Abstract: An improved method for MRI-guided sonosensitized focused ultrasound treatment of malignant tissue is disclosed herein.

Abstract: The present invention relates to a preparation method of chiral primary amine. The chiral primary amine is prepared through a one-pot method that under the action of a ruthenium-chiral diphosphine catalyst, a simple ketone and an ammonium salt RCOONH4 have reductive amination by adding hydrogen and then are heated and hydrolyzed by adding acid.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's extend the buffering range resulting in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: A synthesis method comprises opening an anhydride to a 4-carbon acid-amide, removing ethanol soluble products, treating the resulting 4-amino-2-methylene-4-oxo-butanoic acid with Ozone in water, and evaporating the ozonolysis products to synthesize 4-amino-2,4-dioxobutanoic acid.

Abstract: A process for synthesizing 4-amino-2,4-dioxobutanoate involves reacting a dialkyl oxalate with an alkoxide in ethanol to form a reaction mixture, and afterward adding an alkyl cyano acetate to the reaction mixture and allowing a reaction to proceed under conditions suitable to form a first reaction product of the formula diethyl 2-cyano-3-hydroxy-butenedioate, and then isolating the diethyl 2-cyano-3-hydroxy-butenedioate, and afterward reacting the diethyl-2-cyano-3-hydroxy-butenedioate with an aqueous hydroxide under conditions suitable to form 4-amino-2,4-dioxobutanoate. The 4-amino-2,4-dioxobutanoate may be acidified into 4-amino-2,4-dioxobutanoic acid.

Abstract: A rare earth metal extractant containing, as the extractant component, dialkyldiglycol amide acid which is excellent in breaking down light rare earth elements is reacted in diglycolic acid (X mol) and an esterification agent (Y mol) at a reaction temperature of 70° C. or more and for a reaction time of one hour or more such that the mol ratio of Y/X is 2.5 or more, and is subjected to vacuum concentration. Subsequently, a reaction intermediate product is obtained by removing unreacted products and reaction residue. Then a nonpolar or low-polar solvent which is an organic solvent for forming an organic phase during solvent extraction of the rare earth metal and which is capable of dissolving dialkyldiglycol amide acid is added as the reaction solvent, and the reaction intermediate product is reacted with dialkyl amine (Z mol) such that the mol ratio of Z/X is 0.9 or more.

Abstract: The present invention relate to a preparation method of high-purity L-carnitine which belongs to an important technique of quality control in different steps of chiral medicine production.

Abstract: A process for synthesizing 4-amino-2,4-dioxobutanoic acid involves reacting diethyl oxalate with sodium ethoxide in ethanol to form a reaction mixture, and afterward adding ethyl cyanoacetate to the reaction mixture and allowing a reaction to proceed under conditions suitable to form a first reaction product of the formula diethyl-2-cyano-3-hydroxy-butenedioate, and then isolating the diethyl-2-cyano-3-hydroxybutenedioate, and afterward reacting the diethyl-2-cyano-3-hydroxy-butenedioate with aqueous sodium hydroxide under conditions suitable to form 4-amino-2,4-dioxobutanoic acid.

Abstract: The invention relates to a method for the production of L-carnitine, wherein a ?-lactone, which is a 4-(halomethyl)oxetane-2-one, is converted into carnitine with trimethylamine (TMA), wherein the ?-lactone is not subjected to a basic hydrolysis step before being contacted with the trimethylamine. The invention also relates to a carnitine having a unique impurity profile.

Abstract: A flavour composition comprising a compound according to the formula (I) or edible salts thereof, wherein R1 is an alkyl residue containing 6 to 20 carbon atoms, or an alkene residue containing from 9 to 25 carbon atoms with 1 to 6 double bonds, R1 together with the carbonyl group to which it is attached is a residue of a carboxylic acid, and NR2R3, in which R3 is H or together with R2 and the N-atom to which they are attached, a 5-membered ring, is a residue of an amino acid, in particular a proteinogenic amino acid, ornithine, gamma-aminobutyric acid or beta alanine, or a 1-amino cycloalkyl carboxylic acid.

