175 results about "Aklanonic acid" patented technology

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.

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.

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.

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.

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.

The invention discloses new 2-hydroxy-3-carbonyl-23, 29-dinorolean-1, 4, 12, 20 (30)-tetraene-28-acid, a preparation method thereof and an application in preparation of glucosidase inhibitor medicines. An alpha-glucosidase inhibitor with strong effects is extracted and separated from an akebia plant, and plant sources are rich. Furthermore, when fruit extraction is performed, the plant can not be damaged and can be utilized for a long time, so that economic benefits are improved, and the environment-friendly effect is further achieved. Pharmacological experiments show that the in-vitro alpha-glucosidase inhibition activity of the compound, namely 2-hydroxy-3-carbonyl-23, 29-dinorolean-1, 4, 12, 20 (30)-tetraene-28-acid is about 5 times of that of a first-line diabetes medicine, namely acarbose, so that the compound is expected to be used for developing medicines for preventing and treating type II diabetes and has good application and development potentials.

The invention discloses a compound traditional Chinese medicine extract preventing glucose metabolism disturbance, 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 and encommiol. A preparation method of the extract is as follows: extracting raw material medicines by C1-3 alcohol and/or water, combining a total extract, extracting the total extract by organic solvents with different polarities so as to obtain all effective ingredients, and finally mixing the ingredients so as to obtain a product. As for the compound traditional Chinese medicine extract, a large number of ineffective chemical ingredients in Chinese medicine are removed, so that the content of effective ingredients is increased greatly, and the influence on product processing and preparation quality caused by the ineffective ingredients is reduced; and simultaneously, the preparation process is stable, the product quality is controllable, the mass production is facilitated, and the drug effect of the compound traditional Chinese medicine is improved.

The invention discloses a cephalosporin C acylase mutant with a high thermal stability constructed by point mutation, which has an amino acid sequence selected from SEQ ID Nos: 3-7. Compared with initial cephalosporin C acylase with SEQ ID No: 1, the cephalosporin C acylase mutant disclosed by the invention has high thermal stability and higher enzyme activity, so that the cephalosporin C acylasemutant can be used for producing 7-aminocephalosporanic acid by adopting an one-step enzymatic method.

The invention discloses a Parkinson's disease specific serum endogenous small molecule marker and application thereof. The marker contains 2-amino-3-(4-hydroxyl-3-methoxyphenyl) propionic acid, ferulic acid and citraconic acid, altrose, pentadecanoic acid, o-phosphoserine, 4, 6 beta-hydroxymorphine, L-thyroxine, 5[epsilon], 9[epsilon], 16[epsilon]-17-hydroxy peraluminum-19-acid, 8-(1,2,dyhydroxy-3-methylbutyl-3-ene-1-yl)-7-methoxy-2H-chromine-2-2-ketone,10-hydroxydecanoic acid, perfluoro caprylic acid, and Corchorifatty acid F. The Parkinson's disease specific serum endogenous small molecule marker provided by the invention has the characteristics of high accuracy and high sensitivity. The prediction offline prediction area AUC of some markers reaches 0.95 or above, the accuracy and sensitivity of the markers are high, and the markers can be directly used for Parkinson's disease indexes.

The invention discloses a preparation method of descarbamoyl cefuroxime, which comprises the following steps: performing condensation reaction on 3-deacetyl-7-aminocephalosporanic acid used as a parent nucleus for synthesis of the descarbamoyl cefuroxime and a 2-methoxyimino-2-furanammoniumacetate acyl chloride solution, standing, crystallizing with ethanol/hydrochloric acid, washing, performing vacuum filtration, and drying to obtain the product descarbamoyl cefuroxime. The method uses 3-deacetyl-7-aminocephalosporanic acid as the raw material, uses ethanol for crystallization, shortens the production cycle, and is safe and low in toxicity; and meanwhile, the method is mild in reaction conditions and convenient to realize industrial production.