СПОСОБ ПОЛУЧЕНИЯ 13C-МОЧЕВИНЫ ИЗ 13CO2

Изобретение относится к способу получения13C-мочевины, которая может быть использована в медицине при тестировании патогенных бактерий Helicobacter pylori. Способ заключается в том, что раствор бис(триалкилсилил)амида металла в органическом растворителе подвергают обработке диоксидом13C-углерода преимущественно в стехиометрическом соотношении. Полученный13C-бис(триалкилсилил)карбодиимид подвергают гидролизу водой, возможно, в присутствии растворителя и кислоты или основания в качестве катализатора. Способ позволяет значительно упростить процесс, сделать его экологически безопасным, а также получить продукт с хорошим выходом (~72%) и высокой степенью чистоты, соответствующей требованиям, предъявляемым к препаратам мочевины, используемым в медицине.

Способ получения -(с7-с9)- анизидина (ан-4)

METHOD FOR DRYING OF APPARATUS FOR CONVERSION OF HYDROCARBONS

УСТАНОВКА ДЛЯ ПОЛУЧЕНИЯ ИЗОПРОПИЛИДЕН-L-СОРБОНИРАНОЗЫ

1. Установка для получения изопропилиден-L-сорбониранозы, содержащая реакционную камеру с патрубками ввода исходных компонентов и патрубком отвода композиционной системы, устройство для перемешивания смеси компонентов в виде импеллера, кожух реакционной камеры, смонтированный с зазором от стенки реакционной камеры для подачи в полость этого зазора хладагента, контейнеры с исходными компонентами, соединенные посредством дозаторов с полостью реакционной камеры, отличающаяся тем, что она снабжена дополнительной смесительной камерой, полость которой с помощью магистрали сообщена с реакционной камерой, установка также снабжена: камерой нейтрализации реакционной массы, камерой разделения получаемого материала и второстепенного вещества, эта камера соединена с вакуум-установкой, емкостью для очистки получаемого материала, камерой отгонки летучих компонентов, при этом патрубок отвода реакционной массы из дополнительной смесительной камеры соединен с камерой нейтрализации реакционной массы, с которой последовательно соединены: указанная камера разделения, емкость для очистки и камера отгонки летучих компонентов, при этом установка оснащена приборами анализа состава и качества отдельных компонентов, реакционной массы и получаемого материала. 2. Установка по п.1, отличающаяся тем, что в качестве приборов анализа и контроля используют хроматограф с ультрафиолетовым и электрохимическим детекторами, прибор ЯМР-спектрометр и хроматографическую камеру тонкослойной хроматографии. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 81 194 U1 (51) МПК C07H 1/00 (2006.01) C07H 15/00 (2006.01) C07B 51/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2008139562/22, 05.11.2008 (24) Дата начала отсчета срока действия патента: 05.11.2008 (45) Опубликовано: 10.03.2009 (73) Патентообладатель(и): Учреждение Российской Академии наук Институт Выскомолекулярных соединений РАН (RU) U 1 8 1 1 9 4 R U ...

Methods for forming dyed microspheres and populations of dyed microspheres

Various methods for forming dyed microspheres are provided. One method includes activating a chemical structure coupled to a dye using heat or light to form a reaction intermediate in the presence of a microsphere. The reaction intermediate covalently attaches to a polymer of the microsphere thereby coupling the dye to the polymer and forming the dyed microsphere. Additional methods are provided for forming a dyed microsphere coupled to a molecule. These methods include dyeing the microspheres as described above in addition to synthesizing the molecule on an outer surface of the dyed microspheres. A population of dyed microspheres is also provided. Each of the dyed microspheres of the population includes a dye attached to a polymer of each of the dyed microspheres by a chemical structure. A coefficient of variation in dye characteristics of the population of dyed microspheres attributable to the dye is less than about 10%.

Elastomeric block copolymers having star-shaped molecular architecture, where the star-shaped molecular architecture has at least two different arms in the star

Elastomeric block copolymers having star-shaped molecular architecture, where the star-shaped molecular architecture has at least two different arms of the star, a process for producing the elastomeric block copolymers, the use of the elastomeric block copolymers for producing moldings, or as adhesive layer in multilayer foils; as seal; as adhesion promoter or thermoplastic component in wood-plastics composites; as hot-melt adhesive component; for impact-modifying thermoplastics or elastomers, or for compatibilization, and to foils, foams, thermomoldings, injection moldings, flexible tubing, or profile extrudates composed of at least one elastomeric block copolymer.

Process for Production of Camptothecin Derivative

Disclosed is a process for production of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin from a camptothecin composition containing 18,19-dehydrocamptothecin without producing any vinyl form of the compound. The process is characterized by catalytically reducing at least one compound selected from a compound (1) and others in the process of producing a compound (5) from a composition containing the compound (1).

Cold weather compatible crosslinker solution

Disclosed herein is a well treatment fluid comprising an aqueous solution comprising greater than or equal to about 1 wt % boron, at least 5 wt % of a co-solvent, and greater than or equal to about 5 wt % sodium hydroxide, potassium hydroxide, or a combination thereof, wherein the co-solvent comprises glycerol, ethylene glycol, propylene glycol, or a combination thereof. Methods of using the well treatment fluid are also disclosed.

Method for re-wetting surface post-cross-linked, water-absorbent polymer particles

A process for producing water-absorbing polymer particles, wherein surface postcrosslinked water-absorbing polymer particles are remoisturized and classified, and wherein the time between remoisturization and classification is at least 15 minutes.

Lipophilic cationic probe for pet-imaging

The present invention provides an imaging probe which comprises a lipophilic cation, a hydrophobic moiety and a PET nucleus. The present invention also provides a precursor molecule for the production of such an imaging probe and methods for using the probe for analysing mitochondrial membrane potential in a subject.

POLYESTERS, METHODS OF MAKING POLYESTERS AND USES THEREFOR

Polyester compositions and functionalized polyester compositions are provided along with methods of making the compositions as well as methods of using the compositions, for example as a tissue engineering bioscaffold and as a drug-delivery vehicle. 3. (canceled)4. (canceled)5. (Cancelled)6. The method of claim 2 , in which one or both of B and B′ are Calkyl groups claim 2 , aliphatic alkyl groups claim 2 , saturated alkyl groups claim 2 , saturated straight-chain alkyl groups claim 2 , selected from the group consisting of: —O(O)C—(CH)—C(O)O— claim 2 , —CH═CH— claim 2 , —CH—CH— claim 2 , phenyl claim 2 , —O —CH—CH—O— claim 2 , —O—CH═CH—O— claim 2 , —O(O)C—CH═CH—C(O)O— claim 2 , —O(O)C-phenyl-C(O)O— claim 2 , —O(O)C-cyclohexy-C(O)O— claim 2 , and —CH(OH)—CH(OH)— claim 2 , —O(O)C—C(NHY)—CH—C(O)O— where Y is a protective group claim 2 , and —O(O)C—C(NHY)—CH—CH—C(O)O where Y is a protective group.7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. The method of claim 2 , in which A and A′ are epoxy groups or oxetane groups.12. (canceled)13. The method of claim 2 , comprising reacting diglycidyl sebacate with sebacic acid (HOC(O)—(CH)—C(O)OH).14. The method of claim 1 , in which the polymerization is conducted in the presence of one or more nucleophilic functional groups.15. The method of claim 1 , in which the polymerization is conducted in the presence of one or more of bis(tetrabutylammonium) sebacate claim 1 , tetrabutylammonium bromide claim 1 , tetrabutylammonium fluoride claim 1 , tetrabutylammonium iodide claim 1 , tetraphenylphosphonium chloride claim 1 , tetramethylphosphonium iodide claim 1 , sodium methoxide claim 1 , lithium acetate claim 1 , and sodium sulfide.16. The method of claim 2 , in which the compound A-B-A′ is prepared by direct esterification of glycidol with a compound XOC(O)—(CH)—C(O)OX′ in which X and X′ are independently halide.17. The method of claim 16 , in which the esterification is carried out in the presence of triethylamine at ...

NITROIMIDAZOLE DERIVATIVES

The present invention provides novel compounds useful in the treatment and diagnosis of mycobacterial infections. Compounds of the present invention have enhanced biological properties as compared to the related known compounds. The present invention also provides a precursor compound useful in the synthesis of certain compounds of the invention, and a method to obtain these compounds using said precursor compound. Methods of treatment and diagnosis in which the compounds of the invention fmd use are also provided. 2. The compound as defined in wherein Ris methyl.3. The compound as defined in wherein X is —O—.4. (canceled)5. The compound as defined in wherein said radioactive halogen is a gamma-emitting radioactive halogen selected from I claim 1 , I and Br.6. (canceled)7. The compound as defined in wherein said radioactive halogen is a positron-emitting radioactive halogen selected from F claim 1 , F claim 1 , Br claim 1 , Br and I.810.-. (canceled)1519.-. (canceled)20. A pharmaceutical composition comprising the compound as defined in together with a biocompatible carrier in a form suitable for mammalian administration.21. An in vivo imaging method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) administration of the compound as defined in ;'}(b) allowing said compound to bind to the cell wall of any mycobacteria present in said subject;(c) detecting by an in vivo imaging procedure signals emitted by said radioactive halogen;(d) generating an image representative of the location and/or amount of said signals; and,(e) determining the distribution of mycobacteria in said subject wherein said distribution is directly correlated with said signals.22. (canceled)23Mycobacterium tuberculosis.. The in vivo imaging method as defined in wherein said mycobacterium is24Mycobacterium tuberculosis.. The in vivo imaging method as defined in which is carried out repeatedly during the course of a treatment regimen for said subject claim 23 , said regimen ...

SOLID-PHASE FLUORINATION OF BENZOTHIAZOLES

The invention provides a process for the production of an F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I) 18-. (canceled)10. A radiopharmaceutical kit for the preparation of an F-labelled tracer for use in PET , which comprises:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, '(i) a vessel containing a compound of formula (I), (Ia), or (Ib) as defined in ; and'}{'sup': 18', '−, '(ii) means for eluting the vessel with a source of F;'}{'sup': 18', '−, '(iii) an ion-exchange cartridge for removal of excess F.'}11. A cartridge for a radiopharmaceutical kit for the preparation of an F-labelled tracer for use in PET which comprises:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, '(i) a vessel containing a compound of formula (I), (Ia), or (Ib) as defined in ; and'}{'sup': 18', '−, '(ii) means for eluting the vessel with a source of F.'}12. A radiopharmaceutical kit for the preparation of an F-labelled tracer for use in PET , which comprises:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, '(i) a vessel containing a compound of formula (III) as defined in ; and'}{'sup': 18', '−, '(ii) means for eluting the vessel with a source of F.'}13. A cartridge for a radiopharmaceutical kit for the preparation of an F-labelled tracer according to for use in PET which comprises:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, '(i) a vessel containing a compound of formula (III) as defined in ; and'}{'sup': '18', '(ii) means for eluting the vessel with a source of F.'}14. A method for obtaining a diagnostic PET image which comprises the step of using a radiopharmaceutical kit according to or a cartridge for a radiopharmaceutical kit according to . The present invention relates to novel solid-phase processes for the production of radiolabelled tracers, in particular for the production of F-labelled benzothiazole compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers. The invention also comprises ...

GRAFTED PHOTOINITIATORS

The invention provides a method for producing a polymeric photoinitiator, of the general formula I: Polymer-[CR2-CHR-Spacer(PI)](I) wherein m is an integer from 1-5000; n is a real number above 0 and below 5; R is as defined herein, and PI is a photoinitiator moiety. The method comprises grafting one or more photoinitiator moieties (PI), each of which comprises at least one activated alkene functional group, onto the polymer. Polymeric photoinitiators are also provided. 2. The method according to claim 1 , wherein the activated alkene functional group is selected from the group consisting of acrylate claim 1 , vinyl ether claim 1 , vinyl amine claim 1 , acrylamide and styrene functional groups.3. The method according to claim 2 , wherein the activated alkene functional group is selected from the group consisting of acrylate claim 2 , vinyl ether claim 2 , vinyl amine and styrene functional groups claim 2 , and is preferably acrylate.4. The method according to claim 1 , wherein the polymer is selected from the group consisting of polyolefines claim 1 , polyacrylates claim 1 , polyesters claim 1 , polyurethanes claim 1 , polyamides claim 1 , polyalkyloxides or various copolymers comprising blocks or repeatable units of these polymers.5. The method according to claim 4 , wherein the polymer is selected from the group consisting of polyolefines claim 4 , polyacrylates claim 4 , polyesters claim 4 , polyurethanes claim 4 , polyamides claim 4 , and polyalkyloxides.6. The method according to claim 5 , wherein the polymer is a polyolefin or polyalkyloxide.7. The method according to claim 1 , wherein the polymer has a molecular weight in the range of 50-500 claim 1 ,000 Da.8. The method according to claim 1 , wherein the spacer is selected from the group consisting of a single bond claim 1 , C1-C25 linear alkylene claim 1 , C3-C25 branched alkylene claim 1 , C3-C25 cycloalkylene claim 1 , arylene claim 1 , heteroarylene claim 1 , amines claim 1 , amides claim 1 , alcohols ...

Functionalization of polyolefins with phenoxy derivatives

Provided herein are telechelic polymers and methods for producing the same. In some embodiments, provided herein are compounds having the formula and methods for producing the same.

Device for the synthesis of radio-labeled compounds

The invention relates to a device for the synthesis of radio-labeled compounds, which comprises a reaction vessel for reacting a precursor compound having protective groups with a radioactive isotope to obtain a first reaction product; a first cartridge for hydrolyzing the protective groups of the first reaction product to obtain a second reaction product; and a second cartridge for purifying the second reaction product, wherein the reaction vessel, the first cartridge, and the second cartridge are connected to each other via pipelines. Here it is provided that the first cartridge contains 801 to 1200 mg of a solid carrier and/or the reaction vessel is a reaction vessel made of a temperature-resistant plastic with the plastic having a temperature resistance of at least 120° C.

Method of preparing ethacrynic amide derivatives and application thereof

The present invention provides a method for preparing [ 18 F]—N-(4-fluorobutyl)ethacrynic amide which is prepared from radiofluorination and deprotection of the precursor tosylate N-Boc-N-[4-(toluenesulfonyloxy)-butyl)ethacrynic amide], obtained from ethacrynic acid via 6-step synthesis in 39% yield, in a radiochemical yield of 44%, aspecific activity of 48 GBq/μmol and radiochemical purity of 98%. The present invention further provides a composition for positron emission tomography (PET) of an animal models of a tumor liver or a liver disease, comprising [ 18 F]—N-(4-fluorobutyl)ethacrynic amide and a pharmaceutically acceptable carrier.

