Abstract: The application relates to a process for the synthesis of organic sulfonic acid salts of amino acid esters comprising the steps of (i) reacting at least one lactam with at least 3 carbon atoms in the lactam ring with at least one organic sulfonic acid in an aqueous solution, (ii) esterification of the organic sulfonic amino acid salt of step (i) with at least one alcohol with at least 8 carbon atoms comprising at least one hydroxyl group, (iii) optionally removal of water and/or removal of excess alcohol of step (ii). The application also relates to organic sulfonic acid salts of amino acid esters of the general formula (I).

Abstract: A formulation and a composition that comprises it for promoting the pollination of almond tree crops (Prunus dulcis) by biasing the foraging preferences of the honey bee (Apis mellifera). The formulation comprises the compounds limonene, linalool and benzaldehyde. Additionally, a method for targeting the bees' pollinizing activity towards the almond tree crops by using the formulation comprising the compounds limonene, linalool and benzaldehyde.

Abstract: Provided are prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof.

Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.

Abstract: The instant invention provides for 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. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Abstract: The subject matter of the present invention is an improvement in the continuous production of methyl (meth)acrylate or of ethyl (meth)acrylate by direct esterification of (meth)acrylic acid with methanol or ethanol, under reaction conditions for which the acid is in excess relative to the alcohol, in particular with an acid/alcohol molar ratio of between 1.0 and 4, and under a pressure ranging from atmospheric pressure to 5 bar. The process of the invention makes it possible to minimize the formation of ethyl ethoxypropionate during the esterification reaction, and results in an improvement in the material balance, simplification of the purification train for the desired ester, and optimization of the energy balance.

Abstract: A process for preparation of diethyl 2-aetamido-2-(4-octyl phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (Ia) having associated impurities below the regulatory limits.

Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.

Abstract: The instant invention provides for 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. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Abstract: This invention relates to semi-solid compositions and semi-solid pharmaceutical products for use in the photodynamic treatment (PDT) of cancer, pre-cancerous conditions and non-cancerous conditions in the female reproductive system, the anus and the penis, preferably for use in PDT of endometrial, cervical, vulvar, vaginal, anal and penile dysplasia and HPV infections of the uterus, cervix, the vulva, the vagina, the anus and the penis. The semi-solid compositions and pharmaceutical products comprise an active ingredient which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative of 5-ALA or pharmaceutically acceptable salts thereof. The invention relates further to methods of PDT of cancer, pre-cancerous conditions and non-cancerous conditions in the female reproductive system, the anus and the penis, wherein said semi-solid compositions and pharmaceutical products are used.

Abstract: The present invention concerns a process for preparing esteramide compounds. More particularly, the invention relates to a process for preparing esteramide compounds by reaction between a diester and an amine, in the presence of a basic compound, wherein the basic compound and the amine in gaseous form are co-added to the diester, the reaction being conducted at a temperature of 30° C. or higher.

Abstract: The invention relates to new derivatives of 5-aminolevulinic acid (5-ALA) and their use as photosensitizing agents. In particular, it relates to compounds of general formula I and their pharmaceutically acceptable salts, to methods for preparing such compounds and their medical and cosmetic use, for example in methods of photodynamic therapy and diagnosis: wherein R1 represents a hydrogen atom or an optionally substituted alkyl or cycloalkyl group; R2, each of which may be the same or different, represents a hydrogen atom or an optionally substituted alkyl group; and X is a linking group.

Abstract: The instant invention provides for 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. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

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: A method of producing an epoxy compound, which comprises reacting hydrogen peroxide with a compound having a carbon-carbon double bond, in the presence of at least one of a tungsten compound and a molybdenum compound; and an onium salt comprising 20 or more carbon atoms and one or more of substituents convertible to a functional group containing an active hydrogen or a salt thereof.

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: 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: The invention pertains to a new route to prepare ?-functionalized carboxylic acid esters in a one-pot reaction, by reacting an olefinic acid ester in the presence of a catalyst system, comprising a Rh(I)-complex, together with an aryl boron or a diamine as nucleophilic compounds, and under oxygen-free conditions and elevated temperatures.

Abstract: Methods to convert unsaturated fatty acids derived from biobased oils to highly functionalized esters, ester polyols, amides, and amide polyols. The products can be used to make polyurethane and polyester films and foams.

Abstract: The present invention relates to stilbene and quinine compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis- or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BBOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior stilbenes.

Abstract: The invention relates to enantiomerically pure DOTAP chloride and stable crystal modifications of (2R,S)-, (2S)- and (2R)-DOTAP chloride, to a process for the preparation of these modifications, and to the use thereof as constituent for the preparation of medicaments.

Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

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: One subject of the present invention is the use, as solvents, of compounds of esteramide type. Another subject of the invention are particularly practical processes for preparing esteramides. Another subject of the invention are novel esteramides, which may in particular be used as solvents, for example in phytosanitary formulations.

