377 results about "Structural analog" patented technology

A compound of a general structure:wherein:B is selected from the group consisting of derivatives of naturally occurring nitrogenous bases having a C-H group at positions 5 or 8, and derivatives of nitrogenous base-analogs having a C-H group at positions 5 or 8;D is at least one derivatizing group, including hydrogen; andM is a maleimide derivative.

An agent for treating various kinds of diseases which contains at least one selected from the group consisting of sexual steroid hormone such as estrogen or its metabolites, its derivative, structural analogues thereof, estrogen acting substance or SERM non-feminizing estrogen (non-hormonal estrogen), and an activator of sirtuin and has a form of eye drops or eye washes, oral preparation, etc. An agent for treating eye diseases which has excellent treatment effects, reduced in side action can be provided.

The present invention relates to the fermentation process of producing L-arginine. By using Corynebacterium crenatum SYA5 screened and preserved by the present lab as parent and through conventional physical and chemical mutation process and multiple structural analog resistance screening, mutant strain SDNN403 is obtained. Through culturing of the mutant strain under optimized condition, L-arginine is produced in the yield level of 30-35 g/L. The strain has high genetic stability, stable yield characteristic, high L-arginine yield level, less produced hetero acids and easy technological amplification, and is suitable four industrial production.

The present invention relates to the use of creatine compound and neuroprotective combinations including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds in combination with neuroprotective agents can be used as therapeutically effective compositions against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases. The creatine compounds which can be used in the present method include (1) creatine, creatine phosphate and analogs of these compounds which can act as substrates or substrate analogs for creatine kinase; (2) bisubstrate inhibitors of creatine kinase comprising covalently linked structural analogs of adenosine triphosphate (ATP) and creatine; (3) creatine analogs which can act as reversible or irreversible inhibitors of creatine kinase; and (4) N-phosphorocreatine analogs bearing non-transferable moieties which mimic the N-phosphoryl group.

The invention belongs to the technical field of sample pretreatment in analytical chemistry and relates to a preparation method and use of a molecular imprinting-absorbing extraction stirring rod. The preparation process of the method comprises the following steps: sintering one end of a capillary glass tube serving as a substrate of the stirring rod, and subjecting to the sintered capillary glass tube to acid and alkali treatment and surface modification by a silylating agent respectively; performing the self-assembly of template molecules and bifunctional monomers in a polymer solvent, adding a crosslinker and an initiator in the solution, plugging the modified capillary glass tube into the solution; drawing the capillary glass tube out; repeatedly coating the capillary glass tube to a required thickness, and aging the coating; cutting a proper length of coated capillary glass tube, putting the length of coated capillary glass tube in a magnetic core, and sintering the capillary glass tube for end sealing; and eluting the template molecules. The molecular imprinting-absorbing extraction stirring rod prepared by the invention can selectively separate and enrich a trace amount of template molecules and analogues at the same time and is suitable for selectively separating, enriching and analyzing a trace amount of template molecules and analogues in complex samples in terms of organism, food and environment.

The invention relates to use of certain compounds including, for example, certain charged amino acids and structural analogs thereof, for reducing the viscosity of aqueous protein-containing formulations. Associated compositions of matter and methods of use are also contemplated within the present invention.

The invention belongs to the field of modern isolation analysis materials science and engineering, it relates to preparation method and application of microwave assistant molecular print magnetic microsphere, the procedure as follows: adopting microwave chemical reactor, taking nanometer magnetic fluid as magnetic nuclei, by cleaning and external modification, ultrasound detracting to water; mounted pattern molecule and functional monomer self-assembly; adding polymeric liquor by step, cross link agent and initiator, making it mixes and separates with magnetic fluid fully by stirring of machine, microwave procedure controlled temperature and heats up, until raising polymerization; Magnetic separates the foregoing magnetic microsphere, removing mounted pattern molecule, vacuum drying, aging. The molecular print magnetic microsphere has not only recognize ability of mounted pattern molecule and its analogue, but also has the approved characteristic of 'gathering hyphen recycle', the process of preparation heats up with microwave, decreasing the time of print aggregation, improving homogeneity and print efficiency of polymer form. The molecular print magnetic sphere applies to gather, isolate and analysis of structure analogue in the environmental sample, eatable etc complex samples.

The invention relates to a strain capable of producing L-arginine and a method for producing the L-arginine by the strain and belongs to the technical field of biological engineering. For the strain, Brevibacterium flavum ATCC 14067 is used as a starting strain; nitrosoguanidine is adopted to carry out mutagenesis step by step; mutant strains with histidine and succinic acid auxotrophic strains are screened out so as to cut off a competitive metabolic pathway; and mutant strains (His-, Suc-, D-Argr, SMCr) with resistances of arginine structural analogs and cysteine structural analogs are screened out. The strain is named as Brevibacterium flavum HX1009, is preserved in the China general microbiological culture collection center, has the preservation number of CGMCC No.4464 and has the genetic characters of histidine auxotroph His-, succinic acid auxotroph Suc-, D-arginine resistance D-Argr and S-methyl cysteine resistance SMCr for improving the yield of the L-arginine. Under the optimized condition, the L-arginine is produced by fermentation on a fermentation tank with the volume of 5L to 5M3 and the arginine production level achieves 50 to 70g/L.

The present invention relates to the use of creatine compound and neuroprotective combinations including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds in combination with neuroprotective agents can be used as therapeutically effective compositions against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases. The creatine compounds which can be used in the present method include (1) creatine, creatine phosphate and analogs of these compounds which can act as substrates or substrate analogs for creatine kinase; (2) bisubstrate inhibitors of creatine kinase comprising covalently linked structural analogs of adenosine triphosphate (ATP) and creatine; (3) creatine analogs which can act as reversible or irreversible inhibitors of creatine kinase; and (4) N-phosphorocreatine analogs bearing non-transferable moieties which mimic the N-phosphoryl group.

The invention belongs to the technical field of enzyme engineering, and concretely relates to a pyrimidine nucleoside high-yielding strain and a carbamyl phosphate synthetase adjusting site thereof. The invention provides a pyrimidine nucleoside production Bacillus subtilis mutant strain and a carbamyl phosphate synthetase encoding gene. A key regulation site related to carbamyl phosphate synthetase end product feedback inhibition is defined, and provides reference for breeding of later pyrimidine nucleoside high-yielding strains. The Bacillus subtilis mutant strain allows the output of fermentation process produced nucleoside pyrimidine uridine to reach 14-16g/L, and has substantially improved tolerance to different pyrimidine nucleoside structure analogs.

The invention discloses a process for preparing high-purity low-molecular heparin sodium and belongs to the field of bioengineering. The process mainly comprises the following steps of: salting-out and impurity removal, supplementary material warming and oxidization, gel elution, ion exchange, ethanol precipitation, vacuum drying and the like. The problems that the existing heparin sodium structure analog is hard to remove, the purity can not achieve the requirements for medicinal use, the preparation process is complicated, and the like are solved. The process has the beneficial effects that by adopting a supplementary material warming and oxidization method, the preparation and the decolorization of the low-molecular heparin sodium are realized, and the heparin sodium structure analogue is effectively removed by using weakly-basic anion exchange resin; and the process has the advantages of shortened production period, saved cost, simple process, easiness in operation and is suitable for industrial production.

Stat3 inhibitor compounds are disclosed, wherein the compounds are structural analogs of Ac-pTyr-Leu-Pro-Gln-Thr-NH₂ and bind to the SH2 domain of Stat3 under physiological conditions to inhibit a cellular signaling activity of Stat3.

The invention relates to a method for preparing hydrophilic molecular imprinting microsphere by using ionic liquid as a novel functional monomer by a suspension method. The method is characterized bycomprising the following steps: (1) synthesizing iminazole type ionic liquid with double-bond carboxylic acid by using alkyl imidazole and brominated trialkyl crylic acid; (2) adding a dispersing agent into water and stirring the water until the dispersing agent is fully dissolved; (3) carrying out self-assembly on template molecules and functional monomers; (4) mixing trimethylolpropane trimethacrylate, an initiating agent and a diluent; (5) mixing the three solutions, leading N2 to an obtained mixed solution and then sealing the mixed solution; (6) washing a polymer obtained by the reactionby an organic solvent; and (7) airing the polymer at normal temperature to obtain the hydrophilic molecular imprinting microsphere. The invention has the advantages that the synthesized molecular imprinting polymer has the characteristics of controllable size, strong rigidity, good hydrophilicity and high selectivity and is quite suitable for the enrichment, the separation and the analysis of analogs in foods, biological samples and aquatic environment samples.

The invention discloses an engineering bacterium through anthracene nucleus antibiotic and appliance, which is characterized by the following: inserting or replacing restriction enzymes site of dnmV gene nucleic acid order of sky blue rufus streptomycete with antibiotic against property gene and surface cerubidin synthetic gene; blocking-up engineering bacterium of dnmV gene; or transforming expressing carrier of anthracene nucleus antibiotic synthetic gene to lead streptomycin (S.lividans)TK24; extracting expressing plasmid from S.lividans TK24; leading-in sky blue rufus streptomycete gene only with antibiotic against property gene to block dnmV gene; blocking-up abrupt change bacterium. This invention can produce cerubidin and/or analogue, such as anthracene nucleus antibiotic.

The invention discloses a new nitrilase and gene thereof, a recombinant expression vector and a recombinant expression transformant containing the gene, a method for preparing the recombinant nitrilase or microbial cell containing the recombinant nitrilase by use of the recombinant expression transformant, and application of the microbial cell in dehydrating ortho-chlorine mandelonitrile or other analogues and producing chiral ortho-chlorine mandelonitrile or other analogues. The recombinant nitrilase disclosed by the invention comes from Labrenzia aggregate and can be used as a catalyst for dehydrating and splitting ortho-chlorine mandelonitrile or other analogues; and the recombinant nitrilase has the advantages of high catalysis efficiency, strong enantioselectivity, mild reaction conditions, environmental friendliness and the like.

Formulations and methods for preventing, inhibiting or controlling metabolic disorder, age-related disease and acute inflammations have been developed. The compositions comprise of bilirubins, bilirubin derivatives, their tetrapyrrolic analogues, tripyrroles, and dipyrroles. The compositions can be administered as a dosage form for oral ingestion, injection, suppository, or topical application. The effective amount of the compound is typically from 0.001-100 mg/kg body weight, preferably in the range from 0.01-50 mg/kg body weight, and most preferably from 0.05-10 mg/kg body weight. Examples demonstrate the efficacy of the compounds in both in vitro and in vivo tests.

The invention relates to an artemisinin molecule imprinting polymer on the surface of porous microsphere silica gel. The artemisinin molecule imprinting polymer is prepared by adopting the steps of: selecting the porous microsphere silica gel as a basal material, taking vinyl triethoxysilane as a coupling agent, artemisinin as a template molecule, methacrylate and acrylamide as functional monomers, ethylene glycol dimethacrylate as a cross-linking agent and azodiisobutyronitrile as an initiating agent, preparing a polymer and removing the artemisinin in the polymer. The invention also provides a preparation method and an application method of the artemisinin molecule imprinting polymer on the surface of the porous microsphere silica gel. The artemisinin molecule imprinting polymer on the surface of the porous microsphere silica gel can separate the artemisinin from other structural analogues, such as artemether, and the like under normal pressure and temperature and supercritical conditions, is especially suitable for supercritical conditions and has specific adsorption property, selectivity and favorable mechanical stability; and the preparation method is simple, convenient and suitable for large-scale popularization and application.

The present invention relates to novel therapeutic uses of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof. Furthermore, the present invention relates to the use of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof, in obtaining methods of screening and of developing drugs. Finally, the present invention relates to the novel therapeutic use of other glutamine synthetase (GS) ligands and to the use of these ligands in obtaining methods for screening and developing drugs.

A process for the preparation of taxanes comprising

wherein R is a tert. butoxycarbonyl or benzoyl group; PMP is p-methoxyphenyl group; G₁ is acetyl group; G₂ is haloacetyl group comprising

• • a) protecting the C-7 hydroxyl group of 10-deacetylbaccatin III with haloacetyl chlorides and then acetylating the C-10 hydroxyl group with acetyl chloride to obtain a protected 10-deacetylbaccatin III (1);
  • b) subjecting the protected 10-deacetylbaccatin III (1) to coupling with an oxazolidine-5-caboxylic acid of formula 2

wherein R is tert. butoxycarbonyl or benzoyl; PMP is p-methoxyphenyl group in the presence of a condensation agent and an activating agent to obtain C-13 esters of formula 3;

c) treating the coupled products 3 with weak acidic medium to open the oxazolidine ring to obtain intermediates of formula 4;

wherein R is a tert. butoxycarbonyl or benzoyl group; G₁ is acetyl group; G₂ is haloacetyl group

d) subjecting the intermediates of compound 4 to selective deprotection of haloacyl group in the presence of acetyl group under mild alkaline condition at −20 to +40° C. for 6-24 h in the presence of ammonia or aliphatic amine or aromatic amines or their combination to obtain paclitaxel or docetaxel.

The invention discloses a preparation method of cajanin and substances with a similar structure. According to the invention, acyl acetate and diketene are subject to a condensation reaction, such that an intermediate compound II is obtained; the intermediate compound II is subject to an alkylation reaction and a halogenation reaction, such that an intermediate compound IV is obtained; the intermediate compound IV is subject to a condensation reaction with an organic phosphine reagent, and is subject to a witting reaction, such that a compound VI is obtained; the compound VI is subject to a dehydrocarbylation and pentanol iosprene conversion reaction, and the reactant is hydrolyzed or alcoholyzed, such that cajanin I and substances with the similar structure are obtained. According to the invention, cajanin and substances with the similar structure are prepared through a chemical synthetic method. The technical process adopted by the synthetic route is easy to operate, the yield is good, and the product purity is high. The method provided by the invention assists in providing a basis for further researches, developments and applications of various pharmacologic actions of cajanin.

The invention relates to a silica gel particle surface artemisinin molecularly imprinted polymer which is obtained by taking artemisinin as template molecules, adopting functional silica gel particles which are as shown in the formula (1) and the silica gel particles (CABS) with the surface modified by calix (4) arene, monomeric compounds as shown in the formula (2) and the monomeric compounds as shown in the formula (3) for carrying out random copolymerization, obtaining the polymer, and then removing the artemisinin in the polymer. The invention further provides a preparation method and an application method of the silica gel particle surface artemisinin molecularly imprinted polymer, the silica gel particle surface artemisinin molecularly imprinted polymer can separate the artemisinin from structural analogues of artemether and the like under the conditions of normal temperature and normal pressure and the supercritical conditions, thereby being particularly applicable to the supercritical conditions and having specific absorption, selectivity and good mechanical stability; and the preparation method is simple and convenient, and applicable to large-scale popularization.

The invention discloses a screening method of grape wine yeast with low-yield ethyl carbamate and application of grape wine yeast in the production of grape wine. The screening method comprises the following steps of: screening out a bacterial strain with the low-yield ethyl carbamate from active dried yeast and mutant strains by adopting a structural analogue of arginine, i.e., canavanine resistance flat plate, wherein the activity dried yeast can be separated from nature or can be purchased in market, and the mutant strains are obtained through the mutagenesis of chemical mutagen. The method is designed by a yeast amino acid metabolism theory and is simple and convenient; and a target bacterial strain can be obtained through rapid separation. According to the screening method, the obtained resistance bacterial strain B1 can be numbered as F15-1-15 bacterial strain (CGMCC (China General Microbiological Culture Collection Center) NO. 4727) and is applied to the brewing of the grape wine in a small-sized fermented container; and on the basis of excellent brewing performance of the grape wine, the bacterial strain has the advantages of being capable of effectively and obviously reducing the content of the ethyl carbamate in the production of the grape wine and having the potential of industrial production and application.

The invention discloses a magnetic molecular imprinting bionic ELISA (enzyme-linked immuno sorbent assay) detecting method. The magnetic molecular imprinting bionic ELISA detecting method includes steps of preparing magnetic molecular imprinted polymer and setting up a direct-competition ELISA method. By the detecting method, uniform-particle MG-MMIPs (malachite green-magnetic molecular imprinted polymers) are prepared by an emulsion polymerization method, adsorption performance is investigated, the MG-MMIPs is used as bionic antibody, and the directly-competitive ELISA detecting method is established by means of competitive adsorption to MG antigen and enzyme labeling MG antigen. Under the optimum reaction conditions, the standard curve sensitivity is 20.14 ugL-1, and the minimum detection limit is 0.12 ugL-1 and is lower than detection limit of 2 ppb (ng/g) of a MG rapid-detection card. Meanwhile, the method has high selectivity for MG, and cross reaction rates for two structural analogues (methyl violet and brilliant green) of the MG are 7.4% and 3.9% respectively.

The invention relates to the technical field of separation medium preparation, in particular to a preparation method and application of an ochratoxin metal organic skeleton-molecular imprinting compounded separation medium. The ochratoxin metal organic skeleton-molecular imprinting compounded separation medium is taken as a filing material for a solid phase extraction column for being applied in selective enrichment and separation of the ochratoxin in complex matrix. A imprinted polymer takes a structural analogue of the ochratoxin as an alternative template, and a metal organic skeleton is combined with the imprinted polymer to prepare the ochratoxin metal organic skeleton-molecular imprinting compounded separation medium. The separation medium prepared by the invention has the porosity characteristic of the metal organic skeleton and the molecular recognition ability of the molecular imprinting polymer to a target molecule, can selectively enrich and isolate the ochratoxin, is applied to the sample pretreatment of the complex matrix to achieve better purification, enrichment effect, and has broad application prospects.

The invention belongs to the technical field of biological medicines, and particularly relates to application of gallic acid as well as derivatives and structural analogues thereof in preparation of anti-coronavirus drugs. Researches show that gallic acid as well as derivatives and structural analogues thereof have an obvious antivirus effect on coronaviridae viruses including 2019 novel coronaviruses (2019-nCoV or SARS-CoV-2), Middle East respiratory syndrome coronaviruses (MERS-CoV) and the like. Gallic acid substances are natural, widely exist in various plants, are polyphenol compounds existing in the nature, are widely applied to the fields of food, biology and medicine, and are very safe, so that the substances have very good application value in the aspect of preparation and development of antiviral drugs for coronaviridae.

The invention relates to the field of medicinal chemistry, in particular to a garcinia derivative (I), a preparation method thereof and the application of the derivative in pharmacy. The derivative is a structural analogue of a garcinia natural product such as gambogic acid and has the molecular weight which is lower than that of the gambogic acid, and hetero atoms and hydrophilic groups are introduced or further salified, so that the absorbability of a gastrointestinal tract is improved; and the derivative has an antitumor effect and can be used for preparing antitumor medicaments.