Abstract: A method for inhibiting the production of cytokines of T helper cell type II (Th2 cell) and/or inhibiting the production of chemokines in a mammal is provided, wherein the method comprises administrating to the mammal an effective amount of an active component selected from a group consisting of a compound of formula (I), pharmaceutically acceptable salts and esters of the compound, and combinations thereof:

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, ocular tissues 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 guanidine 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.

Abstract: It is provided herein methods, devices, and compositions for trans-arterial local delivery of therapeutic agent for the treatment of liver cancers.

Abstract: Disclosed are nanoparticles comprising a block copolymer and optionally one or more active agent(s), compositions comprising said nanoparticles and methods of preparing said nanoparticles. The block copolymer comprises blocks (i) a first polymer that is a polyester or polyamide and (ii) a second polymer comprising a hydrocarbon chain containing ester or ether bonds with hydroxyl number ?10. The active agent(s) may be present within the nanoparticles or on the surfaces of the nanoparticles. The nanoparticles may optionally be associated with a surface-modifying moiety such that they are useful as drug delivery and molecular imaging devices. The surface-modifying moiety may target the nanoparticles to a desired target, cell, tissue or biomarker.

Abstract: A method of treating a neoplastic disease in a subject includes administering to neoplastic cells of the subject an MGMT inhibitor and at least one of an antimitotic agent or a DNA damaging agent.

Abstract: The present invention relates to a stable pharmaceutical composition for injection containing docetaxel and a method of preparing the same. More particularly, the present invention relates to a pharmaceutical composition for injection containing docetaxel having better storage stability than conventional medications, which is prepared by dissolving docetaxel, a water-insoluble compound, in distilled water after mixing it with cyclodextrin (CD) and a water-soluble polymer such as hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG) or polyvinylpyrrolidone (PVP) and lyophilizing the mixture, and a method of preparing the same.

Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.

Abstract: The present invention is an ophthalmic composition containing a relatively high concentration of olopatadine. The composition is typically an ophthalmic aqueous solution containing relatively high concentrations of olopatadine solubilized within the solution. The composition is preferably capable of providing enhanced relief from symptoms of ocular allergic conjunctivitis, particularly late phase symptoms of ocular allergic conjunctivitis.

Abstract: The invention relates to a method for producing biodegradable, functionalised polymer particles, and to the use of the same as medicament carriers.

Abstract: A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: The present invention is directed to stents made of a magnesium alloy degradable under physiological conditions and an outer polymeric coating. Herein, the stents according to the invention can be additionally coated with at least one anti-inflammatory, antiproliferative, antiangiogenic, antirestenotic and/or antithrombogenic active agent.

Abstract: The present invention provides methods and compositions for treating cancer by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and/or b) a therapeutic agent (e.g., gemcitabine) based upon K-ras mutation status.

Abstract: The disclosure provides a pharmaceutical composition. The pharmaceutical composition includes a chitosan with palmitoyl groups and an active agent. According to another embodiment, the pharmaceutical composition can further include a gelling accelerating agent. According to an embodiment of the disclosure, the active agent of the disclosure can be administered in the form of a nano-drug, liposome, micelle, or microparticle.

Abstract: The present invention provides methods and compositions for treating cancer by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and b) a nucleoside analog (e.g., gemcitabine) based upon levels of a nucleoside transporter (e.g., hENT1).

Abstract: A method of making an endoperoxide from a diene and oxygen in the presence of a photocatalyst having an excited state lifetime of at least 100 nanoseconds, the endoperoxide being represented by the formula: where R1 is an aryl substituted with at least one group selected from the group consisting of alkoxy, hydroxyl, halogen, carbamate, sulfonamide, silyloxy, amide, and combinations thereof or a substituted or unsubstituted heteroaryl, R2 is hydrogen, alkyl, alkynyl, or aryl, R3 is hydrogen, alkyl, alkynyl, or aryl, R4 is alkynyl or aryl, R5 is hydrogen or a substituent, R6 is hydrogen or a substituent, and A1, A2, and A3 are the same or different atoms and form a divalent group that combines with the two carbon atoms of the endoperoxide ring to form a saturated or unsaturated, substituted or unsubstituted ring system of a size of from five to six atoms.

