7585results about "Carboxylic acid amides preparation" patented technology

An antimicrobial composition comprising: a complex of an anionic polyester with an antimicrobial cationic surfactant, wherein the anionic polyester has at least one carboxylic group. A medical device having an antimicrobial composition comprising: a complex of an anionic polyester with an antimicrobial cationic surfactant wherein the anionic polyester has at least one carboxylic group.

The present invention relates to novel acid-free quaternized nitrogen compounds, to the preparation thereof and to the use thereof as a fuel and lubricant additive, more particularly as a detergent additive, as a wax antisettling additive (WASA) or as an additive for reducing internal diesel injector deposits (IDID); to additive packages which comprise these compounds; and to fuels and lubricants thus additized. The present invention further relates to the use of these acid-free quaternized nitrogen compounds as a fuel additive for reducing or preventing deposits in the injection systems of direct-injection diesel engines, especially in common-rail injection systems, for reducing the fuel consumption of direct-injection diesel engines, especially of diesel engines with common-rail injection systems, and for minimizing power loss in direct-injection diesel engines, especially in diesel engines with common-rail injection systems.

The invention relates to novel crosslinkable copolymers which are obtainable by (a) copolymerizing at least two different hydrophilic monomers selected from the group consisting of N,N-dimethyl acrylamide (DMA), 2-hydroxyethyl acrylate (HEA), glycidyl methacrylate (GMA), N-vinylpyrrolidone (NVP), acrylic acid (AA) and a C1-C4-alkoxy polyethylene glycol (meth)acrylate having a weight average molecular weight of from 200 to 1500, and at least one crosslinker comprising two or more ethylenically unsaturated double bonds in the presence of a chain transfer agent having a functional group; and (b) reacting one or more functional groups of the resulting copolymer with an organic compound having an ethylenically unsaturated group.

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel 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 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.

The invention provides substituted diaryl compounds as shown in general formula (I) or their pharmaceutically acceptable salts, and also provides a preparation method; a class of novel broad-spectrum antiviral compounds and pharmaceutical salts targeting cytokines are screened and obtained through studies on structure-activity relationship and action mechanism of active compounds; the compounds not only have significant broad-spectrum antiviral activity, but also have the advantages of low toxicity and good pharmaceutical properties.

The invention is directed to a process for the preparation of α,β-unsaturated acids, esters and amides from α- or β-hydroxycarboxylic acids or esters or precursors in high yields and high selectivity. The α,β-unsaturated acids or esters are optionally prepared in the presence of specific dehydration and / or esterification catalysts. The α,β-unsaturated amides or substituted amides are prepared optionally in the presence of a dehydration and / or amidation catalyst. The source of α- or β-hydroxycarboxylic acids or precusor is preferably from a renewable resource. The precursor is defined herein.

Nitrogen-containing lipids prepared from the conjugate addition of amines to acrylates, acrylamides, or other carbon-carbon double bonds conjugated to electron-withdrawing groups are described. Methods of preparing these lipids from commercially available starting materials are also provided. These amine-containing lipids or salts forms of these lipids are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these lipids, they are particularly suited for the delivery of polynucleotides. Complexes or nanoparticles containing the inventive lipid and polynucleotide have been prepared. The inventive lipids may also be used to in preparing microparticle for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Transport reagents and conjugates of therapeutic agents linked to transport reagents are described. In particular, the transport reagents have a plurality of guanidinium moieties that are either contiguous or spaced along a backbone, but are sufficiently removed from the backbone via tethers, to allow their interaction with a cell or tissue surface, leading to uptake of the therapeutic agent.

The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and / or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and / or other clinical therpauetic and / or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

The invention relates to a catalyst for selective hydrogenation reaction of an aromatic nitrocompound and a preparation method of the catalyst. The catalyst consists of a catalyst carrier and active metal coated with carbon, wherein the catalyst carrier includes a carbon-base carrier, SiO2, TiO2 or Al2O3; the active metal is selected from Co, Fe, Ni or Cu and other poor and noble metals. The catalyst is prepared by adopting a Pechini type sol-gel process which comprises the steps of dispersing an active metal precursor to water containing a coordination compound, adding a polyhydric alcohol solution and a macromolecule auxiliary, then adding the carrier, stirring for dispersion, carrying out hydrothermal reaction, separating out solid on the lower layer, and calcining in the inert atmosphere to obtain the catalyst in which carbon coats the active metal. Compared with the prior art, the catalyst can realize the hydrogenation reaction of a substituted aromatic nitrocompound in the mild condition; substrate conversion rate and production selectivity are high; the catalyst has recyclable economy and good application prospect.

The present invention provides compositions and methods for relieving pain at a site in a human or animal in need thereof by administering at a discrete site in a human or animal in need thereof a dose of capsaicin in an amount effective to denervate a discrete site without eliciting an effect outside the discrete location, the dose of capsaicin ranging from 1 μg to 3000 μg.