Abstract: The present invention relates to aqueous concentrate formulations for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its anhydrate; N-(phosphonomethyl)glycine in the form of its free acid, in the form of the ammonium salt or a substituted ammonium salt or a mixture thereof; at least two different non-ionic surfactants with at least one of them comprising an ethylene oxide polymer moiety or an ethylene oxide/C3-C4-alkylene oxide block copolymer moiety, and water; wherein the pH-value of the formulation is below 6.

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: The invention relates to a method for the synthesis of ?-amino alkanoic acids or esters thereof starting from unsaturated natural fatty acids passing through an ?-unsaturated nitrile intermediate compound.

Abstract: Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.

Abstract: Cleansing compositions include a mixture of alkyl ether carboxylic acids and/or salts thereof, each having a structure according to formula (1): R1—O—(CH2CH2O)n—CH2—COOM??(1) where R1 is an alkyl group having 4 to 22 carbon atoms, n is a number of from 0 to 20, and M is a hydrogen atom, alkali metal, alkaline earth metal, ammonium, or organic ammonium. The mixture includes alkyl ether carboxylic acids and/or salts having at least two different alkyl groups R1, an average carbon number of alkyl groups R1 of alkyl ether carboxylic acids and/or salts in the mixture is from 10.8 to 12.

Abstract: The presently disclosed subject matter provides compounds of the formula, formula (Ia): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, and n are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting acid ceramidase and ceramidase-related activity, and their use as drugs and prodrugs in the treatment and/or prevention of diseases associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, asthma, and atopic dermatitis.

Abstract: The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula in which W is methyl, X is alkyl, alkenyl or alkinyl, Y is hydrogen, methyl, ethyl, i-propyl, alkenyl or alkinyl, and Z is hydrogen, alkyl, alkenyl or alkinyl, with the proviso that at least one of X, Y, or Z represents a chain having at least two carbon atoms and with the further proviso that X is not ethyl when Z is hydrogen and Y is methyl, and CKE represents the group in which B is hydrogen, alkyl or alkoxyalkyl, A and Q1 together are optionally substituted alkanediyl or alkenediyl, Q2 is represents hydrogen or C1-C4-alkyl, and G represents hydrogen or an acyl or acyl-like group, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The invention relates to a method for the synthesis of amino acids/esters of general formula NH2—(CH2)n—COOR in which n is an integer between 5 and 14, and R is either H or an alkyl radical including from 1 to 4 carbon atoms, from natural long-chain mono-unsaturated fatty acids or esters including at least 10 adjacent carbon atoms per molecule, said method comprising: first converting, if necessary, said natural long-chain fatty acid or ester into a monounsaturated fatty acid/ester of general formula R1—(CH2)m—CH?CH—(CH2)p—COOR in which R1 is H, CH3 or a COOR radical, m is an integer between 0 and 14 and p is an integer between 2 and 11, then submitting the latter to a crossed catalytic metathesis reaction with a compound of formula R2—CH?CH—R3 in which R2 is either H or CN and R3 is CN or CH2NH2, provided that if R2 is CN, R3 can be only CN, and finally converting the resulting product of the general formula R3—CH?CH—(CH2)p—COOR into an amino-acid, either by hydrogenation, or by hydrogenation of the triple t

Abstract: A method for delivering a nucleic acid to a cell can include exposing sample cells to a composition which includes charged lipids.

Abstract: Multifunctional green (eco-friendly) and antimicrobial compositions are described containing cationic glycine betaine esters and/or cationic glycine betaine amides. Particular glycine betaine esters and amides are alkyl(ene) betainate methane sulfonates and betainyl amino alkyl(ene) methane sulfonates. The glycine betaine components are cationic, have a hydrophobic group attached to a carboxylate group through an ester or amide linkage, and are derived from a natural source, such as sugar beets. The glycine betaine esters and amides serve as cationic surfactants which have effective antimicrobial activity. The surfactant compositions are effective as crude mixtures or semi-purified mixtures or purified surfactant compounds of glycine betaine components. The addition of sodium chloride or potassium chloride or magnesium chloride or natural gum or polysaccharide to compositions containing the cationic glycine betaine ester and/or glycine betaine amide derivatives serves to thicken or gel the composition.

Abstract: The present invention is directed to a process for the production of high density polyethylene by polymerisation of ethylene in the presence of a supported chromium oxide based catalyst which is modified with an organic compound comprising oxygen and a nitrogen atom which is selected from the group consisting of saturated heterocyclic organic compounds with a five or six membered ring, amino esters and amino alcohols. Such organic compounds allow manufacturing of HDPE with increases molecular weight distribution and increased molecular weight.

Abstract: An anti-foam additive for a cement composition, including a fatty alcohol ester that is soluble in an aqueous medium at acidic pH, and hydrolysable in a basic medium, i.e. when the ester is incorporated into the cement composition, while releasing an active anti-foam molecule. This ester is preferably a fatty alcohol ester of a quaternary ammonium carboxylate, that is soluble in an aqueous solution of a superplasticizer, such as a polycarboxylate with poly(ethylene oxide) side chains. The additive can used for reducing the amount of air entrained during mixing or blending of mortars or concretes.

