Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: Structures and methods of making biodegradable trehalose co-polymers are disclosed. Specifically, biodegradable trehalose co-polymers consist of the general structure R5—[R1R2C—CR3R4]n-[DG]m—R6, wherein R1-R4 are independently selected from hydrogen or a side chain comprising at least one carbon atom, and wherein at least one of R1-R4 is a side chain comprising -L-trehalose, wherein L is a linker molecule that links trehalose to the monomer through at least one of the trehalose hydroxyl groups (—OH), wherein DG is a biodegradable group, and wherein R5 and R6 are end groups.

Abstract: The present application relates to imidazolidinecliones, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with the hypercitrullination of proteins by peptidyl arginine deiminase (PAD) enzymes. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: (I).

Abstract: The present invention provides for a slow release composition, preferably as a tablet, for industrial water systems, under an alkaline pH or high water hardness, using as an active ingredient a multifunctional amine of Formula (I) and a hydrophilic polymer, and other components such as a compression agent, in one composition as a biocide, biostat, biodispersant, deposit penetrant aid, organic deposit remover, detergent, surfactant, antifoam, scale inhibitor, scale remover, and a corrosion inhibitor. The composition is used in multiple water cycles, can remove, disperse or inhibit fouling. The active ingredient(s) of the composition is released over a long time, up to 6 months.

Abstract: A composition including a solution suitable for introduction into a blood vessel comprising particles including a treatment agent and a tunable stimuli-responsive polymer. A method including introducing a delivery device into a blood vessel; and introducing a solution into the blood vessel, the solution including particles comprising a treatment agent and a tunable stimuli-responsive polymer. A method including combining a treatment agent and a tunable stimuli-responsive polymer; and forming particles of the combination suitable for delivery through a blood vessel.

Abstract: Biocidally active cationic analogs of N-halamine having two biocidally active groups covalently bonded together in a single molecule and having general Formula (I). Compounds of Formula (I), and precursors thereof, can be in solution form immobilized onto a substrate via physical coating or covalent chemical bonding to functionalize surfaces or added into materials as additives so as to render them biocidal. The biocidal solutions and substrates comprising the compounds or precursors of the present invention can then be used to inactivate pathogenic microorganisms.

Abstract: The present invention is directed membrane active poly(vinyl ester) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cells in vivo. RNAi polynucleotides are conjugated to the poly(vinyl ester) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(vinyl ester) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.

Abstract: The present invention relates to compositions for the treatment of cancerous tissues in warm-blooded animals containing one or two anticancer agents attached to polymeric carriers having monomer units derived from one or more of N-(2-carboxypropyl)methacrylamide (2-CPMA), N-(3-carboxypropyl)methacrylamide (3-CPMA), N-(2-aminopropyl)methacrylamide (2-APMA) and/or N-(3-aminopropyl)methacrylamide (3-APMA) are also included. Anticancer agents in compositions can be attached to said polymeric carrier by side-chains which can be susceptible to hydrolysis by lysosomal enzymes intracellularly. Compositions can also include a targeting ligand attached to the polymeric carrier, optionally through a second linker.

Abstract: The present invention relates to branched polymer comprising a support moiety and at least three block co-polymer chains covalently coupled to and extending from the moiety, wherein: (i) each of the at least three block co-polymer chains comprise (a) a cationic polymer block that is covalently coupled to a hydrophilic polymer block, or (b) a cationic polymer block that is covalently coupled to a hydrophobic polymer block, said hydrophobic polymer block being covalently coupled to a hydrophilic polymer block; and (ii) at least one of said covalent couplings associated with each of said block co-polymer chains is biodegradable.

Abstract: The present invention provides random copolymers containing phosphorylcholine and one or more functional agents, and methods of preparing such random copolymers.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: Provided is a triblock copolymer represented by General Formula (I): CNR-PEG-CNR??(1) or a polycation thereof, wherein each CNR is independently a polymer segment having a repeating unit containing as part of a pendant group a cyclic nitroxide radical that binds to the polymer main chain via a linking group having at least one imino group or ether bond, and PEG is a segment containing poly(ethylene glycol).

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: Controlled-release formulations of carboxy-terminal C5a analogs (such as sustained-release formulations of the analogs), and their use in methods for treating and preventing an infection or a disease such as cancer, for directly killing microorganisms, for vaccine preparation, for inducing an immune response and for targeting antigen-presenting cells and other cells bearing a C5a receptor, are provided.

Abstract: A hyaluronic acid conjugates including hyaluronic acid, a disulfide bond-containing crosslinking agent, and a cationic, amphiphilic polymer; a hyaluronic acid-nucleic acid complex in which a nucleic acid is bound to the hyaluronic acid conjugate; a composition in which the hyaluronic acid-nucleic acid complexes are crosslinked with each other; a nucleic acid delivery composition including the hyaluronic acid-nucleic acid complex; and a method of nucleic acid delivery using the hyaluronic acid-nucleic acid complex.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes, coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof.