FUNCTIONAL MATERIALS HAVING A CONTROLLABLE VISCOSITY OR REVERSIBLE CROSSLINKING VIA AZA DIELS-ALDER REACTIONS WITH BISHYDRAZONES OR CONJUGATED BIS-SCHIFF BASES

The present invention relates to innovative materials which are reversibly crosslinkable by means of a thermoreversible mechanism and/or whose viscosity is reversibly adjustable. Through the use of bishydrazones or conjugated bis-Schiff bases as diene components in aza-Diels-Alder reactions, functional materials are generated that feature controllable viscosity and/or reversible crosslinking. 1. A formulation , comprising:a component A which comprises at least two dienophilic double bonds, anda component B which comprises at least two diene functionalities, with at least one of the diene functionalities comprising two carbon-nitrogen double bonds,whereinthe formulation is crosslinkable via an aza-Diels-Alder reaction, and couplable or crosslinkable at room temperature, anda coupling or crosslinking in the formulation is reversible to an extent of at least 50% at a higher temperature.2. The formulation according to claim 1 , wherein all the diene functionalities comprise two carbon-nitrogen double bonds.3. The formulation according to claim 1 , wherein at least one of the components A and B comprises more than two functionalities.4. The formulation according to claim 1 , wherein at least one of the components A and B is a polymer.5. The formulation according to claim 1 , wherein the diene functionality is a bishydrazone.6. The formulation according to claim 1 , wherein the diene functionality is a bis-Schiff base.7. The formulation according to claim 1 , wherein each of the components A and B is independently a polymer.8. The formulation according to claim 4 , wherein the polymer is a polyacrylate; a polymethacrylate; polystyrene; a copolymer of acrylates claim 4 , methacrylates or styrene; polyacrylonitrile; a polyether; a polyester; a polylactic acid; a polyamide; a polyesteramide; a polyurethane; polycarbonate; an amorphous or a partially crystalline poly-α-olefin; EPDM; EPM; a hydrogenated or an unhydrogenated polybutadiene; ABS; SBR; a polysiloxane; or a block ...

PROCESS FOR THE MODIFICATION OF POLYMERS, IN PARTICULAR POLYMER NANOPARTICLES

A process for the preparation of modified polymers by a photo-initiated polymerization includes preparing a polymerization medium comprising at least one photoinitiator comprising at least one phosphorous oxide (P═O) group or at least one phosphorous sulfide (P═S) group, and at least one polymerizable monomer. The at least one polymerizable monomer is polymerized by irradiating the polymerization medium with electromagnetic radiation so as to induce a generation of radicals so as to obtain a polymer. The polymer is modified by irradiating the polymer with electromagnetic radiation so as to induce a generation of radicals from the polymer in a presence of at least one modifying agent. 132-. (canceled)33. A process for the preparation of modified polymers by a photo-initiated polymerization , the method comprising: at least one photoinitiator comprising at least one phosphorous oxide (P═O) group or at least one phosphorous sulfide (P═S) group, and', 'at least one polymerizable monomer;, 'A) preparing a polymerization medium comprisingB) polymerizing the at least one polymerizable monomer by irradiating the polymerization medium with electromagnetic radiation so as to induce a generation of radicals so as to obtain a polymer; andC) modifying the polymer obtained in B) by irradiating the polymer with electromagnetic radiation so as to induce a generation of radicals from the polymer in a presence of at least one modifying agent.34. The process as recited in claim 33 , wherein step B) is carried out as a bulk polymerization claim 33 , a solution polymerization or as a heterophase polymerization in a heterophase medium.35. The process as recited in claim 34 , wherein the process further comprises forming modified lattices or modified polymer nanoparticles by a photo-initiated heterophase polymerization claim 34 , the process further comprising: at least one surfactant,', 'at least one photoinitiator, and', 'at least one polymerizable monomer;, 'A) preparing a heterophase ...

Hydrophilic vinylidene fluoride polymers

The present invention pertains to a process for the manufacture of a grafted fluorinated polymer comprising at least one grafted side chain comprising one or more glycosidic recurring units [polymer (F)], said process comprising polymerizing: 2. The process of claim 1 , wherein the polysaccharide derivative comprises as recurring units glycosidic units selected from the group consisting of D-glucopyranosides linked to each other by glycosidic bonds.4. The process of claim 1 , wherein the polysaccharide derivatives has a dynamic viscosity comprised between 2 and 10 mPa×s claim 1 , as measured according to ASTM D445 at 20° C. in an aqueous solution at a concentration of 2% by weight.5. The process of claim 1 , wherein one or more suspension stabilizers are used.6. A fluorinated polymer [polymer (F)] comprising:a main chain comprising recurring units derived from vinylidene fluoride (VDF), optionally, said recurring units derived from one or more other fluorinated monomers [monomers (F)] and, optionally, said recurring units derived from one or more (meth)acrylic monomers [monomers (MA)], andat least one side chain grafted to said main chain, said grafted side chain comprising one or more glycosidic recurring units.7. The polymer of claim 6 , comprising at least 40 ppm of hydrogen atoms of one or more glycosidic recurring units in at least one grafted side chain of polymer (F) with respect to the total amount of hydrogen atoms of VDF recurring units in the main chain of polymer (F).8. The polymer of claim 6 , wherein at least one side chain comprises one or more β-D-glucopyranosides of formula (III-b) as described in linked to each other by β-glycosidic bonds.9. A composition comprising the polymer of and at least one VDF polymer.10. A hydrophilic membrane comprising the polymer of or the composition of . This application claims priority to European application No. 10196420.3 filed on 22 Dec. 2010, the whole content of this application being incorporated herein by ...

Purificiation of precursor compound by crystallisation

The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [ 18 F]-1-amino-3-fluorocyclobutanecarboxylic acid ([ 18 F] FACBC) PET tracer.

PROCESS SIMPLIFICATION FOR PRECURSOR COMPOUND

The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [F]-1-amino-3-fluorocyclobutanecarboxylic acid ([F] FACBC) PET tracer. 2) The method as defined in wherein X is a group represented by the group —O—SO—R.3) The method as defined in wherein Ris selected from the group consisting of toluenesulfonic acid claim 2 , nitrobenzenesulfonic acid claim 2 , benzenesulfonic acid claim 2 , trifluoromethanesulfonic acid claim 2 , fluorosulfonic acid claim 2 , perfluoroalkylsulfonic acid claim 2 , trimethylstannyl and triethylstannyl.4) The method as defined in wherein Ris trifluoromethanesulfonic acid.5) The method as defined in wherein X is halogen.6) The method as defined in wherein said halogen is bromo or chloro.7) The method as defined in wherein Ris ethyl.8) The method as defined in wherein Ris selected from the group consisting of a t-butoxycarbonyl group claim 1 , an allyloxycarbonyl group claim 1 , a phthalimide group and N-benzylideneamine substituent.9) (canceled)11) (canceled)12) (canceled)13) The method as defined in wherein said deprotection comprises removal of Rfollowed by removal of R.14) (canceled)15) The method as defined in wherein Ris ethyl.16) The method as defined in wherein Ris a t-butoxycarbonyl group.18) The method as defined in wherein said deprotection step comprises removal of Et by basis hydrolysis and removal of Boc by acidic hydrolysis.19) The method as defined in wherein steps (c) and (d) are carried out on an automated synthesiser. The present invention relates to a method to obtain radiopharmaceutical precursors, and in particular to protected amino acid derivatives which are used as precursors for ...

POLYMER PRECURSORS OF RADIOLABELED COMPOUNDS, AND METHODS OF MAKING AND USING THE SAME

One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds. 115-. (canceled)16. A method for preparing a radiolabeled compound , the method comprising: reacting a polymer precursor compound with an oxidant , a radiolabeled compound and optionally a buffer , wherein the compound is selected from the group consisting of:Poly-(4S, 5S)-2-(5-{dibutyl[2-(4-vinylphenyl)ethyl]stannyl}-2,3-dihydrobenzofuran-7-yl)-3, 4-dimethyl-5-phenyl-1, 3-oxazolidine-co-divinylbenzene;Poly-5-{dibutyl[2-(4-vinylphenyl)ethyl]stannyl}-2, 3-dihydrobenzofuran-7-carbaldehyde-co-divinylbenzene;Poly-5-{dibutyl[2-(4-vinylphenyl)ethyl]stannyl}-2, 3-dihydrobenzofuran-7-carboxylic acid-co-divinylbenzene;Poly-(4S, 5S)-2-(4-{dibutyl[2-(3-vinylphenyl)ethyl]stannyl}phenyl)-3, 4-dimethyl-5-pheynyl-1, 3-oxazolidine-co-divinylbenzene; andPoly-(4S, 5S)-2-(4-{dibutyl[2-(4-vinylphenyl)ethyl]stannyl}phenyl)-3, 4-dimethyl-5-phenyl-1, 3-oxazolidine-co-divinylbenzene.17. A method of claim 16 , further comprising a purification of the radiolabeled compound.18. A kit containing a radiolabeling system claim 16 , comprising: a polymer precursor compound and instructions for using said polymer precursor compound claim 16 , wherein said polymer precursor compound comprises the polymer precursor compound of .19. The kit of that further includes a filter or a filtration device.20. The kit of that further includes a chelating agent and optionally an auxiliary molecule.21. A method of synthesizing radiolabeled benzamides on a solid support comprising:a) selecting a solid support comprising at least one compound attached to said solid support which compound comprises a benzoic acid moiety;b) reacting said moiety of said compound attached to said solid support with at least one amine to afford a benzamide bound to a solid support; andc) reacting said ...

Hydrogenation of diene-based polymers

This invention relates to a process for the hydrogenation of diene-based copolymers in the presence of catalysts on specific carrier materials containing at least one hyper-branched polymer.

In-Situ Methods of Generating Water Through the Dehydration of Metal Salt Hydrates for Moisture Crosslinking of Polyolefins

Compositions comprising a polymer resin comprising at least one copolymer with hydrolysable groups, a water-generating metal salt hydrate, and a catalyst that comprises a metal atom and at least two ligands taken from the set alkyloxy and carboxylate are used to form articles that moisture-cure through in-situ generation of water via dehydration of the metal hydrate. The compositions are melt mixed to promote the dehydration and start the cure process during the mixing step. The curing compositions are formed and allowed to harden. 1. A process for forming a moisture-cured article , the process comprising:{'sub': x', 'y', '2', 'z, 'blending a copolymer of ethylene and a vinyltrialkoxysilane in which the alkoxy group is RO and R is an alkyl group of 1 to 8 carbon atoms, a hydrated salt of the general formula MQ(HO), wherein M is a cation of a metal selected from groups 1 through 13 of the periodic table, Q is an organic anion, x and y are integers taken to balance the overall charge of the salt, and z is the hydration number of the salt on a molar basis at 25° C., the hydrated salt having an onset temperature of dehydration of greater than 100° C. and less than 200° C.; and a catalyst that comprises a metal ion and at least two ligands taken from the set alkoxide and carboxylate to form a composition, wherein the blending is done at a temperature above the melting point of the resin;'}generating water in-situ in the composition during the blending step to form a molten curing composition;forming the molten curing composition into an article; and,allowing the molten curing composition to harden.2. The process of wherein the cure is done at a temperature below about 250° C.3. The process of further comprising curing the article by exposure to external moisture after the molten curing composition has hardened.4. The process of wherein the article is formed by molding claim 1 , extrusion claim 1 , rolling or rotary molding.5. The process of wherein the hydrated salt is ...

Method of preparing radioisotope nanostructure with ligand-metal framework and application

This invention relates to a method of preparing a radioisotope nanostructure having a ligand-metal framework, and a radioisotope nanostructure prepared thereby. The method of preparing the radioisotope nanostructure of the invention has a simple preparation process and can thus be applied to mass production of a radioisotope nanostructure. Also, because this radioisotope nanostructure is nano-sized spherical particles and has no reactive group, it can be easily dispersed in a fluid, and this nanostructure is physically and chemically stable and thus can be utilized as a radioisotope tracer in the fields of refineries, chemistry, cement, agriculture, water resources, marine, etc. Furthermore, this nanostructure can be used for diagnosis and/or treatment in medical fields, and can be applied to checking whether a nanomaterial is harmful. In addition, this nanostructure is expected to be applicable in a variety of fields using radioisotopes.

Measuring Tube Lining

A measuring tube for a lining of a measuring tube of a flow measuring device, wherein a nanoparticle is chemically bound to a polymer. 115-. (canceled)16. A measuring tube lining of a synthetic material or plastic produced with a method for manufacturing a synthetic material or plastic for a lining of a measuring tube of a flow measuring device , wherein:nanoparticles are bound chemically to monomers, oligomers or polymers as components of the synthetic material or plastic; andmonomers having predetermined end groups are combined with nanoparticles having predetermined end groups to form polymers.17. The measuring tube lining as claimed in claim 16 , wherein:said nanoparticles are chemically bound to said monomers, oligomers or polymers by one of: radical reactions, condensation-, addition- and metathesis reactions.18. The measuring tube lining as claimed in claim 16 , wherein:said nanoparticles each have one or more end groups, which are suitable for forming a chemical bond with said monomer, said oligomer or said polymer.19. The measuring tube lining as claimed in claim 16 , wherein:said polymers comprise PUR, PFA or PTFE.20. The measuring tube lining as claimed in claim 16 , wherein:said nanoparticles comprise end group modified, pyrogenic, silicic acids.21. The measuring tube lining as claimed in claim 16 , wherein:said nanoparticles are added in a predetermined concentration to the starting substances, so that said nanoparticles are present in the synthetic material or plastic in a concentration of 0.1 to 5 wt.-%.22. The measuring tube lining as claimed in claim 16 , wherein:a liquid multicomponent system is formed, which contains monomers or prepolymers, an alcohol, a catalyst and said nanoparticles;said monomers or said prepolymers react with said nanoparticles to form a chemically stable bond; andsaid multicomponent system hardens.23. The measuring tube lining as claimed in claim 16 , wherein:a liquid multicomponent system is formed of an isocyanate, an ...

Ligands for imaging cardiac innervation

Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

METHOD FOR RAPID PREPARATION OF SUITABLEFLUORIDE FOR NUCLEOPHILICFLUORINATION

The invention generally relates to the preparation of F-labeled radiopharmaceuticals. In particular, this invention relates to the advanced processes for an efficient eiution of [F]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 [F]fluoride solution, which is also less basic to reduce the formation of byproducts, finally to increase radiochemical yield and purity of F-radiopharmaceuticals. 2. quaternary ammonium polymer according to claim 1 , wherein NRis selected from the group consisting of trimethylamine claim 1 , triethylamine claim 1 , tri-n-propylamine claim 1 , tri-n-butylamine claim 1 , N-methylimidazole claim 1 , and pyridine.3. A quaternary ammonium polymer according to claim 1 , wherein the X is selected from the group consisting of methanesulfonate (OMs) claim 1 , trifluoromethanesulfonate (OTf) claim 1 , para-toluenesulfonate (OTs) claim 1 , para-nitrobenzenesulfonate (ONs) claim 1 , tetrafluoroborate (BF) claim 1 , hexafluorophosphate (PF) claim 1 , hexafluoroantimonate (SbF) claim 1 , and N claim 1 ,N-bis(trifluoromethanesulfonyl)amide (N(Tf)).6. A polymer cartridge 6 containing neutral ammonium polystyrene of for solid-phase anion extraction.7. A method for separation of [F]fluoride from aqueous solution claim 6 , wherein [F]fluoride dissolved in aqueous solution is passed through the polymer cartridge of .8. A method for the preparation of an eluting solution for eluting [18F] from a cartridge according to claim 6 , wherein the eluting solution is prepared by composing three ingredients (Ingredient A claim 6 , Ingredient B claim 6 , and Ingredient C) claim 6 , and dissolving in an alcohol solvent.9. A method according to claim 8 , wherein Ingredient A is K222 that is used as a phase transfer catalyst of [F]fluorination in a range from 10 to 20 mg.10. A method according to claim 8 ...