Abstract: The present disclosure generally relates to polymer-drug systems, and more particularly to nanoscopic particles comprising amphiphilic block copolymers conjugated, physically encapsulated, or otherwise combined with chemotherapeutic agents along a selective region or regions of the backbone of the copolymer, so as to package the chemotherapeutic agent in selective domains within each nanoscopic particle, as well as to methods for making such particles, and applications and methods for using such particles, including in the formation of polymer micelles.

Abstract: The present invention provides an implantable article comprising an amorphous terpolymer and a semi-crystalline polymer. The amorphous terpolymer can be admixed with the semi-crystalline polymer or form a block copolymer with the semi-crystalline polymer.

Abstract: An aliphatic polyester polymer for stent coating is described.

Abstract: Embodiments of the invention are directed to methods of determining the prognosis of a breast cancer patient by evaluating the activity of the glucocorticoid receptor in tumor cells. Other embodiment include methods of treating breast cancer cells, particularly, chemo-resistant cells, with a glucocorticoid receptor antagonist and an anticancer agent or compound.

Abstract: The present invention provides compositions (such as pharmaceutical compositions) comprising nanoparticles comprising albumin and paclitaxel. The compositions have a specific albumin polymer/monomer profile and are particularly suitable for use in treating diseases such as cancer.

Abstract: The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Abstract: This disclosure relates to diagnostic and therapeutic methods and systems related thereto. In certain embodiments, the disclosure contemplates methods of improving chemotherapy treatments by administering chemotherapy agents, analyzing CHFR gene expression, methylation, or both, and determining an appropriate therapeutic strategy. Analysis of data herein revealed that reduced CHFR expression levels was a predictor of improved overall survival of subject with non-small cell lung cancer.

Abstract: Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.

Abstract: A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056 M?1-13051 M?1), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 ?m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.

Abstract: Systems and methods for magnetic targeting of therapeutic particles are provided. Therapeutic particles comprise one or more magnetic or magnetizable materials and at least one therapeutic agent. Therapeutic particles are specifically targeted using uniform magnetic fields capable of magnetizing magnetizable materials, and can be targeted to particular locations in the body, or can be targeted for capture, containment, and removal. Also provided are bioresorbable nanoparticles prepared without the use of organic solvents, and methods for therapeutically using such bioresorbable nanoparticles.

Abstract: The present invention relates to a stable liquid cabazitaxel formulation in an enclosed container. The enclosed container comprises a liquid phase and an gaseous phase, wherein the liquid phase comprises cabazitaxel, polysorbate 80, ethanol, and one or more pH adjusters to maintain pH about 2.8-6.0, and the gaseous phase is saturated with CO2. The present invention is also directed to a process for preparing the enclosed liquid pharmaceutical composition container.

Abstract: The present invention provides polymer aggregates as delivery vehicles for therapeutics and diagnostics. The present invention additionally provides methods of synthesis and uses for such aggregates.

Abstract: The invention relates to treatment and/or prevention of nerve injury. In one embodiment, the present invention provides a method of preserving the neuromuscular junction (NMJ) in an individual by administering a therapeutically effective dosage of a composition comprising an inhibitor of Wnt3a, and an inhibitor of MMP3 to the individual. In another embodiment, the present invention provides a method of stabilizing NMJ after nerve injury by inhibiting the WNT and beta-catenin signaling pathway and preserving agrin.

Abstract: The present invention provides combination therapy methods of treating a proliferative disease (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 the administration of an effective amount of at least one other agent that modifies the epigenetics in a cell.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.

Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.

Abstract: The present invention relates to specific beta-lactone compounds and compositions thereof for the treatment of infections, such as, e.g., infections with bacteria or infections with protozoa, in particular infections with Gram-positive and/or Gram-negative bacteria and of infectious diseases caused by or related to Gram-positive and/or Gram-negative bacteria, and to the modulation of virulence of Gram-positive and/or Gram-negative bacteria or of protozoa by specific beta-lactone compounds. The invention further relates to the use of the compounds or compositions for preventing or eliminating biofilms.

