Abstract: Provided are an environmentally-friendly high-efficiency method of manufacturing an ester compound based on an esterification reaction using a salt ion-exchange method and an ester compound manufactured thereby. In the conventional esterification reaction, an ester was produced in low yields due to the hydrolysis (i.e., reverse reaction) caused by water, or it was required to continuously supply hydrochloric acid gas or use thionyl chloride, which is a hazardous material, and thus there were limitations in terms of environmental friendliness or cost. On the other hand, in the present invention, hydrochloric acid gas is continuously supplied using the salt ion-exchange method, and since magnesium sulfate acts as a dehydrating agent, the water generated in the esterification reaction is removed, and thus the occurrence of hydrolysis (i.e., reverse reaction) is suppressed and a conversion rate to the desired ester compound is increased.

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 agricultural plant-protecting agent including a dipeptide derivative or an agro-pharmaceutically acceptable salt thereof as an active ingredient, which has a plant disease-preventing effect, a plant growth-promoting effect, and a plant immunity-activating effect.

Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: Disclosed are a compound including an oxalate, a carbon dioxide absorbent including the same, a method of preparing the carbon dioxide absorbent and a method of removing carbon dioxide, which may overcome issues of high recycling energy and low absorptivity of a conventional carbon dioxide absorbent to considerably reduce recycling energy and absorb a greater amount of carbon dioxide per unit absorbent, so that a size of a carbon dioxide absorption tower may be reduced and a less amount of recycling energy may be used, contributing to a substantial decrease in device manufacture costs and management costs.

Abstract: The present invention is directed to a new class of lipids, more specifically ether-lipids having a polar headgroup, as well as vesicles comprising these lipids, methods of their preparation as well as their uses in medical applications, wherein the ether-lipids are represented by general formula I

Abstract: A photochromic curable composition containing, as a radically polymerizable monomer component (A), a (meth)acrylic-amide polymerizable monomer (A1) having 2 to 6 (meth)acryloyloxy groups and 2 to 6 divalent amide groups (—NHCO—), and a non-amide polymerizable monomer (A2) having at least 3 radically polymerizable groups but having no amide bond. From the photochromic composition, there can be obtained a photochromic cured body having excellent photochromic properties such as a high color density, a high fading rate, and excellent mechanical strength.

Abstract: The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.

Abstract: A process for preparing amino acid-modified siloxanes that can be carried out under mild conditions is provided as well as organically modified silicones for care formulations for skin, hair and textiles that are toxicologically unobjectionable.

Abstract: [Problem] Provision of a novel compound having read-through activity and a drug for the treatment of nonsense mutation-type disease containing this compound. [Solution] A compound represented by the following general formula (1): and a pharmaceutical composition containing this compound.

Abstract: Provided is a compound capable of gelling various aqueous compositions containing salt, acid and the like. An amphoteric ion-type basic amino acid derivative represented by the formula (1A): wherein each substituent is as defined in DESCRIPTION, or a salt thereof.

Abstract: An object of the present invention is to provide an oil soluble compound and a lubricating composition and method of using the same in a differential. The compound can be of formula R?N((CH2)2CONHR?)2, wherein R? can be H or a C8-28 hydrocarbyl group wherein up to 4 carbon atoms in the hydrocarbyl group may optionally be replaced by nitrogen or oxygen atoms, and R? can be H or a C8-28 hydrocarbyl group. The invention further provides a method of producing an oil soluble compound suitable for limited slip performance. The method comprises preparing a Michael adduct from an acrylate and an alkylamine of formula R?NH2, followed by subjecting the Michael adduct to an amidation reaction with a further alkylamine of formula R?NH2.

Abstract: The present invention discloses compounds of 4,4?-diaminostilbene-2,2?-disulphonic acid which are useful as optical brighteners to bleach fibres, cellulose and in particular paper and cardboard.

