189 results about "Aklanonic acid" patented technology

The instant invention relates to a lubricant composition stabilized against the deleterious effects of heat and oxygen. The composition comprises a hydrotreated or hydrodewaxed oil and an effective antioxidant stabilizing amount of a mixture of a phenolic antioxidant; an N,N-disubstituted aminomethyl-1,2,4-triazole; an aromatic amine antioxidant; an alkyl phenoxy alkanoic acid; and an N-acyl sarcosine derivative. Optionally, further additives are added to the subject lubricant compositions.

A task often encountered in very recent times is the rapid provision of prototypes. Particularly suitable processes are those based on pulverulent materials and in which the desired structures are produced layer-by-layer through selective melting and solidification. The invention provides the constitution, production and use of a copolyamide powder which was produced using the following monomer units: a) laurolactam or ω-aminoundecanoic acid, and also b) dodecanedioic acid, and either c) decanediamine or dodecanediamine, in shaping processes, and also to mouldings produced through a layer-by-layer process which selectively melts regions of a powder layer, using this specific powder. Once the regions previously melted layer-by-layer have been cooled and solidified, the moulding can be removed from the powder bed. The mouldless layer-by-layer processes for the production of components using the copolyamide powder result in simplified and more reliable conduct of the process and better recyclability.

Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

The invention relates to the medicine technical field and concretely relates to a mixture formed by two enantiomorphous eremophilane acids separated from murrey ligularia and the officinal salt as well as the medicine combined material. The enantiomorphous eremophilane acid can be used for preparing the medicine curing hepatitis B virus infectious diseases due to the ability of suppressing the antigenic activity on the surface of hepatitis B virus.

The present invention relates to novel hypolipidemic, antihyperglycemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel beta-aryl-alpha-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R', where D, A, and R' are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

The invention relates to CuInS2 quantum dots with a water-soluble zinc blende structure, CuInS2 / ZnS core shell quantum dots with a water-soluble zinc blende structure and a preparation method thereof. In the CuInS2 quantum dots with the water-soluble zinc blende structure, the atomic ratio of Cu to In to S is 1.17 to 1 to 2.62, the XRD pattern of the CuInS2 quantum dots has three main structural characteristic peaks comprising 28.61 DEG, 47.51 DEG and 55.81 DEG which are corresponding to (111), (220) and (222) in the zinc blende crystal structure. The range of fluorescence-emission peak position of the CuInS2 / ZnS core shell quantum dots with the water-soluble zinc blende structure is 554-710 nm, and the fluorescence quantum yield is 15-30 %, so that the biomedical diagnostic requirements are satisfied. The method combines the popular and mature colloid chemistry synthesis method for preparing oil soluble quantum dots at present, the CuInS2 quantum dots with the water-soluble zinc blende structure and CuInS2 / ZnS core shell quantum dots with the water-soluble zinc blende structure are prepared by using PEG as solvent, sulfhydryl undecanoic acid as ligand and sulfur source, so that the step of biocompatibility modification is saved for later biomedical diagnosis. The quantum dots and the preparation method disclosed in invention have the advantages of short synthesis cycle, simple technology and good repeatability, and are beneficial to the mass production.

Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR / PPARalpha, RXR / PPARgamma, and RXR / PPARdelta heterodimers, are useful in the treatment and / or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

A toxicological friendly antifreeze composition having improved thermal stability is provided. In one embodiment, the antifreeze composition comprises from 5 to 80 wt. % of an aqueous freezing point depressant selected from alkali metal salts of acetates, formates, proprionates, adipiates, and succinates, and mixtures thereof; 0.1 to 10 wt. % of at least one of a 2-ethylhexanoic acid, isononanoic acid and 3,5,5-trimethylhexanoic acid; and 0.1 to 10 wt. % of at least one of octanoic acid, nonanoic acid, decanoic acid, undecanoic acid, dodecanoic acid, neodecanoic acid, benzoic acid, 2-hydroxybenzoic acid, p-terbutylbenzoic acid, and mixtures thereof. In one embodiment, the composition is employed as a concentrate in admixture with 10 to 90 wt. % water.

(20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.

The invention discloses a penicillin antibiotic aptamer obtained by the screening technology for an improved aptamer without a fixed point target substance in the field of screening a penicillin antibiotic aptamer without a fixed point target substance, and an application thereof. The unfixed nucleic acid is eluted through a fixed oligonucleotide library; the parent nucleus 6-APA (6-aminopenicillanic acid) of the penicillin antibiotic is added in positive screening to act on the fixed nucleic acid; after eluting the nucleic acid molecules which can be combined with 6-APA, PCR (polymerase chain reaction) amplification is directly performed for next screening; and other antibiotics are added in negative screening, and the nucleic acid molecules in non-specific binding with the penicillin antibiotics are removed by elution. Through multiple rounds of positive and negative screening, 10 nucleic acid aptamers with high specificity and strong affinity with 6-APA are obtained; and the nucleic acid aptamer with a stable secondary structure is selected for developing a nucleic acid aptamer sensor for detecting 6-APA.

