Abstract: A microparticle detection system includes a stage unit including a mounting surface on which a fluid device having a flow path through which a sample containing microparticles is movable is capable of being mounted, an emission unit configured to emit illumination light to the flow path, an imaging unit configured to image scattered light generated from microparticles in the sample when illumination light is emitted, an identification unit configured to identify the microparticles included in the image for each of the microparticles on the basis of the image captured by the imaging unit, a particle size determination unit configured to determine a particle size of the microparticle for each of the microparticles identified by the identification unit, a zeta potential determination unit configured to determine a zeta potential of the microparticle for each of the microparticles identified by the identification unit, and a correlation unit configured to associate the particle size for each of the microparticles

Abstract: This disclosure relates to synthetic coupling methods using a catalytic molecule comprising two bonded atoms wherein one atom is an amide nitrogen and the second atom is not nitrogen or carbon, such as sulfur, such as a sufur amide nitrogen bond, typically in a heterocycle, such as substituted benzoisothiazolones and derivatives thereof, as a catalyst in the transformation of hydroxy group containing compounds to amides, esters, ketones, and other carbon to heteroatom or carbon to carbon transformations.

Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.

Abstract: A dipeptide derivative as formyl peptide receptor 1 (FPR1) antagonist is provided. The dipeptide derivative is represented by formula (I), wherein: the chiral centers in formula (I) are S and R configurations respectively; each of RK and RT is selected from a group consisting of a hydrogen, a hydroxyl group, a C1-C4 alkyl-substituted hydroxyl group, a C1-C4 alkoxyl group, a carboxylic acid group, a C1-C4 alkyl nitrile-substituted, C1-C4 alkyl-substituted or C1-C4 alkoxyl-substituted amido group, a C1-C4 alkyl-substituted ester group and a benzoyl group having a C1-C4 alkyl-substituted benzene ring; and each of RM and RS is selected from a group consisting of a hydrogen, a hydroxyl group, a phenyl group, a pyridinyl group, a carboxylic acid group, a C1-C4 alkoxyl substituted ester group, and a benzoyl group having a hydroxyl-substituted, a halogen-substituted, a C1-C4 alkoxyl-substituted or a C1-C4 alkyl-substituted benzene ring.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: The present invention relates to an indole derivative, The indole derivative according to the present invention effectively inhibits the activity of diacylglycerol acyltransferase (DGAT) which induces metabolic diseases, such as obesity, diabetes, hyperlipidemia, or fatty liver and the like in lipid metabolism, thereby effectively regulating lipid metabolism and energy metabolism, and thus can be useful in pharmaceutical compositions for preventing or treating metabolic disease.

Abstract: Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.

Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

Abstract: A method is described for using IL-12R 1/IL-23R, CCR6, BATF, AHR, STAT3, IRF4 crucial actors in Th17 cells differentiation as markers for acne. Also described are method of their use to diagnose acne, to screen inhibitors of Th17 differentiation. In particular, methods are described for inhibiting IL12R 1/IL-23R, CCR6, BATF, AHR, STAT3, IRF4 and the use of these screened inhibitors in acne treatment.

Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.

Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: Novel p53-Mdm2 antogonists that conform to Formula I or to Formula II: where the prescribed substituent groups are defined, are useful in treating or preventing cancer. In particular, the compounds and their pharmaceutical compositions are useful for treating relapsed/refractory acute myeloid and lymphoid leukemia and refractory chronic lymphocytic leukemia/small cell lymphocytic lymphomas.

Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Abstract: Substituted indole derivatives of formula (I) wherein the radicals have e.g. the following meaning: R1 is hydrogen, C1-6-alkyl, R2 is hydrogen, —C1-6-alkyl or cycloC3-12-alkyl; R3 is OR R4 is hydrogen or halogen, R5 is hydrogen, —C1-6-alkyl R6 is hydrogen, —C1-6-alkyl R is hydrogen or —C1-6-alkyl; X is a group —C(O)CH2— or —CH?CH—; R7 is hydrogen are potent inhibitors of Abeta peptide polymerization and can be used for the treatment of e.g. Alzheimers disease or ocular disorders.

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: N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide and starting materials therefore are prepared by new synthetic methods.

Abstract: The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.

Abstract: The invention is related to compounds for prevention of cell injury or protection of cells. The compounds are involved in the maintenance or the increase of hydrogen sulphide in cells, which results in a protection of the cells or the prevention of cell injury. The compounds of the invention can be used in cell culture and tissue culture techniques. They can also be used in several medical conditions such as ischemia, reperfusion and hypothermia, or for preserving organs which are used for transplantation.

Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the specification, exhibit a salty taste enhancing activity and are useful as salty taste enhancers for foods and drinks.

Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 2 (polymorphic form I) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.

Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.

