48 results about "Phosphocholine" patented technology

The object of the present invention is to provide a novel ascorbic acid derivative with excellent stability, and its applications. [Solution] A compound (compound of general formula (1) below) is used, in which a phosphocholine group is introduced to the hydroxyl group at the 2 position of ascorbic acid via a phosphate ester bond. The ascorbic acid derivative of the present invention has excellent whitening and antioxidant properties, and is also highly stable. Therefore, the ascorbic acid derivative of the present invention can be preferably used as an active ingredient in cosmetics and topical skin preparations. TIFF2026055124000012.tif39101

The invention belongs to the technical field of organic synthesis, and relates to a preparation method of N-palmitoyl-O-phosphorylcholine serine and a deuterated substance thereof. The N-palmitoyl-O-phosphorylcholine serine and the deuterated substance thereof are obtained by taking L-serine methyl ester hydrochloride and palmitic acid as raw materials through amidation reaction, phosphate esterification reaction, quaternization reaction, oxidation reaction, reduction reaction and the like. The invention provides an approach for industrial production of the N-palmitoyl-O-phosphorylcholine serine and the deuterated substance thereof, and is very important for standardization of the detection method of the N-palmitoyl-O-phosphorylcholine serine.

The present invention relates to ophthalmic compositions comprising at least one substance of at least one nicotinic acetylcholine receptor (nAChR) modulator, in particular varenicline, megamine and derivatives thereof, and / or the endogenous Kennedy metabolic pathway, as well as salts and derivatives or pharmaceutically acceptable salts of these substances, and choline-containing phospholipids, salts and derivatives of these substances. From these groups, particularly preferred are choline, phosphocholine, CDP-choline (citicoline), phosphatidylcholine (e.g. Lecithin having a phosphatidylcholine content of > = 80% by weight, e.g. Soybean lecithin), ethanolamine, phosphoethanolamine, CDP-ethanolamine, phosphatidylethanolamine, L-alpha-glycerophosphorylcholine, phosphatidylcholine, phosphatidylethanolamine.

The invention discloses application of a marker to preparation of a kit for diagnosing chronic obstructive pulmonary diseases. According to the application disclosed by the invention, the accuracy of diagnosing the chronic obstructive pulmonary disease by using (R)-3-hydroxytetradecanoic acid alone or in combination with the azelayl platelet activating factor is relatively high; on the basis of combination of (R)-3-hydroxytetradecanoic acid and an azelayl platelet activating factor, the compound is prepared. The compound can be further combined with one or two of 1-hexadecyl-2-(5-oxovaleryl)-sn-glycerol-3-phosphorylcholine, 1-O-hexadecyl-SN-glycerol-3-choline phosphoric acid, lauroyl-L-carnitine and beta-acetyl-gamma-O-alkyl-L-alpha-phosphatidylcholine to be used for diagnosing the chronic obstructive pulmonary disease. Therefore, a diagnostic kit for diagnosing the chronic obstructive pulmonary disease can be prepared on the basis of the scheme, and the kit contains a compound standard substance corresponding to the scheme and can also contain an internal standard compound for mass spectrum quantitative analysis.

The present invention provides therapeutic and / or prophylactic treatments against leishmaniasis in non-human mammals in need of such treatment, said treatments comprising administering oleyl phosphocholine to said non-human mammal. The invention also relates to veterinary (pharmaceutical) compositions adapted, suitable and / or intended for use in these treatments.

This invention relates to the field of building materials technology, and particularly to a viscosity-reducing polycarboxylate superplasticizer and its preparation method. The viscosity-reducing polycarboxylate superplasticizer uses polyethylene glycol dicyclopentenyl ether methacrylate as the macromonomer, combined with 2-methacryloyloxyethyl phosphocholine, 4-vinylphenylboronic acid, and polyethylene glycol phenyl ether methacrylate as small monomers, prepared via free radical polymerization. Finally, it undergoes freeze-drying and grinding to obtain the target powder product. When the prepared superplasticizer is added to concrete mixtures, it swells and unfolds into a comb-shaped polymer under mechanical stirring and alkaline conditions. Through PEG long side-chain lubrication and steric hindrance, the regulation of surface tension / interfacial energy by phosphocholine groups, and the selective adsorption of borate groups, the initial viscosity is significantly reduced, the viscosity increase over time is controlled, and segregation and bleeding are effectively suppressed, making it suitable for various cementitious systems.

The present application relates to a kind of cytidine choline dextrohydrotalcid derivatives and its preparation method and application, belong to biological medicine technical field.The present application is aimed at solving the technical problems of low blood-brain barrier penetration rate and limited treatment effect of existing edaravone dextrohydrotalcid compound preparation.The present application prepares a dextrohydrotalcid derivative (C-B) with boronic acid structure, then it is compounded with cytidine choline in specific pH buffer system, and forms cytidine choline dextrohydrotalcid derivative (C-D-B).The present application can effectively improve the efficiency of drug crossing blood-brain barrier by using the dynamic covalent characteristics of boronic ester bond and free radical responsiveness.The experimental results show that, compared with existing combination drug, the derivative of the present application can significantly reduce the infarction area of cerebral ischemia model animal, reduce cell damage and active oxygen level, and promote vascular regeneration, and show better treatment effect on ischemic brain injury.

The invention belongs to the technical field of organic synthesis, and particularly relates to a polymeric organic base and application of the polymeric organic base in catalytic preparation of a phosphatidylcholine compound. The polymeric organic base disclosed by the invention is a diblock polymer formed by polymerizing a biimidazole guanidine organic tertiary phosphine chain segment and a functional phosphorylcholine chain segment; wherein the biimidazole guanidine organic tertiary phosphine chain segment has strong basicity and can efficiently catalyze the transesterification, and the functionalized phosphorylcholine chain segment is similar to L-alpha-choline alfoscerate in structure and can promote the solubility of organic base and increase the reaction activity at the initial stage of the reaction. The polymeric organic base disclosed by the invention can be used as an immobilized catalyst for preparing phosphatidylcholine compounds from fatty acid ester and L-alpha-choline alfoscerate through transesterification.

This invention relates to proliposomal powder dispersions of testosterone undecanoate (TU) and phospholipids, including dispersions of TU and palmitoylphosphatidylcholine (DPPC), wherein the weight / weight (w / w) ratio of TU:DPPC in the proliposomal powder dispersion is about 1:2; or TU and 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), wherein the weight / weight (w / w) ratio of TU:DMPC in the proliposomal powder dispersion is about 1:3; or TU and a 1-myristoyl-2-palmitoyl-sn-glycero 3-phosphocholine (MPPC), wherein the weight / weight (w / w) ratio of TU:MPPC in the proliposomal powder dispersion is about 1:3.

The object of the present invention is a liposomal composition comprising the tripeptide glycyl-L-histidyl-L-lysine-copper (GHK-Cu) complex, wherein said complex is encapsulated in lipid carrier A comprising 19 to 39 wt % of the sodium salt of 1,2-distearoyl-sn-glycero-3- phosphoglycerol (DSPG-Na), 29 to 42 wt % of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and 24 to 41 wt % of cholesterol, or in lipid carrier B comprising 16 to 21 wt % of N- [carbonyl-methoxy(polyethylene glycol)-2000]-1,2-distearoyl-sn-glycero-3- phosphoethanolamine (DSPE-PEG2000), 48 to 63 wt % of hydrogenated soybean phosphatidylcholine (HSPC) and 16 to 36 wt % of cholesterol. A further object of the invention is a method for preparing the liposomal composition of the invention and its use as a component of a cosmetic formulation.

The invention discloses a saponin liposome immunologic adjuvant and a preparation method thereof, and belongs to the technical field of vaccine adjuvants. The preparation method comprises the following steps: firstly, preparing a blank liposome from 1, 2-dioleoyl-sn-glycerol-3-phosphorylcholine, cholesterol and DSPE-PEG-NHS, and then carrying out surface modification on the liposome by introducing a polyvinyl alcohol-protein graft polymer to form a stable core-shell structure; and finally, encapsulating the QS-21 in the liposome through active drug loading, and freeze-drying to obtain a final product. Through the synergistic effect of the DSPE-PEG-NHS and the polyvinyl alcohol-protein graft polymer, the structural integrity of the liposome in the freeze-drying and storage process is remarkably enhanced, hydrolysis and rearrangement of QS-21 are effectively inhibited, and the problem of chemical instability of QS-21 is solved. The obtained saponin liposome immunologic adjuvant has the advantages of high stability and strong immunogenicity.

The application discloses a kind of phase change microcapsule-MXene-modified polyacrylate fabric coating and its preparation method and application, belong to fabric coating technical field, including the following steps: MXene dispersion liquid and phosphocholine modified polyacrylate emulsion are mixed, then octadecane polystyrene-polyaniline microcapsule dispersion liquid is added, mixed uniformly, to obtain composite coating slurry;Composite coating slurry is deposited on the surface of fabric using vacuum filtration process, and is dried to obtain phase change microcapsule-MXene-modified polyacrylate fabric coating.The fabric coating preparation method provided by the application is simple and efficient, and the coated fabric is applied in the field of intelligent wearable devices, which can simultaneously realize the multiple responses of conductivity, humidity and thermal management function, and has wide application value.

The present disclosure provides a Lipid-Phosphocholine-Carboxylic Acid Agent being a compound comprising one or more groups, wherein each group is independently selected from Lipid Moiety (LM), Phosphocholine Moiety (PCM), Carboxylic Acid Moiety, Amide Moiety, and Attachment Moiety (AM), and wherein each group is covalently attached, directly or indirectly, to a multivalent linker (i.e., Composition Linker Moiety (CLM)), or pharmaceutically acceptable salts thereof, and related conjugates. The present disclosure also relates to uses of the Lipid-Phosphocholine-Carboxylic Acid Agents and conjugates, e.g., in delivering nucleic acid and / or treating or preventing diseases.

This invention provides a method for synthesizing zwitterionic copolymers, comprising the following steps: a betaine-based zwitterionic monomer and a 2-methacryloyloxyethyl phosphocholine (MPC) monomer are subjected to a free radical copolymerization reaction in a solvent to obtain the zwitterionic copolymer; wherein the betaine-based zwitterionic monomer is selected from carboxybetaine methacrylate (CBMA) monomer or sulfobetaine methacrylate (SBMA) monomer; the free radical copolymerization reaction is selected from reversible addition-fragmentation chain transfer (RAFT) polymerization or free radical polymerization (FRP); when the free radical copolymerization reaction is RAFT polymerization, the copolymerization reaction is carried out in the presence of both an initiator and a chain transfer agent (CTA); when the free radical copolymerization reaction is FRP, the copolymerization reaction is carried out in the presence of an initiator without the addition of a chain transfer agent. This invention can be widely applied in fields such as in vitro diagnostic sealing agents, and is a new generation of fully synthetic biomaterial solutions to replace animal-derived sealing agents and traditional PEG coatings.

The present disclosure provides a Lipid-Phosphocholine-Carboxylic Acid Agent being a compound comprising one or more groups, wherein each group is independently selected from Lipid Moiety (LM), Phosphocholine Moiety (PCM), Carboxylic Acid Moiety, Amide Moiety, and Attachment Moiety (AM), and wherein each group is covalently attached, directly or indirectly, to a multivalent linker (i.e., Composition Linker Moiety (CLM)), or pharmaceutically acceptable salts thereof, and related conjugates. The present disclosure also relates to uses of the Lipid-Phosphocholine-Carboxylic Acid Agents and conjugates, e.g., in delivering nucleic acid and / or treating or preventing diseases.

This invention belongs to the field of petroleum extraction technology, specifically relating to a polyhydroxysulfonic acid type allyl multi-component polymer and its preparation method. The multi-component polymer is obtained by polymerization of the following monomers: allyl-β-cyclodextrin (self-made), 2-methacryloyloxyethyl phosphocholine (CAS: 67881-98-5, commercially available), and [3-(methacryloylamino)propyl]dimethyl(3-thiopropyl)ammonium hydroxide (CAS: 5205-95-8, commercially available). The structural formula of the allyl-β-cyclodextrin is as follows: [Insert structural formula here], and the molecular structural formula of the multi-component polymer is as follows: [Insert molecular structural formula here], where: x = 1000-5000; y = 2000-40000; z = 400-20000. The multi-component polymer of this invention has the advantages of high apparent viscosity, wide pH range tolerance, good salt and hardness resistance, and good oil displacement effect.

This invention, entitled "A Pharmaceutical Composition, Formulation, Preparation Method, and Application for Alleviating Cerebral Ischemia-Reperfusion Injury," belongs to the field of pharmaceutical technology. The technical problem to be solved is to improve the efficacy of drugs in preventing and / or treating cerebral ischemia-reperfusion injury. The key technical solution is a pharmaceutical composition for alleviating cerebral ischemia-reperfusion injury, comprising sinapic acid and a second therapeutic agent, wherein the second therapeutic agent comprises at least one of edaravone, citicoline, and tetramethylpyrazine.

This disclosure provides polypeptides that specifically bind to phosphocholine (PC). Also provided are pharmaceutical compositions comprising these polypeptides, nucleic acids encoding these polypeptides, expression vectors and host cells for producing these polypeptides, and methods for treating a target using these polypeptides.

The application belongs to the technical field of bioengineering and particularly relates to a phosphocholine cytidylyltransferase mutant and application thereof. On the basis of phosphocholine cytidylyltransferase MsCCT001, any one or several of N194D, K91E, G98S, S148A and C156V are mutated, and a series of phosphocholine cytidylyltransferase mutants are screened. The catalytic efficiency of the obtained mutant in catalyzing the reaction of generating cytidine diphosphate choline from phosphocholine and cytidine triphosphate is 1.90-2.41 times that of the initial phosphocholine cytidylyltransferase, and the mutant provides a biological enzyme preparation with stronger catalytic capacity for preparing cytidine diphosphate choline by biological conversion.

The invention discloses a phosphorylcholine cytidyltransferase mining method based on a deep learning model. According to the method, the limitation of traditional homologous comparison is broken through, and the CCT candidate enzyme which is high in catalytic activity, excellent in solubility and suitable for engineering application can be recognized in hundreds of millions of protein sequence spaces with higher screening efficiency and prediction precision. On the basis, a rational design and a zero sample mutation prediction strategy are combined to further obtain a CCT mutant with remarkably improved performance, so that a core catalytic element is provided for efficient biosynthesis of citicoline.

The present specification discloses a composition comprising 17-AAG and staurosporin for use in the treatment of melanoma, non-small cell lung cancer, pancreatic cancer, mastadenoma or glioma, and a stable polymer-lipid nanoparticle for drug binding and delivery, the nanoparticle consisting of a core and a core envelope, the core contains a poly (lactic acid-glycolic acid) copolymer (PLGA) and polyvinyl alcohol (PVA), and the core coating film contains a mixture of the following lipids: 1, 2-dipalmitoyl-sn-glycerol-3-phosphorylcholine (DDPC), cholesterol and 1, 2-distearoyl-sn-glycerol-3-phosphoethanolamine-N-[amino (polyethylene glycol)-2000] ammonium salt (DSPE-PEG (2000) NH2).

The present invention provides: a compound with which it is possible to easily introduce a phosphocholine group into a hydroxyl group of a compound serving as a substrate, without using phosphorus oxychloride or trimethylamine; and a method for producing said compound.　This compound is a phosphocholine compound containing a nitrogen-containing heterocyclic ring and is represented by general formula (1). [Chemical formula 1] (In the formula, A is selected from the structural formulae.) [Chemical formula 2] (In the structural formulae, Ra and Rb each independently represent a C1-C22 alkyl group, an alkenyl group, or an alkynyl group, R1, R2, R3, R4, R5, R6, R7, R8, and R9 each independently represent a C1-C12 alkyl group, and symbol * indicates a bond.)

The invention discloses a UV photoresponse fluorinated phosphorylcholine hybrid and a preparation method and application thereof, and belongs to the technical field of nuclear magnetic resonance imaging, and the structure of the UV photoresponse fluorinated phosphorylcholine hybrid is shown in the specification. According to the UV photoresponse fluorinated phosphorylcholine hybrid as well as the preparation method and the application thereof, a strategy of firstly polymerizing and then grafting is adopted, and fluorinated phosphorylcholine zwitterions are integrated into a dual-mode imaging system containing < 19 > F atoms and Gd < 3 + > as hydrophilic units; the contradiction between the high < 19 > F loading capacity and signal attenuation caused by hydrophobic aggregation is effectively solved through the super-hydrophilic characteristic of the zwitter-ion structure. Meanwhile, in combination with activatable 19F / 1H MRI dual-mode imaging, an excellent 19F and 1H MRI dual-mode imaging effect is shown, and an important reference is provided for design of a water-soluble fluorine-containing polymer based PRE mediated and activated 19F / 1H MRI dual-mode imaging probe.

The invention belongs to the field of pharmaceutical preparations, and provides an auxiliary material system for pulmonary administration of insoluble drugs and a preparation method of the auxiliary material system. According to the invention, a collaborative design of lipid-coated indissolvable drug nanocrystal core-shell particles and a ternary lipid dispersion intermediate is adopted, and an anti-solvent precipitation in-situ coating and high-pressure microjet refining technology is adopted; the preparation method comprises the following steps: coating the outer surface of a nintedanib nanocrystal with a lipid shell layer composed of dipalmitoyl-sn-glycerol-3-phosphorylcholine, cholesterol and propylene glycol caprylate to form core-shell particles with the mass median particle size D50 value of 150-250 nm and the volume distribution D90 value of less than or equal to 400 nm. According to the invention, high drug loading capacity, low viscosity and atomizable property are realized, lung deposition distribution and long-term particle size stability are optimized, the contradiction between high solid content and rheological property, low irritation and colloid stability, and atomization efficiency and core-shell structure integrity in lung administration of insoluble drugs is effectively relieved, and the preparation method has wide clinical application value.

The present application belongs to the field of microbial technology, and particularly relates to a phospholipid from extracellular vesicles of plant lactobacillus and application thereof. Specifically, the extracellular vesicles of plant lactobacillus can restore skin barrier; can reduce the expression of proinflammatory factors in a cell inflammation model, and has good anti-inflammatory effect. Through metabolomic analysis, it is found that effective substances effective for skin barrier damage include phospholipid 1-palmitoyl-sn-glycero-3-phosphocholine (PC, 16:0 / 0:0); experiments prove that PC (16:0 / 0:0) can regulate the expression of skin barrier related genes in a SDS induced damage cell model; and can regulate the expression of skin inflammation related genes in the SDS induced damage cell model, which indicates that PC (16:0 / 0:0) can be used as a drug for treating skin barrier damage.

The present disclosure relates, in general, to compositions comprising phosphatidylcholine and phosphatidylcholine derivatives, e.g., DLPC (1, 2-dilauroyl-sn-glycero-3-phosphocholine) or DPPC, for the treatment of fibrosis, including liver fibrosis and associated conditions such as fatty liver disease, non-alcoholic steatohepatitis (NASH) and cirrhosis, or lung fibrosis and conditions associated with lung fibrosis.

The object of the present invention is to provide a novel kojic acid derivative with excellent solubility in water, and its applications. [Solution] A compound (compound of general formula (1) below) is used in which a phosphocholine group is introduced to the hydroxymethyl group at the 2-position of the γ-pyrone ring of kojic acid via a phosphate ester bond. The kojic acid derivative of the present invention has high solubility in water and can be incorporated into cosmetics and topical skin preparations at high concentrations. Furthermore, the kojic acid derivative of the present invention can be converted to kojic acid in the body, thereby exhibiting the excellent physiological activity of kojic acid, such as melanin production inhibition. TIFF2026055125000008.tif39110

The application discloses a pet diet agent based on hyperbranched polylysine-starch compound and a preparation method thereof, and the pet diet agent is composed of hyperbranched polylysine (HBPL) and starch. The hyperbranched polylysine (HBPL) and the starch generate the hyperbranched polylysine-starch compound through electrostatic interaction. The pet diet agent can effectively decompose emulsion containing cholate and phosphocholine, further inhibit lipase activity, reduce the absorption of fat in the small intestine, and achieve the effect of inhibiting pet obesity, and the polylysine-starch compound can significantly change the intestinal flora structure and improve the immunity of pets.

A nucleic acid vaccine composition comprising one or more of a plasmid-based nucleic acid vaccine and immunotherapy, as well as a lipid formulation, is provided. In addition, the present invention provides a method of enhancing the potency of plasmid-based DNA vaccines and immunotherapies, by formulating a vaccine and / or immunotherapy in a lipid formulation, which is stable when refrigerated or stored frozen, is then delivered to a vaccinee by either needle / syringe, jet injection, or microneedles. The lipid formulation of the present invention comprises one or more lipid excipients selected from 1,2-Distearoyl-sn-glycero-3-phosphocholine, Cholest-5-en-3β-ol, 1,2-Dimyristoyl-rac-glycero-3-methylpolyoxyethlene, and or more symmetric ionizable cationic lipids. The present invention increases vaccine potency dramatically. It was unexpectedly discovered that the level of immunogen, or immune response molecules, produced in vivo is increased (versus administering merely the vaccine or immunotherapy) and, in the case of a vaccine immunogen, the immune response is enhanced.