SURFACE MODIFICATION METHOD AND SURFACE-MODIFIED ELASTIC BODY

The present invention aims to provide a surface modification method for a rubber vulcanizate or a thermoplastic elastomer, which can impart excellent sliding properties and excellent durability against repeated sliding motion and can allow the surface to maintain the sealing properties, without using expensive self-lubricating plastics. The present invention relates to a surface modification method for modifying a rubber vulcanizate or a thermoplastic elastomer as an object to be modified, the method including: step 1 of forming polymerization initiation points on the object to be modified; step 2 of radically polymerizing a monomer, starting from the polymerization initiation points, by irradiation with LED light at 300 nm to 400 nm to grow polymer chains on a surface of the object to be modified; and step 3 of esterifying, transesterifying or amidating side chains of the polymer chains. 1. A surface modification method for modifying a rubber vulcanizate or a thermoplastic elastomer as an object to be modified , the method comprising:step 1 of forming polymerization initiation points on the object to be modified;{'b': 300', '400, 'step 2 of radically polymerizing a monomer, starting from the polymerization initiation points, by irradiation with LED light at nm to nm to grow polymer chains on a surface of the object to be modified; and'}step 3 of esterifying, transesterifying or amidating side chains of the polymer chains.2. The surface modification method according to claim 1 ,wherein the step 1 comprises allowing a polymerization initiator to be adsorbed on the object to be modified.3. The surface modification method according to claim 1 ,wherein the step 1 comprises allowing a polymerization initiator to be adsorbed on the object to be modified, and then fixing the polymerization initiator on a surface of the object by use of LED light at 300 nm to 400 nm.4. The surface modification method according to claim 1 ,wherein the rubber vulcanizate or thermoplastic ...

LIGNIN-DERIVED THERMOPLASTIC CO-POLYMERS AND METHODS OF PREPARATION

The present invention relates to a crosslinked lignin comprising a lignin structure having methylene or ethylene linking groups therein crosslinking between phenyl ring carbon atoms, wherein said crosslinked lignin is crosslinked to an extent that it has a number-average molecular weight of at least 10,000 g/mol, is melt-processible, and has either a glass transition temperature of at least 100° C., or is substantially soluble in a polar organic solvent or aqueous alkaline solution. Thermoplastic copolymers containing the crosslinked lignin are also described. Methods for producing the crosslinked lignin and thermoplastic copolymers are also described. 1. A thermoplastic copolymer , wherein said thermoplastic copolymer has a two-phase morphology and is comprised of crosslinked lignin copolymerized with non-lignin thermoplastic polymer segments , wherein said crosslinked lignin is comprised of a lignin structure having methylene or ethylene linking groups therein crosslinking between phenyl ring carbon atoms , and said crosslinked lignin is crosslinked to an extent that it has a number-average molecular weight of at least 10 ,000 g/mol , is melt-processible , and has a glass transition temperature of at least 100° C. , or is substantially soluble in a polar organic solvent or aqueous alkaline solution.2. The thermoplastic copolymer of claim 1 , wherein said thermoplastic copolymer is a block copolymer or multiphase copolymer.3. The thermoplastic copolymer of claim 1 , wherein said thermoplastic copolymer is a graft copolymer.4. The thermoplastic copolymer of claim 1 , wherein said thermoplastic copolymer has a glass transition temperature selected from a temperature in the range of −100° C. up to 200° C.5. The thermoplastic copolymer of claim 1 , wherein said non-lignin thermoplastic polymer segments contain unsaturated carbon-carbon bonds.7. The thermoplastic copolymer of claim 6 , wherein said non-lignin thermoplastic polymer segments comprise polyisoprene units.8. ...

Method of utilizing recycled deuterium oxide in the synthesis of deuterated compounds

The present invention provides a method for utilizing recycled deuterium oxide synthesis of deuterated compounds.

Novel Amphiphilic Graft Copolymers

A novel amphiphilic graft copolymer is described. A process to make amphiphilic graft copolymers via grafting either poly(ethylene oxide) or polylactide side chains onto an EVA platform using oxo-anion ring-opening polymerization chemistry is also described. Polyethylene or polypropylene based graft copolymers are prepared starting from poly(ethylene-co-vinyl acetate) or maleic anhydride grafted isotactic polypropylene respectively. The amphiphilic character will result from the incorporation of hydrophilic poly(ethylene oxide) (PEO) side-chains. Various applications of the novel amphiphilic graft copolymer are also described including, but not limited to, thermoplastic elastomer, films, fibers, fabrics, gels, breathable packaging materials, additive for biodegradable system, surfactant, antistatic additives, polymer compatibilizers, phase transfer catalysts, solid polymer electrolytes, biocompatible polymers, or incorporation into the materials listed above. 4. The process of wherein the molar values of n is in the range from 10 to 60 mole percent.5. The process of wherein the molar values of m is in the range from 40 to 90 mole percent for m.6. The process of wherein the molar values of p is in the range from 5 to 400.7. The process of wherein the ethylene vinyl acetate copolymer has a melt index from 0.3 to 500 dg/min.8. The process of wherein the ethylene oxide ring-opening polymerization is performed at a reaction temperature in the range of −20 to 100° C.9. The process of wherein the ethylene oxide ring-opening polymerization is performed at a reaction temperature greater than 30° C.10. The process of wherein the ethylene oxide ring-opening polymerization is performed at a reaction temperature of 60° C.11. The process of wherein the ethylene oxide ring-opening polymerization is performed under alkaline conditions.12. The process of wherein the ethylene oxide ring-opening polymerization is performed using 1 claim 3 , 3 propane sultone.13. The process of wherein ...

Deuterated cftr potentiators

This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.

Methods and Materials for the Functionalization of Polymers and Coatings Including Functionalized Polymer

The disclosure provides a functionalized polymer for use in coating compositions and a method for making the functionalized polymer. In some embodiments, the functionalized polymer is a water-dispersible polymer, more preferably a water-dispersible polyester polymer, having one or more side groups including one or more salt groups. Packaging containers (e.g., food or beverage cans) comprising the functionalized polymer and methods of making such containers are also provided. 139-. (canceled)40. An article comprising a food or beverage can , or a portion thereof , the article comprising:a metal substrate; and a backbone having at least one heteroatom; and', 'a side group that includes at least one salt group, wherein the side group comprises the reaction product of an unsaturated compound having at least one salt or salt-forming group that is attached to another portion of the polymer via reaction of the unsaturated compound with one or more double or triple bonds, with the proviso that the reaction of the unsaturated compound with the one or more double or triple bonds does not require the participation of a free-radical initiator., 'a coating disposed on at least a portion of the metal substrate, the coating formed from a coating composition comprising an aqueous dispersion of a water-dispersible polymer, wherein the polymer includes41. The article of claim 40 , wherein the side group is attached directly to the backbone.42. The article of claim 40 , wherein the side group is attached to another portion of the polymer via a carbon-carbon bond.43. The article of claim 40 , wherein the side group includes at least a portion of a cyclic group that links the side group to the backbone or another portion of the water-dispersible polymer that is attached to the backbone.44. The article of claim 43 , wherein the cyclic group has at least one carbon-carbon double bond present in a ring of the cyclic group.45. The article of claim 40 , wherein the reaction of the ...

F-18 RADIOLABELED COMPOUNDS FOR DIAGNOSING AND MONITORING KIDNEY FUNCTION

The invention relates to F-labeled compounds of formula (I), hydrates, isomers, or pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions. The invention relates to the methods of diagnosing kidney function in humans by PET imaging. 2. The F-labeled compound of formula (I) as claimed in claim 1 , wherein Y claim 1 , Z claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each H.3. The F-labeled compound of formula (I) as claimed in claim 1 , wherein:{'sup': 1', '2', '3, 'Y, Z, R, R, and Rare each H; and'}{'sup': 4', '5', '4', '5, 'sub': '3', 'one of Ror Ris H and the other of Ror Ris COCH.'}5. The compound of claim 1 , wherein said compound is selected from the group consisting of:2-(4-amino-2-(18)fluorobenzamido)acetic acid;2-(4-acetamido-2-(18)fluorobenzamido)acetic acid;2-(3-amino-4-(18)fluorobenzamido)acetic acid;2-(5-amino-2-chloro-4-(18)fluorobenzamido)acetic acid;2-(5-amino-2-(18)fluorobenzamido)acetic acid;2-(4-amino-3-(18)fluorobenzamido)acetic acid;2-(4-acetamido-3-(18)fluorobenzamido)acetic acid;2-(2-amino-6-(18)fluorobenzamido)acetic acid;2-(2-acetamido-6-(18)fluorobenzamido)acetic acid;(S)-2-(4-amino-2-(18)fluorobenzamido)propanoic acid;(R)-2-(4-amino-2-(18)fluorobenzamido)propanoic acid;(S)-2-(2-amino-6-(18)fluorobenzamido)propanoic acid;(R)-2-(2-amino-6-(18)fluorobenzamido)propanoic acid.8. The process for the preparation of compound of formula (I) as claimed in claim 6 , wherein the chemical reactions are conducted at ambient temperature under thermal or microwave or ultrasonic conditions.9. The process for the preparation of compound of formula (I) as claimed in claim 7 , wherein the chemical reactions are conducted at ambient temperature under thermal or microwave or ultrasonic conditions.10. The process for the preparation of F-labeled compound of formula (I) as claimed in claim 6 , wherein said phase transfer catalyst is selected from 18-crown-6 claim 6 ,15-crown-5 claim 6 , kryptofix-222 claim 6 ...

METHOD FOR MAKING SPECIFIC PRODUCTS FROM POLYSACCHARIDE MOLECULE

A method for preparing a specific product from a polysaccharide in which at least one hydroxyl of a saccharide unit is substituted with an ether or ester moiety. The ether or ester moiety is provided with ethenyl and/or epoxy functionality for preparing an activatable polysaccharide polymer and the activatable polysaccharide polymer with ethenyl and/or epoxy functionality is optionally reacted with an additional coupling reagent, having at least two coupling functionality for preparing polysaccharide polymer with additional activatable crosslinker. Thereafter, the activatable polysaccharide polymer or the polysaccharide polymer with an additional activatable crosslinker, is activated for crosslinking the polysaccharide polymer with another polysaccharide polymer by reacting the activatable polysaccharide polymer or polysaccharide polymer with an additional activatable crosslinker with a crosslinking initiator for crosslinking the polysaccharide polymer chains with each other, for preparing a product such as hydrogel, film, coating or membrane with polysaccharide backbone. 1. A method for making specific products from polysaccharide molecule(s) containing ether or ester bonded substituents , wherein said method comprisesproviding hydroxyl groups of a polysaccharide molecule with numerous of coupling substituents, wherein said coupling substituents are substituted via ether or ester bonds, preferably via ether bonds, to said polysaccharide molecule, wherein said coupling substituents enable crosslinking two polysaccharide polymers with each other or enable coupling a polysaccharide polymer with another polymer or enable grafting of a polymer side chain from same kind or different kind of monomer(s) onto said polysaccharide molecule andmaking a selected product from said polysaccharide molecule with numerous coupling substituents by crosslinking said polysaccharide molecule with the same kind of different kind of polysaccharide molecule or forming bonds between said ...

Production of Vinyl Terminated Polyethylene Using Supported Catalyst System

This invention relates to processes to produce vinyl terminated polyethylene involving contacting ethylene with a supported metallocene catalyst system; wherein the supported catalyst system comprises a support material; an alumoxane activator; and a metallocene compound. A supported metallocene catalyst system is also disclosed. Processes to produce ethylene copolymers are also disclosed.

Chiral Separation System

A system for separation of enantiomers includes a column packed with a stationary phase; a magnetic field generator generating a magnetic field, within which the column is placed, and the magnetic field interacts with the enantiomers as the enantiomers elute through the column with a mobile phase; and a control unit, in communication with the magnetic field generator and the column, to adjust the strength and direction of the magnetic field to separate the enantiomers. 1. A system for separation of enantiomers , comprising:a column packed with a stationary phase;a magnetic field generator to generate a magnetic field, within which the column is placed, and the magnetic field interacting with the enantiomers as the enantiomers elute through the column with a mobile phase; anda control unit in communication with the magnetic field generator and the column to adjust the strength and direction of the magnetic field to separate the enantiomers.2. The system of claim 1 , wherein the magnetic field generator comprises at least one solenoid claim 1 , at least one permanent magnet claim 1 , a superconducting magnet claim 1 , or any other suitable magnetic field generator.3. The system of claim 1 , wherein the magnetic field is a static magnetic field.4. The system of claim 1 , wherein the strength of the magnetic field is adjusted to induce a magnetic dipole in each of the enantiomers and to align the induced magnetic dipole with the magnetic field.5. The system of claim 1 , wherein the direction of the magnetic field is adjusted by varying an angle or a distance claim 1 , or both thereof claim 1 , between the magnetic filed and the column.6. The system of claim 1 , wherein the stationary phase comprises a ferromagnetic material.7. The system of claim 6 , wherein the ferromagnetic material comprises FeOnanocrystals having a size of smaller than 1000 nm.8. The system of claim 1 , wherein the column is a C18 claim 1 , monolithic claim 1 , ion exchange claim 1 , hydrophilic ...

Interpolymers Containing Isobutylene And Diene Mer Units

This disclosure relates to a block interpolymer comprising at least one diene block and at least one butyl block, wherein the at least one butyl block comprises residue from a functionalizing agent on at least one end adjacent to the diene block(s). The disclosure also relates to methods of making such block interpolymers. Also disclosed is a rubber composition comprising: (a) a block interpolymer comprising at least one diene block and at least one butyl block, and (b) a filler, wherein said at least one butyl block comprises residue from a functionalizing agent on at least one end adjacent to said diene block(s).

RADIOACTIVE IODINE LABELED PYRIDO[1,2-a]BENZOIMIDAZOLE DERIVATIVE COMPOUND

The present invention relates to a radioactive iodine-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a definite general formula or a salt thereof, or a radiopharmaceutical comprising the same. 2. The radioactive iodine-labeled compound or a salt thereof according to claim 1 , wherein the radioactive iodophenyl group is a substituent having a phenyl group which hydrogen atom at position 4 is substituted with a radioactive iodine atom.3. The radioactive iodine-labeled compound or a salt thereof according to claim 1 , wherein the radioactive iodine atom is I claim 1 , I claim 1 , I claim 1 , or I.4. A radiopharmaceutical comprising a radioactive iodine-labeled compound or a salt thereof according to .5. The radiopharmaceutical according to claim 4 , which is for use in single photon emission computed tomography (SPECT).6. A diagnostic agent for Alzheimer's disease comprising a radioactive iodine-labeled compound or a salt thereof according to . The present invention relates to a radioactive iodine-labeled pyrido[1,2-a]benzimidazole derivative compound or a salt thereof, and a radiopharmaceutical comprising the same.Accumulation of senile plaque (SP) composed mainly of amyloid β protein (Aβ) and neurofibrillary tangle (NFT) composed mainly of tau protein is found in the brain with Alzheimer's disease (AD). Since the accumulation of NFT exhibits high correlation with clinical symptoms, as compared with SP, development of radioactive molecule imaging probes for nuclear medicine diagnosis targeting the tau protein has received attention recently.For example, Patent Document 1 describes radioactive iodine-labeled compounds comprising rhodanine and thiohydantoin derivatives having affinity for the tau protein.Also, Patent Documents 2 and 3 describe compounds having binding activity against both of the Aβ and the tau protein. Specifically, Patent Document 2 describes a radioactive iodine-labeled compound having styrylbenzimidazole as a nucleus, and ...