Abstract: A pentaerythritol core, phosphonic acid terminated dendrimer, its preparation method and application are provided. A preparation method of the pentaerythritol core, phosphonic acid terminated dendrimer (PETA-ADA-12PO3H2) comprises steps of processing Michael addition reaction on pentaerythritol tetraacrylate (C(CH2OCOCH2=CH2)4) and alkylidene diamine (NH2CH2(CH2)nNH2), wherein n is an integer from 1 to 5, so as to obtain pentaerythritol core, amino group terminated dendrimer, and modifying the amino group by methylene phosphonic acid to obtain the PETA-ADA-12PO3H2 having a chemical formula of C[CH2OCOCH2CH2N(CH2PO3H2)CH2(CH2)nN(CH2PO3H2)2]4, wherein n is an integer from 1 to 5.

Abstract: Disclosed are salt compositions of lysinol and dicarboxylic acids; and lysinol derived polymers including polyamide, polyimide, polyurea, cross-linked polyurea comprising urethane linkages, polyurea foams, cross-linked polyurea foams, and lysinol-epoxy thermoset.

Abstract: The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Abstract: The invention relates to a washing or cleaning agent, wherein use thereof generates hydrogel layers surfaces, comprising a hydrogel former having a molecular weight less than 3500 g/Mol, wherein the hydrogel former is water-soluble at concentrations below the minimum gel formation concentration, wherein the minimum gel formation concentration is the concentration at which a yield point of at least 0.05 Pa is formed in a binary solution of water and hydrogel former at T=25° C., and wherein said minimum gel formation concentration lies below 2 wt % of hydrogel former, relative to the system consisting of water and hydrogel former. The washing or cleaning agents according to the invention enable the hydrophiliation of surfaces, and the specific and retarded releasing of active substances embedded in the hydrogel layers, such as aromatic substances or antimicrobial active substances, for example.

Abstract: The invention relates to nitric oxide donor compounds and their use for treating cardiovascular diseases, inflammation, pain, fever, gastrointestinal disorders, ophthalmic diseases, hepatic disorders, renal diseases, respiratory disorders, immunological diseases, bone metobolisms dysfunctions, central and peripheral nervous system diseases, sexual dysfunctions, infectious diseases, for the inhibition of platelet aggregation and platelet adhesion, for treating pathological conditions resulting from abnormal cell proliferation, vascular diseases. The invention also relates to compositions comprising at least one nitric oxide releasing compounds of the invention and composition comprising at least one nitric oxide releasing compounds according to the invention and at least one 15 therapeutic agent.

Abstract: A composition having a polyurea made by reacting a polyisocyanate with one of the below compounds. The value x is 2 or 3. A method of: providing a polyisocyanate and one of the below compounds, spraying the polyisocyanate and the compound with a plural component pump onto a surface to form a mixture, and allowing the mixture to cure to a polyurea.

Abstract: A particulate material for the production of a cement foam which material includes particles including, attached to the particle surface, a surfactant which renders the particles hydrophilic, the surfactant including a moiety which is hydrolysable under alkaline conditions, which surfactant, after loss of the moiety by alkaline hydrolysis, renders the particles partially hydrophobic.

Abstract: The present invention relates to topical trisodium diethylenetriamine pentaacetic acid (DTPA) prodrug formulations and methods of using the same.

Abstract: The invention provides poly(ethylene glycol)-lipid conjugates for use in drug delivery.

Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.

Abstract: The invention relates to the field of pharmaceutical chemistry, specifically to processes for preparing biologically active substances (BAS), in particular creatine amides. What is proposed is a process for preparing creatine amides which comprises treating creatine with para-toluenesulfonic acid in an organic solvent with subsequent reaction of the resultant complex with compounds comprising a primary or secondary amino group in the presence of a condensing agent and a base which are introduced subsequently. The claimed process makes it possible to increase the yield of the end product by 2-5 times in comparison with known similar processes and also to extend the range of the compounds prepared.