One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

The invention discloses a method for synthesizing a novel amphoteric slow-breaking quick-setting asphalt emulsifier, belonging to the technical field of organic chemical synthesis. The method comprises the following steps of: reacting oleic acid with polyamine to generate acid amide polyamine, and then adding chloroactic acid to generate halogenating reaction to prepare the asphalt emulsifier, wherein the polyamine is the mixture of diethylenetriamine and triethylene tetramine. The water solubility of the hydrophilic radical of the emulsifier synthesized by the process is stronger than those of like emulsifiers, thereby obviously lowering the critical micelle concentration (CMC) value, and the particles of the produced asphalt emulsion are finer, smoother and evener. The emulsifier can effectively prevent asphalt from settling, increases the storage stability of the asphalt emulsion, reasonably regulates the charge ratio, widens the selectivity on stone materials in the application of slurry seal construction, enables the mixing time to be sufficient, and has obvious quick-setting effect and improved project quality.

A method for preparing a highly purified N-long chain acyl neutral amino acid for use of a detergent and the like in a simple and convenient manner and in a high yield by reacting a neutral amino acid such as glycine, gamma-aminobutyric acid, and alanine, with a saturated or unsaturated fatty acid halide having 8 to 22 carbon atoms, wherein the reaction is performed in a mixture of water and one or more kinds of hydrophilic organic solvents selected from the group consisting of acetone, acetonitrile, a secondary alcohol having 3 or 4 carbon atoms, and a tertiary alcohol having 4 carbon atoms such as isopropanol, sec-butanol, and tert-butanol in the presence of a base.

Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration are provided, and methods of preparation of the modified amino acid compound are provided.

The invention relates to an improved process for producing organomolybdenum compositions with high molybdenum content that are highly useful as lubricant additives, in which the process involves reacting a fatty oil with a diamine, followed by reaction with a molybdenum source. The process of the present invention does not require a volatile organic solvent to promote molybdenum incorporation and produces an organomolybdenum composition having a high molybdenum content. In addition, the process can be conducted in the absence of sulfur and phosphorus-containing reactants.

The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.

The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and / or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and / or other clinical therpauetic and / or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

Cleaning compositions comprising (A) N-long-chain acyl neutral amino acid or a salt thereof, (B) N-long-chain acyl neutral amino acid dipeptide or a salt thereof, and (C) N-long-chain acyl neutral amino acid tripeptide or a salt thereof provide abundant foam, are excellent in foam retaining properties, and furnish a cleaned and dried body or hair with both a smooth feeling and a moist feeling. Compositions which further comprise (D) a higher fatty acid having 8 to 22 carbon atoms or a salt thereof exhibit enhanced creamy properties in foam quality. N-long-chain acyl neutral amino acids or salts thereof may be conveniently prepared by mixing a neutral amino acid, a long-chain fatty acid, and at least one of an alkaline substance selected from sodium hydroxide and potassium hydroxide, and maintaining the mixture with heating, while removing the water produced during the reaction, with no catalyst being employed.

A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Economical and efficient processes for producing an alpha, beta-unsaturated carboxylic acid heterocycle-inserted ester and an alpha,beta-unsaturated carboxylic acid polyheteroalkylene ester as well as a catalyst suited for use in economically and efficiently producing an alpha,beta-unsaturated carboxylic acid ester are provided. The invention provides (1) a process for producing an alpha,beta-unsaturated carboxylic acid ester which comprises reacting an alpha,beta-unsaturated carboxylic acid ester with a heterocyclic compound, (2) a process for producing an alpha,beta-unsaturated carboxylic acid ester which comprises reacting an alpha,beta-unsaturated carboxylic acid with a heterocyclic compound in the presence of a polymerization inhibitor and a metal oxide catalyst, and (3) a catalyst for the production of an alpha,beta-unsaturated carboxylic acid ester comprising a metal oxide.

A method for preparing diphenol compounds, which method includes the steps of coupling a hydroxyphenyl carboxylic acid with a L-tyrosine ester in a water-miscible organic reaction solvent containing a carbodiimide capable of forming a water-solvent urea by-product, thereby forming a diphenol reaction product; and combining the reaction mixture with an amount of water effective to precipitate the diphenol as a water-immiscible organic phase, so that a water-immiscible organic phase is formed containing the diphenol reaction product. New diphenol monomers and polymers polymerized therefrom are also disclosed.

Saturated and unsaturated compounds having sweet, salt or umami taste enhancement qualities. The compounds have the structure: where R1═H or methyl; R2 is selected from the group consisting of H, C1-C4 alkyl, alkenyl and methylene; R3 is selected from the group consisting of H, C1-C8 straight or branched chain alkyl, alkenyl, dienalkyl or phenyl; or if R1═H, R2 and R3 taken together can represent cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, or cyclohexenyl; R4 is selected from the group consisting of H, methyl and ethyl; R5 is selected from the group consisting of H, methyl and ethyl; R6 is selected from the group consisting of H, C1-C9 straight or branched chain alkyl, alkenyl, alkyldienyl, acyclic or containing no more than one ring; with the proviso that in structure 1 when R4 is H or Me; and R5═H or methyl, R6 may be selected from the group described above or phenyl.

The invention provides a cationic lipid comprising:(i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor;(ii) a linking moiety of formula (5):—(HNR5)2NC(O)R3C(O)—  (5),wherein:each R5 is independently an optionally substituted C1-4 alkylene moiety; andR3 is an optionally substituted alkylene or alkenylene moiety; and(iii) two lipophilic moieties,wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.