Abstract: The instant invention provides for 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. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Abstract: The invention relates to a series of novel chiral phosphorus ligands of formulae (Ia) and (Ib): wherein R, 1-rR>4 and X are as defined herein. The invention also relates to chiral metal complexes prepared with these chiral phosphorus ligands. The chiral metal complexes are useful as catalysts for carrying out asymmetric hydro genation.

Abstract: The invention provides use of a photosensitiser, which is a derivative (e.g., an ester) of 5-aminolevulinic acid (5-ALA) or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the prevention or treatment of acne.

Abstract: The present invention relates to a method for preparing esteramide compounds. More particularly, the invention relates to a method for preparing esteramide compounds by reaction between a diester and an amine, in the presence of a basic compound, wherein the amine is solubilized in an organic solvent or in the diester, when the amine is solubilized in an organic solvent, the diester is added onto the reaction mixture comprising the amine and the basic compound, when the amine is solubilized in the diester, the basic compound is added onto the reaction mixture comprising the amine and the diester (II), the reaction is conducted at a temperature greater than or equal to 30° C., the amine is present in molar excess ranging from 0.01 to 50% relatively to the diester.

Abstract: Crosslinked polymers, methods for their preparation and use, are described in which the crosslinked polymers are formed from at least two polymer precursors, one of which is designed, upon degradation of the crosslinked polymer, to release the second polymer precursor in its original, unmodified chemical form.

Abstract: The invention pertains to a new route to prepare ?-functionalized carboxylic acid esters in a one-pot reaction, by reacting an olefinic acid ester in the presence of a catalyst system, comprising a Rh(I)-complex, together with an aryl boron or a diamine as nucleophilic compounds, and under oxygen-free conditions and elevated temperatures.

Abstract: The use of an esteramide compound, alone or as a mixture of the following formula (I): R1OOC-A-CONR2R3??(I) is described, wherein: A is a covalent bond or a methylene group —CH2—, R1 is an optionally substituted hydrocarbon group having from 1 to 36 carbon atoms, R2 and R3, either identical or different, are groups selected from a hydrogen atom and optionally substituted hydrocarbon groups comprising from 1 to 36 carbon atoms, R2 and R3 may form together a ring having the nitrogen atom to which they are bound, said ring being, if need be, substituted and/or having an additional heteroatom and R2 and R3 not being simultaneously hydrogens. Also described, are applications for using the esteramide compound as a solvent, a co-solvent, a coalescence agent, a crystallization inhibitor, a plasticizer or an agent for increasing biological activity.

Abstract: An esteramide compound of the following formula (I): R1OOC-A-CONR2R3??(I) is described, wherein: A is a covalent bond or a methylene group —CH2—; R1 is an optionally substituted, saturated or unsaturated aliphatic or cycloaliphatic hydrocarbon group including from 5 to 36 carbon atoms, R2 and R3, either identical or different, are groups selected from a hydrogen atom, and optionally substituted hydrocarbon groups, preferably including from 1 to 36 carbon atoms, and R2 and R3 not being simultaneously hydrogen atoms. Also described, are applications for using the esteramide compound, notably as a solvent.

Abstract: The present invention concerns a process for preparing esteramide compounds. More particularly, the invention relates to a process for preparing esteramide compounds by reaction between a diester and an amine, in the presence of a basic compound, wherein the basic compound and the amine in gaseous form are co-added to the diester, the reaction being conducted at a temperature of 30° C. or higher.

Abstract: A positive resist composition comprising (A) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, (B) a resin capable of increasing the solubility in an alkali developer by the action of an acid, and (C) a compound having a specific structure, which decomposes by the action of an acid to generate an acid, a pattern forming method using the positive resist composition, and a compound for use in the positive resist composition are provided as a positive resist composition exhibiting good performance in terms of pattern profile, line edge roughness, pattern collapse, sensitivity and resolution in normal exposure (dry exposure), immersion exposure and double exposure, a pattern forming method using the positive resist composition and a compound for use in the positive resist composition.

Abstract: The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrates, alcohols are preferred examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.

Abstract: Described herein are the synthesis and polymerization of a series of N-Boc-protected amino acid vinyl ester (BAAVE) monomers. Homopolymers and heteropolymers containing the monomers are described, particularly heteropolymers with vinyl ester monomers such as vinyl acetate. Deprotection can be used to produce hydrophilic and hydrophobic polymers that are particular useful in biological applications such as cellular delivery of biological materials.

Abstract: The invention relates to a process for preparing omega-amino acids or their esters, which is characterized by the following steps: c) ozonolysis of unsaturated fatty acids or fatty acid derivatives, d) reductive amination of the reaction mixture obtained from the reaction with ozone, to give the omega-amino acid or ester thereof, the reaction being carried out with a C1-C5 alcohol in a mixture with at least 0.5% by weight of water as solvent, based on the total amount of solvent.