Abstract: Systems, techniques and methods for estimating the metabolic state or flux, e.g., the body energy state (“BES”) of a patient, are disclosed. The BES provides deep insight into the nutritional needs of the patient, thus allowing for a sort of exquisite glycemic control with regard to the patient. The invention discloses systems and methods for estimating fractional gluconeogenesis, which is the % of glucose production that comes from gluconeogenesis (“GNG”), as opposed to glycogenolysis (“GLY”), the other form of glucose production. Nutritional formulations, materials, cocktails and methods for feeding patients by parenteral and other means are disclosed. The amount, type and rate of such nutritional feeding are typically based upon the above estimating. The invention discloses formulations that contain labels, such as deuterium, for medical diagnostics, such as for estimating BES and fractional gluconeogenesis.

Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.

Abstract: Poly(?-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Abstract: Compositions and methods of inhibiting the formation of hydrate agglomerates in fluids including water, gas, and optionally liquid hydrocarbons are disclosed. The compositions may include counterions, such as halides or carboxylates. The compositions may also include a thermodynamic hydrate inhibitor, a kinetic hydrate inhibitor, an additional anti-agglomerant, an asphaltene inhibitor, a paraffin inhibitor, a corrosion inhibitor, a scale inhibitor, an emulsifier, a water clarifier, a dispersant, an emulsion breaker, and combinations thereof.

Abstract: Novel macromolecules for filtering contaminants from water and non-aqueous solutions. Molecules such as polyethyleneimine (PEI) may be functionalized, cross-linked, and/or quaternized to improve their binding capacity or selectivity with particular water contaminants such as bromide, nitrate, and sulfate. The macromolecules may be either recyclable or non-recyclable, and may be recovered or separated from water using means such as ultrafiltration, flocculation, or immobilization on a substrate.

Abstract: The present invention provides a method for preparing a sample characterized by binding a substance A containing a hydrazide group to a sugar chain and/or a sugar derivative via hydrazone formation between the hydrazide group of the substance A and the reducing end of the sugar chain and/or the sugar derivative thereby to enable the separation and purification of the sugar chain and/or the sugar derivative for an analytical sample from a biological sample containing the sugar chain and/or the sugar derivative by a simple operation.

Abstract: The present invention provides a compound of Formula Ia, wherein R1 is H or phosphate and the double bond is between N1 and C1 or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N1 C1, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: A dendritic structure includes a core and repeating units, wherein the repeating units comprise units of the type ABxCy, wherein x is 2, 3, or 4, wherein y is 1, 2, or 3, wherein C is selected from the group consisting of azides and alkynes, and wherein every repeating unit is bound to at least one other unit with at least one bond selected from the group consisting of the group consisting of an ester, an amide, a thioether, an ether, a urethane, an amine, and an imine. Advantages include that a “one-pot” growth of the dendritic structure is possible. It is possible to have more functional groups in a dendritic structure. It is possible to add different functional groups simultaneously both to an inner layer and to an outer layer in a dendritic structure.

Abstract: A compound represented by following formula (I): A-L-{D1-(E)q-D2-(B)m—Z1—R}p. In the formula, A represents a p-valent chain or cyclic residue; L represents a single bond or a divalent linking group; p represents an integer of 2 or more; D1 represents a carbonyl group (—C(?O)—) or a sulfonyl group (—S(?O)2—); D2 represents a carbonyl group (—C(?O)—), a sulfonyl group (—S(?O)2—), a carboxyl group (—C(?O)O—), a sulfonyloxyl group (—S(?O)2O—), a carbamoyl group (—C(?O)N(Alk)-) or a sulfamoyl group (—S(?O)2N(Alk)-); E represents a divalent group; and R represents a hydrogen atom, a substituted or non-substituted C8 or longer alkyl group, a perfluoroalkyl group or a trialkylsilyl group.

