Abstract: In one aspect, the present disclosure provides compounds of the formula (I): In other aspects, the present disclosure provides compositions and methods of targeting GPER for the treatment of cancers, such as breast cancers and leukemias, gallstone disease, cardiovascular disease, and for conferring of neuroprotection on a subject. Also disclosed are high throughput assays for identifying antagonists of GPER.

Abstract: An açai berry seed extract (açai palm fruit, Euterpe oleracea) and a process for obtaining the seed extract is provided which has an effect in the treatment of diseases or disorders individually or jointly related to the metabolic syndrome. A process is also provided for obtaining an açai berry seed extract or a fraction thereof, and a pharmaceutical and a food composition is provided for treating diseases or disorders individually or jointly related to the metabolic syndrome. A method for treating diseases or disorders individually or jointly associated with metabolic syndrome in humans or animals is also provided.

Abstract: Biologically active cannabidiol analogs comprising a compound of the formula wherein one of R1 or R2 or both is/are the residue of a moiety formed by the reaction of an amino group of the amino acid ester of R1 or R2 or both with a dicarboxylic acid or a dicarboxylic acid derivative and the other R1 or R2 (in the case of the mono) is the residue of a dicarboxylic acid or dicarboxylic acid derivative or Hydrogen (H), (i.e. underivatized), and salts thereof. These CBD analogs are be useful in pain management in oncology and other clinical settings in which neuropathy is presented. Furthermore, these CBD-analogs are useful in blocking the addictive properties of opiates.

Abstract: A method of preparing ?-hydroxycarboxylic acid ester comprises mixing an alkylene oxide, a monohydric alcohol and a composite catalyst, and performing a carbonylation esterification reaction in a carbon monoxide atmosphere to obtain the ?-hydroxycarboxylic acid ester. The composite catalyst comprises a main catalyst, a cocatalyst and a reducing agent. the main catalyst is at least one of a cobalt salt, cobalt oxide and cobalt hydroxide. The cocatalyst is a nitrogen-containing heterocyclic compound. The reducing agent is a base metal. The method is an atomic reaction type process, does not produce three wastes, and has high conversion rate. It is a green environmental protection process. The composite catalyst used does not contain Co2(CO)8. The raw materials and catalyst used are all cheap and easily available. The composite catalyst can be used repeatedly at a lower cost, and is suitable for industrial applications.

Abstract: The use of a granulated xanthan gum comprising, relative to 100% by mass of the granulated xanthan gum: xanthan gum granules having a degree of hardness of 2 N or higher and lower than 8 N in an amount of 5% by mass or higher; and xanthan gum granules having a degree of hardness of 8 N or higher in an amount of 20% by mass or lower makes it possible to provide a granulated xanthan gum and a thickening composition comprising the granulated xanthan gum which undergo suppressed formation of unmixed lumps in a wide variety of water-containing foods such as water, teas, refreshing beverages, dairy beverages, soups, and thick liquid foods, even when the xanthan gum concentration is 50% by mass or higher.

Abstract: Single walled carbon nanotubes can be synthesized and production efficiency of carbon nanotubes can be enhanced by a method including a supplying step (S11) in which particulate carriers are supplied into a drum, a sputtering step (S12) for supporting a catalyst, in which sputtering is performed while this drum 10 is rotated around the axis and is swung so that one end portion and the other end portion in the axial direction of the drum 10 are relatively vertically switched, and a recovering step (S13) in which the particulate carriers are recovered by inclining the drum to discharge the particulate carriers from the drum.

Abstract: Single walled carbon nanotubes can be synthesized and production efficiency of carbon nanotubes can be enhanced by a method including a supplying step (S11) in which particulate carriers are supplied into a drum, a sputtering step (S12) for supporting a catalyst, in which sputtering is performed while this drum 10 is rotated around the axis and is swung so that one end portion and the other end portion in the axial direction of the drum 10 are relatively vertically switched, and a recovering step (S13) in which the particulate carriers are recovered by inclining the drum to discharge the particulate carriers from the drum.

Abstract: The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.

Abstract: Provided is a method of depolymerizing polyesters from post-consumer products, such as beverage bottles, to produce a high purity reaction product. For the depolymerization reaction, the polyesters are reacted with an alcohol having 2 to 5 carbons and an amine organocatalyst at a temperature of about 150° C. to about 250° C. In one application, the use an organocatalyst with a boiling point significantly lower than the boiling point of the reactant alcohol allows for the ready recycling of the amine organocatalyst. In another application, performing the depolymerization reaction under pressure at a temperature above that of the alcohol allows for accelerated depolymerization rates and the recovery of the organocatalyst with no further heat input.

