Abstract: A tacrolimus injection preparation comprising tacrolimus, polyoxyethylene castor oil (35), and non-aqueous solvent is disclosed. Preferably the weight ratio of polyoxyethylene castor oil (35) to tacrolimus in the injection preparation is 10-20:1. The injection preparation significantly decreased the clinical risk.

Abstract: A method for treating endocrine tumors by administration of an mTOR inhibitor, optionally in combination with another drug.

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.

Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.

Abstract: The present invention provides an implantable device having a coating including a slow dissolving polymer or material and the methods of making and using the same.

Abstract: The disclosed molecules are inhibitors of Bcr-Abl and Src kinases. The molecules are cytotoxic to Gleevec resistant cells. Inhibitors of Bcr-Abl and Src kinases are used in the treatment of Chronic Myelogenous Leukemia among other diseases.

Abstract: The present invention relates to novel methods for the prevention, treatment and diagnosis of Alzheimer's disease. In addition, the invention relates to methods for assessing an individual's susceptibility or pre-disposition to Alzheimer's disease. The methods of the present invention involve the use of therapeutic targets and diagnostic and/or predictive markers within the mTOR signalling pathway. The methods also involve screening subjects for genetic polymorphisms associated with rapamycin-sensitive genes.

Abstract: A pharmaceutical composition for inhalation comprising aclidinium in the form of a dry powder of a pharmaceutically acceptable salt in admixture with a pharmaceutically acceptable dry powder carrier, providing a delivered dose of aclidinium equivalent to about 322 micrograms aclidinium free base.

Abstract: A system is described for long-term controlled release delivery of a drug or a therapeutic agent. According to the invention, one or more drugs or therapeutic agents contained in microspheres are mixed with a temperature sensitive hydrogel which is then introduced directly to the desired situs of the drug or therapeutic agent. The temperature sensitive hydrogel may also contain a drug or a therapeutic agent, for example, a pain relieving drug, for a short-term controlled release. The temperature sensitive hydrogel is in liquid state at room temperature, but upon injection, shortly becomes gelatinous. This system is particularly suitable for treatment of diseases, disorders, or conditions, for example, tumors, discogenic back pain, or arthritis, warranting localized administration of a drug or a therapeutic agent. In addition, the specification provides a method for production of a drug- or therapeutic agent-containing microspheres.

Abstract: This invention relates to tritoqualine for use in the treatment of cystic fibrosis or any one of its complications. The invention also relates to the method for the treatment of cystic fibrosis or any one of its complications by administering tritoqualine. The invention can be used to improve the condition of individuals with cystic fibrosis.

Abstract: The present invention is directed to polymeric materials comprising biodegradable, dioxanone-based copolymers and implantable devices (e.g., drug-delivery stents) formed of such materials. The polymeric materials can also contain at least one additional biocompatible moiety, at least one non-fouling moiety, at least one biobeneficial material, at least one bioactive agent, or a combination thereof. The polymeric materials are designed to improve the mechanical, physical and biological properties of implantable devices formed thereof.

Abstract: A method for identifying a kidney transplant recipient at an increased risk of developing interstitial fibrosis or tubular atrophy which comprises obtaining a post-transplant urine sample from the kidney transplant recipient; measuring the level of clusterin in the urine sample; comparing the level of clusterin in the patient sample to the level of clusterin in a control sample from the urine of a non-fibrotic kidney transplant recipient; diagnosing a kidney transplant recipient with a clusterin level that is significantly higher than the clusterin level in the control as being at an increased risk of developing interstitial fibrosis or tubular atrophy.

Abstract: The invention relates to the use of inhibitors of the enzyme mTOR kinase (mammalian target of rapamycin) in the treatment of neuro-oncologic diseases, in particular tuberous sclerosis, neurodegenerative diseases, in particular Alzheimer's disease, and neuroinflammatory diseases, in particular multiple sclerosis and primary progressive aphasia, via intrathecal, or preferably intraventricular, administration of said inhibitors.

Abstract: Provided herein is a device comprising: a. stent; b. a plurality of layers on said stent framework to form said device; wherein at least one of said layers comprises a bioabsorbable polymer and at least one of said layers comprises one or more active agents; wherein at least part of the active agent is in crystalline form.