Abstract: A process for synthesizing 4-amino-2,4-dioxobutanoic acid involves reacting diethyl oxalate with an alkoxide in ethanol to form a reaction mixture, and afterward adding ethyl cyanoacetate to the reaction mixture and allowing a reaction to proceed under conditions suitable to form a first reaction product of the formula diethyl 2-cyano-3-hydroxy-butenedioate, and then isolating the diethyl 2-cyano-3-hydroxy-butenedioate, and afterward reacting the diethyl-2-cyano-3-hydroxy-butenedioate with an aqueous hydroxide under conditions suitable to form 4-amino-2,4-dioxobutanoic acid.

Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.

Abstract: This disclosure teaches the novel use of trifluoroacetamide for N-terminal protection. The disclosure also teaches novel compositions and chemical structures associated therewith. These methods and compositions are useful for site-specific methylation of peptide backbone amides, performed, for example, to modulate the pharmacokinetic properties of peptide drugs.

Abstract: Methods for treating a subject determined to have a cancer comprising a heterozygous inactivation of a housekeeping gene (or a homozygous deletion of a functionally redundant housekeeping gene) by treating the subject with an inhibitor of the gene. For example, a subject having a cancer with an ENO gene deletion can be treated with a glycolysis inhibitor, such as an enolase inhibitor. In some aspects, a subject having a cancer with an ARS gene deletion can be treated with an ARS inhibitor.

Abstract: The ?,?-unsaturated ?-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.

Abstract: A phytosphingosine derivatives of chemical formula IA or IB, and a cosmetic composition including the phytosphingosine derivative. The phytosphingosine derivatives are involved with transcription factors related to inflammation and hyperkeratotic diseases, the expression and the generation of inflammatory mediators, signal transduction mechanisms, and the expression and the activity of relevant enzymes and the like.

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: [Problem] To provide an agent for preventing and/or treating veisalgia. [Solution] Provided is an agent for preventing and/or treating veisalgia, the agent including an ALA (5-aminolevulinic acid).

Abstract: A phytosphingosine derivative of chemical formula IA or IB, and a composition comprising the phytosphingosine derivative for preventing and treating inflammatory skin diseases, autoimmune diseases, and hyperkeratotic diseases. The phytosphingosine derivatives of the present disclosure are involved with transcription factors related to inflammation, autoimmune diseases and hyperkeratotic diseases, the expression and the generation of inflammatory mediators, signal transduction mechanisms, and the expression and the activity of relevant enzymes and the like.

Abstract: A rare earth metal extractant in the form of a dialkyl diglycol amic acid is synthesized by reacting diglycolic anhydride with a dialkylamine in an aprotic polar solvent, with a molar ratio of dialkylamine to diglycolic anhydride being at least 1.0, and removing the aprotic polar solvent.

Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

Abstract: A method for ameliorating and/or preventing cancerous anemia includes administering to a subject in need thereof an agent containing 5-aminolevulinic acid (ALA) or a derivative thereof, or a salt thereof. Preferably, these ALAs contain a metal-containing compound, such as sodium ferrous citrate. The above-mentioned ALAs, ALA; various esters such as ALA methylester, ALA ethylester, ALA propylester, ALA butylester, and ALA pentylester; and hydrochlorides, phosphates, and sulfates, and the like of these ALA esters are preferred examples.

Abstract: A therapeutic and/or prophylactic agent for renal anemia comprising ALAs and an erythropoietin production promoter comprising ALAs.

Abstract: A rare earth metal extractant containing, as the extractant component, dialkyldiglycol amide acid which is excellent in breaking down light rare earth elements is reacted in diglycolic acid (X mol) and an esterification agent (Y mol) at a reaction temperature of 70° C. or more and for a reaction time of one hour or more such that the mol ratio of Y/X is 2.5 or more, and is subjected to vacuum concentration. Subsequently, a reaction intermediate product is obtained by removing unreacted products and reaction residue, and an aprotic polar solvent is added as the reaction solvent. Then, the reaction intermediate product is reacted with dialkyl amine (Z mol) such that the mol ratio of Z/X is 0.9 or more and the aprotic polar solvent is removed. As a consequence, a rare earth metal extractant is efficiently synthesized at a low cost and at a high yield without having to use expensive diglycolic acid anhydride and harmful dichloromethane.