Abstract: To provide a composition for hair growth (hair growth agent) which has high hair growing effects and can be used for prevention or treatment of alopecia. The composition for hair growth comprises as an active ingredient at least one member selected from the group consisting of a compound represented by the formula (1) and a salt thereof. In the formula, R is a carboxy group or an alkoxycarbonyl group.

Abstract: Provided is an optical film used for the optical compensation, in which additives are added to thereby have a good stability at high temperature and high humidity, a higher chromaticity, a higher Haze and a higher moisture resistance, as well as a small thickness direction retardation (Rth).

Abstract: A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.

Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.

Abstract: The present invention relates to biodegradable polymers (e.g., polyesters and polyester amides) derived from functionalized biologically active compounds that can provide site specific delivery of bioactive compounds upon biodegradation in a controlled manner.

Abstract: The present invention discloses polyester-polyether polyols suitable for blending with other polyols or other materials mutually compatible with the polyester polyols to achieve polyurethane and polyisocyanurate products. In particular the present invention discloses polyester-polyether polyols produced by the reaction of: 1) phthalic anhydride with an alcohol having a nominal functionality of 3 and a molecular weight of 90 to 500 under conditions to form a phthalic anhydride half-ester; and 2) alkoxylating the half-ester formed in step 1 to form a polyester-polyether polyol having a hydroxyl number of from 200 to 350; with the proviso when the alcohol is a polyether polyol, the polyether polyol contains at least 70 weight percent of polyoxypropylene.

Abstract: The present invention includes the use of pelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIP 1 activity. This invention also provides novel terpene compounds capable of modulating SHIP 1 activity and methods of synthesis thereof.

Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.

Abstract: The present invention relates to biodegradable polymers (e.g., polyesters and polyester amides) derived from functionalized biologically active compounds that can provide site specific delivery of bioactive compounds upon biodegradation in a controlled manner.

Abstract: The present invention relates to a novel process for preparing substituted and unsubstituted (2,4-dimethylbiphenyl-3-yl)acetic acids and their esters of the formula (I) using homogeneous and heterogeneous palladium catalysts, and also the intermediates 4-tert-butyl-2,6-dimethylphenylacetic acid and 4-tert-butyl-2,6-dimethylmandelic acid, and to processes for their preparation.

Abstract: The present invention discloses a method of purification of prostaglandins including fluorine atoms by using preparative HPLC. Tafluprost and Travoprost are prostaglandins including fluorine. The chemical structure of the impurities in crude Tafluprost and crude Travoprost also contain fluorine, therefore, the removal of the impurities is difficult. Purification by using preparative high performance liquid chromatography (HPLC) can achieve high-quality liquid bulk drugs.

Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.

Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.

Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.

Abstract: Compounds of the formula (I) in the form of a mixture of predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1??(I), wherein: Z1 is a C-bonded, secondary phosphine group of the formula —P(R)2, wherein R is a hydrocarbon radical or O-atom(s)-containing heterohydrocarbon radical having 1 to 18 carbon atoms and optionally substituted by C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, trifluoromethoxy, (C1-C4-alkyl)2-amino, (C6H5)3Si, (C1-C12-alkyl)3Si or halogen; Q is selected from the group consisting of: (i) an optionally substituted achiral aromatic group, wherein the achiral aromatic group is bonded directly to Z1 through a carbon atom of the achiral aromatic group and bonded directly to P*R0R1 through a carbon atom of the achiral aromatic group, and (ii) an optionally substituted C1-C4-alkylene group; P* is a chiral phosphorus atom; R0 is methyl; and R1 is a C-bonded optically enriched or optically pure chiral, mono- or polycyclic, nonaromatic hydrocarbon ring; and prepar

Abstract: The present invention relates to a chiral spiro-pyridylamidophosphine ligand compound, synthesis method therefor and application thereof. The chiral spiro-pyridylamidophosphine compound is a compound having a structure of Formula (I), a racemate or optical isomer thereof, or a catalytically acceptable salt thereof, and is mainly characterized by having a chiral spiro-dihydro-indene skeleton in its structure. The chiral spiro-pyridylamidophosphine compound may be synthesized with optical active 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene or substituted 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene having a spiro-skeleton as chiral starting material. The chiral spiro-pyridylamidophosphine compound may be used as a chiral ligand in asymmetric hydrogenation of a carbonyl compound catalyzed by iridium, in which the reaction activity is very high, the amount of the catalyst may be 0.0001 mol %, and the enantioselectivity of the reaction is up to 99.9% ee.

Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.

Abstract: The present invention relates to a process for synthesizing a multifunctional compound, including the reaction of a compound of formula (II) with atmospheric or molecular oxygen, in the presence of at least one aldehyde of formula (III), and optionally in the presence of at least one catalyst or at least one radical initiator; wherein: R10, R20, R30, R40, R50, L2, R60, R7, R8, and R9 are as described in the claims. The invention also relates to the use of these compounds as monomers for the preparation of polyurethane. The invention also relates to the use of these compounds as monomers of polymers or of biopolymers.

Abstract: The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.

Abstract: The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF2?-series, including latanoprost, travoprost, and bimatoprost, which are active pharmaceutical ingredients used for the reduction of elevated intra-ocular pressure in patients with glaucoma and ocular hypertension.

Abstract: Conjugates comprising at least two active agents linked by a diglycolic acid or polyglycol diacid linker are disclosed. The invention also concerns oligomers and polymers of these conjugates and their use in therapeutic and industrial applications for localized, immediate or fast release delivery of an active agent, such as an anti-microbial, anti-infective, or antiseptic agent.

Abstract: Fatty acid conjugates of salicylate derivatives and compositions thereof are disclosed. Further disclosed are methods for treating various diseases comprising the administration of an effective amount of at least one compound according to the present disclosure.

Abstract: [Object] An object of the present invention is to provide a human sweet taste receptor-acting sweet taste regulating substance to a sweet taste substance by which the advantageous effects such as improvement in a taste, saving of a sweetener, reduction in calorie, low caries etc. can be obtained by applying to various foods and beverages. [Solution] The sweet taste receptor-acting sweet taste regulating substance of the present invention is identified by measurement of a physiological response by a sweet taste substance, using a cultured cell strain which is allowed to express hT1R2 and hT1R3, and a G protein ? subunit, by transferring an expression construct obtained by inserting respective cDNAs encoding the hT1R2 and the hT1R3, and the G protein ? subunit into the same plasmid, into a 293 cell in which an FRT (Flippase Recognition Target) site has been incorporated into one place in a genome DNA.

Abstract: Chemical light producing systems and the chemiluminescent formulations contained therein are taught which exhibit reduced hydrolysis and thereby are characterized by an inherently long shelf-life and commercial viability. By replacing the typical oxalate ester, e.g. (bis{3,4,6-trichloro-2-[(pentoxy)carbonyl]phenyl}oxalate) with a branched chain oxalic acid ester represented by the general formula: wherein the group designated as R contains from 4-15 carbons, wherein the carbon of attachment of R to the oxygen is via a primary carbon, and wherein substructure A is composed of substituents selected from the group including alkyl chains, alkyl rings, aromatic rings and combinations thereof such that R is nonlinear, water hydrolysis of the oxalate ester is retarded. This retardation of the hydrolysis changes the storage constraints of the oxalate ester.

Abstract: The invention relates to a process for the synthesis of (Z)-3-[2-butoxy-3?-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-methoxyacrylic acid of formula (I): and also to the process for the synthesis of the reaction intermediates of general formula (XII), and to the said compounds when R2 is chosen from the methyl, trifluoromethyl, phenyl and 4-tolyl radicals:

Abstract: Polyester polyols are produced by reacting terephthalic acid with a glycol corresponding to the formula H—(OCH2CH2)n—OH and an aliphatic dicarboxylic acid. These polyester polyols are particularly useful for the production of polyurethane) (PUR) and polyurethane/polyisocyanurate (PUR/PIR) foams for use in insulation applications.

Abstract: This invention relates to the discovery of functionalized triclosan monomers and oligomers that, when incorporated into a substrate of, or applied as part of a coating to, medical devices and/or consumer products may extend the duration of antimicrobial properties to the medical devices and/or consumer products.

Abstract: Disclosed is a method for producing a compound represented by Formula (4), the method including Step I of adding a solution in which hydrogen chloride is dissolved in an alcohol, to a mixture containing an organic solvent and a compound represented by Formula (1), and Step II of mixing a compound obtained in Step I, represented by Formula (3), with water.

Abstract: Compounds having useful biological activity, particularly antioxidant and anti-inflammatory activity, derived from Centipeda cunninghamii, and biologically active derivatives thereof, pharmaceutical compositions comprising these compounds, and prophylactic and therapeutic use of the compounds.

