Abstract: The present invention relates to compounds of Formula I as defined herein, and salts and solvates thereof. (I) The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to compounds of Formula (I) for use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which inhibition of a RAS-effector protein-protein interaction is implicated.

Abstract: A topical composition comprising a Polymer, a high molecular weight hyaluronic acid (HWM HA) and/or its salt, a low molecular weight hyaluronic acid (LWM HA) and/or its salt, and a polyamino acid and/or its salt; and water and a method for identifying a test polymer that forms a micro-mesh structure when combined with such ingredients.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: Embodiments provide, among other compounds, a family of compounds that can be used as therapeutic anti-cancer agents, methods for using such compounds to treat cancer, and methods of making such compounds.

Abstract: This invention relates to an acid labile surfactant. In particular, the surfactants of the present invention include a dioxolane or dioxane functional group which enables the surfactant to hydrolyze in an acidic environment. Surfactants of this type can be utilized to enhance protein solubilization/enzyme digestion. Following hydrolysis to destroy the surfactant (which may chromatographic issues), there are generally two components formed—a hydrophilic one, and a hydrophobic one. By altering the chemistry of the hydrolysable linker, the polarity of the hydrophobic residue can be altered, allowing it to be solubilized by significantly less organic solvent, and to minimize the potential loss of peptide material and to expand the chromatographic conditions that can be utilized.

Abstract: A method, system and computer-readable medium are provided for determining compliance with one or more patient care rules and protocols, the method including the steps of sending infusion information from a pump to a processor pertaining to one or more drugs provided to a patient, sending ventilation information from a ventilator to the processor pertaining to ventilation provided to the patient and determining, with the processor, a variation between actual care of the patient and a set of rules and protocols associated with care of the patient at least in part based on the infusion information and the ventilation information.

Abstract: A compound having the formula (I): is disclosed. A method of preparing the compound of formula (I) is also disclosed.

Abstract: Disclosed are methods for treating a meylodysplastic syndrome (MDS) in a subject that involves administering to the subject a therapeutically effective amount of an inflammasome inhibitor. Also disclosed are methods for diagnosing a myelodysplastic syndrome (MDS) in a subject. In some embodiments, the method involves assaying a sample from the subject to detect inflammasome activation, wherein an increase in inflammasome activation in the sample compared to a control is an indication of MDS in the subject. In some embodiments, the method involves assaying a sample from the subject to detect s100A9 protein levels, wherein an increase in s100A9 protein levels in the sample compared to a control is an indication of MDS in the subject. The disclosed methods can further involve treating the subject for MDS if an increase in inflammasome activation and/or s100A9 levels are detected.

Abstract: The present invention relates to a method for the treatment of cancer in a cancer patient.

Abstract: The invention relates to compounds of the following general formula (I) in the form of one of the enantiomers thereof or a mixture of the enantiomers thereof, and the pharmaceutically acceptable salts and/or solvates thereof, especially for the use thereof as a medicament, more specifically in cancer treatment. The invention also relates to pharmaceutical compositions containing same and to the methods for the production thereof.

Abstract: The present disclosure provides a composition of artesunate, a process of preparing the same, and a method of treatment.

Abstract: A compound represented by formula (4): can be produced by adding a heterogeneous transition metal catalyst to a solution containing a compound represented by formula (3): obtained by performing a nitration reaction by adding a nitrating agent to a solution containing a compound represented by formula (2): obtained by oxidizing a compound represented by formula (1): with hydrogen peroxide in the presence of sodium tungstate and a saturated C8 carboxylic acid, then adding water to the resultant mixture, and separating the resultant solution.

Abstract: The present invention relates to novel compounds of formula (I) to compositions comprising same, and also to the use thereof for preventing and/or cosmetically treating the signs of aging of the skin.

Abstract: Aspects of the present disclosure involve systems and methods for passing optimization information, which may be used to optimize input/output (“I/O”) requests, from a database management system to a file system, using various protocols of a network file system. The optimization information provided by the database management system may relate to various aspects of an I/O request that may be optimized.