Abstract: The invention relates to a compound of the following formula (I): to its method for making it and to its uses for preparing a polymer useful for increasing the heat resistance of polymeric compositions.

Abstract: Disclosed and claimed is a composition and method of inhibiting the formation of hydrate agglomerates in a fluid comprising water, gas, and optionally liquid hydrocarbon comprising adding to the fluid an effective anti-agglomerant amount of the following formula and optionally salts thereof: wherein each R1 is independently absent, C1-C10 alkyl, benzyl, or H; wherein R2 is C1-C10 alkyl; wherein R3 C1-C10 alkyl; and wherein R4 is C4-C22 alkyl or alkenyl.

Abstract: The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved by incorporating amide-extended maleimides into an adhesive formulation. Amide-extended maleimides described herein can be used to toughen bismaleimide thermosetting materials without sacrificing any thermal stability. Amide-extended maleimides are readily prepared by reacting a bismaleimide with an appropriate amine via the well-known Michael addition reaction. Acylation of the resulting secondary amines provides the amide-extended maleimide. The acylating agent can also be used to introduce polymerizable functional groups into the backbones of these thermoset monomers. Amide-extended acrylate and methacrylate monomers can also be prepared.

Abstract: The present invention is in relation to a dendritic molecule having symmetrically sited branches having four or more generations of dendrimers wherein the branch points are tertiary amines linked together with oxygen atom of ether and the heteroatoms are separated by a substituted or non-substituted linear three methylene linker. In addition the invention also provides a process to prepare such dendritic macromolecules.

Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 each independently of the other are identical or different organic radicals which do not contain Zerewitinoff-active hydrogen, and R4, R5, R6 each independently of the others are saturated, linear or branched organic radicals which do not contain Zerewitinoff-active hydrogen and which are also optionally substituted in the chain by heteroatoms, for use in a polyurea system which is provided in particular for sealing, bonding, gluing or covering cell tissue. The invention further provides a polyurea system comprising the compound according to the invention, and a metering system for the polyurea system according to the invention.

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: 2R-dodecyl 2-(N,N dimethylamino)-propionate (R-DDAIP) provides an unexpectedly improved activity in facilitating transport of a pharmaceutically active compound across biological membranes and tissues, compared to S-DDAIP of the same enantiomeric purity, or racemic DDAIP. Purified S-DDAIP is also provided.

Abstract: The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): wherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(?O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.

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 present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.

Abstract: The objective of the present invention is to provide a process for simple and efficient preparation of an intermediate compound to synthesize a gadolinium complex having a substituent for improving a retention property in blood time and specificity to an intended organ. The objective of the present invention is also to provide an intermediate compound produced by the said production process. The process for preparation of the diethylenetriaminepentaacetic acid derivative (I): wherein R1 to R5 are independently C1-6 alkyl groups; comprising the steps of: reacting a diethylenetriaminepentaacetic acid pentaester with a halogenated ally compound in an aprotic solvent; removing the excess halogenated ally compound (III); and reacting a reaction product of the diethylenetriaminepentaacetic acid pentaester and the halogenated ally compound with a base in a solvent.

Abstract: The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enzyme.

Abstract: This invention discloses a method of preservation of a food product comprising the step of adding 1) a first component comprising between 10 ppm and 1% of a biocidal salt of N?—(C1-C22) alkanoyl di-basic amino acid alkyl (C1-C22) ester cationic biocidal molecule with an anionic counterion, and 2) a second component comprising from 10 ppm to 1% by weight an acyl monoglyceride, directly to a food product. The preferred cationic biocidal molecule comprises N?-lauroyl-L-arginine ethyl ester (“LAE”). The invention also discloses the method of preservation of a food product using salts of a N?—(C1-C22) alkanoyl di-basic amino acid alkyl (C1-C22) ester cationic biocidal molecule and an anionic counterion with or without a monoglyceride of a fatty acid, whereby the packaging film is compounded with the salts and the optional monoglyceride of a fatty acid.

Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.