RESIN COMPOSITION FOR UNDERLAYER FILM FORMATION, IMPRINT FORMING KIT, LAMINATE, PATTERN FORMING METHOD, AND METHOD FOR PRODUCING DEVICE

Disclosed herein are a resin composition for underlayer film formation which is capable of forming an underlayer film having good adhesiveness to a base material and good surface state, an imprint forming kit, a laminate, a pattern forming method, and a method for producing a device. Provided is a resin composition for underlayer film formation, including a resin, a nucleophilic catalyst, and a solvent, in which the content of the nucleophilic catalyst is 0.01 to 0.3 mass % with respect to the solid content of the resin composition for underlayer film formation. 1. A resin composition for underlayer film formation , comprising:a resin;a nucleophilic catalyst; anda solvent,wherein the content of the nucleophilic catalyst is 0.01 to 3 mass % with respect to the solid content of the resin composition for underlayer film formation.2. The resin composition for underlayer film formation according to claim 1 , wherein the nucleophilic catalyst is at least one selected from an ammonium salt claim 1 , a phosphine-based compound claim 1 , a phosphonium salt claim 1 , and a heterocyclic compound.3. The resin composition for underlayer film formation according to claim 1 , wherein the resin includes a resin having a radical reactive group.6. The resin composition for underlayer film formation according to claim 1 , wherein the content of water is 0.01 to 3 mass % with respect to the resin composition for underlayer film formation.7. The resin composition for underlayer film formation according to claim 1 , wherein the content of the solvent is 95 to 99.9 mass % with respect to the resin composition for underlayer film formation.8. The resin composition for underlayer film formation according to claim 1 , which is used for the formation of an underlayer film for photoimprints.9. An imprint forming kit comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the resin composition for underlayer film formation according to ; and'}a photocurable composition.10. A laminate ...

RESIN COMPOSITION FOR MASTERBATCH

A masterbatch of a liquid additive is provided, the resin composition for the masterbatch comprising (a) a block copolymer or a hydrogenated product thereof, the block copolymer containing a polymer block having a vinyl aromatic compound as a main component and a polymer block having a conjugated diene compound as a main component, and 40 to 100 parts by mass of a polyolefinic resin and 100 to 150 parts by mass of an ethylene.α-olefin copolymer with respect to 100 parts by mass of the (a) component, wherein the kinematic viscosity at 100° C. is 10 to 5,000 mm/s; the ethylene molar content is in the range of 30 to 85 mol %; and the molecular weight distribution (Mw/Mn) for the molecular weight measured by gel permeation chromatography (GPC) with reference to polystyrene is not more than 2.5. 1. A resin composition for a masterbatch , comprising: (a) a block copolymer or a hydrogenated product thereof , the block copolymer containing a polymer block having a structural unit derived from a vinyl aromatic compound as a main component and a polymer block having a structural unit derived from a conjugated diene compound as a main component; and 40 to 100 parts by mass of (b) a polyolefinic resin; and 100 to 150 parts by mass of (c) an ethylene.α-olefin copolymer having characteristics (c1) to (c3) described below , with respect to 100 parts by mass of the (a) component ,{'sup': '2', '(c1) a kinematic viscosity at 100° C. is 10 to 5,000 mm/s;'}(c2) a content of a structural unit derived from ethylene is in the range of 30 to 85 mol %; and(c3) a molecular weight distribution (Mw/Mn) for the molecular weight measured by gel permeation chromatography (GPC) with reference to polystyrene is not more than 2.5.2. The resin composition for a masterbatch according to claim 1 , wherein the (a) component is a hydrogenated product of the block copolymer.3. The resin composition for a masterbatch according to claim 1 , wherein the kinematic viscosity of the (c) ethylene.α-olefin ...

HETEROCYCLIC COMPOUNDS AS IMAGING PROBES OF TAU PATHOLOGY

Pyridazinone compounds of Formula I: (I) wherein: R′ is alkyl or Ar, optionally substituted with at least one alkyl, halogen, hydroxyl, alkoxy, haloalkoxy, acid, ester, amino, nitro, amide, or alkoxyhalo; 2 R is independently alkyi, alkynyl, ester, amino, amide, acid, aryl, heteroaryl, aminoalkyl, —C(=0)alkyl, —C(=0)aryl, —C(=0)heteroaryl, —C(=0)heterocycloalkyl, —C(=0)heterocycloalkylAr, —C(=0)(CH)halo, —C(═O)(CH)nheterocyclyl, or —SĈAr, optionally substituted with at least one alkyi, alkylhalo, halogen, nitro, aryl, heteroaryl, or heteroaryl(CH)nhalo; Rand Rare independently hydrogen, alkyi, alkenyl, alkynyl, aryl, heteroaryl; Ar is an aryl, heteroaryl, cycloalkyl, heterocycloalkyl group; n is an integer from 0-10; or a radiolabeled derivative thereof. The compounds are useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described. 3. (canceled)10. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. A composition comprising a compound according to and a pharmaceutically acceptable carrier or excipient.18. (canceled)19. A method of imaging using a compound according to or a pharmaceutical composition thereof.20. A method of detecting tau aggregates in vitro and/or in vivo using a compound according to or a pharmaceutical composition thereof.21. (canceled)22. (canceled)23. (canceled) The present invention relates to radiolabeled pyridazinone compounds, compositions thereof, methods of making such compounds and their use as imaging probes of Tau pathology especially as it relates to Alzheimer's Disease. Compounds of the present invention may be used for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging.Alzheimer's disease (AD) is the most common cause of dementia in the elderly. It is definitively diagnosed and staged on the basis of post-mortem neuropathology. The pathological hallmark of AD is a ...

HEATSEAL

The present invention relates to systems and methods to facilitate replacement between runs of a kit or cassette from an automated radiosynthesis device located in a hot cell. The method and apparatus of the invention enable automated disconnection of the outlet line by sealing the tubing hermetically by means of heat and by cutting the tubing where it is sealed in such a way that there is no risk of environmental contamination with radioactive material. The invention enables disconnection of the outlet line without manual intervention before opening the shielded enclosure. 1. A method comprising:(i) providing a kit that can be fitted to an automated radiosynthesis device in order to synthesise a positron emission tomography (PET) tracer and one or more sections of thermoplastic tubing;(ii) fitting said kit and said one or more sections of thermoplastic tubing to the automated radiosynthesis device;(iii) introducing a PET isotope into said kit to carry out a radiochemical process to form a radiolabelled product;(iv) transferring said radiolabelled product from said kit to a product collection device and/or a product processing device; and,(v) heat sealing and cutting said one or more sections of thermoplastic tubing.2. The method as defined in wherein said product collection device is a product collection vial.3. The method as defined in wherein said product processing device is a chromatography device claim 2 , a dispensing device or a quality control device.4. The method as defined in wherein each of said radiosynthesis device claim 3 , product collection device and product processing device is contained within a shielded enclosure.5. The method as defined in wherein said shielded enclosure is a hot cell.6. The method as defined in wherein said automated radiosynthesis device is contained within a first shielded enclosure and said product collection device and/or said product processing device are contained within a second shielded enclosure.7. The method as ...

IN VIVO IMAGING OF MATRIX METALLOPROTEINASES IN LUNG DISEASE

The present invention provides a method of imaging a subject's lung which comprises contacting the subject's lung with a matrix metalloproteinase inhibitor labeled with a radioisotope under conditions such that the inhibitor binds to matrix metalloproteinase in the lung, and then imaging the radiolabeled inhibitor bound to matrix metalloproteinase in the subject's lung. 1. A method of imaging a subject's lung which comprises contacting the subject's lung with a matrix metalloproteinase inhibitor labeled with a radioisotope under conditions such that the inhibitor binds to matrix metalloproteinase in the lung , and then imaging the radiolabeled inhibitor bound to matrix metalloproteinase in the subject's lung so as to image the subject's lung.2. The method of claim 1 , wherein the matrix metalloproteinase inhibitor is Ro 32-3555 or a modified form of CGS27023A.3. The method of claim 2 , wherein the radioisotope is I-123.4. The method of claim 3 , wherein the matrix metalloproteinase inhibitor is Ro 32-3555.5. The method of claim 3 , wherein the matrix metalloproteinase inhibitor is a modified form of CGS27023A.8. The method of claim 1 , wherein the subject is claim 1 , or is suspected of being claim 1 , afflicted with a destructive lung disease.9. (canceled)10. The method of claim 8 , wherein the destructive lung disease is chronic obstructive pulmonary disease (COPD) claim 8 , lymphangioleiomyomatosis (LAM) claim 8 , idiopathic pulmonary fibrosis (IPF) claim 8 , or acute lung injury (ALI).11. The method of claim 8 , wherein the destructive lung disease is emphysema.12. The method of claim 1 , wherein the imaging is single-photon emission computed tomography (SPECT) imaging.13. The method of claim 1 , wherein the contacting comprises administering to the subject an imageable amount of the matrix metalloproteinase inhibitor labeled with a radioisotope.14. (canceled)15. The method of claim 1 , wherein the imaging is effected with a computer tomography (CT) scanner.167 ...

Radiosynthesiser Add-On Device

The present invention relates to an automated radiosynthesis device adapted for the addition of multiple additional components. The automated radiosynthesis device of the invention enables a wider range of radiochemical synthetic processes to be carried out in an automated fashion. 1. An automated radiosynthesis device comprising:(i) a plurality of connectors for removably attaching a disposable kit;(ii) a plurality of actuators to selectively control moving parts of said disposable kit;(iii) a control unit for directing the selective control of the moving parts of said disposable kit by said plurality of actuators;(iv) a reaction vessel heating well;(v) an inert gas conduit;(vi) a vacuum conduit;(vii) a radioisotope conduit;(viii) means to fix add-on devices onto the radiosynthesis device at various locations.2. The automated radiosynthesis device as defined in claim 1 , wherein said plurality of connectors is selected from the group comprising fasteners and fluidic connectors.3. The automated radiosynthesis device as defined in claim 2 , wherein said fluidic connectors are selected from the group comprising push-on type connectors claim 2 , luer slip connectors or luer screw connectors.4. The automated radiosynthesis device as defined in claim 1 , wherein said disposable kit is suitable for the synthesis of a radiotracer compound.5. The automated radiosynthesis device as defined in claim 4 , wherein said radiotracer compound is a positron-emission tomography (PET) tracer.6. The automated radiosynthesis device as defined in claim 5 , wherein said radiotracer compound is an F-labelled PET tracer.7. The automated radiosynthesis device as defined in claim 1 , wherein said disposable kit is a single-use cassette.8. The automated radiosynthesis device as defined in claim 1 , wherein said plurality of actuators is selected from the group comprising rotatable arms for stopcocks of valves claim 1 , linear actuators claim 1 , arms that press onto reagent vials and pinch ...

Deuterium-Substituted 7-Substituted-2-(Benzylamino)-6-Ozopurine Compounds and Uses Thereof

The invention relates to compounds of formula (I): The compounds are useful as antibacterial agents, especially again -associated diseases. 2. The compound of claim 1 , wherein at least one of Y claim 1 , Y claim 1 , Y claim 1 , and Yis deuterium.4. The compound of claim 2 , wherein the level of deuterium incorporation at each of Y claim 2 , Y claim 2 , Y claim 2 , and Ydesignated as deuterium is at least 52.5% claim 2 , at least 75% claim 2 , at least 82.5% claim 2 , at least 90% claim 2 , at least 95% claim 2 , at least 97% claim 2 , at least 98% claim 2 , or at least 99%.5. The compound of claim 1 , wherein at least one of least one of Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Yand Yis deuterium.7. The compound of claim 5 , wherein the level of deuterium incorporation at each of Y Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Yand Ydesignated as deuterium is at least 52.5% claim 5 , at least 75% claim 5 , at least 82.5% claim 5 , at least 90% claim 5 , at least 95% claim 5 , at least 97% claim 5 , at least 98% claim 5 , or at least 99%.8. The compound of claim 1 , wherein at least one of Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Yand Yis deuterium.10. The compound of claim 8 , wherein the level of deuterium incorporation at each of Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Y claim 8 , Yand Ydesignated as deuterium is at least 52.5% claim 8 , at least 75% claim 8 , at least 82.5% claim 8 , at least 90% claim 8 , at least 95% claim 8 , at least 97% claim 8 , at least 98% claim 8 , or at least 99%.12. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable excipient.13Clostridium difficileClostridium difficile. A method of inhibiting ...

CYCLIC POLYOLEFINS DERIVED FROM HEXYNE, OCTYNE, NONYNE, PENTADECYNE AND THEIR COPOLYMERS WITH ACETYLENE

Disclosed are saturated cyclic monopolymers derived from hexyne, octyne, nonyne, pentadecyne and saturated cyclic copolymers derived from acetylene and a second alkyne monomer that is hexyne, octyne, nonyne, or pentadecyne. 121.-. (canceled)23. The composition of claim 22 , wherein each R is n-butyl.24. The composition of claim 22 , wherein each R is n-hexyl.25. The composition of claim 22 , wherein each R is n-heptyl.26. The composition of claim 22 , wherein each R is n-tetradecyl.28. The composition of claim 27 , wherein each R is n-butyl.29. The composition of claim 27 , wherein each R is n-hexyl.30. The composition of claim 27 , wherein each R is n-heptyl.31. The composition of claim 27 , wherein each R is n-tetradecyl.33. The composition of claim 32 , where each R is n-butyl.34. The composition of claim 32 , where each R is n-tetradecyl. This application makes reference to the following patent applications and patents: International Patent Application No. PCT/US2015/034888, entitled “Metallacycloalkylene Complexes and Use for Alkyne Polymerization to Cyclic Polyacetylenes,” filed Jun. 9, 2015; which is a continuation-in-part of U.S. patent application Ser. No. 14/299,449, entitled “Tridentate Pincer Ligand Supported Metal-Alkylidyne and Metallacycloalkylene Complexes for Alkyne Polymerization,” filed Jun. 9, 2014, now U.S. Pat. No. 9,206,266, issued Dec. 8, 2015, which claims priority from U.S. Provisional Patent Application No. 61/845,764, filed Jul. 12, 2013, and is a continuation-in-part of PCT/US2012/065841, filed Nov. 19, 2012, which claims priority from U.S. Provisional Patent Application No. 61/567,909, filed Dec. 7, 2011.U.S. patent application Ser. No. 15/286,780, entitled “ONO Pincer Ligands and ONO Pincer Ligand Comprising Metal Complexes,” filed Oct. 6, 2016, which is a division of U.S. patent application Ser. No. 14/077,822, filed Nov. 12, 2013, now U.S. Pat. No. 9,464,104, issued Oct. 11, 2016, which is a continuation in part of PCT/US2012/037302, ...