Abstract: A process for synthesizing 4-amino-2,4-dioxobutanoic acid involves reacting diethyl oxalate with sodium ethoxide in ethanol to form a reaction mixture, and afterward adding 2-cyano-3-hydroxy-butenedioate to the reaction mixture and allowing a reaction to proceed under conditions suitable to form a first reaction product of the formula diethyl-2-cyano-3-hydroxy-butenedioate, and then isolating the cyano-3-hydroxy-butenedioate, and afterward reacting the diethyl-2-cyano-3-hydroxy-butenedioate with aqueous sodium hydroxide under conditions suitable to form 4-amino-2,4-dioxobutanoic acid.

Abstract: The invention relates to the field of medicament use, in particular to the clinical use of photosensitizers for inactivating viruses in the treatment of blood vessel plaque, leukemia, AIDS, hepatitis and the like. The invention is based on the affinity of photosensitizer to blood vessel plaque focus, leukemia cells, tumor, and/or virus, which is several times higher than that to normal tissues, to destroy focus cells or virus by generating singlet oxygen (1O2) under the effect of a method using laser, X-ray, ultrasound and medicament. The effects for treating the above diseases are achieved without serious side effects to the normal human tissues and organs.

Abstract: A method for ameliorating and/or preventing chronic kidney disease includes administering to a subject in need thereof an agent containing 5-aminolevulinic acid (ALA) or a derivative thereof, or a salt thereof as an active ingredient. Preferably, these ALAs contain a metal-containing compound, such as sodium ferrous citrate. The above-mentioned ALAs, ALA; various esters, such as ALA methylester, ALA ethylester, ALA propylester, ALA butylester, and ALA pentylester; and hydrochlorides, phosphates, and sulfates, and the like of these ALA esters are preferred examples.

Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: The invention provides a pharmaceutical composition, medical food, dietary supplement or micronutrient for the treatment of a movement disorder comprising an NMDAR agonist or partial agonist as active ingredient therein in combination with a pharmaceutically acceptable carrier.

Abstract: The present disclosure relates to an ASD genetically engineered model carrying a deletion of Shank2 gene and having reduced NMDA receptor function. According to the present disclosure, genetically engineered mice that show the clinical features of ASD due to the deletion of the Shank2 gene can be obtained, and the genetically engineered mice can be effectively used to screen candidate therapeutic agents.

Abstract: The disclosure provides a series of 2-oxoamides based on dipeptides and pseudodipeptides, which were synthesized and their activities toward two human intracellular phospholipases A2 (GIVA CPLA 2 and GVIA 1PLA 2) and one human secretory phospholipase A2 (GV sPLA 2) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA 2 inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA 2. The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied. It was found that selective GIVA cPLA 2 inhibitors preferentially inhibited cellular arachidonic acid release; in which one pseudodipeptide gave an IC50 value of 2 ?M.

Abstract: Provided herein, inter alia, are novel compositions and methods having application in the field of enhanced oil recovery. In particular, the quaternary ammonium compounds and mixtures thereof presented herein can be used, inter alia, for the recovery of a large range of crude oil compositions from challenging reservoirs.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

Abstract: This disclosure describes draw solution compositions for FO processes which increase the available membrane area for permeation and are also amenable to reconcentration with standard techniques, such as membrane filtration and evaporative technologies. The composition are comprised of a water soluble draw solute having surface active properties, i.e., a surfactant.

Abstract: A rare earth metal extractant in the form of a dialkyl diglycol amic acid is synthesized by reacting diglycolic anhydride with a dialkylamine in a synthesis medium. A molar ratio (B/A) of dialkylamine (B) to diglycolic anhydride (A) is at least 1.0. A non-polar or low-polar solvent in which the dialkyl diglycol amic acid is dissolvable is used as the synthesis medium.

Abstract: The present invention is directed to the use of compounds of the formula: for treating pain, in particular neuropathic pain, bipolar disease and migraine headaches.

Abstract: Provided is a preventive and/or therapeutic agent for malaria, comprising, as an active ingredient, 5-acetamido-4-oxo-5-hexenoic acid (Alaremycin) or a derivative thereof. A preventive and/or therapeutic agent for malaria is used which comprises, as an active ingredient, Alaremycin or a derivative thereof represented by formula (I) (wherein R1 represents a hydroxy group, an amino group, or a substituted or unsubstituted straight chain or branched alkoxy group or alkylamino group having 1 to 8 carbons; R2 represents hydrogen, a substituted or unsubstituted straight chain or branched alkyl group having 1 to 8 carbons, or a substituted or unsubstituted aromatic group having 4 to 10 carbons; and R3 represents hydrogen or a methyl group).