Abstract: Conjugates of hydroxypropyl methacrylamide (HPMA)-derived copolymers having attached thereto TNP-470 and a high load (e.g., higher than 3 mol %) of alendronate (ALN), and processes of preparing same are disclosed. Conjugates of polymers or copolymers having attached thereto an anti-angiogenesis agent and an oligoaspartate bone targeting agent, and processes of preparing same, are further disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment and monitoring of bone related disorders are also disclosed.

Abstract: A polymer composition including a polymer having a hydroxyl group and a histidine or a histidine derivative grafted to the polymer having a hydroxyl group. A polymer material is also provided, including a polymer composition which includes a polymer having a hydroxyl group, and a histidine or a histidine derivative grafted to the polymer having a hydroxyl group.

Abstract: A rotaxane consisting of a cucurbituril and an uncharged guest molecule, having low or null affinity therebetween is provided as well as processes for providing the same. Various uses as energy converters (“frictionless” molecular motors), biochips and biosensors using the same are also provided.

Abstract: The invention provides a novel system of nano-assemblies and related method for delivery of therapeutic, diagnostic or imaging agent to biological sites. The compositions and methods of the invention enable the syntheses of novel polymeric nano-assemblies (nanoparticles) under non-emulsion conditions with the incorporation of hydrophobic guest molecules. The versatilities and advantages of the polymer nanoparticles of the invention include: (i) the guest molecules (e.g.

Abstract: Conjugates of a polymer having attached thereto an angiogenesis targeting moiety and a therapeutically active agent such as an anti-cancer agent or anti-angiogenesis agent, and processes of preparing same are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of angiogenesis-related medical conditions such as cancer and cancer metastases are also disclosed.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: Particles and conjugates for delivering nucleic acid agents. Compositions containing the particles, the conjugates, or both. Methods of using the particles, the conjugates, and the compositions.

Abstract: The present invention provides nanogel formulations and methods of use thereof.

Abstract: The present disclosure provides inter alia conjugates of formula (I): wherein n, R1, R2, Rx, Z, X, Y and Z are as defined herein. A conjugate of formula (I) can also be converted to a conjugate of formulae (II) or (III) as described herein. Without limitation, the conjugates can be used to make controlled release materials and chemical sensors.

Abstract: Methods and compositions for controlled release of amine, alcohol and thiol drugs, e.g., narcotic analgesics, and tricyclic amine antidepressants, are provided. The drug is releasably covalently bonded to a polymer or other activity-blocking moiety. Release is by an unmasking reaction resulting in the formation of a chemical group that undergoes a second reaction releasing the drug. For example, the narcotic analgesic fentanyl covalently attached to an inert polymer by way of its nitrogen through formation of a quaternary vinylammonium salt is released by hydrolysis of an acetal exposing an alcohol that undergoes an intramolecular nucleophilic substitution reaction involving displacement of the fentanyl nitrogen. Process rate is controlled by controlling the rate of the intramolecular substitution reaction through varying the number of atoms in the chain connecting the alcohol group and the vinylic carbon and/or by the addition of substituents on that chain, and/or by the acetal hydrolysis rate.

Abstract: A composition for treating or preventing inflammatory-related conditions includes as an active principle a carrier which exhibits a plurality of a scavenger structure capable of mitigating the activity of a mediator of inflammatory-related conditions. The scavenger structure includes a nucleophilic centre complying with the formula X1(—R?—)(—R?)mHnwhere: a) X1 is a single-bonded heteroatom selected amongst N, O and S and exhibits a free electron pair; b) m is 0 or 1 and n is 1 or 2; c) —R?— is a bivalent organic group providing attachment to the carrier via one of its free valences and to X1 at the other free valence; and d) R?— is a monovalent organic group attached to the X1 via its free valence. A method for treating or preventing inflammatory-related conditions in an individual suffering from such conditions includes: providing the composition; and contacting the mediator within or separate from the individual.

Abstract: The disubstituted piperazine analogs (DPAs) derivative compound and DPAs amine complex compound disclosed in the present aspects have characterized by presented pharmaceutics having functions to improve lipolysis, such as inhibiting obesity hyperlipidemia, and atherosclerosis.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: A method for treating a disease is provided. The method includes steps of: providing a subject in need thereof; and administering one selected from a group consisting of KMUPS compound represented by formula I, a pharmaceutically acceptable salts thereof; and a pharmaceutical composition thereof to the subject in a dosage from 1 to 2.5 milligram per kilogram of body weight, wherein R2 and R4 are each selected independently from a group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group and a halogen atom.

Abstract: An implantable device including a conjugate formed of an acrylamide-based copolymer and a bioactive agent is provided.