Abstract: The present invention relates to the use of the measure of anelloviral load for the determination of immunosuppression. More precisely, the present invention provides a method for characterizing the immunosuppressed or non-immunosuppressed status of a subject, comprising the steps of determining the anelloviral load from a biological sample of the said subject, and determining from the said comparison the immunosuppressed or non-immunosuppressed status. The determination of the immunosuppressed status of the subject can then be used to design or adapt a therapeutic treatment.

Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.

Abstract: Methods for diagnosing and treating cancer associated with an oncogenic Kras mutation in a subject are provided.

Abstract: A method of modifying the surface of a medical device to release a drug in a controlled way by providing a barrier layer on the surface of one or more drug coatings. The barrier layer consists of modified drug material converted to a barrier layer by irradiation by an accelerated neutral beam derived from an accelerated gas cluster ion beam. Also medical devices formed thereby.

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 method for depositing a coating comprising a polymer and at least two pharmaceutical agents on a substrate, comprising the following steps: providing a stent framework; depositing on said stent framework a first layer comprising a first pharmaceutical agent; depositing a second layer comprising a second pharmaceutical agent; Wherein said first and second pharmaceutical agents are selected from two different classes of pharmaceutical agents.

Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

Abstract: Provided herein are methods comprising providing a tyrosine derivative and a solid particulate material (and, optionally, melanin) and applying force to said tyrosine derivative and said solid particulate material for a time and under conditions effective to impregnate at least one of said tyrosine derivative and said solid particulate material with the other of said tyrosine derivative and said solid particulate material. The invention also provides compositions comprising at least one of a tyrosine derivative impregnated with a solid particulate material and a solid particulate material impregnated with a tyrosine derivative.

Abstract: A centrifugal mixing device can include a shaft assembly that is operably coupled to a motor such that the motor rotates the shaft assembly about a first axis. The devices can further include a turret that is rotatably coupled to the shaft assembly such that the turret rotates about the first axis relative to the shaft assembly. The turret can include a first support, a first canister rotatably coupled to the first support such that the first canister rotates about a second axis, and a second canister rotatably coupled to the first support such that the second canister rotates about a third axis. The turret is configured to rotate about the first axis in a first rotational direction and each of the first and second canisters is configured to rotate about the second and third axes, respectively, in a second rotational direction that is opposite the first rotational direction.

Abstract: The present invention relates to suspension formulations, especially those for delivering a pharmaceutically active agent in aerosol form using a spray or aerosol device, such as a pressurized metered dose inhaler (pMDI). The formulations may be for pulmonary, nasal, buccal or topical administration, but are preferably for pulmonary inhalation.

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: 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: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.

Abstract: Implantable devices formed of or coated with a material that includes a polymer having a non-fouling acrylate or methacrylate polymer are provided. The implantable device can be used for treating or preventing 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: Compositions and methods are disclosed for treating vitiligo and promoting the formation of collagen.

Abstract: This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).

Abstract: An ambroxol hydrochloride composition and a preparation method therefor. 0.1%-99.9% by mass of ambroxol hydrochloride and 99.9%-0.1% by mass of scopolamine serving as main ingredients and mannitol are added into water for injection; dissolve, then adjust to pH 5.0; add 0.1% of activated carbon with stirring; filter out the activated carbon, and then filter the liquid; send into a lyophilizer, cool to ?40° C., and hold the temperature for 2 hours; warm to ?5° C. to 0° C. slowly to lyophilize the liquid, heat to 35° C., and hold the temperature for 3 hours; take out of the lyophilizer to obtain a lyophilized powder injection containing ambroxol hydrochloride and scopolamine; crush the lyophilized powder injection under sterile conditions, and sieve to obtain sterile lyophilized powder containing ambroxol hydrochloride and scopolamine; and prepare various dosage forms by using the lyophilized powder as a raw material.