The invention discloses a process for preparing 6-aminopenicillanic acid, which comprises the following steps: (1) filtering the penicillin fermentation liquid, acidifying, extracting and concentrating with butanol, decoloring to obtain butyl extract of penicillin, (2) subjecting butyl extract of penicillin to back extraction with alkaline solvent, obtaining aqueous solution of penicillin salts, (3) degreasing the aqueous solution of penicillin salts, (4) loading the degreased aqueous solution of penicillin salts into penicillin acylated enzyme retort for enzyme conversion, charging 6-APA seeds, cultivating quartz, crystallizing and drying.

An antifreeze composition having improved thermal stability is provided. In one embodiment, the antifreeze concentrate composition comprises from 50 to 99 wt. % of a glycol-based freezing point depressant selected from the group of: alkylene glycols, glycol monoethers, glycerins, and mixtures thereof; 0.01 to 10 wt. % of at least one of a 2-ethylhexanoic acid, isononanoic acid and 3,5,5-trimethylhexanoic acid; and 0.01 to 5 wt. % of at least one of octanoic acid, nonanoic acid, decanoic acid, undecanoic acid, dodecanoic acid, neodecanoic acid, benzoic acid, 2-hydroxybenzoic acid, p-terbutylbenzoic acid, and mixtures thereof. In one embodiment, the composition is employed as a concentrate in admixture with 10 to 90 wt. % water.

The invention discloses a method for synthesizing cephalothin acid by using 7-aminocephalosporanic acid (7-ACA) as a raw material, which is characterized in that: the 7-ACA and a 2-thiophene acetylation reagent are subjected to condensation reaction in a water phase solvent, and the production process sequentially comprises the following steps of: performing condensation reaction on the 7-ACA in a water phase; performing centrifugal filtration on a reaction product; refining and decolorizing; and performing crystallization separation, centrifugal filtration and vacuum drying to obtain a cephalothin acid product. The production process is simplified, the requirement on equipment is reduced, the amount of an organic solvent can be saved by over 70 percent, potential safety hazard and environmental pollution due to high consumption of the inflammable, explosive and volatile organic solvent are eliminated, the safety requirement level of the production field is reduced, production cost is greatly reduced, and the method is easy to operate and suitable for mass production and has high technical and economic feasibility.

The invention provides uses and methods for reducing nephropathy in persons with diabetes mellitus (particularly Type 2 diabetes), in persons with metabolic syndrome, in persons with triglyceride levels over 215 mg / dL, and in persons with a cholesterol level over 200 mg / dL, by administering an inhibitor of soluble epoxide hydrolase (“sEH”). Optionally, a cis-epoxyeicosantrienoic acid (“EET”) can be administered with the sEH inhibitor. The invention further provides for using EETs in conjunction with one or more sEH inhibitors to reduce hypertension, and for compositions of EETs coated with a material insoluble in an acid of pH 3 but soluble in a solution with a pH of 7.4 or higher.

The present invention relates to a process for preparation of 7-amino-3-[2-(furylcarbonyl)thiomethyl]-3-cephem-4-carboxylic acid (I) by the condensation of 7-aminocephalosporanic acid (II) with furyl-2-carbonylthiol (III) in the presence of borontrifluoride or its complex, in an organic solvent or mixture of solvents at 0-50° C.

The method of the invention relates to an OmCI polypeptide or a polynucleotide encoding an OmCI polypeptide for the treatment of a disease or condition mediated by a leukotriene or hydroxyeicosanoid.

The invention discloses a compound Chinese medicine extract preventing arteriosclerosis, comprising the following effective ingredients: dried alcohol, Beta-sitosterol, hexacosanoic acid, butenolide III, oleanolic acid, berberine, jateorhizine, coptisine, salvianic acid A, salvianolic acid B, ring-tetracosane, 9,12-octadecadienoic acid, 5,7-dimethoxy coumarin, specnuezhenide, ginsenoside Rb1 and Rg1, notoginsenoside R1, encommiol and the like. A preparation method of the extract is as follows: taking salvia miltiorrhiza, fructus ligustri lucidi, rhizoma coptidis, cirsium japonicum, eucommia bark, atractylodes macrocephala koidz, radix pseudo-ginseng and bergamot as raw materials, conducting C1-3 alcohol extraction and / or water extraction on a total extract, then extracting the total extract by organic solvents with different polarities so as to obtain all the effective ingredients, and finally mixing the effective ingredients so as to obtain the compound Chinese medicine extract preventing arteriosclerosis. As for the compound Chinese medicine extract, a large number of ineffective chemical ingredients are removed, so that the content of effective ingredients is improved greatly, the influence on product processing and preparation quality caused by the ineffective ingredients is reduced, the preparation process is stable, the product quality is controllable, and the mass production is facilitated.

