at a concentration of less than 10% w/w compared to the total weight of the composition.

Abstract: The present invention provides compounds and pharmaceutically acceptable salts thereof methods for synthesizing thienopyridines and methods for inhibiting TNF-? activity for the treatment of cancer, asthma, arthritis, diabetes and inflammation. Provided are compounds of formula (I).

Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in an ocular tissue. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.

Abstract: Compositions comprising poly(hydroxyalkanoates) and agents for use with medical articles are described.