Abstract: The present specification provides compositions comprising a thioxanthone-based autophagy inhibitor and/or a cancer therapeutic autophagy inducing compound, pharmaceutical kits comprising these compositions, and methods of treating cancer using such compounds, compositions and kits. Additionally, the present specification provides methods of treating cancer using a thioxanthone-based autophagy inhibitor and a radiotherapy.

Abstract: A drug-delivering insertable medical device for treating a medical condition associated with a body lumen is disclosed. The drug-delivering insertable medical device includes an outer surface coated with two or more nano-carriers having two or more average diameters. A nano-carrier of the two or more nano-carriers has an average diameter suitable for penetrating one or more layers of two or more layers of the body lumen. The nano-carrier includes a drug surrounded by an encapsulating medium. The encapsulating medium includes one or more of a biological agent, a blood excipient, and a phospholipid.

Abstract: A drug delivery composition including a lipophilic agent or a biologic agent and a polymer wherein the lipophilic agent exhibits sustained release and wherein there is less than 35% agent release within the first hour of elution. A drug delivery composition including a lipophilic agent or a biologic agent and a polymer wherein the elution profile is substantially linear, and wherein there is less than 35% agent release within the first hour of elution. The lipophilic agent may be crystalline and the biologic agent may be in active form.

Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.

Abstract: NK cell licensing predisposes patients to chronic inflammatory disease. Methods and kits to diagnose and treat chronic inflammatory disease based on genetic haplotype and cytokine profile are described herein.

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: A drug-delivering medical device for delivering a drug to a target site in a human body is disclosed. The drug-delivering medical device may have a hydrophilic surface, with one or more portions of the hydrophilic surface coated with one or more nano-carriers bearing one or more drugs. Each nano-carrier may include a drug surrounded by an encapsulating medium. As the drug is surrounded by the encapsulating medium, the surface of each nano-carrier can be devoid of the respective drug. A non-implantable medical device coated with nano-carriers can deliver one or more drugs to a blood vessel, organ cavity, sac, capsule, lining, layer, coating, membrane, connective tissue, fluid surrounding an organ, and so forth.

Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.

Abstract: The present invention relates to novel tigecycline compositions with improved stability in both solid and solution states and processes for making these compositions. These compositions comprise tigecycline, a suitable carbohydrate, and an acid or buffer.

Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.

Abstract: A method is disclosed for making a pharmaceutical composition for pulmonary administration, the method comprising a step in which an inhalable pharmaceutically active material is acoustically blended in a resonant acoustic blender. The invention also relates to compositions for inhalation prepared by the method.

Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.

Abstract: Disclosed herein are implantable medical devices comprising controlled release biodegradable block copolymers or coated with controlled release block copolymers and at least one drug releasable from the block copolymer. The controlled release block copolymers comprise least two blocks selected from the group consisting of polyesters, polyethers, and polyurethanes.

Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.

Abstract: The present invention relates to a calcineurin inhibitor for use in the treatment of a lesional vestibular disorder.

Abstract: A coating composition for drug eluting medical devices, which is capable of forming a drug coating layer that is not susceptible to peeling during delivery to a target tissue is provided. This coating composition contains: a water-insoluble drug; at least one selected from the group consisting of hyaluronic acid, alkanoyl hyaluronic acids obtained by substituting at least part of hydrogen atoms in the hydroxyl groups of hyaluronic acid with an alkanoyl group, and salts of hyaluronic acid and the alkanoyl hyaluronic acids; and at least one selected from the group consisting of amino-acid esters and salts thereof. A drug coating layer, a medical device and a method of treatment are also provided.

Abstract: Described are compositions and methods for administering scopolamine and ketamine in the treatment of depression (e.g., Major Depressive Disorder and Treatment-Resistant Depression).

Abstract: A coating composition for drug-eluting medical devices, which enables a medical device to be delivered to a target tissue for the purpose of treating an affected blood vessel part such as restenosis, without easy separation of a drug from the medical device during the delivery process is provided. The coating composition for drug-eluting medical devices contains a water-insoluble drug and at least one selected from the group consisting of ester compounds of amino acids, which have a hydropathy index of the amino acid of zero or less than zero, and salts thereof. A drug coating layer, a drug-eluting medical device and a method of treatment are also provided.

Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.