2978results about "Carboxylic acid amides preparation" patented technology

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.

Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.

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 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.

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 generally relates to compositions comprising and methods for forming functionalized carbon-based nanostructures.

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 object of the present invention is to provide PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity.

The present invention provides PPAR activity regulators which comprise an acylamide compound having the specific structure, prodrugs thereof, or pharmaceutically acceptable salts thereof.

Compounds are synthesized that contain nitrogen and hindered phenol functionalities of an aromatic amine and hindered phenol for use as oxidative stabilizers for organic materials, paints, lubricants, elastomers, and in other applications. The disclosed methods can efficiently synthesize target monomers and polymers without the use of expensive catalysts. Further, the disclosed methods can scale up to industrially useful quantities. In general, the methods provide an improved, highly efficient and economical process for the synthesis of macromonomers having nitrogen containing moiety and sterically hindered phenols and their corresponding polymers.

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

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

A process for the industrial synthesis and a new crystalline form of the compound of formula (I):

Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

The invention provides a method of preparing a compound of formula 2

wherein R¹ and R⁶ are as defined herein, by a catalytic amidation process in the presence of added carbon dioxide. The inventive methods show surprising rate enhancement relative to the corresponding uncatalyzed reaction.

In an alcohol fermentation process, oil derived from biomass is chemically converted into an extractant available for in situ removal of a product alcohol such as butanol from a fermentation broth. The glycerides in the oil can be chemically converted into a reaction product, such as fatty acids, fatty alcohols, fatty amides, fatty acid methyl esters, fatty acid glycol esters, and hydroxylated triglycerides, and mixtures thereof, which forms a fermentation product extractant having a partition coefficient for a product alcohol greater than a partition coefficient of the oil of the biomass for the product alcohol. Oil derived from a feedstock of an alcohol fermentation process can be chemically converting into the fermentation product extractant. The oil can be separated from the feedstock prior to the feedstock being fed to a fermentation vessel, and the separated oil can be chemically converted to a fermentation product extractant, which can then contacted with a fermentation product comprising a product alcohol, whereby the product alcohol is separated from the fermentation product.

The present invention generally relates to processes for the chemocatalytic conversion of a carbohydrate source to an adipic acid product. The present invention includes processes for the conversion of a carbohydrate source to an adipic acid product via a furanic substrate, such as 2,5-furandicarboxylic acid or derivatives thereof. The present invention also includes processes for producing an adipic acid product comprising the catalytic hydrogenation of a furanic substrate to produce a tetrahydrofuranic substrate and the catalytic hydrodeoxygenation of at least a portion of the tetrahydrofuranic substrate to an adipic acid product. The present invention also includes products produced from adipic acid product and processes for the production thereof from such adipic acid product.

The invention relates to a solid emulsifier used for oil base drilling fluid, a preparation method and an application of the oil base drilling fluid. The preparation method comprises the following steps: adding diethylenetriamine in organic acidity, adding a catalyst, heating to the temperature of 175-185 DEG C, and reacting for 1-3 hours to obtain an intermediate product which has a code name AMI-1. cooling the reaction temperature to 90-120 DEG C, adding acid anhydrides, continuously reacting for 2-4 hours, cooling to the room temperature, wherein the products is the dark brown solid, using a pulverizer for crushing to obtain the brown-red solid powder which is the emulsifier with code name EmuL-S. The emulsifier has good emulsification effect on the diesel oil, the white oil and a synthesis group, and has strong anti-temperature capability, and is cooperated with organic soil, a filtrate reducer, a wetting agent and a weighting material for constructing a high performance oil base drilling fluid system; because that the emulsifier is the powdery solid, so that the influence due to environment is little, and the storage and transport are convenient.

The invention specifically relates to a preparation method for a dual inhibitor LCZ696 of angiotensin II receptor and neprilysin, which belongs to the technical field of drug synthesis. The preparation method comprises the following steps: preparing valsartan and AHU-377 or AHU-377 calcium salt at first; and then mixing valsartan with AHU-377 or AHU-377 calcium salt under stirring so as to prepare LCZ696. The LCZ696 prepared in the invention has good quality and high purity; and the preparation method has the advantages of simplicity, low energy consumption, low cost and suitability for large batch production.

The present invention provides the S enantiomer of a compound of formula (I); wherein R¹ represents 2,4-difluorophenyl or cyclohexyl as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R₃ are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.

Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.