Abstract: The present invention relates to a cosmetic composition containing a hydroxypyranone derivative compound as an active ingredient for promoting the differentiation of adipocytes. The composition according to the present invention has an effect of promoting the differentiation of adipocytes, and thus allows the differentiation of adipocyte in a skin layer, thereby increasing the skin volume or elasticity. Therefore, the composition of the present invention can be variously used as a cosmetic composition or a pharmaceutical composition in the field, such as skin damage.

Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Abstract: This disclosure relates to taste modifiers of formula (I) wherein, n is 1, 2 or 3; R1 is selected from C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 dihydroxyalkyl and —CHYCOOH wherein Y is selected from C1-C3; R3 is hydrogen, hydroxy or C1-C3 alkoxy; R4 is hydrogen, or C1-C3 alkyl; R5 is selected from hydrogen, or C1-C3 alkyl; or R4 and R5 form together a bivalent radical —CH2—; that are able to impart, enhance or modify salt or umami taste.

Abstract: Provided herein are eckol derivatives, methods of synthesis thereof and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, Alzheimer's disease, microbial infections, obesity, diabetes, cancer or inflammation using the compounds and pharmaceutical compositions disclosed herein.

Abstract: The present invention relates generally to the field of lipids and in particular aims at improving lipid absorption, for example under conditions of lipid maldigestion or malabsorption. One embodiment of the present invention relates to a composition comprising a sn-2 monoacylglycerol derivative, wherein the sn-1 and sn-3 positions are blocked by protective groups. The acyl group may be a fatty acid, for example one with anti-inflammatory properties.

Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

Abstract: The present application discloses a compound which is which activates Wnt/?-catenin signaling and thus treats or prevents diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

Abstract: The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.

Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Abstract: The present invention provides a 1,2,4-trioxane or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof for use as an adjuvant for a tyrosine kinase inhibitor to enhance the activity of said tyrosine kinase inhibitor in a method for the treatment of a patient suffering from cancer, a pharmaceutical composition comprising a tyrosine kinase inhibitor as an active ingredient and said 1,2,4-trioxane adjuvant or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof in an amount sufficient to enhance the activity of the tyrosine kinase inhibitor, preferably for use in a method for the treatment of cancer.

Abstract: Disclosed are methods of treating a muscle disease and improving normal muscle function by administering a therapeutically effective amount of an isoprenoid antibiotic. Also disclosed are methods of upregulating hnRNP L and hnRNP L targets by administering a therapeutically effective amount of an isoprenoid antibiotic. Methods of screening compounds for use in treating muscle disease and improving muscle function are also described.

Abstract: A liquid crystal compound is described, having a large dielectric anisotropy, a high voltage holding ratio and stability to heat, light and so forth, maintaining a nematic phase in a wide temperature range, and having a suitable optical anisotropy and an excellent compatibility with other liquid crystal compounds. Particularly, a liquid crystal compound having a large dielectric anisotropy is described. The compound is represented by formula (1): In the formula, for example, R1 is alkyl having 1 to 20 carbons; ring A1, ring A2, ring A3, ring A4, ring A5 and ring A6 are independently 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3, Z4, Z5, Z6 and Z7 are independently a single bond, —(CH2)2—, —COO—, —OCO—, —CF2O—, —OCF2— or —CH?CH—; X1 is fluorine, —CF3 or —OCF3; and Y1 and Y2 are independently hydrogen or fluorine.

Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

Abstract: The invention relates to a preparation containing several amino acids and plant extracts and its alcohol detoxification activity. The component (a) in the preparation contains a mixture of two or more amino acids or derivatives thereof; the component (b) in the preparation contains a mixture of three or more extracts from plants. There are several plant extracts used in this invention such as the extract of ginseng radix, the extract of ginkgo biloba leaf, the extract of Silibinin, the extract of barbury wolfberry fruit and tea polyphenols. The invention also relates to the biological activities of said preparation, such as the liver protection from chemical injury, the tolerance enhancement of hypoxy and the rapid decrease till elimination of the blood alcohol content.

Abstract: The present application discloses a compound which is which activates Wnt/?-catenin signaling and thus treats or prevents diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

Abstract: A therapy for renal diseases characterized by alterations of the kidney function, such as Chronic Kidney Disease (CKD), acute and chronic renal impairment, and renal diseases that develop in diabetic patients or in patients who underwent an anticancer chemotherapic treatment with a platinum derivative. The invention is a combination of compounds selected from mono- or diamide of a C12-C20 monocarboxylic acid, saturated or monounsaturated, or a C4-C14 dicarboxylic acid, saturated or monounsaturated, with an aminoalkanol, and compounds selected from Silymarin, derivatives thereof or conjugates or complexes thereof, for use in the treatment of renal diseases.

Abstract: A liquid crystal compound of formula (I): where A1, A2, A3, A4, R1, R2, Z1, Z2, Z3, n, and m are as defined in the specification.

Abstract: An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal systems.

Abstract: The present invention provides a series of derivatives of stilbenoid which are useful as new inhibitory agents against head and neck squamous cell carcinoma (HNSCC) and hepatoma.

Abstract: The invention relates to the use of a silibinin component for the production of a medicament that is adapted for parenteral administration for the treatment of viral hepatitis, preferably of hepatitis B or C, in particular for the reduction of the virus load. The medicament preferably contains no silidianin and/or no silichristin and/or no isosilibinin.

Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.

Abstract: A high-efficacy, long-acting formulation of silibinin, comprising silibinin solid dispersion, silibinin-loaded silica nanoparticles, slow-release matrix material and release enhancer, wherein the mass ratio of these components is silibinin solid dispersion:silibinin-loaded silica nanoparticles:slow-release matrix material:release enhancer=1:0.5˜1.25:0.1˜0.3:0.1˜0.3; the drug loading rate of the said silibinin-loaded silica nanoparticles is 51.29˜51.77%; the said silibinin solid dispersion contains povidone K30, soybean lecithin, acrylic resin IV, wherein the mass ratio between silibinin and other medical accessories is silibinin:povidone K30:soybean lecithin:acrylic resin IV=1:1˜3:0.3˜0.8:0.2˜0.5. Compared with the existing formulations, the half life of the high-efficacy, long-acting formulation of silibinin disclosed in this invention is 14.8 times longer while the mean residence time (MRT) of which is 4.

Abstract: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.

Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.

Abstract: The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.

Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.

Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.

Abstract: The present invention relates to methods of the treatment and diagnosis of bone mineral density related disorders. More particularly, the present invention relates to a method of diagnosing or predicting a hone mineral density related disease, or a risk of a bone mineral density related disease, in a subject, which method comprises detecting a mutation in the TBXAS1 gene, wherein the presence of said mutation is indicative of a bone mineral density related disease or of a risk of a bone mineral density related disease. The invention also relates to a compound selected in the group consisting of a thromboxane synthase (TXAS) encoding polynucleotide, a TXAS, thromboxane A2 or an analog thereof for treating or preventing a disease associated with an increased bone mineral density (e.g., Ghosal hematodiaphyseal dysplasia syndrome).

Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.

Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.

Abstract: The invention provides method of treating cancers that express MUC1 by the administration of eIF4A helicase inhibitors. These inhibitors may advantageously be combined with peptides that inhibit MUC1 oligomerization, or with other standard anticancer therapies such as chemo-, radio- and surgical therapies.

Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.

Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.

Abstract: An olefin polymerization catalyst component comprising an internal electron donor compound shown in formula (I) below is provided in this disclosure: wherein X is O, S, NRa, PRb, or POORc, Ra is independently hydrogen, halogen, carbonyl hydrocarbon, linear or branched unsaturated or saturated alkyl hydrocarbon, cyclic, aromatic, or aliphatic hydrocarbon, Rb is independently hydrogen, halogen, carbonyl hydrocarbon, linear or branched unsaturated or saturated alkyl hydrocarbon, linear or branched unsaturated or saturated alkoxy hydrocarbon, cyclic, aromatic, or aliphatic hydrocarbon, Rc is independently hydrogen, carbonyl hydrocarbon, linear or branched unsaturated or saturated alkyl hydrocarbon, cyclic, aromatic, or aliphatic hydrocarbon, R1-R8 are identical or different hydrogen, halogen, linear or branched unsaturated or saturated C1-C30 alkyl, alone or in combination with C5-C30 substituted or unsubstituted 5-or 6-membered aliphatic or aromatic hydrocarbon rings, each of Ra, Rb, Rc, and/or R1-R8 are op