Abstract: The present invention relates to a method of identifying candidate compounds useful as chemotherapeutics or anti-infective compounds or anti-inflammatory drugs. This method involves providing a plurality of test compounds. The plurality of test compounds are incubated with human Regulatory T (Treg) cells expressing Disc-Large Homo log 1 (Dlgh1) or in which Dlgh1 is suppressed, where the Treg cells have an immunological synapse (IS). Test compounds which inhibit Dlgh1 expression, recruitment to the IS, and/or activity in the Treg cells are identified as candidate compounds potentially useful as chemotherapeutics or anti-infective compounds. Test compounds which enhance Dlgh1 recruitment to the IS and/or activity in the Treg cells are identified as candidate compounds potentially useful as anti-inflammatory drugs. The present invention also relates to methods of treating inflammatory conditions, cancers, and infectious diseases in a subject, as well as methods of inhibiting Treg cell activity.

Abstract: The present invention provides siRNAs for inhibiting the expression of plk1 gene, and the method for inhibiting the expression of plk1 gene in mammalian cells. The siRNAs of the present invention have the double-stranded structure, and said double-stranded structure is composed of the first single strand and the second single strand that are fully complementary, wherein the sequence of said first single strand is the same as the target sequence within the sequence as shown in SEQ ID NO: 1, and the sequence of said second single strand is complementary to the target sequence within the sequence as shown in SEQ ID NO: 1. The siRNAs of the present invention can sequence specifically mediate the inhibition of plk1 gene expression, and have a good serum stability. By the introduction of the siRNAs of the present invention into the tumor cells, the expression of plk1 gene can be effectively inhibited, and the growth of tumor cells is inhibited and the apoptosis of tumor cells is promoted.

Abstract: This invention relates to modified short interfering RNA (siRNA) nucleic acid molecules, particularly siRNA's which have been modified by the addition of a 2-0-guanidinopropyl (GP) modified nucleoside. In particular the invention relates to modified siRNAs which are capable of silencing target sequences, methods of treating and preventing infection by using the siRNAs, medicaments containing the siRNAs and use of the siRNAs.

Abstract: An approach to identify and evaluate potential insecticide targets using publicly available genome (DNA) sequence information for arthropod disease vector is provided. The utility of this approach is demonstrated by first determining the molecular and pharmacological properties of two different dopamine (neurotransmitter) receptors identified in the genome of the yellow fever- and dengue-transmitting mosquito, Aedes aegypti. Next, different chemistries were tested for their ability to interact with one of these dopamine receptors in a chemical compound screen, and “hit” compounds were identified. Finally, it is shown that some of these chemistries, are selective for the mosquito over the human dopamine receptor and that these chemistries caused significant mortality in mosquito larvae 24 hours after exposure.

Abstract: The invention provides, in one aspect, peptides and a complex comprising one of the peptides and a cargo molecule, wherein the peptide and the cargo molecule are coupled by non-covalently. The peptides of the invention were found to facilitate the delivery of siRNA molecules into cells and to function in siRNA mediated silencing of cellular targets.

Abstract: A process is provided of introducing an RNA into a living cell to inhibit gene expression of a target gene in that cell. The process may be practiced ex vivo or in vivo. The RNA has a region with double-stranded structure. Inhibition is sequence-specific in that the nucleotide sequences of the duplex region of the RNA and of a portion of the target gene are identical. The present invention is distinguished from prior art interference in gene expression by antisense or triple-strand methods.

Abstract: The invention generally features compositions and methods that are useful for modulating angiogenesis.

Abstract: This invention relates to a composition and its use for formulating nucleic acid-based drugs/vaccines with sugar alcohol compositions into complexes for both in-vitro and in-vivo delivery. Particularly, the present invention includes the ingredients and processes necessary for formulating therapeutic and pharmaceutical nucleic acid compositions, such as miRNA, microRNA precursors, shRNAs, siRNAs, ribozymes, antisense RNAs/DNAs, RNA-DNA hybrids and DNA vectors/vaccines, with glycylated sugar alcohols/sugars into delivery complexes, which can then be absorbed by cells in vivo and in vitro via active endocytosis. Also, the present invention discloses that chemical compounds containing sugar alcohol- and/or sugar-like structures can protect nucleic acids, in particular miRNAs, shRNAs, siRNAs and ribozymes, from degradation in vivo as well as in vitro.

Abstract: The present invention concerns methods and compositions for introducing miRNA activity or function into cells using synthetic nucleic acid molecules. Moreover, the present invention concerns methods and compositions for identifying miRNAs with specific cellular functions that are relevant to therapeutic, diagnostic, and prognostic applications wherein synthetic miRNAs and/or miRNA inhibitors are used in library screening assays.

Abstract: Provided herein are non-viral nucleic acid vectors, including non-viral oncovectors, that are autonomously replicating plasmids (ARPs). The non-viral nucleic acid vectors exhibit fusogenic activity and can exhibit other anti-tumor or cytotoxic activities. Also provided herein are methods and uses of the non-viral nucleic acid vectors for treating cancer.

Abstract: The present invention is related to a method for generating a nucleic acid molecule capable of binding to a target molecule comprising the following steps: a) providing a reference nucleic acid molecule, wherein the reference nucleic acid molecule is capable of binding to the target molecule and wherein the reference nucleic acid molecule comprises a sequence of nucleotides, wherein the sequence of nucleotides comprises n nucleotides; b) preparing a first level derivative of the reference nucleic acid molecule, wherein the first level derivative of the reference nucleic acid molecule differs from the reference nucleic acid molecule at one nucleotide position, wherein the first level derivative is prepared by replacing the ribonucleotide at the one nucleotide position by a 2?-deoxyribonucleotide in case the reference nucleic acid has a ribonucleotide at the nucleotide position and wherein the first level derivative is prepared by replacing the 2?-deoxyribonucleotide at the one nucleotide position by a ribonucl

Abstract: The present invention is directed to a synthetic nucleic acid sequence which encodes a protein wherein at least one non-common codon or less-common codon is replaced by a common codon. The synthetic nucleic acid sequence can include a continuous stretch of at least 90 codons all of which are common codons.

Abstract: Described herein are compositions and methods for the inhibition of miR-122 activity. The compositions have certain nucleoside modifications that yield potent inhibitors of miR-122 activity. The compounds may comprise conjugates to facilitate delivery to the liver. The compositions may be administered to subjects infected with hepatitis C virus, as a treatment for hepatitis C virus and related conditions.

Abstract: The invention provides highly concentrated chitosan-nucleic acid polyplex compositions and dispersions, and methods for producing the compositions and dispersions. Methods of mixing the chitosan-nucleic acid polyplexes include an inline mixing of chitosan solution and nucleic acid solution, followed by further concentrating the dispersion of chitosan-nucleic acid polyplexes, optionally with an aggregation inhibitor. Further provides are methods for altering the diameter of chitosan-nucleic acid polyplexes.

Abstract: The intermolecular mutual recognition between a disease-state inducing substance (e.g., allergen group, pathogen et cetera) and a living body which functions at the time when such a disease-state inducing substance reaches the living body is inhibited by making use of pectins and nucleic acids.

Abstract: Disclosed are methods of treating an animal for insulin resistance and associated diseases or conditions, activating the transcriptional activity of heat shock factor 1 (HSF1), or inducing the expression of heat shock protein 70 (HSP70) in an animal in need thereof, wherein the methods involve administering an effective amount of one or more compounds of formula (I) or an epimer thereof, wherein Ar, and R1-R6 are described herein. Examples of diseases or conditions associated with insulin resistance include diabetes, obesity, inflammation, metabolic syndrome, polycystic ovary disease, arteriosclerosis, non-alcoholic fatty liver disease, reproductive abnormality in a female, and growth abnormality.

Abstract: A solid composition which contains a large amount of catechins and has solved problems concerning quality and producibility for exerting useful action and effects derived from catechins. The solid composition contains catechins and glycerol.

Abstract: Equatorial 2,3-fluorinated glycosides compounds of formula (I) useful for the treatment or prophylaxis of viral infection, particularly viral influenza, the methods for their preparation, and their pharmaceutical compositions. The therapeutic effect is achieved via inhibition of viral neuraminidases.

Abstract: The present invention provides a method for preparing antrocin of pharmaceutically acceptable salts thereof via a series of gold-catalyzed cyclization to construct the (6-6-5) tricyclic core frame. The present invention also provides a use of a composition in preparing drugs for suppressing growth of non-small cell lung cancer cells, wherein the composition comprises an effective amount of antrocin or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier.

Abstract: There is provided a method for the prevention and/or treatment of hypotension associated with hemodialysis, which method includes administering to a subject in need thereof an effective amount of at least one physiologically compatible compound which, in combination with iron, binds nitric oxide. There is further provided a method for identifying hemodialysis subjects for whom treatment with an effective amount of at least one physiologically compatible compound which, in combination with iron, binds nitric oxide is indicated. The method includes monitoring the subject's nitric oxide levels, and selecting those subjects having elevated nitric oxide levels for treatment with an effective amount of at least one physiologically compatible compound which, in combination with iron, binds nitric oxide, wherein the effective amount is sufficient to maintain the subject's nitric oxide levels within an acceptable range.

Abstract: This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic

Abstract: Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula I: in which: the dotted line represents a single or a double bond; and R5 and R5? are independently —H, —OH or —OR6, where R6 is a linear or branched C1-C4 alkyl; X is —CH2O—; Z is —CH2CH2O—, —CH(CH3)CH2O— or —CH2CH(CH3)O—; m is 1; and n is an integer of 1-5. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.

Abstract: The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor.

Abstract: Substantially anhydrous topical gel compositions comprising a homogeneous mixture of: (a) ingenol-3-angelate in dissolved form; and (b) anon-aqueous carrier.

Abstract: This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Abstract: A method of decreasing intraocular pressure (IOP) in an eye of a patient in need thereof includes implanting a first lacrimal implant through a firsts punctum and into a first lacrimal canaliculus of the eye of the patient. The method may further comprise implanting a second lacrimal implant through a second punctum and into a second lacrimal canaliculus of the eye of the patient, and releasing, on a sustained basis a therapeutically effective amount of an intraocular pressure-reducing therapeutic agent.

Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V) or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1 —SR2 or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.

Abstract: Beta-hydroxybutyrate mineral salts in combination with medium chain fatty acids or an ester thereof such as medium chain triglycerides were used to induce ketosis, achieving blood ketone levels of (2-7 mmol/L), with or without dietary restriction. The combination results in substantial improvements in metabolic biomarkers related to insulin resistance, diabetes, weight loss, and physical performance in a short period of time. Further, use of these supplements to achieve ketosis yields a significant elevation of blood ketones and reduction of blood glucose levels. Use of these substances does not adversely affect lipid profiles. By initiating rapid ketosis and accelerating the rate of ketoadaptation, this invention is useful for the avoidance of glucose withdrawal symptoms commonly experienced by individuals initiating a ketogenic diet, and minimizes the loss of lean body mass during dietary restriction.

Abstract: Compositions and methods for urea silicone gels for treating skin conditions that may benefit from barrier protection and from urea silicone gel ability to return water balance to the skin are disclosed. Skin conditions that may be treated with urea silicone gel may be excessive dryness, insect bites, keloids and scars, among others. Disclosed urea silicone gel may include micronized urea USP, an anhydrous silicone base, and a PEG ointment base, among other ingredients. Anhydrous silicone base may include Amazonian oils such as pracaxi oil and seje oil, which are rich in oleic, linolenic, linoleic acids, and sterols, particularly beta-sitosterol and stigmasterol that may increase skin permeability to urea. PEG ointment base may be water-washable and includes meadowsweet extract. Additionally, PEG urea silicone gel may provide occlusion, and may maintain a moist environment within the skin condition which allows optimal healing. Pain also may be decreased by maintaining a moist environment.

Abstract: The present invention provides a therapeutic treatment for a neurodegenerative disease with a pan-PPAR agonist, such as bezafibrate. In particular, the present invention provides that pan-PPAR agonists enhance PPAR related responses in both the central nervous system and peripheral tissues in Huntington's Disease (HD) and tauopathy. Therapeutic compositions comprising one or more pan-PPAR agonist(s), and kit thereof, for treating a neurodegenerative disease or disorder are also provided.

Abstract: Method for preventing paresthesia in a human is disclosed. The method includes administering to the human an effective amount of N-Acetyl Beta Alanine or an N-Acetyl Beta Alanine composition.

Abstract: Method for increasing beta alanine absorption and cell membrane permeability through both passive diffusion and active transport in a human is disclosed. The method includes administering to the human an effective amount of N-Acetyl Beta Alanine or an N-Acetyl Beta Alanine composition.

Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.

Abstract: Methods for treatment of and prophylaxis against hemorrhoids are disclosed, including methods of treatment of and prophylaxis against hemorrhoids comprising administering naproxen to an individual.

Abstract: The present invention relates to novel 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising the same and therapeutic uses thereof, in particular in the fields of human and animal health. The compounds according to the present invention have intrinsic PPAR agonist properties. They are therefore of particular interest in the treatment of metabolic and/or inflammatory diseases and particularly peripheral and central diseases associated with the metabolic syndrome, such as diverse forms of steatohepatitis, type 2 diabetes, diverse neurodegenerative disorders, such as Alzheimer's disease, Parkinson's disease and multiple sclerosis.

Abstract: Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD-556.

Abstract: The invention is directed to formulations of pharmaceutical compounds, such as the Cyclohexylamines and Aminoadamantanes which have antimicrobial properties. In particular, it is directed to aqueous based formulations with reduced amounts of preservatives which allow safe and convenient administration and flexible dosing and which, in the case of oral formulations, are easy to swallow. Optionally, the compositions contain components that provide the requisite stability and shelf life while reducing or avoiding incrustation of the composition around the container closure which leads to leaks and difficulty in opening the container.

Abstract: At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.

Abstract: The invention provides methods for enhancing histone acylation, learning, memory and/or cognition in subjects with compound (I) or compositions comprising compound (I), or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure describes a topical scar treatment composition that may include tamoxifen citrate in a concentration of about 0.01% by weight to about 1% by weight, with about 0.1% by weight being preferred, and an anhydrous silicone base for enhancing skin permeation and scar removing effects, in a concentration of about 10% by weight to about 100% by weight, with about 100% being preferred being preferred. The small concentration of tamoxifen citrate may prevent dangerous side effects and may be successful in treating abnormal scars such as keloids and hypertrophic scars.

Abstract: The present invention relates to improved topical gel compositions comprising an active agent, and uses thereof.

Abstract: An ophthalmic composition comprising geranylgeranylacetone which (a) is a mixture of (5E,9E,13E)-geranylgeranylacetone and (5Z,9E,13E)-geranylgeranylacetone, the (5E,9E,13E)-geranylgeranylacetone content of the mixture being 80% by weight or more, (b) consists of (5E,9E,13E)-geranylgeranylacetone, or (c) consists of (5Z,9E,13E)-geranylgeranylacetone protects various types of retinal cells from degeneration, impairment or destruction, thereby remarkably promoting the survival. Consequently, the composition exhibits a remarkable effect of preventing, ameliorating or treating various retinal diseases. In addition, the composition hardly becomes white turbid during storage.

Abstract: A substantially anhydrous topical composition comprises a homogenous mixture of (a) a therapeutically effective amount of an ingenol derivative in dissolved form; (b) an oily solvent for the ingenol derivative, (c) an acidic compound, and (d) optionally a pharmaceutically acceptable non-solvent lipid carrier.

Abstract: The present invention relates to an antimicrobial composition and a method for disinfection involving the antimicrobial composition. It particularly relates to an antimicrobial composition for personal cleaning, oral care or hard surface cleaning applications. It was found that compositions comprising one or more monosubstituted phenols, terpineol and a carrier provide synergistic antimicrobial action. In a preferred aspect the composition also comprises 1 to 80%-wt of one or more surfactants.

Abstract: The present invention relates to an antimicrobial composition and a method for disinfection involving the antimicrobial composition. It particularly relates to an antimicrobial composition for personal cleaning, oral care or hard surface cleaning applications. It was found that compositions comprising thymol, selected propen-2-yl-methyl-cyclohexanols, and a carrier provide synergistic antimicrobial action. In a preferred aspect the composition also comprises 1 to 80%-wt of one or more surfactants.

Abstract: Described are methods of dispersing and hydrating a water soluble polymer, comprising forming a nonaqueous slurry of polypropylene glycol, water soluble polymer, and hydrophobically modified ethoxylated urethane, provided that the slurry contains less than five percent water; and then contacting the nonaqueous slurry with water to disperse and hydrate the water soluble polymer.

Abstract: The invention provide a class of linear chain-extended polysiloxane crosslinkers which comprises two terminal ethylenically unsaturated groups, at least two polysiloxane segments, and dangling hydrophilic polymer chains each covalently attached to a divalent organic radical separating each pair of adjacent polysiloxane segments. The present invention is also related to a polymer comprising crosslinking units derived from chain-extended polysiloxane crosslinker of the invention and to ophthalmic lenses comprising such a polymer.

Abstract: An oil-in-water emulsion includes: 5 to 55 wt % of an oil phase consisting of at least one oil and/or one wax; 0.06 to 4.5 wt % of at least one cross-linked anionic polyelectrolyte resulting from the polymerization of at least one monomer having a strong acid function, the monomer being partially or totally salified 2-methyl 2-[(1-oxo 2-propenyl)amino] 1-propanesulfonic acid, with at least one neutral monomer selected from the N,N-dialkyl acrylamides, wherein each of the alkyl groups include between one and four carbon atoms, and at least one monomer of formula (I), where R is a straight or branched alkyl radical including eight to twenty carbon atoms and 1?n?20, in the presence of at least one cross-linking agent; and 0.0025 to 1 wt % of xanthan gum; 0.0025 to 1 wt % acacia gum; 38.5 to 94.835 wt % of a cosmetically acceptable aqueous phase.

Abstract: A linear, branched or cross-linked anionic polyelectrolyte, resulting from the polymerisation, for 100 molar percentage: a) 50% to 99% of monomeric units including a strong, free and partially or completely salified acid function ; b) 1% to 50% of a monomeric units of formula (I): CH2?CH(R1)-C(=0)-0-(CH2)n-CF3 (I), wherein R1 represents H or CH3, and n is 1, 2 or 3; c) optionally greater than 0% to 5% of monomeric units of formula (II): R2-C(=0)-0-[(CH2-CH(R4)-0]m-R3 (II), wherein m is 0 to 50, R2 represents an unsaturated aliphatic monovalent radical with 2 to 4 carbon atoms, R4 represents H, CH3 or CH3CH2 and R3 represents a linear or branched, saturated or unsaturated hydrocarbon aliphatic radical with 8 to 30 carbon atoms, and d) optionally greater than 0% to 5% of at least one monomer with diethylenic or polyethylenic cross-linking. The use thereof as a thickener in topical compositions.

Abstract: The present disclosure provides colorant compounds and methods of isolation of the colorant compounds derived from a reaction of genipin and an amine. The colorant compositions comprise purified compounds (e.g., a purified polymer or a purified dimer) obtained from multiple fractioning by chromatography of the reaction resulting material. The purified polymer or dimer can be used as a colorant by itself or in combination with another colorant for imparting color to a food, a drug, a cosmetic, a medical device, and textile products.