METHOD FOR HYDROGENATING STYRENIC BLOCK COPOLYMERS AND HYDROGENATED POLYMER

A catalyst composition, a method for hydrogenating styrenic block copolymer employing the same, and a hydrogenated polymer from the method are provided. The method for hydrogenating styrenic block copolymer includes subjecting a hydrogenation process to a styrenic block copolymer in the presence of a catalyst composition. In particular, the catalyst composition includes an oxide carrier, and a catalyst disposed on the oxide carrier, wherein the catalyst includes a platinum-and-rhenium containing phosphorus compound. 1. A method for hydrogenating styrenic block copolymer , comprising:subjecting a styrenic block copolymer to a hydrogenation process in the presence of a catalyst composition;wherein the catalyst composition comprises:an oxide carrier; anda catalyst disposed on the oxide carrier, wherein the catalyst comprises a platinum-and-rhenium containing phosphorus compound.2. The method for hydrogenating styrenic block copolymer as claimed in claim 1 , wherein the oxide carrier comprises titanium oxide claim 1 , aluminum oxide claim 1 , zirconium oxide claim 1 , silicon oxide claim 1 , or a combination thereof.3. The method for hydrogenating styrenic block copolymer as claimed in claim 1 , wherein the styrenic block copolymer is formed by polymerizing a conjugated diene monomer and a vinyl aromatic hydrocarbon monomer.4. The method for hydrogenating styrenic block copolymer as claimed in claim 3 , wherein the conjugated diene monomer comprises 1 claim 3 ,3-butadiene claim 3 , 2 claim 3 ,3-dimethyl-1 claim 3 ,3-butadiene claim 3 , 3-butyl-1 claim 3 ,3-octadiene claim 3 , isoprene claim 3 , 1-methylbutadiene claim 3 , 2-phenyl-1 claim 3 ,3-butadiene claim 3 , or a combinations thereof.5. The method for hydrogenating styrenic block copolymer as claimed in claim 3 , wherein the vinyl aromatic hydrocarbon monomer comprises styrene claim 3 , methylstyrene claim 3 , ethylstyrene claim 3 , cyclohexylstyrene claim 3 , vinyl biphenyl claim 3 , 1-vinyl-5-hexyl naphthalene ...

SEALANT COMPOSITION FOR USE IN SUBTERRANEAN FORMATIONS

Sealant compositions that may be used for creating fluid flow preventing barriers in a subterranean formation. A method may comprise reacting components comprising an oxazoline functionalized polymer and a crosslinking agent in a subterranean formation to create a barrier in the subterranean formation. 1. A method comprising:reacting components comprising an oxazoline functionalized polymer and a crosslinking agent in a subterranean formation to create a barrier in the subterranean formation.2. The method of wherein the oxazoline functionalized polymer is a polymer with one or more oxazoline functional groups attached to the polymer backbone.3. The method of wherein the oxazoline functionalized polymer is a copolymer of an oxazoline monomer and an addition monomer that does not contain an oxazoline functional group.4. The method of wherein the oxazoline functionalized polymer comprises a copolymer of one or more monomers selected from the group consisting of acrylate claim 1 , methacrylate claim 1 , and a styrene monomer.5. The method of wherein the crosslinking agent comprises reactive groups selected from the group consisting of a carboxylic group claim 1 , phenol group claim 1 , thiol group claim 1 , a combination thereof claim 1 , and a derivative thereof.6. The method of wherein the crosslinking agent comprises reactive groups that are delayed release such that step of reacting is delayed until release of the reactive groups.7. The method of further comprising introducing a sealant composition comprising an aqueous-base fluid claim 1 , the oxazoline functionalized polymer and the crosslinking agent into the subterranean formation.8. The method of wherein crosslinking agent comprises an ester or amide of a carboxylic acid that hydrolyzes to release groups reactive to oxazoline functionality.9. The method of wherein the crosslinking agent comprises an ester of at least one carboxylic acid selected from the group consisting of oxalic acid claim 7 , malonic acid ...

INITIATOR COMPOSITION, UNSATURATED POLYESTER RESIN COMPOSITION COMPRISING SAME, AND METHOD FOR CURING RESIN

An initiator composition, including: at least two compounds represented by the chemical formula of R—CO—O—O—CO—R and a compound represented by the chemical formula of R—CO—O—O—R, where R represents a C-Calkyl or a C-Caryl or substituted aryl, Rrepresents a C-Calkyl or a C-Caryl, and Rrepresents a C-Calkyl. 1. An initiator composition , comprising: at least two compounds represented by formula R—CO—O—O—CO—R and a compound represented by formula R—CO—O—O—R , wherein R represents a C-Calkyl or a C-Caryl or substituted aryl , Rrepresents a C-Calkyl or a C-Caryl , and Rrepresents a C-Calkyl.2. The initiator composition of claim 1 , wherein the two compounds represented by the formula of R—CO—O—O—CO—R are a diacyl peroxide selected from the group consisting of benzoyl peroxide claim 1 , 2 claim 1 ,4-dichlorobenzene acyl peroxide claim 1 , lauroyl peroxide claim 1 , and diacetyl peroxide claim 1 , and the compound represented by the formula of R—CO—O—O—Ris a carboxylic ester peroxide selected from the group consisting of tert-butyl peroxybenzoate (TBPB) claim 1 , tert-butyl peroxy diethyl acetate claim 1 , t-butyl peroctoate (TBPO).3. The initiator composition of claim 2 , comprising between 50 and 95 parts by weight of the two compounds represented by the formula of R—CO—O—O—CO—R and between 5 and 50 parts by weight of the compound represented by the formula of R—CO—O—O—R.4. The initiator composition of claim 3 , comprising between 75 and 95 parts by weight of the two compounds represented by the formula of R—CO—O—O—CO—R and between 5 and 25 parts by weight of the compound represented by the formula of R—CO—O—O—R.5. The initiator composition of claim 4 , comprising 75 parts by weight of the diacyl peroxide and 25 parts by weight of the carboxylic ester peroxide claim 4 , wherein the diacyl peroxide comprises 25 parts by weight of the benzoyl peroxide claim 4 , 20 parts by weight of 2 claim 4 ,4-dichlorobenzene acyl peroxide claim 4 , 15 parts by weight of lauroyl peroxide ...

SURFACE PROTECTION FILM

A surface protection film includes an adhesion layer that includes a blend of a first hydrogenated styrene block copolymer, a second hydrogenated styrene block copolymer different from the first hydrogenated styrene block copolymer, and polyethylene. An Adhesion Build Value of the surface protection film is less than 2.5 after the adhesion layer has been attached to a textured polycarbonate substrate and heated to 90° C. for 10 minutes. 1. A surface protection film comprising:an adhesion layer comprising a blend of a first hydrogenated styrene block copolymer, a second hydrogenated styrene block copolymer different from the first hydrogenated styrene block copolymer, and polyethylene,wherein an Adhesion Build Value of the surface protection film is less than 2.5 after the adhesion layer has been attached to a textured polycarbonate substrate and heated to 90° C. for 10 minutes.2. The surface protection film according to claim 1 , wherein the Adhesion Build Value of the surface protection film is less than 2.0 after the adhesion layer has been attached to a textured polycarbonate substrate and heated to 90° C. for 10 minutes.3. The surface protection film according to claim 1 , wherein the Adhesion Build Value of the surface protection film is less than 1.5 after the adhesion layer has been attached to a textured polycarbonate substrate and heated to 90° C. for 10 minutes.4. The surface protection film according to claim 1 , wherein the first hydrogenated styrene block copolymer comprises about 34 wt % styrene and has a Melt Flow Rate at 230° C. and 2.16 kg of about 48 grams/10 minutes.5. The surface protection film according to claim 1 , wherein the second hydrogenated styrene block copolymer comprises about 65 wt % styrene and has a Melt Flow Rate at 230° C. and 2.16 kg of about 0.4 grams/10 minutes.6. The surface protection film according to claim 1 , wherein the adhesion layer blend comprises a total of 25 wt %-50 wt % hydrogenated styrene block copolymer claim 1 ...

DEUTERATED ANALOGS OF PRIDOPIDINE USEFUL AS DOPAMINERGIC STABILIZERS

The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. 2. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '2, 'R-Rrepresent deuterium (D); and'}{'sup': 3', '23, 'all of R-Rrepresent hydrogen (H).'}3. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '7, 'at least one of R-Rrepresents deuterium (D); and'}{'sup': 1', '23, 'the remaining of R-Rrepresent hydrogen (H).'}4. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '7, 'all of R-Rrepresent deuterium (D); and'}{'sup': 8', '23, 'all of R-Rrepresent hydrogen (H).'}5. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 8', '9', '10', '11, 'R, R, Rand Rrepresent deuterium (D); and'}{'sup': 1', '7', '12', '23, 'all of R-Rand R-Rrepresent hydrogen (H).'}6. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '12', 'Rrepresents deuterium (D); and'}{'sup': 1', '11', '13', '23, 'all of R-Rand R-Rrepresent hydrogen (H).'}7. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 17', '20, 'R-Rrepresent deuterium (D); and'}{'sup': 1', '16', '21', '23, 'all of R-Rand R-Rrepresent hydrogen (H).'}8. A pharmaceutical composition claim 1 , comprising a therapeutically effective amount of a deuterated analog of 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine according to any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , together with at least one pharmaceutically acceptable carrier claim 1 , excipient or diluent.9. The deuterated ...

2-(2,4,5-SUBSTITUTED ANILINE) PYRIMIDINE DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Disclosed are a 2-(2,4,5-substituted aniline) pyrimidine derivative, a pharmaceutical composition and a use thereof. The pharmaceutical composition comprises a therapeutically effective amount of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. Also disclosed is a use of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating cancers. The compounds of the present invention have a relatively high solubility in water and a relatively high permeability, and/or a relatively low binding ability to plasma proteins, and at the same time have a relatively low toxicity characteristic and a relatively high anti-tumor activity. 2. The 2-(2 claim 1 ,4 claim 1 ,5-substituted aniline)pyrimidine derivative represented by formula I claim 1 , or the solvate claim 1 , or the pharmaceutically acceptable salt thereof according to claim 1 , wherein claim 1 , the methyl substituted by 1 to 3 of deuterium atom(s) is a tri-deuterated methyl.3. The 2-(2 claim 1 ,4 claim 1 ,5-substituted aniline)pyrimidine derivative represented by formula I claim 1 , or the solvate claim 1 , or the pharmaceutically acceptable salt thereof according to claim 1 , which is selected from the group consisting of{'sub': '3', 'N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-(D-methyl)indol-3-yl)pyrimidin-2-yl]amino}phenyl)-2-acrylamide;'}{'sub': '3', 'N-(2-{2-dimethylaminoethyl-methylamino}-4-(D-methoxy)-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)-2-acrylamide;'}{'sub': '3', 'N-(2-{2-dimethylaminoethyl-(D-methyl)amino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)-2-acrylamide;'}{'sub': '3', 'N-(2-{2-di(D-methyl)aminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)-2-acrylamide;'}{'sub': '3', 'N-(2-{2-[methyl(D-methyl)amino]ethyl- ...

PEPTIDE FOR TREATING OCULAR DISEASES AND COMPOSITION FOR TREATING OCULAR DISEASES COMPRISING SAME

The present specification discloses a pharmaceutical composition for preventing or treating ophthalmopathy. More particularly, disclosed is a composition comprising a peptide derived from telomerase and being effective in treating and preventing ophthalmopathy. The disclosed peptide, a peptide having a sequence 80% identical to the sequence thereof, or a peptide as a fragment thereof is superiorly effective in treating ophthalmopathy. 113-. (canceled)14. A method of inhibiting choroidal neovascularization , comprising:administering to a subject in need thereof an effective amount of an isolated peptide consisting of the amino acid sequence of SEQ ID NO: 1.15. The method of claim 14 , wherein the peptide is administered at a daily dose of 10 ng/kg to 10 mg/kg.16. The method of claim 14 , wherein the peptide is administered at a daily dose of 2 μg/kg to 50 μg/kg.17. The method of claim 14 , wherein the peptide is administered 1 to 3 times a day.18. A method of inhibiting choroidal neovascularization claim 14 , comprising:administering to a subject in need thereof a composition comprising an effective amount of an isolated peptide consisting of the amino acid sequence of SEQ ID NO: 1.19. The method of claim 18 , wherein the composition further comprises a pharmaceutically acceptable excipient and an additive.20. The method of claim 18 , wherein the composition is a food composition.21. The method of claim 18 , wherein the composition comprises 0.01 g/L to 1 kg/L of the peptide.22. The method of claim 18 , wherein the composition comprises 1 g/L to 10 g/L of the peptide.23. The method of claim 18 , wherein the peptide is administered at a daily dose of 10 ng/kg to 10 mg/kg.24. The method of claim 18 , wherein the peptide is administered at a daily dose of 2 μg/kg to 50 μg/kg.25. The method of claim 18 , wherein the peptide is administered 1 to 3 times a day.26. A kit for inhibiting choroidal neovascularization claim 18 , comprising a composition that contains the ...

STABILISED RADIOLABELLING REACTION

The present invention provides a method for the synthesis of an injectable composition comprising a [F]-labelled pyridaben derivative that is advantageous over prior methods. In particular, the method of the present invention comprises a method of radiosynthesis that permits a more facile purification using solid phase extraction (SPE). 1. A method comprising reacting a precursor compound with F-fluoride in the presence of (2 ,2 ,6 ,6-Tetramethylpiperidin-1-yl)oxyl (TEMPO) to obtain an F-labelled compound wherein: {'br': None, 'BTM-LINKER-LG \u2003\u2003(I)'}, 'said precursor compound is of Formula Iwherein:BTM is an analogue of pyridaben;LINKER is an alkylene or an alkoxyalkylene; and,LG is a sulfonate-containing leaving group; and{'sup': '18', 'claim-text': {'br': None, 'sup': '18', 'BTM-LINKER-F \u2003\u2003(II)'}, 'said F-labelled compound is of Formula IIwherein BTM and LINKER are as defined for Formula I.3. The method as defined in wherein Ris Calkyl.4. The method as defined in wherein Ris methyl claim 2 , ethyl claim 2 , propyl claim 2 , n-butyl claim 2 , s-butyl claim 2 , or t-butyl.5. The method as defined in wherein Ris halo.6. The method as defined in wherein Ris chloro.7. The method as defined in wherein W is heteroalkylene.8. The method as defined in wherein W is alkoxyalkylene.11. The method as defined in wherein LG is selected from mesylate claim 1 , tosylate claim 1 , triflate claim 1 , nosylate claim 1 , or 1 claim 1 ,2-cyclic sulfate.12. The method as defined in wherein LG is tosylate.13. The method as defined in wherein said precursor compound is dissolved in acetonitrile.14. The method as defined in wherein said TEMPO is present in a molar ratio to the precursor compound of between 0.01:1 and 5:1.15. The method as defined in wherein the starting radioactivity is at least 100 GBq.16. The method as defined in wherein the starting radioactivity is between 100-1000 GBq.17. The method as defined in wherein the starting radioactivity is between 100-750 ...

