124 results about "Phosphocholine" patented technology

Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.

The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds, which comprise an alkyl lipid or phospholipid moiety covalently conjugated with a therapeutic agent (e.g., a nucleoside analogue). The invention also includes pharmaceutical compositions for combating cancer and facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.

The present invention relates to a method, which comprises that (R)-(-)-3-chloro-1,2-propanediol and a phosphocholine tetramethyl ammonium salt are subjected to a substitution reaction, and ion exchange resin purification is performed to obtain a L-alpha-choline glycerophosphate pure product. According to the present invention, the used chiral intermediate (R)-(-)-3-chloro-1,2-propanediol is further a key chiral intermediate of an antitussive agent levodropropizine, has characteristics of stable chemical property and convenient and easy obtaining, and is especially for L-alpha-choline glycerophosphate industrial production.

Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorus-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby. Further disclosed is substantially pure 1-hexadecyl-2-(4′-carboxy)butyl-sn-glycero-3-phosphocholine (CI-201).

The present invention provides a pharmaceutical composition, comprising: (a) cationic lipids, wherein said lipids are a liposomal mixture of a diacyl-ethyl-phosphocholine and 1,2-diacyl-sn-glycero-3-phosphoethanolamine; and (b) a plasmid cDNA sequence encoding a protein having tumor suppressor or pro-apoptotic activity. This composition has a high gene transfection efficiency at non-toxic doses and is designed to transfect human bronchial premalignant lesions and early endo-bronchial malignancies. Also provided is a method of method of treating a cancerous or pre-cancerous condition of the respiratory tract in an individual in need of such treatment, comprising the step of administering to said individual a pharmacologically effective dose of a pharmaceutical composition, comprising: (a) cationic lipids, wherein said lipids are a liposomal mixture of a diacyl-ethyl-phosphocholine and 1,2-diacyl-sn-glycero-3-phosphoethanolamine; and (b) a plasmid cDNA sequence encoding a protein having tumor suppressor or pro-apoptotic activity.

The invention belongs to the technical field of materials, in particular to a method for preparing a biocompatible polymer nano-vesicle in pure water, which comprises the following specific steps that: an amphiphilic block copolymer PCL-b-PMPC (polycaprolactone-b-1-palmitoyl-2-myristoyl-sn-glycero-3-phosphocholine) is obtained by a series of reactions (caprolactone is subjected to ring-opening polymerization to obtain PCL-OH (hydroxyl-terminated polycaprolactone), the terminal group modification is conducted to obtain PCL-Br (bromine-terminated polycaprolactone) in an esterification reaction, the PCL-Br initiates MPC (2-myristoyl-sn-glycero-3-phosphocholine) atom transfer radical polymerization), and is added with hot water for few minutes to form vesicles. In the invention, the biocompatible vesicles are directly prepared in water without any organic co-solvents and pH adjustment, even without stirring. The method is simpler and more convenient than the widely used solvent exchange method. A PCL membrane has certain hydrophobicity and can be completely degraded, and PMPC has hydrophilicity and good biocompatibility.

Provided herein are compositions designed to reduce or prevent bacterial infections (for example pneuomococcal infections), nasal carriage, nasal colonization, and central nervous system invasion. Provided herein is a composition comprising a pneumococcal neuraminidase, phosphocholine, pneumococcal teichoic acid, pneumococcal lipoteichoic acid, or an antigenic portion of either neuraminidase, phosphocholine, pneumococcal teichoic acid, pneumococcal lipoteichoic acid. Optionally, the composition can comprise any combination of a pneumococcal neuraminidase, a phosphocholine, a pneumococcal teichoic acid, a pneumococcal lipoteichoic acid or an antigenic portion of any one of these. Optionally the agents are detoxified. Further provided are methods of making and using the compositions disclosed herein. Specifically provided are methods of generating antibodies in a subject comprising administering to the subject an agent or composition taught herein. Also provided are methods of reducing or preventing nasal carriage or pneumococcal infection in a subject comprising administering to the subject a composition taught herein.

The invention discloses a method for preparing phosphocholine chloride calcium salt tetrahydrate, which comprises the steps of (1) subjecting a choline chloride crude product and a phosphorylating agent to phosphorylation reaction to obtain a phosphocholine chloride mixture; (2) subjecting the phosphocholine chloride mixture and a calcium-source aqueous solution to replacement reaction to obtain a metathetical mixture; (3) subjecting the metathetical mixture to reduced pressure distillation to separate out solids and obtain a solid-liquid mixture; (4) crystallizing, filtering and drying the solid-liquid mixture at -10 to -1 DEG C to obtain phosphocholine chloride calcium salt tetrahydrate. The phosphorylating agent is selected from phosphoric acid and/or polyphosphoric acid. The calcium-source aqueous solution is one or more selected from calcium chloride aqueous solution, calcium carbonate aqueous solution, calcium hydroxide aqueous solution and calcium bicarbonate aqueous solution. The method is mild in environment condition, high in yield and high in product purity.

The invention provides a bioengineering method for synthesis of citicoline. The method comprises the following steps: constructing an escherichia coli engineering strain containing choline phosphate cytidylyltransferase by recombination through a genetic engineering method; utilizing the engineering strain to perform large-scale high-density culture as well as separation and purification, thereby obtaining the choline phosphate cytidylyltransferase with high purity and high activity; utilizing the choline phosphate cytidylyltransferase to perform enzymatic catalysis synthesis under appropriate conditions to obtain the citicoline; and adding cation exchange resin into a system of the enzymatic catalysis synthesis of the citicoline to enable the citicoline to be constantly adsorbed on the resin in the synthesis process, thereby realizing coupling of reaction and separation of the citicoline. The bioengineering method has the advantages that the substrate utilization rate is high, the product recovery rate is high, reaction conditions are mild, the reaction time is short, the environment pollution is small, the cost is low, and the like, thus being suitable for industrial mass production.

The present invention relates to a method for treating the risk of increased C-reactive protein (CRP) levels by conducting extracorporeal perfusion of blood plasma from patients with risk for cardiovascular diseases or immune dysfunctions, such as autoimmune diseases, through a device, such as a column, which contains absorbent matrix material including lipids, peptides, polypeptides, phosphocholine (PC) or PC derivatives so as to remove C-reactive protein. Moreover, the present invention relates to the use of compounds which have the characteristic to bind CRP at least temporarily, for removing CRP from biological fluids of a patient for prophylaxis and/or treatment of autoimmune diseases, cardiovascular diseases, such as infarction, stroke, diabetes, rheuma and renal failure.

The present invention relates to an antiviral composition comprising any one selected from the group consisting of chlorine, phosphocholine, cytidine triphosphate, CDP-choline, phosphorylcholine, and phosphatidylcholine. The antiviral composition is harmless to the human body and exhibits an excellent inhibitory effect on virus proliferation. Therefore, it can be applied to a pharmaceutical composition for preventing or treating viral diseases as well as a health functional food, a quasi-drug composition, and a feed composition for preventing or ameliorating viral diseases.

The invention discloses a preparation method of citicoline. The method comprises the following steps: the culture of a single gene engineering bacterium or the treatment material of the culture is used as enzyme source to catalyze the reaction of a substrate comprising ammonium chloride, orotic acid and phosphocholine and ensure that citicoline is generated and accumulated in the reaction solution, and citicoline is extracted from the reaction solution. The invention has the following beneficial effects: (1) the single microorganism is utilized to catalyze the reaction, reaction conditions are easy to control; (2) the cost of the substrate is lower so that the production cost of citicoline is lower; and (3) the reaction is fast and the conversion rate is higher. The method can be widely used in the preparation of citicoline.

The invention relates to the field of drug carrier design, and particularly relates to an amphipathic phospholipid molecule with reducing response and application thereof in drug sustained release. According to the amphipathic phospholipid molecule, n-alkyl thiol serving as an initial raw material is firstly activated by 2,2'-dithiodipyridine, and further reacts with mercaptopropionic acid to obtain fatty acid containing a disulfide bond on delta 3 position; carboxylic acid performs an esterification reaction with 1-hexadecanoyl-sn-glycero-3-phosphocholine to obtain an amphipathic phospholipid molecule of glycerol 2-hydroxyl ester containing disulfide bond on the delta 3 position. The phospholipid molecule can be prepared by a simple organic unit reaction, and the phospholipid vesicle prepared from the phospholipid molecule has excellent drug encapsulating and controlled-release capabilities.

The present disclosure provides compositions and methods for the biosynthetic production of choline, ethanolamine, phosphoethanolamine, and phosphocholine.