Abstract: Organocatalysts, particularly proline sulfonamide organocatalysts, having a first general formula as follows are disclosed. Embodiments of a method for using these organocatalysts also are disclosed. The method comprises providing a disclosed organocatalyst, and performing a reaction, often an enantioselective or diastereoselective reaction, using the organocatalyst. Solely by way of example, disclosed catalysts can be used to perform aldol reactions, conjugate additions, Michael additions, Robinson annulations, Mannich reactions, ?-aminooxylations, ?-hydroxyaminations, ?-aminations and alkylation reactions. Certain of such reactions are intramolecular cyclizations used to form cyclic compounds, such as 5-or 6-membered rings, having one or more chiral centers Disclosed organocatalysts generally are much more soluble in typical solvents used for organic synthesis than are known compounds.

Abstract: A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.

Abstract: A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.

Abstract: Methods and compositions that can be used to make monatin from glucose, tryptophan, indole-3-lactic acid, indole-3-pyruvate, and 2-hydroxy 2-(indol-3-ylmethyl)-4-keto glutaric acid, are provided. Methods are also disclosed for producing the indole-3-pyruvate and 2-hydroxy 2-(indol-3-ylmethyl)-4-keto glutaric acid intermediates. Compositions provided include nucleic acid molecules, polypeptides, chemical structures, and cells. Methods include in vitro and in vivo processes, and the in vitro methods include chemical reactions.

Abstract: To provide a novel monatin crystal capable of forming a sweetener composition which is less likely to be degraded even when being exposed to high temperature and high humidity conditions in the coexistence of a reducing sugar. It was found that the object can be achieved by a crystal of a multivalent metal salt of (2R,4R)-monatin.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: Derivatives of psammaplin A responding to formula (I), a method for their synthesis and their use for the preparation of a medicament for preventing and for treating a tumor or a cancer. Formula (I).

Abstract: Methods for preparing a polymer using Hansen solubility parameters are described. Also described is a polymer having certain properties, including those related to the Hansen solubility parameters, having utility in the separation of monatin from a monatin-containing mixture.

Abstract: The present invention provides salt crystals of non-natural stereoisomer forms of monatin and to the use thereof.

Abstract: New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.

Abstract: Methods and systems for separating and purifying monatin are described. In the production of monatin, a mixture is formed which includes monatin, starting materials and intermediates. The methods and systems include a membrane having a zeta potential of from about ?19 to ?6 such that the membrane rejects greater than about 90% of the monatin. In some embodiments, the membrane is a nanofiltration membrane.

Abstract: The present invention is directed to stable protein formulations, related methods and uses thereof. In particular, the invention relates to a method of stabilizing therapeutic proteins in aqueous solution.

Abstract: The present invention generally relates to inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt), in particularly to compounds that inhibit Icmt activity and pharmaceutical compositions thereof. The invention also relates to methods of disease treatment using the same.

Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F), the crystal modification 2 (polymorphic form I), and the crystal modification 3 (polymorphic form X) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Abstract: The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).

Abstract: The invention relates to a compound of the following formula (I), or to a pharmaceutically acceptable salt thereof or to a stereoisomer or mixture of stereoisomers at any proportions, where: X1 is a CH2 or C?O group; X2 is a linear saturated or unsaturated carbohydrate chain with 8 to 24 carbon atoms; R1 is a hydrogen atom or an OH or (C1-C6)alkoxy group such as methoxy; and R2 is a CH3 or CH2OR3 group, with R3 being a hydrogen atom or a (C1-C6)alkyl, CO—(C1-C6)alkyl or NH—(C1-C6)alkyl group. The invention also relates to the use of said compound as a drug, in particular for treating neurodegenerative diseases, and to a method for preparing same.

Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or un

Abstract: The present invention is to provide an industrially advantageous method for producing an amino acid derivative. Provided is a method for producing an amino acid derivative including contacting a microorganism and/or an enzyme with a hydroxyimino acid represented by the following general formula (I): wherein R1 represents an optionally substituted predetermined hydrocarbon group; R2 represents a C1 to C3 alkyl group or a hydrogen atom; and n is 0 or 1, to produce an amino acid derivative represented by the following general formula (III): wherein R1 and n have the same meanings as those of R1 and n in the general formula (I), wherein the microorganism and/or the enzyme is capable of catalyzing the reaction.

Abstract: A normal person (i.e. a control) and liver diseases such as drug induced liver injury, an asymptomatic hepatitis B carrier, an asymptomatic hepatitis C carrier, chronic hepatitis B, chronic hepatitis C, liver cancer, a nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and simple steatosis (SS) are identified by measuring the concentrations of ?-Glu-X (X represents an amino acid or an amine) peptides or the levels of AST or ALT in blood and carrying out, for example, a multiple logistic regression based on the measured value.

Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.