Abstract: Preparation method of a compound of general formula (I) comprises the following steps: (1) a compound of general formula (II) reacts with a formylating agent in an aprotic solvent at a temperature between ?20° C. and 200° C. in the presence of a Lewis acid, then an organic base is added to promote the reaction to obtain an intermediate product; (2) the above intermediate product reacts with a methylating agent in the presence of an alkali at a temperature between ?20° C. and 100° C. to obtain the compound of formula (I).

Abstract: Bi-functional cobalt-containing catalysts useful for making stereo specific compounds and compositions, along with methods of making, and uses thereof in the syntheses of optically pure ?-lactones from aldehydes and ketene are described. Precursors, intermediates, compositions, and particular features of the use if the compositions, such as high enantiomeric selectivity, high yield and low mole percent of catalyst useful are provided.

Abstract: To provide a fluorinated compound having an RF group with at most 6 carbon atoms, whereby a fluorinated polymer having a highly durable water/oil repellency can be produced, and an environmental load is little, and a fluorinated polymer having a highly durable water/oil repellency and presenting little environmental load, obtainable by polymerizing such a fluorinated compound. A fluorinated compound represented by the following formula (I) and its polymer: CH2?C(M)COO(CH2)nPhXPhZCrF2r+1??(I) (in the formula (I), M is a hydrogen atom, a methyl group or a halogen atom, n is an integer of from 0 to 2, Ph is a phenylene group, X is CH2O or OCH2, Z is a single bond, a C1-4 alkylene group containing an etheric oxygen atom, or COO(CH2)m (wherein m is an integer of from 1 to 4), and r is an integer of from 1 to 6).

Abstract: The invention pertains to an oligomer or polymer substituted by one or more bisacylphosphine oxide moieties, characterized in that said bisacylphosphine oxide moiety is linked via the phosphorous atom, optionally via a spacer group, to the oligomer or polymer backbone; as well as to specifically functionalized bisacylphosphine oxides, suitable to prepare said polymers or oligomers.

Abstract: The invention relates to a nanoparticulate material comprising long ultrathin metal nanowires, and to processes for making it. The nanoparticulate material may be used as a catalyst and, in the presence of a chiral modifier, can catalyse enantioselective reactions.

Abstract: This invention relates to the discovery of functionalized triclosan monomers and oligomers that, when incorporated into a substrate of, or applied as part of a coating to, medical devices and/or consumer products may extend the duration of antimicrobial properties to the medical devices and/or consumer products.

Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumours. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumours presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumour glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.

Abstract: An ink jet liquid composition which is used with an ink containing a pigment and which contains an ABC triblock polymer formed from an A block having an aryl group, a B block having a unit represented by the general formula (1), and a C block having a unit represented by the general formula (2), wherein an acid value of the polymer is 20 mgKOH/g or more and less than 150 mgKOH/g, the ratio of the number average molecular weight of the polymer to the acid value is 50 or more and 200 or less, the proportion of the A block in the polymer is 20.0 percent by mass or more and 80.0 percent by mass or less and is 5.0 times or more and 15.0 times or less the proportion of units derived from all acidic monomers contained in the polymer.

Abstract: Polyester polyols are produced by reacting terephthalic acid with a glycol corresponding to the formula H—(OCH2CH2)n—OH and an aliphatic dicarboxylic acid.

Abstract: The invention relates to compounds derived from betulin, and to the use thereof in plant pest control, particularly as antifeedants for butterfly larvae, beetles and snails. Further, the invention relates to novel betulin derivatives and methods for the production thereof either directly from betulin, or via intermediates derived therefrom.

Abstract: This invention provides a platinum/carbon nanotube catalyst applicable to heterogeneous asymmetric hydrogenation, which is fabricated by supporting platinum on carbon nanotube carriers. The catalyst is prepared by the steps of: heating purified carbon nanotubes in nitric acid, filtering and washing the same with water until pH value of the filtrate becomes neutral, drying the carbon nanotubes; immersing the carbon nanotube carriers obtained in an aqueous chloroplatinic acid solution and carrying out ultrasonic treatment at room temperature; immersing the mixture of the carbon nanotubes and the aqueous chloroplatinic acid solution under stirring; drying the material by heating to 110° C. from room temperature and maintaining this temperature; grinding the product to fine powders, reducing the fine powders with an aqueous sodium formate solution under a heating condition, filtering and washing the product with deionized water, and drying the product.

Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.