Abstract: The present invention relates to siRNA hydrogel and a method for manufacturing the same, and more particularly, to siRNA hydrogel for targeted gene silencing, which is nano-structured for targeted gene silencing, and a method for manufacturing the same.

Abstract: The present invention provides random copolymers containing phosphorylcholine and one or more functional agents, and methods of preparing such random copolymers.

Abstract: This invention relates to compositions, and related methods, of synthetic nanocarriers that comprise polymers that comprise at least two immunomodulatory agent moieties.

Abstract: Cationic polymers hydrolyzable to zwitterionic polymers, monomers for making the cationic polymers, surfaces that include the polymers, therapeutic agent delivery systems that include the cationic polymers, methods for administering a therapeutic agent using the delivery systems, and methods for making and using the cationic polymers, monomers, surfaces, and therapeutic agent delivery systems.

Abstract: An inhibiting heart failure disease pharmaceutical composition is provided. The pharmaceutical composition includes: an effective amount of a KMUP-3 amine salt of formula (I); wherein RX contains a carboxylic group donated from one selected from a group consisting of a sodium carboxyl methylcellulose (sodium CMC), a ?-polyglutamic acid derivative, and co-polymer salt; RX? is an anion form of the carboxylic group; and a pharmaceutically accepted carrier.

Abstract: We provide methods and compositions for the treatment of dysregulation of blood vessel growth by regulation of neovascularization. Embodiments accomplish this by restricting the diffusion and transport of therapeutic agents through conjugating them to polymers or polymer constructs while retaining the binding affinities and functions of the therapeutic agents.

Abstract: Disclosed herein are novel siRNA-cochleate and morpholino-cochleate compositions. Also disclosed are methods of making and using siRNA-cochleate and morpholino-cochleate compositions.

Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

Abstract: The synthesized piperazium salt of KMUPs disclosed in the present invention is characterized by presented pharmaceutics having functions to improve 5-HT function and eNOS expression of KMUPS in lung diseases, such as proliferation, obliteration, pulmonary artery hypertension. The pharmaceutical composition for inhibiting monocrotaline (MCT)-induced proliferation of pulmonary artery includes an effective amount of a complex salt of formula (I): wherein R2 and R4 are each selected independently from the group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group, and a halogen atom; RX contains a carboxylic group donated from one selected from a group consisting of a Statin, a Co-polymer, a poly-?-polyglutamic acid (?-PGA) derivative and sodium CMC; and ?RX substituent is an anion of the carboxylic group carrying a negative charge; and a pharmaceutically accepted carrier.

Abstract: The present invention is directed to compounds, compositions, and methods useful for delivering polynucleotides or other cell-impermeable molecules to mammalian cells. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery vehicles. The use of multiple reversible or labile linkages connecting component parts provides for physiologically responsive activity modulation.

Abstract: The invention provides TLR agonists and conjugates thereof useful in vaccines and to prevent, inhibit or treat a variety of disorders including pathogen infection and asthma.

Abstract: Methods and compositions for controlled release of amine, alcohol and thiol drugs, e.g., narcotic analgesics, and tricyclic amine antidepressants, are provided. The drug is releasably covalently bonded to a polymer or other activity-blocking moiety. Release is by an unmasking reaction resulting in the formation of a chemical group that undergoes a second reaction releasing the drug. For example, the narcotic analgesic fentanyl covalently attached to an inert polymer by way of its nitrogen through formation of a quaternary vinylammonium salt is released by hydrolysis of an acetal exposing an alcohol that undergoes an intramolecular nucleophilic substitution reaction involving displacement of the fentanyl nitrogen. Process rate is controlled by controlling the rate of the intramolecular substitution reaction through varying the number of atoms in the chain connecting the alcohol group and the vinylic carbon and/or by the addition of substituents on that chain, and/or by the acetal hydrolysis rate.

Abstract: A new technique to stabilize transition metal phosphors in a wide variety of stimuli-sensitive polymers and gels is disclosed herein. Other than stabilization in stimuli sensitive/biocompatible matrix some of these transition metal based phosphors are also shown to act as phosphorescent crosslinkers that physically or chemically crosslink polymeric chains to form micro/nanoparticles. The microspheres/nanospheres of the present invention show decreased size and photoluminescence enhancement with particularly high sensitization at physiological pH and temperature. The so formed phosphorescent micro/nanospheres are useful for biological or environmental applications including biological labeling, imaging, and optical sensing. The techniques in the present invention enable usage of imaging agents and sensors at very low concentrations and also minimize or eliminate the usage of toxic chemical crosslinkers typically used to synthesize polymeric micro/nanoparticles.

Abstract: The present disclosure provides inter alia conjugates of formula (I): wherein n, R1, R2, Rx, Z, X, Y and Z are as defined herein. A conjugate of formula (I) can also be converted to a conjugate of formulae (II) or (III) as described herein. Without limitation, the conjugates can be used to make controlled release materials and chemical sensors.