Novel Aspartylamide Inhibitors of Excitatory Amino Acid Transporters

The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: 2. The compound of claim 1 , wherein said halogen is fluorine.3. The compound of claim 1 , wherein said halogen or radionuclide is fluorine-18.4. The compound of claim 1 , wherein said radionuclide is selected from the group consisting of carbon-11 claim 1 , nitrogen-13 claim 1 , oxygen-15 claim 1 , fluorine-18 claim 1 , zinc-62 claim 1 , copper-62 claim 1 , gallium-68 claim 1 , germanium-68 claim 1 , strontium-82 claim 1 , technicium-94m claim 1 , iodine 124 claim 1 , or rubidium-82.5. The compound of claim 3 , wherein said fluorine-18 has a specific activity of at least 1.0 Ci/mmol.6. The compound of claim 3 , wherein said fluorine-18 has a specific activity of at least 2.0 Ci/mmol.7. The compound of in combination with a pharmaceutically acceptable excipient.11. The method of claim 10 , wherein said neuronal disorder is caused by amyotrophic lateral sclerosis claim 10 , Alzheimer's disease claim 10 , Huntington's disease claim 10 , or ALS-parkinsonism dementia complex.12. The method of claim 10 , wherein said neuronal disorder is caused by ischemia claim 10 , hypoglycemia claim 10 , spinal cord injury or traumatic brain injury.13. The method of claim 10 , wherein said halogen or radionuclide is fluorine or fluorine-18.14. The method of claim 10 , wherein said radionuclide is selected from the group consisting of carbon-11 claim 10 , nitrogen-13 claim 10 , oxygen-15 claim 10 , fluorine-18 claim 10 , zinc-62 claim 10 , copper-62 claim 10 , gallium-68 claim 10 , germanium-68 claim 10 , strontium-82 claim 10 , technicium-94m claim 10 , iodine 124 claim 10 , or rubidium-82.16. The method of claim 15 , wherein said radiographic scanner is a positron emission tomography scanner.17. The method of claim 15 , wherein said excitatory amino acid ...

Disconnector Device

The present invention relates to an automated radiosynthesis device adapted for enhanced automatic disconnection of a disposable kit once a radiosynthesis has been carried out. The automated radiosynthesis device of the invention therefore reduces the time to remove the disposable kit from the radiosynthesis device and reduces radiation exposure to the operator. 21. The automated radiosynthesis device as defined in claim , wherein said plurality of connectors is selected from the group comprising fasteners , and fluidic connectors.3. The automated radiosynthesis device as defined in claim 2 , wherein said fluidic connectors are selected from the group comprising push-on type connectors luer slip connectors and luer screw connectors.41. The automated radiosynthesis device as defined in claim claim 2 , wherein said disposable kit is suitable for the synthesis of a radiotracer compound.5. The automated radiosynthesis device as defined in claim 4 , wherein said radiotracer compound is a positron-emission tomography (PET) tracer.6. The automated radiosynthesis device as defined in claim 5 , wherein said radiotracer compound is an F-labelled PET tracer.71. The automated radiosynthesis device as defined in claim claim 5 , wherein said disposable kit is a single-use cassette.81. The automated radiosynthesis device as defined in claim claim 5 , wherein said plurality of actuators is selected from the group comprising rotatable arms for stopcocks of valves claim 5 , linear actuators claim 5 , arms that press onto reagent vials and pinch valves.91. The automated radiosynthesis device as defined in claim claim 5 , wherein said moving parts of said disposable kit are selected from the group comprising reagent vials claim 5 , syringes and valves.101. The automated radiosynthesis device as defined in claim claim 5 , wherein said control unit includes software comprising instructions for a particular radiosynthesis method to be carried out on said disposable kit attached to said ...

RADIOLABELED PABA AND DERIVATIVES THEREOF FOR USE AS FUNCTIONAL RENAL IMAGING AGENTS

The present invention provides positron emitter radiolabeled versions of PABA, metabolites and derivatives, with good radiochemical yield, high specific activity, high chemical and radiochemical purity and having excellent characteristics for PET imaging. The inventive composition and methods provide high quality dynamic images of the kidneys while reducing the radiation exposure. The short biological half-life of PABA, added to the short physical half-life of positron emitters such as C will also benefit patients that require multiple renography assessments in a short period of time. 1. An imaging agent for use in functional renal imaging of one or both kidneys in a subject in need thereof , characterized in that the imaging agent comprises para-amino benzoic acid (PABA) or a metabolite or derivative thereof , labeled with a positron emitting radionuclide , and wherein the imaging agent is administered to the subject in conjunction with obtaining a series of images at regular intervals of at least one or more regions of interest of the kidney of the subject for a period of time , and quantifying the amount of radioactivity in each interval during said time period.2. An imaging agent for use as in claim 1 , wherein the a positron emitting radionuclide is selected from the group consisting of C claim 1 , N claim 1 , O claim 1 , F claim 1 , K claim 1 , Ti claim 1 , Mn claim 1 , Mn claim 1 , Fe claim 1 , Co claim 1 , Cu claim 1 , Cu claim 1 , Cu claim 1 , Ga claim 1 , As claim 1 , Rb claim 1 , Sr claim 1 , Y claim 1 , and Zr.3. An imaging agent for use as in or claim 1 , wherein the PABA metabolite is selected from the group consisting of N-acetyl-PABA claim 1 , p-aminohippuric acid claim 1 , and p-acetylaminohippuric acid.5. An imaging agent for use in functional renal imaging of one or both kidneys in a subject in need thereof claim 1 , characterized in that the imaging agent comprises para-amino benzoic acid (PABA) or a metabolite or derivative thereof claim 1 , ...

OPIOID RECEPTOR MODULATING OXABICYCLO[2.2.2]OCTANE MORPHINANS

The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R, R, Y, Z, and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I), and pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain. 4. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein Ris hydrogen , hydroxy , halo , cyano , carboxy , or aminocarbonyl; or alkyl , alkenyl , alkynyl , alkoxy , alkenyloxy , or alkynyloxy , any of which is optionally substituted with 1 , 2 , or 3 substituents , each independently selected from the group consisting of hydroxy , halo , haloalkyl , amino , alkylamino , dialkylamino , carboxy , alkoxy , alkoxycarbonyl , aryl , heteroaryl , heterocyclo , cycloalkyl , and cycloalkenyl , wherein said aryl , heteroaryl , heterocyclo , cycloalkyl , and cycloalkenyl are optionally substituted with 1 , 2 , or 3 independently selected Rgroups.5. The compound of claim 4 , or a pharmaceutically acceptable salt or solvate thereof claim 4 , wherein Ris hydroxy or unsubstituted Calkoxy claim 4 , preferably unsubstituted Calkoxy claim 4 , further preferably methoxy.6. The compound of any one of - claim 4 , or a pharmaceutically acceptable salt or solvate thereof claim 4 , wherein Ris —O-PG.7. The compound of claim 6 , or a pharmaceutically acceptable salt or solvate thereof claim 6 , wherein PG is selected from the group consisting of alkyl claim 6 , arylalkyl claim 6 , heterocyclo claim 6 , (heterocyclo)alkyl claim 6 , acyl claim 6 , silyl claim 6 , and carbonate claim 6 , any of which is optionally substituted.8. The compound of claim 7 , or a pharmaceutically acceptable salt or solvate thereof claim 7 , wherein PG is selected from ...

DEUTERATED CFTR POTENTIATORS

This invention relates to compounds of Formula I: 119.-. (canceled)21. The compound of claim 20 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.22. The compound of claim 20 , wherein the isotopic enrichment coefficient for each designated deuterium is at least 3500 claim 20 , wherein the isotopic enrichment coefficient refers to the ratio between the isotopic abundance and the natural abundance of a specified isotope.24. The salt of claim 23 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.25. The salt of claim 23 , wherein the isotopic enrichment coefficient for each designated deuterium is at least 3500 claim 23 , wherein the isotopic enrichment coefficient refers to the ratio between the isotopic abundance and the natural abundance of a specified isotope. This application is a continuation-in-part of International Application No. PCT/US12/38297, filed May 17, 2012, which claims the benefit of U.S. Provisional Application Ser. No. 61/487,497, filed May 18, 2011. This application also claims the benefit of U.S. Provisional Application Ser. No. 61/727,941, filed Nov. 19, 2012; U.S. Provisional Application Ser. No. 61/780,681, filed Mar. 13, 2013; and U.S. Provisional Application Ser. No. 61/860,602, filed Jul. 31, 2013. The contents of these applications are incorporated herein by reference in their entirety.Many current medicines suffer from poor absorption, distribution, metabolism and/or excretion (ADME) properties that prevent their wider use or limit their use in certain indications. Poor ADME properties are also a major reason for the failure of drug candidates in clinical trials. While formulation technologies and prodrug strategies can be employed in some cases to improve certain ADME properties, these approaches often fail to address the underlying ADME problems that exist for many drugs and drug candidates. One such problem is rapid metabolism that causes a number of ...

Method for Racemisation of (5R)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H¬isoxazol-3-yl]-2-Methyl-Benzoic Acid

The present invention relates to a method for racemizing (5R)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-2-methyl-benzoic acid. 2. The Method according to claim 1 , wherein the alkaline compound is an inorganic compound.3. The Method according to claim 1 , wherein the alkaline compound is selected from the group consisting of sodium hydroxide claim 1 , potassium hydroxide claim 1 , cesium hydroxide claim 1 , calcium hydroxide claim 1 , barium hydroxide claim 1 , magnesium oxide claim 1 , calcium oxide claim 1 , barium oxide claim 1 , cesium carbonate and mixtures thereof.4. The Method according to claim 1 , wherein the organic solvent is selected from the group consisting of water claim 1 , an alcohol with 1 to 5 carbon atoms claim 1 , dioxane claim 1 , tetrahydrofuran claim 1 , toluene claim 1 , ethyl acetate and mixtures thereof.5. The Method according to claim 1 , further comprising the steps of:(ii) acidifying the reacted mixture from step (i), to form a result mixture and(iii) separating the result mixture from step (ii) in a compound mixture and supernatant6. The Method according to claim 1 , wherein step (i) is carried out in the absence of phase transfer catalysts.8. The Method according to claim 1 , wherein in step (a) the solvent is selected from the group consisting of an alcohol with 2 to 5 carbon atoms claim 1 , dioxane claim 1 , tetrahydrofuran and mixtures thereof.9. The Method according to claim 7 , wherein in step (a) the solvent is 2-propanol.10. The Method according to claim 7 , wherein in step (a) R of Formula (2A) is methyl and the solvent is 2-propanol or R of Formula (2A) is ethyl and the solvent is 2-propanol.11. The Method according to claim 7 , wherein step (a) comprises heating (5RS)-4-[5-(3 claim 7 ,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]2-methyl-benzoic acid with the compound of Formula (2A) claim 7 , (2b) or (2C) in the solvent to an elevated temperature.12. The Method according to claim 7 , wherein ...

BENZYL COMPOUND

The purpose of the present invention is to provide a protecting group which improves the solubility of a compound having a functional group protected with the protecting group in an organic solvent and which is easily separated and purified after a reaction with avoiding solidification or insolubilization. Provided is a benzyl compound represented by Formula (1) where Xrepresents —CHOR(where Rrepresents a hydrogen atom, a halogenocarbonyl group, or an active ester-type protecting group), —CHNHR(where Rrepresents a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group), a halogenomethyl group, a methyl azide group, a formyl group, or an oxime; and at least one of R, R, R, R, and Ris a group represented by Formula (2), and the remainders each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or an alkoxy group having 1 to 4 carbon atoms, where Rrepresents a linear or branched alkylene group having 1 to 16 carbon atoms; Xrepresents O or CONR(where Rrepresents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms); and A represents a group represented by Formula (3), (4), (5), (6), (7), (8), (9), (10), (11), (12), or (13). 2: The benzyl compound according to claim 1 , wherein Xis —CHORwhere Rrepresents a hydrogen atom claim 1 , a halogenocarbonyl group claim 1 , or an active ester-type protecting group claim 1 , —CHNHRwhere Rrepresents a hydrogen atom claim 1 , a linear or branched alkyl group having 1 to 6 carbon atoms claim 1 , or an aralkyl group claim 1 , or a halogenomethyl group.3: The benzyl compound according to claim 1 , wherein Ris a linear or branched alkylene group having 2 to 16 carbon atoms.4: The benzyl compound according to claim 1 , wherein Ris a linear or branched alkylene group having 6 to 16 carbon atoms.5: The benzyl compound according to claim 1 , wherein Ris a single bond or a methylene group; and R claim 1 , R claim 1 , and Rare methylene groups.6: A method claim ...

SOLID PHASE EXTRACTION

The present invention provides a method for the synthesis of an injectable composition comprising a [F]-labelled pyridaben derivative that is amenable to automation. In particular, the method of the present invention comprises a method of purification carried out by means of solid phase extraction (SPE) alone. 1. A method comprising: [{'br': None, 'BTM-LINKER-LG\u2003\u2003(I)'}, 'wherein:', 'BTM is a biological targeting moiety;', 'LINKER is an alkylene or an alkoxyalkylene; and,', 'LG is a sulfonate-containing leaving group, '(a) reacting in acetonitrile a precursor compound of Formula I{'sup': 18', '18, 'claim-text': {'br': None, 'sup': '18', 'BTM-LINKER-F\u2003\u2003(II)'}, 'with F-fluoride to obtain a crude reaction mixture comprising an F-labelled compound of Formula IIwherein BTM and LINKER are as defined for Formula I;(b) diluting the crude reaction mixture obtained in step (a) to obtain a diluted crude reaction mixture; (i) transferring said diluted crude reaction mixture to an SPE cartridge;', '(ii) optionally passing water through said SPE cartridge;', '(iii) passing a wash solution comprising an organic solvent through said SPE cartridge;', '(iv) optionally passing water through said SPE cartridge to remove said organic solvent; and,', '(v) passing an elution solution comprising ethanol through said SPE cartridge to elute said compound of Formula I from said SPE cartridge;, '(c) purifying the diluted crude reaction mixture obtained in step (b) by means of one or more solid phase extraction (SPE) cartridges to obtain a purified compound of Formula II where said purifying comprises the sequential steps ofwherein step (b) includes adding a hydrolyzing reagent to said crude reaction mixture and/or said water of step (ii) and/or step (iv) comprises a hydrolyzing reagent.2. The method as defined in wherein said BTM is a small molecule.3. The method as defined in wherein said small molecule is an analogue of pyridaben.5. The method as defined in wherein Ris ...

