101results about "Isotope introduction to sugar derivatives" patented technology

The present application relates to microfluidic devices and related technologies, and to chemical processes using such devices. More specifically, the application discloses a fully automated synthesis of radioactive compounds for imaging, such as by positron emission tomography (PET), in a fast, efficient and compact manner. In particular, this application describe an automated, stand-alone, microfluidic instrument for the multi-step chemical synthesis of radiopharmaceuticals, such as probes for PET and a method of using such instruments.

A process and a device for synthesizing labeled compounds. The process involves preparing a labeling agent, labeling a precursor with the labeling agent, where the precursor is a protected substrate, and deprotecting the labeled precursor to convert the labeled precursor to a labeled compound by passing the labeled precursor through a solid support in a column or a cartridge. The process may be used to convert labeled tetraacetylfluoroglucose (TAFg) to labeled fluoro-deoxy-glucose (FDG) for use in nuclear medical imaging. The process is more rapid than conventional methods and is performed at room temperature rather than high temperature for conventional technology.

The invention provides a method and apparatus for preparation of radiochemicals wherein the reaction that couples the radioactive isotope to the reactive precursor to form a positron-emitting molecular imaging probe is performed in a microfluidic environment. The method comprises: providing a micro reactor; introducing a liquid reactive precursor dissolved in a polar aprotic solvent into an inlet port of the micro reactor, the reactive precursor adapted for reaction with a radioactive isotope to form a radiochemical; introducing a solution comprising a radioactive isotope dissolved in a polar aprotic solvent into another inlet port of the micro reactor; contacting the reactive precursor with the isotope-containing solution in a microchannel of the micro reactor; reacting the reactive precursor with the isotope-containing solution as the reactive precursor and isotope-containing solution flow through the microchannel of the micro reactor, wherein the reacting step is conducted at a temperature above the boiling point of the polar aprotic solvent at 1 atm and at a pressure sufficient to maintain the polar aprotic solvent in liquid form; and collecting the resulting radiochemical from the micro reactor.

A nucleoside monomer that is protected by a thionocarbamate protecting group and contains one or more 2H, 13C, or 15N isotopes in the ribose and / or base part is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.

The invention relates to an application of nucleoside analogs in virus resistance. Specifically, the invention relates to the use of nucleoside analogs and pharmaceutical compositions thereof as (a) inhibitors for inhibiting the replication of coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and / or porcine epidemic diarrhea virus (PEDV); and / or (b) medicines for treating and / or preventing and relieving related diseases caused by infection of coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and / or porcine epidemic diarrhea virus (PEDV). The nucleoside analogue disclosed by the invention can be used for treating and / or preventing and relieving related diseases such as respiratory tract infection, pneumonia (COVID-19) and the like caused by 2019 novel coronavirus infection.

Deuterated dipeptide boric acids or esters thereof, or crystal forms thereof, or pharmaceutically acceptable hydrates or solvates thereof are disclosed. The general structure of the compounds is shown as a formula (a) in the specification, wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, deuterium or halogens, or C1-C4 alkyl one or a plurality of or all hydrogen atoms of which are deuterated; and at least one of the R1, the R2, the R3, the R4, the R5 and the R6 is deuterated or deuterium. The compounds can effectively inhibit proteasomes and effectively treat or prevent cancer, cardiovascular disease, inflammation, immune disease, nephropathy, vasculogenesis or prostate disease.

The invention discloses a deuterated compound synthesis method, which comprises: carrying out a mixing reaction on a halogenated compound represented by a formula (I), a sulfide represented by a formula (II), a promoter, an alkali and a deuteration solvent to obtain a reduced deuterated product represented by a formula (III), wherein the reaction equation of the reaction is defined in the specification, R<1>, R<2>, R<3> and R<4> respectively are at least one selected from alkyl, aryl, acyl, hydrogen atom and deuterium atom, and X is at least one selected from iodine, bromine and chlorine. According to the present invention, the deuteration marking of the compound is efficiently achieved by using the common heavy water and the deuterated alcohol as the deuterium source through the simple reduction reaction, such that the use of expensive, toxic, flammable and explosive deuterium source reagents is not required compared with the prior art. The formulas I, II and III are defined in the specification.

The present disclosure provides fluorogenic azide compounds. Also provided are methods of using the subject compounds for labelling a target biomolecule that includes an alkyne. In some embodiments, the method includes contacting the biomolecule with a fluorogenic azide compound, wherein the contacting results in covalent linkage of the compound with the alkyne moiety of the target biomolecule.

The invention discloses deuterated Sofosbuvir and application thereof. Deuterated Sofosbuvir is a nucleoside phosphoramidate compound shown in the formula I or II, or stereisomer, salt, hydrate, solvate or crystal of the nucleoside phosphoramidate compound. The compound and the composition are used for treating flaviviridae viruses, and particularly used for treating infection of hepatitis c virus (HCV); and the deuterated Sofosbuvir has good HCV resistance.

A deuterated nucleoside analog of the formulaand the pharmaceutically acceptable salts thereof are provided by this disclosure. The disclosure also includes pharmaceutical compositions comprising a compound or salt of the formula and a carrier. Compounds and salts of this formula are useful for treating viral infections, including HCV infections. A method for treating a host afflicted with hepatitis C or other disorders is also presented that includes administering an effective treatment amount of a nucleoside or nucleotide that has deuterium with at least 50% enrichment at the 5′-position of the nucleoside or nucleotide.

Deuterated nucleoside analogs of Formula (I) and the pharmaceutically acceptable salts thereof are provided by this disclosureThe variables, e.g., B1, Y, R1, R2, R3, R3′, R4, R5, R6, R7, R8, and R9 carry definitions set forth in the disclosure. Compounds of Formula (I) are deuterated at one or more positions and the deuterium enrichment at each deuterated positions is at least 50%. Compounds and salts of Formula (I) are useful for treating viral infections, including HCV infections.

The invention generally relates to the preparation of 18F-labeled radiopharmaceuticals. In particular, this invention relates to the advanced processes for an efficient eiution of [18F]fluoride trapped in a cartridge filled with quaternary ammonium polymer which comprises inert non-basic and non-nucleophilic counter anions. The said methods and polymer cartridges allow the rapid preparation of suitable [18F]fluoride solution, which is also less basic to reduce the formation of byproducts, finally to increase radiochemical yield and purity of 18F-radiopharmaceuticals.

The invention discloses a boron-containing compound for BNCT and a preparation method and application thereof, and belongs to the field of medicines. The novel boron-containing compound is obtained through condensation, ammonolysis and cyclization reaction, and is easy to prepare, low in cost, and has good biological properties; the boron-containing compound is better than BPA on uptake, accumulation and reservation of tumour cells, free of any signs of toxicity, and has a good application prospect in BNCT. Moreover, the boron-containing compound is further expected to be a clinical potential positron emission tomography tumor imaging agent after being labeled through radioactive elements, and creates the advantage conditions for diagnosis of malignant tumor, identification of benign and malignant diseases, exploration of systematic metastatic lesions and the like.

The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and / or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

The subject invention relates to the compositions for radiolabeling Diethylenetriaminepentaacetic Acid (DTPA)-dextran with Technetium-99m and for stabilizing the DTPA-dextran Cold Kit. The composition contains Stannous Chloride ions to reduce 99mTc-pertechnetate, Ascorbic Acid to reduce stannic ions to stannous ions to maintain a reducing environment, α,α-Trehalose to add bulk and to stabilize the lyophilized composition without interfering with the radiochemical yield, and Glycine to transchelate Technetium-99m under highly acidic conditions to facilitate radiolabeling DTPA-dextran with high radiochemical purity. In addition, the invention pertains to methods for making and using the compositions. The reconstitution of the lyophilized composition by 99mTc-pertechnetate, resulting in radiolabeled 99mTc-DTPA-dextran in a composition between pH 3 to 4. This invention contains a Diluent vial, which when used will shift the pH to a moderately acidic pH, which would provide less pain on injection and ease-of-use to clinical practioners for adjusting its potency.

The present invention relates to methods of synthesizing 18F-FMAU. In particular, 18F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully automated cGMP-compliant radiosynthesis module, which results in a reduction in synthesis time and simplifies reaction conditions. The one-pot reaction conditions are also suitable for the production of 5-substitued thymidine or cytidine analogues. The products from the one-pot reaction (e.g. the labeled thymidine or cytidine analogues) can be used as probes for imaging tumor proliferative activity. More specifically, these [18F]-labeled thymidine or cytidine analogues can be used as a PET tracer for certain medical conditions, including, but not limited to, cancer disease, autoimmunity inflammation, and bone marrow transplant.

The invention relates to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a benzene ring-containing glucose derivative and an application thereof. The benzene ring-containing glucose derivative has a structure as shown in a general formula (I), and a radioactive preparation obtained by labeling the benzene ring-containing glucose derivative withradionuclide has high uptake in tumors and good tumor / non-target ratio, and is a novel tumor radiopharmaceutical with popularization and application values.

The present invention relates to a method for synthesizing a radiopharmaceutical using a cartridge, which makes it possible to carry out several steps of reaction required for synthesizing a radiopharmaceutical in the cartridge filled with a polymer. A method for synthesizing a radiopharmaceutical according to the present invention enables each step's reaction to be carried out with the solution confined in the cartridge so as not to flow out, thus being simplified compared to the conventional methods for synthesizing radiopharmaceuticals, and expediting the synthesis thereof.

The present invention is directed towards the synthesis of high purity deuterated sugars, deuterated phosphoramidites, deuterated nucleobases, deuterated nucleosides, deuterated oligonucleotides, and deuterated RNA's of defined sequences which can exhibit biochemically useful and biologically valuable properties, thus having potential for therapeutic uses.

The present disclosure relates to the novel multistep procedure for preparation of polymer monoliths for use in solvent exchange, such as methods to exchange and activate fluoride ions on a flow through microfluidic chip for subsequent chemical synthesis. Methods according to the present disclosure include the application of such microfluidic platforms for rapid F18 radiosynthesis on a flow through microfluidic chip with high efficiency, followed by a subsequent nucleophilic fluorination reaction. Various other methods of exchanging and activating fluoride ions on a flow through microfluidic chip are also disclosed. Methods incorporating features of the present invention can be applicable to any flow through microfluidic device in any field, such as radiosyntheses, chemical syntheses, concentration of ions for environmental analyses and sample preparation such as concentrating minute amounts of analyte to improve the downstream detection.

The present invention relates to method for producing fluorinated compounds using alcohol solvent having carbonyl group. The method for manufacturing an organic fluoro-compound including fluorine [18F] which uses a solvent in a nucleophilic fluorinated reaction wherein the solvent is expressed by chemical formula 1 so as to manufacture an organic fluoro-compound at high yield. The solvent has veryexcellent solubility with respect to a precursor compound to have a merit suitable for automatic combination of [18F]-labelled radiopharmaceutical.

A method of preparing fluorine-18 labeled radiopharmaceuticals (18F-radiopharmaceuticals) is disclosed. More particularly, the present invention relates to a method of preparing an 18F-radiopharmaceutical by reacting a salt containing fluorine-18 (18F) with an alkyl halide or an alkyl sulfonate in the presence of water and ethanol to obtain a high yield of the 18F-radiopharmaceutical. The synthetic method eliminates the use of toxic and / or environmentally-unfriendly organic solvents.

The invention discloses isotope-labeled bionic sugar or sugar group and a preparation method and applications thereof. Specifically, the isotope-labeled bionic sugar or sugar group disclosed by the invention include a reducing alcohol hydroxyl located at the reducing end of the sugar chain and an isotope label, wherein the molecular weight of each bionic sugar chain is increased by 3 Daltons compared with that of corresponding unmodified sugar chain, and the bionic sugar (group) has the same sugar chain composition and similar sugar chain abundance as the unmodified sugar (group). The invention also provides a method for analyzing the sugar group in a sample by using the isotope-labeled bionic sugar or the sugar group, and the method comprises the step: carrying out mass analysis on the mixture of the isotope-labeled internal standard bionic sugar chain and the sample sugar chain which is not labeled by the isotope so as to carry out qualitative and / or quantitative analysis on the sugar group in the sample. The method has the advantages of both the simple operation of a non-isotope-labeled glycomics method and the accuracy of an isotope-labeled glycomics method, can be used for high-throughput detection, and has wide application prospect.

The invention provides 18F-FDG drug synthesis equipment for a double-batch PET imaging agent. The 18F-FDG drug synthesis equipment comprises a shunt selection module and a double-batch synthesis module of F-18 nuclein; the double-batch synthesis module comprises two sets of synthesis modules respectively adopting a dual channel design; the synthesis module comprises an F-18 negative ion processing unit, an 18O-oxygen-rich water recovery unit, an automatic sampling unit, a reaction unit, a heating unit, a positive pressure transmission unit and a cold and hot air circulation unit. The 18F-FDG drug synthesis equipment provided by the invention is stable in synthetic efficiency and good in synthetic effect and can realize the double-batch hydrolysis of acid and alkali hydrolysis at the same time.

This invention relates to the miniaturisation of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).