The invention provides new phenoxy carboxylic acid derivatives represented by the formula A-COX-L-ONO2. The structure is characterized by linking nitrate and carboxyl in phenoxy carboxylic acid molecule through coupling bridge structure. In the formula, A is the role for the phenoxy residues of phenoxy acetic acid compounds with lipid-lowering effect, X represents O or NH, and L is for C2-C6 alkyl and substituted alkyl, C3-C6 naphthene, hydroxyl-containing amino acid residues such as serine and threonine residues, or dialkyl substituted piperazine. The invention also provides the drug combinations using the new phenoxy carboxylic acid derivatives as active components and their applications in liver treatment and lipid-lowering.

This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (ii) at a side-chain carboxylate of one or more Asp or GIu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulfhydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and / or (v) at the N-terminus with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group, wherein said N-terminus is previously amidated with an alpha- or beta-hydroxy acid, and wherein the ester is formed between the hydroxy group of said alpha- or beta-hydroxy acid and the carboxylic group of said guanidinium alkanoic acid or said PEG substituted with a guanidinium group and a carboxyl group; and / or (b) which contains one or more disulfides, the disulfide being formed between the sulfhydryl group of a Cys reside, if present, and a guanidinium alkanethiol or a PEG substituted with a guanidinium group and a sulfhydryl group.

The invention discloses a compound 2-hydroxyl-3-carbonyl-23-oleanolic acid-1,4,12-triene-28-acid as well as a preparation method and application of the compound preparation of a glycosidase inhibitor medicine. An alpha-glucosidase inhibitor with high efficiency is extracted and separated from an akebia plant, a plant material is rich in source, an extraction preparation method is easy to operate, the plant can be used for a long time without being damaged when extraction is performed by adopting a plant fruit, and thus the economic benefit can be increased, and the environment friendliness is achieved; the monomeric compound is stable and easy to store. Pharmacological experiments prove that the inhibitory activity of the compound 2-hydroxyl-3-carbonyl-23-oleanolic acid-1,4,12-triene-28-acid is stronger than that of a first-grade diabetes drug acarbose by about 16 times, and thus the compound 2-hydroxyl-3-carbonyl-23-oleanolic acid-1,4,12-triene-28-acid can be expected to be further developed into a medicine for clinically treating type 2 diabetes mellitus and is good in prospect.

The invention belongs to the technical field of biopharmaceuticals and biochemicals, and particularly relates to a method for synthesizing (R)-beta-hydroxyl-tetradecanoate compounds. The method includes the steps that beta-carbonyl-tetradecanoate is reacted in a mixed solution of ketoreductase, glucose, glucose dehydrogenase, NADP<+> and a buffer solution to obtain (R)-beta-hydroxyl-tetradecanoate. The method is an enzyme-catalyzed biosynthesis method, the operation is simple, the equipment is conventional equipment, the process is environmentally friendly, and obtained products are high in purity, high in yield and high in ee value.

Disclosed are novel oxylipins, referred to herein as docosanoids and eicosanoids, that are derived from C22 polyunsaturated fatty acids and from C20 polyunsaturated fatty acids, respectively, and methods of making and using such oxylipins. Also disclosed is the use of docosapentaenoic acid (C22:5n-6) (DPAn-6), docosapentaenoic acid (C22:5n-3) (DPAn-3), and docosatetraenoic acid (DTAn-6: C22:4n-6),docosatrienoic acid (C22:3n-3) (DTrAn-3), docosadienoic acid (C22:2n-6) (DDAn-6), eicosatrienoic acid (C20:3n-3) (ETrAn-3) eicosapentaenoic acid and arachidonic acid as substrates for the productionof novel oxylipins, and to the oxylipins produced thereby. Also disclosed is the use of DPAn-6, DPAn-3, DTAn-6, and / or the oxylipins derived therefrom, and / or novel docosanoids derived from the structures of C22 fatty acids in therapeutic and nutritional or cosmetic applications, and particularly as anti-inflammatory or anti-neurodegenerative compounds. The invention also relates to novel ways ofproducing long chain polyunsaturated acid (LCPUF A)-rich oils and compositions that contain enhanced and effective amounts of LCPUF A-derived oxylipins, and particularly, docosanoids.

A process for producing medium-chain-length 3-hydroxyalkanoic acids in a liquid medium, the process comprising: (i) intermixing a liquid culture medium and a microbial inoculum comprising a pure culture of a Pseudomonas putida strain having a portion of a phaC1 gene deleted and / or a portion of a phaC2 gene deleted and / or a portion of a phaZ gene deleted, (ii) culturing the mixture for a period of time to allow for microbial cell growth to occur in the liquid culture medium thereby producing a spent liquid medium and a plurality of microbial cells wherein medium-chain-length 3-hydroxyalkanoic acids are synthesized, (iii) separating the medium-chain-length 3-hydroxyalkanoic acids from the plurality of microbial cells and the spent liquid medium; and (iv) recovering the separated medium-chain-length 3-hydroxyalkanoic acids. A pure culture comprising transgenic microbial cells wherein a portion of a phaC1 gene and / or a phaC2 gene and / or a phaZ gene has been deleted.

The invention discloses DNA (Deoxyribose Nucleic Acid) of a novel acetylxylan esterase, which has a nucleotide sequence shown as SEQ AXENO.1 and an amino acid sequence shown as SEQAXENO.2. Highest activity is obtained when a protein structure is a homotrimer. The invention also discloses a cloning vector containing the DNA of the novel acetylxylan esterase, a cloning technology and application of a recombinant esterase to hydrolysis of a short-chain fatty acid and acyl saccharides and application of the recombinant esterase to production of deacetylated 7-aminocephalosporanic acid and deacetylated cephalosporin C which are important intermediates of beta-lactam antibiotics; and the novel acetylxylan esterase has an important industrial application value.

The invention provides uses and methods for reducing nephropathy in persons with diabetes mellitus (particularly Type 2 diabetes), in persons with metabolic syndrome, in persons with triglyceride levels over 215 mg / dL, and in persons with a cholesterol level over 200 mg / dL, by administering an inhibitor of soluble epoxide hydrolase (“sEH”). Optionally, a cis-epoxyeicosantrienoic acid (“EET”) can be administered with the sEH inhibitor. The invention further provides for using EETs in conjunction with one or more sEH inhibitors to reduce hypertension, and for compositions of EETs coated with a material insoluble in an acid of pH 3 but soluble in a solution with a pH of 7.4 or higher.

The invention discloses a method of producing a dalbavancin precursor A40926. In particular, during a fermentation cultivation proves, 10-methyl undecanoic acid, or several 10-methyl undecanoic undecanoate solutions, is flow-fed to a fermentation liquid to increase the yield of the dalbavancin precursor A40926. The method is simple in operation, greatly increases fermentation yield, reduces production cost and is suitable for industrial production.

According to the conception of a novel drug design, the present invention provides improved decoration based on the existing ACEI and relates to a design comprising the following two types of conception: first, the toxic side-effect points of the existing ACEI are avoided to the greatest extent; secondly, the effects of the ACEI are improved to the greatest extent. Thus the present invention provides a novel ACEI compound. Based on the basic structure of enalapril, the present invention provides a synthetic route for improving decoration. The structure of propanamine-sulfonyl is changed into cattle sulphonyl; the praline is changed into timonacic acid and derivatives thereof, so as to prepare a series of compounds, namely, N-[2-(1-ethoxycarbonyl-3-phenylalanine)-cattle-sulfonyl]-timonacic acid and derivatives thereof. The drugs are screened to prepare novel high-efficiency and low-toxicity ACEI.

The invention discloses a method for preparing a semaglutide side chain. The preparation method comprises the following steps: protecting amino of an initial raw material 2-(2-aminoethoxy) ethanol byusing R1; then carrying out nucleophilic substitution reaction with alpha halogenated ester to prolong a carbon chain; preparing an aliphatic chain with two protected ends by a one-pot method; removing a protecting group at one end of each aliphatic chain and condensing to obtain a compound 7; removing the R1 protecting group to obtain a compound 8, performing condensation reaction on the compound8 and fluorenylmethoxycarbonyl-L-glutamic acid 1-tert-butyl ester to obtain a compound 10, removing the fluorenylmethoxycarbonyl, performing amidation condensation reaction on the compound 10 and 18-(tert-butoxy)-18-oxooctadecanoic acid to obtain a compound 13, and removing the R2 protecting group to obtain a target product chain 1. Compared with solid-phase synthesis, the method disclosed by theinvention is lower in cost and wider in selection of protecting groups, and has industrial production and application prospects.