Abstract: The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together to form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for th

Abstract: The present invention provides combination therapy methods of treating a proliferative disease (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 the administration of an effective amount of at least one other agent that modifies the epigenetics in a cell.

Abstract: A composition comprising intact killed bacterial cells that contain a therapeutic nucleic acid, a drug or a functional nucleic acid is useful for targeted delivery to mammalian cells. The targeted delivery optionally employs bispecific ligands, comprising a first arm that carries specificity for a killed bacterial cell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target killed bacterial cells to specific mammalian cells and to cause endocytosis of the killed bacterial cells by the mammalian cells. Alternatively, the delivery method exploits the natural ability of phagocytic mammalian cells to engulf killed bacterial cells without the use of bispecific ligands.

Abstract: Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.

Abstract: The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.

Abstract: Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.

Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.

Abstract: A method for manufacturing a porous ceramic scaffold having an organic/inorganic hybrid coating layer containing a bioactive factor includes (a) forming a porous ceramic scaffold; (b) mixing a silica xerogel and a physiologically active organic substance in a volumetric ratio ranging from 30:70 to 90:10 and treating by a sol gel method to prepare an organic/inorganic hybrid composite solution; (c) adding a bioactive factor to the organic/inorganic hybrid composite solution and agitating until gelation occurs; and (d) coating the porous ceramic scaffold with the organic/inorganic composite containing the bioactive factor added thereto. In accordance with the method, the porous ceramic scaffold may be uniformly coated with the organic/inorganic hybrid composite while maintaining an open pore structure, and stably discharge the bioactive factor over a long period of time.

Abstract: Micellar preparation in which the solubility of a sparingly water-soluble anticancer agent has been heightened and which after intravenous administration, enables a high blood concentration to be maintained. The preparation has high medicinal activity and/or reduced side effects, and is formed from a block copolymer represented by formula (1): [wherein R1 represents hydrogen or C1-5 alkyl; R2 represents C1-5 alkylene; R3 represents methylene or ethylene; R4 represents hydrogen or C1-4 acyl; R5 represents hydroxyl, optionally substituted aryl C2-8 alkoxyl, substituted C1-4 alkylamino, or amino having a residue of either an amino acid or a peptide derivative; n is an integer of 5 to 1,000; m is an integer of 2 to 300; and x is an integer of 1 to 300; provided that the proportion of hydroxy in the R5's is 0 to 99% and x is not larger than m] and a sparingly water-soluble anticancer agent.

Abstract: Disclosed herein are therapeutic compositions for treating and preventing diseases such as neointimal hyperplasia (NIH), where the compositions comprise a therapeutic particle that has a localized association with a blood vessel and a therapeutic agent, such as an anti-NIH agent. Methods of use of the therapeutic compositions are also disclosed.

Abstract: The disclosure is directed to a nanoparticle comprising a porous framework core including a porous framework material and a compound, and a lipid layer disposed on the surface of the porous framework core.

Abstract: Provided are a composition for preparing a lyophilized preparation, comprising a drug-encapsulating polymer micelle and saccharides and/or polyethylene glycol as a stabilizing agent, a lyophilized preparation and a process for producing them. The lyophilized preparation thus provided is easily restructured to an aqueous preparation using an aqueous medium.

Abstract: The present invention relates to a combination of a curcuminoid and a taxane for use in the treatment of a hormone-refractory prostate cancer (HRPC) in a patient in need thereof.

Abstract: Disclosed herein is a delivery composition for administering a hydrophobic active agent. In one embodiment, a delivery composition for local administration of a hydrophobic active agent to a tissue or organ of a patient is disclosed. In one embodiment, the delivery composition includes a cationic delivery agent, a therapeutically effective amount of a hydrophobic active agent and a pharmaceutically acceptable aqueous carrier. In one embodiment, the cationic delivery agent includes polyethyleneimine (PEI). In a more specific embodiment, the cationic delivery agent includes branched PEI. Methods of making the delivery composition, as well as kits and methods of use are also disclosed.

Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.

Abstract: The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefore. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug.