Abstract: The present invention relates to co-crystals, salts and crystalline forms of tenofovir alafenamide and methods for preparation, use and isolation of such compounds.

Abstract: The present invention relates to nanoparticles for encapsulating compounds, the preparation and uses thereof, said nanoparticles being based on half (C1-C4) alkyl esters of poly (methyl vinyl ether-co-maleic anhydride) (PVM/MA) copolymers. Said nanoparticles can encapsulate or incorporate a product of interest for use in the agricultural, cosmetic, food or pharmaceutical fields.

Abstract: The present application relates to novel 3-phenylpropionic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.

Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: This invention relates to a method for obtaining optically pure amino acids, including optical resolution and optical conversion. This method significantly shortens the time taken for optical transformation, and enables the repeated use of an organic solution containing a enantioselective receptor, to thereby obtain optically pure amino acids in a simple and remarkably efficient manner, and to enable the very economical mass production of optically pure amino acids.

Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, RAMALIN™, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the RAMALIN™, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the RAMALIN™ as an active ingredient. The RAMALIN™ according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.

Abstract: A method for manufacturing a composite is disclosed. The method includes steps of (a) providing a powder in a first weight ratio, a graphene oxide in a second weight ratio, a first modifying agent having a first electric charge, and a second modifying agent having a second electric charge; (b) reacting the first modifying agent with the powder so that a surface of the powder has the first electric charge; (c) reacting the second modifying agent with the graphene oxide so that a surface of the graphene oxide has the second electric charge; and (d) mixing the powder having the first electric charge and the graphene oxide having the second electric charge to form a composite, wherein the first and the second electric charges are of opposite electrical polarities.

Abstract: Aniline derivatives for anticancer treatment including a compound of the Formula 1, or a derivative thereof, as an active ingredient,

Abstract: The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR4R5, —NHC(?Y)R4, —NHC(?Y)NR5R?, —NHC(?O)OR4, —NHSO2R4, C(?Y)NR4R5, C(?O)OR6 [wherein Y is oxygen or sulphur], OR5, —O(C?O)NR4R5, O-acyl, S(O)mR4, —SO2N(R4)2, cyano, amidino or guanidino [wherein R4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R5 is hydrogen or R4; Rx is R4 or —SO2N(R4)2 and R6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR4, —OC(?O)NR4R5, O-acyl, NH2, NR4R5, —NHC(?Y)R4, —NHC(?Y)NR5Rx, —NHC(?O)OR4, —NHSO2R4, and to processes for t

Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.

Abstract: The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.

Abstract: Disclosed are oral care compositions, for example dentifrice compositions, comprising an oral care composition comprising an orally acceptable vehicle, metal oxide particles having an average particle size of no greater than a dentin tubule and at least one amino acid capable of chelating the metal oxide. The composition may comprise a polymeric adherent material for adhering the metal oxide particles in the dentin tubule. The metal oxide particles have a median particle size of 5 microns or less, and may comprise zinc oxide.

Abstract: A rubber composition obtained by kneading at least one selected from the group consisting of (A1), (B1), (C1) and (D1), a rubber component and a filler, and a method of improving the viscoelastic property of vulcanized rubber, comprising a first step of kneading at least one selected from the group consisting of (A1), (B1), (C1) and (D1), a rubber component, a filler and a sulfur component and a second step of thermally treating the kneaded material obtained in the previous step.

Abstract: The field involves compositions useful for pain relief, including diclofenac solution and gel formulations, in particular methods of use thereof, articles of manufacture and kits that provide novel preclinical, clinical and other information to users.

Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.

Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.

Abstract: This disclosure relates to methods and compositions for modulating disease resistance in plants and transgenic plants.

Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.

Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.

Abstract: The invention relates to an N-acyl anthranilic acid derivative or it's salt having collagen production inhibitory action.

Abstract: The invention relates to 3-[4-(phenylaminooxalylamino)phenyl]hex-4-ynoic acids, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3 and R4 are each defined as specified, and to physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

Abstract: Phenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The present invention relates to a compound of the general formula (III):

Abstract: The present application describes organic compounds of a general formula: and salts, and isomers thereof, wherein R, R2 and R3 are defined in the specification. The compounds are useful for treating a gram-negative bacterial infection.

Abstract: Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro brmobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.

Abstract: The present invention is directed to novel phenyloin derivative compounds and the use of such compounds as sodium channel blockers. Such compositions have utility as anti-cancer agents and can be used to limit or prevent PCa growth and/or metastasis.

Abstract: A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.

Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.

Abstract: A method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described in the general formula I below is administered in a therapeutically effective amount:

Abstract: The field involves compositions useful for pain relief, including diclofenac solution and gel formulations, in particular methods of use thereof, articles of manufacture and kits that provide novel preclinical, clinical and other information to users.

Abstract: The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. The compositions may be used in ophthalmic compositions and ophthalmic devices.

Abstract: A composition for treating damaged tissue and promoting healthy tissue growth, healing and tissue regeneration, wherein said composition comprises an extracellular matrix compound, a surface-active lipid, one or more enantiomerically pure L-amino acids or glycine, a hydrophilic surfactant with a high HLB, as well as vitamins, minerals or trace elements. Not only does it maintain good health, but the components are non-intrusive, bio-safe, non-coalescent and can mimic normally occurring stem-cells within a body. When applied to diseased tissues, the subject compositions can stimulate, facilitate, and accelerate protein synthesis for the regeneration of diseased organs and tissues. The healing efficacy of these tissue components gives us further appreciation of the protective action of human tissue over and above and other than the immune protective system or perhaps an integral component part of the immune system.

Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.

Abstract: A process for purifying at least one product from a substrate containing at least one product, includes subjecting the substrate to centrifugal partition chromatography in an ion exchange displacement mode to purify the at least one product from the substrate, the at least one product being an amphoteric product.

Abstract: The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.

Abstract: The invention relates to a process for separating, in an aqueous medium, at least one actinide element from one or more lanthanide elements by using at least one molecule which sequesters the said actinide element to be separated and membrane filtration, the said process successively comprising: a) a step of bringing at least one molecule which sequesters the said actinide element in contact with the aqueous medium, the said molecule not being retained in the non-complexed state by the said membrane and being capable of forming a complex with the actinide element to be separated, comprising the said element and at least two of the said sequestering molecules, which complex is capable of being retained by the membrane; b) a step of passing the aqueous medium over the membrane in order to form a permeate on one side, comprising an aqueous effluent depleted of the said actinide element, and a retentate comprising the said complex.

Abstract: The invention provides a helicene derivative, axially chiral amino acid, amine or amino alcohol derivative, and azaperylene, such as compounds represented by Formulae (I), (I?), (II), (II?), and (III): and a method for producing the same.

Abstract: Use is disclosed of (a) an AlDH-inhibitory amount of a Trp metabolite, or an analogue or derivative thereof or (b) a bioprecursor thereof, or (c) a potentiator of (a) and/or (b), in the preparation of a medicament for treating alcoholism and/or alcohol dependence.

Abstract: An anthranilic acid derivative represented by the general formula (X) [wherein R1 represents hydrogen or a carboxy-protecting group; R2 represents optionally substituted phenyl, a heterocyclic group, etc.; R3 represents optionally substituted phenyl, a monocyclic heterocyclic group, etc.; X1 represents carbonyl, etc.; X2 represents optionally substituted alkylene group, a bond, etc.; X3 represents oxygen, a bond, etc.; and X4 represents a group represented by the general formula —X5—X6— or —X6—X5— (wherein X5 means oxygen, a bond, etc.; and X6 means optionally substituted alkylene, a bond, etc.)] or a salt of the derivative. The derivative or salt has the inhibitory activity of MMP-13 production and is hence useful as a therapeutic agent for articular rheumatism, osteoarthritis, cancer, etc.

Abstract: The invention is concerned with novel anthranilic acid derivatives of formula (I) wherein R1 to R14, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.

Abstract: Compounds of the formula are disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: A composition includes ascorbate, zinc gluconate, and tropocollagen factors including L-proline, glycine and L-lysine. The composition contains the ascorbate, tropocollagen factors and zinc gluconate in concentrations effective to accelerate the production of collagen proteins within at least one collagen-containing tissue of an animal when administered to the animal. The at least one collagen-containing tissue includes at least one of cartilage tissue, tendon tissue, ligament tissue, vitreous humor tissue, connective tissue, hair tissue, bone tissue, and corneal tissue.

Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.

Abstract: Novel biaromatic compounds having the following structural formula (I): are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, in particular in dermatology as well as in the fields of cardiovascular diseases, immune diseases and/or diseases related to the metabolism of lipids, or, alternatively, into cosmetic compositions.

Abstract: The present invention discloses processes for the preparation and isolation of the individual stereoisomers of 1-amino, 3-substituted phenylcyclopentane-carboxylates.

Abstract: The present invention consists on the synthesis of new products for the treatment of the iron chlorosis. These products may have improved properties regarding the currently known treatments. The new products are non-symmetrical ethylene diamino hydroxyphenyl acetic acid derivatives possessing only five coordination sites able to chelate metals.

Abstract: Methods and compounds useful for inhibiting a phospholipase A2 are provided, the methods comprising contacting the phospholipase A2 with a compound having the structure A, or pharmaceutically acceptable salts thereof: wherein R1 is H, F, NH2, or COOH; R2 is, H, linear saturated or unsaturated alkyl, alkenyl, or alkynyl; each of R3 and R4 is independently H, linear saturated or unsaturated alkyl, alkenyl, alkynyl, phenyl, or substituted phenyl; R5 is H, (C1-C6) alkyl such as methyl or ethyl; X is aryl or substituted aryl, such as phenyl or a substituted phenyl; and Y is O or S.