Abstract: A 5-aminolevulinic acid salt which is useful in fields of microorganisms, fermentation, animals, medicaments, plants and the like; a process for producing the same; a medical composition comprising the same; and a plant activator composition comprising the same.

Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

Abstract: Provided is an enhancer for cancer thermotherapy not combined with photodynamic therapy. Cancer treatment not combined with photodynamic therapy is made available by using, as an enhancer for cancer thermotherapy, 5-aminolevulinic acids represented by formula (1): R2R1NCH2COCH2CH2COR3 ??(1) [wherein R1 and R2 each independently represent a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryl group, or an aralkyl group; and R3 represents a hydroxy group, an alkoxy group, an acyloxy group, an alkoxycarbonyloxy group, an aryloxy group, an aralkyloxy group, or an amino group] or a salt thereof.

Abstract: Polymer compositions having the chemical structure: as well as monomer compositions for producing said polymers are described. Methods for preparing these polymers and combinatorial libraries of these polymers are also described.

Abstract: A rare earth metal extractant containing, as the extractant component, dialkyldiglycol amide acid which is excellent in breaking down light rare earth elements is reacted in diglycolic acid (X mol) and an esterification agent (Y mol) at a reaction temperature of 70° C. or more and for a reaction time of one hour or more such that the mol ratio of Y/X is 2.5 or more, and is subjected to vacuum concentration. Subsequently, a reaction intermediate product is obtained by removing unreacted products and reaction residue. Then a nonpolar or low-polar solvent which is an organic solvent for forming an organic phase during solvent extraction of the rare earth metal and which is capable of dissolving dialkyldiglycol amide acid is added as the reaction solvent, and the reaction intermediate product is reacted with dialkyl amine (Z mol) such that the mol ratio of Z/X is 0.9 or more.

Abstract: The present invention is related to a composition comprising a serine as an active ingredient for treating or preventing fatty liver diseases. The inventive compound significantly inhibits the SREBP-1 transcription activity involved in lipid synthesis and reduced the fatty liver formation through various in vitro test and in vivo test therefore it can be useful in the prevention and treatment of the fatty liver diseases as a medicament or health functional food.

Abstract: The invention relaters to a process for the production of an (S)- or (R)-4-halo-3-hydroxybutyrate, comprising reacting a 4-haloacetoacetate with hydrogen in the presence of a solvent, the solvent being a solvent mixture, which comprises a first solvent and a second solvent, wherein the first solvent is an aliphatic alcohol, preferably methanol, ethanol or propanol, and the second solvent is aprotic and comprises at least one oxygen atom; and a catalyst of the formula [RuXYZ]X, wherein X is halogen, preferably Cl or Br, or OAc, acetoacetate, allyl or ClO4, Y is a bidentate organic ligand having two phosphine groups, and Z is an arene, preferably cymene, benzene, xylene or toluene, or a polyene, preferably a diene, or an alkene.

Abstract: It is to provide a method for detecting urothelial cancer simply and with high accuracy. It is a method for detecting urothelial cancer comprising administering 5-aminolevulinic acid (ALA), a derivative thereof, or a salt of these to a test subject, collecting urine from the test subject, and detecting the presence of fluorescence or amount of fluorescence in the collected urine.

Abstract: Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: This invention relates to octahydro-binaphthol derivatives, which can recognize amino acids and amino alcohols enantioselectively and transform L-amino acids into D-amino acids and optically resolve amino acids or amino alcohol with high efficiency.

Abstract: The present invention provides atazanavir sulfate substantially free of diastereomeric impurities. The present invention also provides atazanavir sulfate having D-tertiary leucine analogues less than 0.1%. The present invention further relates to an improved process for preparing atazanavir sulfate, substantially free of its diastereoisomeric impurities, which comprises of reacting diamino compound (IV) with N-methoxycarbonyl-(L)-tertiary-leucine (V) having D-isomer less than 0.1% to obtain atazanavir base; conversion of atazanavir base to atazanavir sulfate by reacting with sulfuric acid and crystallization of atazanavir sulfate from suitable organic solvent(s).