METHOD FOR PRODUCING PEPTIDE

An object of the present invention is to provide a novel solid phase peptide synthesis method for synthesizing a large amount of a peptide. Another object of the present invention is to provide a novel solid phase peptide synthesis method for synthesizing a high-purity long-chain peptide. Still another object of the present invention is to provide a novel solid phase peptide synthesis method causing fewer side reactions. The present invention relates to a method for producing a peptide, and the method comprises solid-phase synthesis of a peptide under stirring with a centrifugal stirrer having no impeller. 1. A method for producing a peptide , the method comprising:performing a solid-phase synthesis of a peptide while stirring with a centrifugal stirrer having no impeller.25-. (canceled)6. The method according to claim 1 , wherein the centrifugal stirrer having no impeller is a stirring rotor comprising:a main body configured to rotate about a rotating shaft,an inlet port provided on a surface of the main body,an outlet port provided on the surface of the main body, anda flow path connecting the inlet port to the outlet port, whereinthe inlet port is provided closer to the rotating shaft than the outlet port, andthe outlet port is provided more distant from the rotating shaft in a centrifugal direction than the inlet port.7. A solid phase peptide synthesis reaction container comprising a centrifugal stirrer having no impeller.8. The solid phase peptide synthesis reaction container according to claim 7 , further comprising a glass filter.9. The solid phase peptide synthesis reaction container according to claim 7 , further comprising a heating medium jacket.10. The solid phase peptide synthesis reaction container according to claim 7 , further comprising a cock.11. The solid phase peptide synthesis reaction container according to claim 7 , further comprising a peptide having between 5 and 150 amino acid residues. The present invention relates to a method for ...

METHOD FOR DEODORIZING HYDROGENATED PETROLEUM RESIN, AND METHOD FOR PRODUCING HYDROGENATED PETROLEUM RESIN

Provided is a new method that effectively reduces odor components that are present in a hydrogenated petroleum resin, and adjusts a softening point to an appropriate range for exhibiting an adhesive performance. 1. A method for deodorizing a hydrogenated petroleum resin , comprising: stripping a hydrogenated petroleum resin at a gas flow rate of 1 to 45 VVM.2. The method for deodorizing a hydrogenated petroleum resin according to claim 1 , wherein the stripping is performed at 150 to 250° C.3. The method for deodorizing a hydrogenated petroleum resin according to claim 1 , wherein the stripping is performed at 160 to 240° C.4. A method for producing a hydrogenated petroleum resin claim 1 , comprising: thermally polymerizing dicyclopentadiene and a vinyl aromatic compound claim 1 , hydrogenating the obtained polymerization reaction product claim 1 , and then stripping the obtained hydrogenated petroleum resin at a gas flow rate of 1 to 45 VVM.5. The method for deodorizing a hydrogenated petroleum resin according to claim 1 , wherein the hydrogenated petroleum resin is a dicyclopentadiene/vinyl aromatic compound hydrogenated petroleum resin. The present invention relates to a method for deodorizing a hydrogenated petroleum resin and a method for producing a hydrogenated petroleum resin. More specifically, the present invention relates to a method for deodorizing and a method for producing a dicyclopentadiene/vinyl aromatic compound hydrogenated petroleum resin obtained by hydrogenating a thermal polymerization reaction product of dicyclopentadiene and a vinyl aromatic compound.A hot melt adhesive is excellent in, for example, high-speed coating properties, fast setting properties, solvent-free properties, barrier properties, energy saving properties, and economic efficiency, and thus is increasingly used as an adhesive for, for example, sanitary materials, packaging materials, automobiles in various fields.A dicyclopentadiene/vinyl aromatic compound hydrogenated ...

METHOD FOR PRODUCING HYDROGENATED PETROLEUM RESIN

Provided is a method for producing a hydrogenated petroleum resin having good compatibility with a base polymer and a good hue under a hydrogen pressure of 4 MPaG or less. 1. A method for producing a hydrogenated petroleum resin , the method comprising hydrogenating a polymerization product of dicyclopentadiene and a vinyl aromatic compound in the presence of a catalyst ,wherein the hydrogenating is performed under the following conditions (A) to (C):(A) an amount of the catalyst employed is 0.125 to 0.4 parts by mass relative to 100 parts by mass of a resin in the polymerization product;(B) a reaction pressure is 4 MPaG or less; and(C) a reaction temperature is 240° C. or higher.2. The method of claim 1 , wherein the catalyst is a palladium catalyst or a nickel catalyst.3. The method of claim 1 , wherein the polymerization product is obtained by thermally polymerizing the dicyclopentadiene and the vinyl aromatic compound.4. The method of claim 1 , further comprising thermally polymerizing the dicyclopentadiene and the vinyl aromatic compound claim 1 , to obtain a polymerization product that is employed in the hydrogenating as the polymerization product of the dicyclopentadiene and the vinyl aromatic compound.6. The method of claim 1 , wherein the catalyst is a nickel catalyst claim 1 , a palladium catalyst claim 1 , a cobalt catalyst claim 1 , a platinum catalyst or a rhodium catalyst.7. The method of claim 1 , wherein the reaction pressure is normal pressure to 4 MPaG.8. The method of claim 1 , wherein the reaction temperature is 240 to 300° C. The present invention relates to a method for producing a hydrogenated petroleum resin. More specifically, the present invention relates to a method for producing a dicyclopentadiene/vinyl aromatic compound-based hydrogenated petroleum resin, including hydrogenating a polymerization product of dicyclopentadiene and a vinyl aromatic compound.A hot melt adhesive is widely used in the fields of, for example, bookbinding, ...

METHODS AND REAGENTS FOR RADIOLABELING

The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things, novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I. 4. The compound of any one of the preceding claims , wherein Yis —CR—.5. The compound of any one of - , wherein Yis —N—.6. The compound of any one of the preceding claims , wherein Yis —CR—.7. The compound of any one of - , wherein Yis —N—.8. The compound of any one of the preceding claims , wherein Ris hydrogen.9. The compound of any one of the preceding claims , wherein Zis —CH—.10. The compound of any one of - , wherein Zis —N—.11. The compound of any one of the preceding claims , wherein Zis —CH—.12. The compound of any one of - , wherein Zis —N—.13. The compound of any one of the preceding claims , wherein Zis —CH—.14. The compound of any one of - , wherein Zis —N—.16. The compound of any one of the preceding claims , wherein L is a straight or branched , Caliphatic group wherein one or more carbons are independently replaced by —NR— , wherein R is other than a -Boc protecting group.17. The compound of any one of the preceding claims , wherein X is —CH— or —S—.18. The compound of any one of the preceding claims , wherein X is —CH—.19. The compound of any one of - , wherein X is —S—.20. The compound of any one of the preceding claims , wherein Ris hydrogen.21. The compound of any one of - , wherein Ris halogen.22. The compound of claim 21 , wherein Ris fluro.23. The compound of any one of - claim 21 , wherein -L-Rcomprises a methylene that is replaced with —NH— to form a secondary amine.24. The compound of any one of the preceding claims claim 21 , wherein L is a straight or branched claim 21 , Caliphatic group wherein a methylene of the aliphatic group is replaced ...

HETEROGENEOUS CATALYST AND METHOD FOR SELECTIVELY HYDROGENATING COPOLYMER UTILIZING THE SAME

Disclosed is a method for selectively hydrogenating a copolymer, including contacting a heterogeneous catalyst with a copolymer to process hydrogenation The copolymer includes aromatic rings and double bonds, and the double bonds are hydrogenated, and the aromatic rings are substantially not hydrogenated. The heterogeneous catalyst includes a metal catalyst such as platinum, palladium, platinum -iridium alloy, or platinum-rhenium alloy formed on a porous support. The hydrogenation is processed at a temperature of 40° C. to 150° C. under a hydrogen pressure of 10 kg/cmto 50 kg/cm. 1. A method for selectively hydrogenating a copolymer , comprising:{'sup': 2', '2, 'contacting a heterogeneous catalyst with a copolymer including aromatic rings and double bonds to process a hydrogenation at a temperature of 40° C. to 150° C. under a hydrogen pressure of 10 kg/cmto 50 kg/cmfor hydrogenating the double bonds and substantially not hydrogenating the aromatic rings, wherein the heterogeneous catalyst comprises a metal catalyst formed on a porous support, and the metal catalyst comprises platinum, palladium, platinum-rhenium alloy, or platinum-iridium alloy.'}2. The method as claimed in claim 1 , wherein the e porous support comprises titanium oxide claim 1 , aluminum oxide claim 1 , zirconium oxide claim 1 , or silicon oxide.3. The method as claimed in claim 1 , wherein the copolymer is copolymerized of a polyenic monomer and a vinyl aromatic monomer.4. The method as claimed in claim 3 , wherein the polyenic monomer comprises butadiene claim 3 , isopentadiene claim 3 , or combinations thereof.5. The method as claimed in claim 3 , wherein the vinyl aromatic monomer comprises styrene claim 3 , ct-methylstyrene claim 3 , or combinations thereof.6. The method as claimed in claim 1 , wherein the hydrogenation is processed at a temperature of 70° C. to 120° C. under a hydrogen pressure of 30 kg/cmto 40 kg/cm.7. The method as claimed in claim 1 , wherein the metal catalyst is ...

SYNTHESIS PROCESS FOR CHIRAL CYCLOPROPYL ETHYNYL TERTIARY ALCOHOL COMPOUND

Provided is a synthesis process for a chiral cyclopropyl ethynyl tertiary alcohol compound, where a chiral amino alcohol or a chiral amino diol is reacted in the presence of an alkaline reagent and a salt to obtain an optically active propynyl alcohol compound. In particular, the process includes (1) reacting cyclopropyl acetylene with a chiral inducing agent, a chiral auxiliary reagent and zinc halide in an organic solvent in the presence of an alkaline reagent and a sulfonate or a sulphinate to obtain a first reaction mixture; (2) reacting the resultant first reaction mixture with 5-chloro-2-aminotrifluorobenzophenone to form (S)-2-amino-5-chloro-α-cyclopropyl acetylene-α-trifluoromethylbenzyl alcohol. The process avoids an organic zinc reagent and a Grignard reagent, and has the advantages of safe production, an environmentally friendly route, low production costs, a high resultant product yield, a high chiral ee value and is suitable for industrial production. 2. The method according to claim 1 , wherein said salt is a sulfonate.3. The method according to claim 1 , wherein the organic solvent is selected from the group consisting of: tetrahydrofuran claim 1 , toluene claim 1 , methyl tert-butyl ether claim 1 , N-methylpyrrolidone claim 1 , dioxane claim 1 , diethyl ether claim 1 , substituted or unsubstituted alkylbenzene claim 1 , benzene claim 1 , dichloromethane claim 1 , cyclohexane claim 1 , n-hexane claim 1 , or combinations thereof.4. The method according to claim 1 , wherein the alkaline agent is selected from alkali hydrides claim 1 , sodium alkoxides claim 1 , potassium alkoxides claim 1 , or combinations thereof; preferably NaH.5. The method according to claim 1 , characterized in that the sulfonate is selected from alkyl sulfonates claim 1 , substituted or unsubstituted aryl sulfonates claim 1 , or combinations thereof; and/orThe sulfinate is selected from alkyl sulfinate, substituted or unsubstituted aryl sulfinate, or combinations thereof.6. The ...

Partially Decarboxylated Polycarboxylic Acid Polymers

The present invention relates to partial decarboxylation of polyitaconic acid polymers or copolymers. The partially decarboxylated resins are suitable for use in preparation of dispersions as well as for anti-scaling applications. 2. The dispersion of wherein said level of decarboxylation is in the range of 40 mole % to 150 mole %.3. The dispersion of wherein said level of decarboxylation is in the range of 50 mole % to 90 mole %.4. The dispersion of wherein said partially decarboxylated polyitaconic acid homopolymer or copolymer has a number average molecular weight (Mn) value of 800 to 10 claim 1 ,000 or a weight average molecular weight (Mw) of 1 claim 1 ,500 to 50 claim 1 ,000.5. The dispersion of wherein 45 mole % to 55 mole % of the carboxylic acid groups (—COOH) in said partially decarboxylated polyitaconic acid homopolymer or copolymer is in salt form (—COOM) wherein M is a metal cation.6. The dispersion of wherein Mis selected from the group consisting of alkyl acrylates claim 1 , alkyl methacrylates claim 1 , alkyl itaconates claim 1 , maleic anhydride claim 1 , styrene claim 1 , acrylonitrile claim 1 , vinyl halides claim 1 , vinyl acetate claim 1 , vinyl alcohols claim 1 , vinyl acetate-vinyl alcohol mixtures claim 1 , olefin monomers claim 1 , and mixtures thereof.7. The dispersion of wherein said inorganic mineral is selected from the group consisting of inorganic carbonates claim 1 , inorganic oxides claim 1 , inorganic sulfates claim 1 , inorganic phosphates claim 1 , inorganic silicates and mixtures thereof.9. The method of wherein said amount of a partially neutralized polyitaconic acid homopolymer or copolymer which is sufficient to complex polyvalent metal ions in the aqueous system is at a level of 1-50 ppm.10. The method of wherein the level of decarboxylation in said partially decarboxylated polyitaconic acid homopolymer or copolymer is in the range of 40 mole % to 150 mole %.11. The method of wherein the partially decarboxylated polyitaconic ...

COMPOSITION, LAMINATE, PACKAGING MATERIAL, BATTERY CASE PACKAGING MATERIAL, AND BATTERY

The present invention relates to a composition, a laminate, a packaging material, a battery case packaging material, and a battery, and the composition includes: a modified olefin polymer (A) that is a modified olefin polymer, the modified olefin polymer being a polymer (a) of a Cto Cα-olefin modified by a monomer (b) having a functional group reactive with an epoxy group or an oxazoline group; a crosslinking agent (B) including at least one of an epoxy compound and an oxazoline compound; and a catalyst (C) having a pKa of 11 or more, 2. The composition according to claim 1 , comprising a hydrocarbon synthetic oil (D) having a kinematic viscosity at 40° C. of 30 to 500 claim 1 ,000 cSt.3. The composition according to claim 1 , wherein the polymer (a) comprises a structural unit derived from propylene.4. The composition according to claim 3 , wherein a content of the structural unit derived from propylene is 40 to 95 mol % with respect to 100 mol % of a structural unit derived from a Cto Cα-olefin.5. The composition according to claim 3 , wherein in the polymer (a) claim 3 , all structural units other than the structural unit derived from propylene are structural units derived from a Cto Cα-olefin.6. The composition according to claim 1 , wherein the Cto Cα-olefin comprises 1-butene.7. The composition according to claim 1 , wherein a content of a structural unit derived from the monomer (b) is 0.1 to 15 mass % with respect to 100 mass % of the modified olefin polymer (A).8. The composition according to claim 1 , wherein the functional group is a carboxyl group or an acid anhydride group.9. The composition according to claim 1 , wherein the crosslinking agent (B) is at least one selected from a bisphenol A liquid epoxy resin claim 1 , an alicyclic epoxy compound claim 1 , and a trimethylolpropane polyglycidyl ether.10. A laminate comprising a substrate and an adhesive layer composed of a cured product of the composition according to .11. A packaging material ...

PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR

Disclosed is a process for the preparation of certain intermediates, e.g. the following compound: 2. A process as claimed in claim 1 , where acyl donor is a compound of the following formula R—R claim 1 , in which:{'sup': '1', 'sub': 1-8', '1-6, 'Rrepresents —C(O)—Calkyl (in which the alkyl moiety is optionally substituted by one or more substituents selected from e.g. halo (e.g. fluoro), —OCalkyl (e.g. methoxy;'}{'sub': 1-3', '1-3, 'itself optionally substituted by one or more fluoro atoms) and phenyl (itself optionally substituted by one or more substituents selected from halo and Calkyl)) or —C(O)phenyl (in which phenyl is optionally substituted by one or more substituents selected from e.g. halo and Calkyl); and'}{'sup': 'x', 'sub': 1-8', '1-6', '2', '1-6', '1-6, 'Rrepresents —O—Calkyl (optionally substituted by one or more substituents selected from fluoro and —OCalkyl; the latter alkyl moiety optionally substituted by one or more fluoro atoms) or —O-phenyl (optionally substituted by one or more substituents selected from halo (e.g. chloro, fluoro, bromo), —NO, Calkyl and —OCalkyl; in which the latter two alkyl moieties are themselves optionally substituted by one or more fluoro atom).'}3. A process as claimed in claim 1 , wherein Rrepresents —C(O)—Calkyl (in which the alkyl moiety is optionally substituted by one or more substituents selected from e.g. halo (e.g. fluoro) and —OCalkyl (e.g. methoxy; itself optionally substituted by one or more fluoro atoms).4. A process as claimed in claim 3 , wherein Rrepresents a —C(O)CH—OCHmoiety or a —C(O)CHCHCHmoiety.5. A process as claimed in claim 1 , wherein the acyl donor is iso-propenyl acetate claim 1 , trifluoroethyl acetate claim 1 , vinyl butyrate claim 1 , isopropyl butyrate claim 1 , phenyl butyrate (e.g. 3-fluoro-phenyl butyrate or 4-fluorophenyl butyrate) claim 1 , o-cresol 2-methoxy acetate or 2 claim 1 ,2 claim 1 ,2-trifluoroethyl butyrate.6. A process as claimed in claim 5 , wherein the acyl donor is 2 ...

IMAGING TUMOR GLYCOLYSIS BY NON-INVASIVE MEASUREMENT OF PYRUVATE KINASE M2

The present disclosure provides a positron emission tomography (PET)-detectable 1-((2-fluoro-6-[F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([F]DASA-23) probe that can selectively bind to the pyruvate kinase variant M2 (PKM2) found in cancer cells, such as of human glioma. Given the importance of PKM2 in the regulation of tumor metabolism, there is an on-going need to non-invasively measure its expression through the development of PKM2-specific radiopharmaceuticals. Precursors useful for the synthesis of the radiolabeled [F]DASA-23-PKM2-specific probe and related compounds, and their methods of synthesis, are provided. Since the half-life of the F isotope is approximately 110 min, it is advantageous for a practitioner to attach the radionuclide to the precursor shortly before administration. Therefore, a precursor compound suitable for receiving the radionuclide and capable of specifically binding to the PKM2 variant can be provided. 2. The pyruvate kinase M2 activator precursor of claim 1 , wherein Ris an alkoxyphenyl or an aminophenyl.3. The pyruvate kinase M2 activator precursor of claim 1 , wherein Ris 4-methoxyphenyl claim 1 , 4-ethoxyphenyl claim 1 , 4-propoxyphenyl claim 1 , or 4-aminophenyl.5. The pyruvate kinase M2 activator precursor of claim 4 , wherein Ris 4-methoxyphenyl.7. The Positron Emission Tomography (PET)-detectable probe of claim 6 , wherein Ris an alkoxyphenyl or an aminophenyl.8. The Positron Emission Tomography (PET)-detectable probe of claim 7 , wherein Ris 4-methoxyphenyl claim 7 , 4-ethoxyphenyl claim 7 , 4-propoxyphenyl claim 7 , or 4-aminophenyl.12. The pharmaceutically acceptable probe composition of claim 10 , further comprising a pharmaceutically acceptable carrier.14. The method of claim 13 , wherein step (d) comprises reacting the TFA salt of 1-((4-methoxyphenyl)sulfonyl)piperazine (9) product of step (c) with 2-fluoro-6-nitrobenzenesulfonyl chloride to generate 1-((2-fluoro-6-nitrophenyl)sulfonyl)-4-((4- ...

SUBSTITUTED ORGANOFLUOROBORATES AS IMAGING AGENTS

Fluoridated organofluoroborates comprising at least one F atom and precursors thereto, for use in PET scanning.

METHOD FOR PRODUCING RING-OPENING METATHESIS POLYMER HYDRIDE, AND RESIN COMPOSITION

A method for producing a hydrogenated ring-opening metathesis polymer includes subjecting a cyclic olefin to ring-opening metathesis polymerization in the presence of a polymerization catalyst to produce a ring-opening metathesis polymer, and hydrogenating at least some of carbon-carbon double bonds of the ring-opening metathesis polymer, at least one ruthenium compound selected from a group made of a ruthenium compound represented by a formula (I), (II), (III), and (IV) being used as the polymerization catalyst; and a resin composition having a hydrogenated ring-opening metathesis polymer produced by this method. It is possible to industrially advantageously produce a hydrogenated ring-opening metathesis polymer that exhibits especially excellent light transmittance. 2. The method according to claim 1 , wherein at least 98% of the carbon-carbon double bonds of the ring-opening metathesis polymer are hydrogenated.10. The method according to claim 1 , wherein the ruthenium compound represented by the formula (III) is a compound represented by the formula (III) wherein Yis an oxygen atom.14. A resin composition comprising a hydrogenated ring-opening metathesis polymer produced by the method according to . The invention relates to a method for producing a hydrogenated ring-opening metathesis polymer that is useful as a material for forming a pixel separation film and a planarization film of an organic electroluminescence (EL) device, a gate insulating film and a protective film of a thin film transistor (TFT), and the like, and a resin composition that includes the hydrogenated ring-opening metathesis polymer.A cyclic olefin ring-opening metathesis polymerization method that utilizes a transition metal compound as a catalyst has been well known in the art. W and Mo that belong to Group 6 in the periodic table, Nb, Ta, Re, Zr, Ti, Ru, Os, Ir, and the like have been known as the center metal of the metathesis catalyst. In particular, since a catalyst system that includes ...

Radiolabeled monoacylglycerol lipase occupancy probe

Provided herein are monoacylglycerol lipase (MGLL) occupancy probes comprising a MGLL inhibitor containing a positron emission tomography (PET) tracer radionuclide. Also provided are methods of assessing MGLL enzyme occupancy of a MGLL inhibitor using the radiolabeled occupancy probes described herein.

Solid phase conditioning

The present invention relates to a method for conditioning reversed phase SPE cartridges that provides certain advantages compared with known such methods. The method of the invention finds particular use in the automated synthesis of radiolabeled compounds where SPE is used for example in the purification steps.

Novel phosphatidylalkanols and compositions thereof

The present invention discloses a composition comprising a compound of formula I and a deuterated solvent. The deuterated solvent is miscible with water in any proportion at a temperature of 20 to 25° C. and comprises less than 5% residual 1 H-isotopes. The concentration of the compound of formula I may advantageously be determined by 1 H-QNMR. Methods of production of the composition and salts of compounds of formula I, as well as related analogs and novel reagents and intermediates for the production thereof, are also described.

MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON

Site-selective conjugation to biomolecules via thiol-based chemistry is superior to the unselective modification of lysine residues, which produce a mixed product and can potentially interfere with binding affinity of the biomolecule. However, in physiological environments, the maleimide-thiol conjugation product which is the current gold-standard for site-selective thiol-conjugation can be susceptible to hydrolysis or a retro-Michael reaction via exchange with reactive thiols such as those in albumin or glutathione residues yet the degradation is relatively slow. Therefore, for in vivo studies, the maleimide-thiol conjugation proposes instability issues. The compositions and methods disclosed herein provide an alternative thiol-based linkage, one that overcomes the instability issues with conventional reagents and methods. The compositions and methods disclosed herein are useful in various contexts, for example, for F-labeling of peptides/proteins in the preparation of positron emission tomography (PET) probes. 3. The composition of or , wherein:the compound is in a powdered form;the compound comprises at least 90% of the composition; and/orthe composition is disposed within a container of a kit.4. The composition of claim 1 , further comprising an organic solvent.5. The composition of claim 1 , further comprising a [F]fluoride molecule.8. The composition of or claim 1 , further comprising a biomolecule having a —SH moiety.9. The composition of claim 8 , wherein the biomolecule comprises a peptide claim 8 , a protein claim 8 , antibody or a sugar.10. A method of making a F labelled vinyl sulfone comprising:{'sup': '18', 'claim-ref': [{'@idref': 'CLM-00001', '#text': 'claim 1'}, {'@idref': 'CLM-00002', '#text': 'claim 2'}], '#text': 'combining a [F]fluoride radionuclide with at least one compound of or ;'}{'sup': '18', '#text': 'performing a fluorination reaction so that a F labelled vinyl sulfone is made.'}11. A method of coupling a F moiety to a biomolecule to ...

SOLID PHASE PEPTIDE SYNTHESIS PROCESSES AND ASSOCIATED SYSTEMS

Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis. 111-. (canceled)12. A process for adding amino acid residues to peptides , comprising:providing a plurality of peptides comprising protection groups, each peptide immobilized on a solid support;performing a first amino acid addition cycle comprising exposing amino acids to the immobilized peptides such that an amino acid residue is added to at least about 99% of the immobilized peptides; andperforming a second amino acid addition cycle comprising exposing amino acids to the immobilized peptides such that an amino acid residue is added to at least about 99% of the immobilized peptides; the total amount of time between the ends of the first and second amino acid addition cycles is about 10 minutes or less and the protection groups comprise fluorenylmethyloxycarbonyl protection groups and/or', 'the total amount of time between the ends of the first and second amino acid addition cycles is about 5 minutes or less., 'wherein1329-. (canceled)30. A process for adding amino acid residues to peptides , comprising:providing a plurality of peptides immobilized on a solid support; andexposing activated amino acids to the immobilized peptides such that at least a portion of the activated amino acids are bonded to the immobilized peptides to form newly-bonded amino acid residues;wherein an amino acid residue is added to at least about 99% of the immobilized peptides within about 1 minute or less.3159-. ...

RADIOLABELING AND FORMULATION FOR SCALE UP OF 64Cu-DOTATATE

The present disclosure relates to methods to create a robust procedure capable of supplying commercial quantities of a radioactive diagnostic agent indicated for use with positron emission tomography (PET) for localization of somatostatin receptor positive neuroendocrine tumors (NETs) in adult patients.

SOLID PHASE PEPTIDE SYNTHESIS PROCESSES AND ASSOCIATED SYSTEMS

Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis. 1. A process for adding amino acid residues to peptides , comprising:providing a plurality of peptides comprising protection groups, each peptide immobilized on a solid support;exposing a deprotection reagent to the immobilized peptides to remove the protection groups from at least a portion of the immobilized peptides;removing at least a portion of the deprotection reagent;exposing activated amino acids to the immobilized peptides such that at least a portion of the activated amino acids are bonded to the immobilized peptides to form newly-bonded amino acid residues; andremoving at least a portion of activated amino acids that do not bond to the immobilized peptides;wherein an amino acid residue is added to at least about 99% of the immobilized peptides during the amino acids exposing step; and the total amount of time taken to perform the combination of all of the deprotection reagent exposing step, the deprotection reagent removal step, the activated amino acid exposing step, and the activated amino acid removal step is about 10 minutes or less and the protection groups comprise fluorenylmethyloxycarbonyl protection groups and/or', 'the total amount of time taken to perform the combination of all of the deprotection reagent exposing step, the deprotection reagent removal step, the activated amino acid exposing step, and the activated amino acid removal step is about 5 minutes or less., ...

ANALOGS OF FEXARAMINE AND METHODS OF MAKING AND USING

Novel compounds having a formula 3. The compound of claim 1 , wherein Ris deuterium.4. The compound of claim 2 , wherein Ror Ror both are halogen.5. The compound of claim 4 , wherein Ror Ror both are F.8. The compound of claim 1 , wherein RC comprises a nitrogen-containing heteroaryl ring.9. The compound of claim 8 , wherein RC is selected from pyridine claim 8 , pyrazole claim 8 , pyrrole claim 8 , imidazole claim 8 , oxazole claim 8 , isoxazole claim 8 , thiazole claim 8 , isothiazole claim 8 , triazole claim 8 , pyrimidine claim 8 , pyrazine claim 8 , triazine claim 8 , benzopyrazole claim 8 , benzimidazole claim 8 , indole claim 8 , quinoline claim 8 , indazole claim 8 , purine claim 8 , quinoxaline claim 8 , or acridine.11. The compound of claim 10 , wherein Z is N; R claim 10 , R claim 10 , Rand Rare all H; Ris methyl; or a combination thereof.13. The compound of claim 12 , wherein Rand Rare both methyl.17. A compound claim 12 , selected frommethyl (E)-3-(3-(N-(4-(1-methyl-1H-indazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;methyl (E)-3-(3-((1R,2S,4S)—N-(4-(1-methyl-1H-indazol-5-yl)benzyl)bicyclo[2.2.1]heptane-2-carboxamido)phenyl)acrylate;methyl (E)-3-(3-(1-methyl-N-(4-(1-methyl-1H-indazol-5-yl)benzyl)piperidine-4-carboxamido)phenyl)acrylate;methyl (E)-3-(5-(N-((1-methyl-1H-benzo[f]indazol-8-yl)methyl)cyclohexanecarboxamido)pyridin-3-yl)acrylate;methyl (E)-3-(3-fluoro-5-((1S,2R,4R)—N-((1-methyl-1H-benzo[1]indazol-8-yl)methyl)bicyclo[2.2.1]heptane-2-carboxamido)phenyl)acrylate;methyl (E)-3-(3-(N-((9-fluoro-1-methyl-1H-benzo[f]indazol-8-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;methyl (E)-3-(3-((1R,4S)—N-((9-fluoro-1-methyl-1H-benzo[f]indazol-8-yl)methyl)bicyclo[2.2.1]heptane-2-carboxamido)phenyl)acrylate;methyl (E)-3-(3-(N-((9-fluoro-1-methyl-1H-benzo[f]indazol-8-yl)methyl)-1-methylpiperidine-4-carboxamido)phenyl)acrylate;methyl (E)-3-(5-(N-((9-fluoro-1-methyl-1H-benzo[f]indazol-8-yl)methyl)cyclohexanecarboxamido)pyridin-3-yl)acrylate;methyl ( ...

ENANTIOPURE TERPHENYLS WITH TWO ORTHO-ATROPISOMERIC AXES

Enantiopure terphenyl presenting two ortho-located chiral axes having the following structural formula (I): their process of synthesis and their use as mono or bidentate ligands for asymmetric organometallic reactions, as organocatalysts, as chiral base and as generator, with metal, of isolable chiral metallic complexes for applications in asymmetric catalysis and others. 2. The enantiopure terphenyl according to claim 1 , wherein{'sub': '1', 'claim-text': an halogen atom,', 'a substituted or unsubstituted branched or straight alkyl group or', 'a substituted or unsubstituted branched or straight alkoxy group or', {'sub': '3', 'a CFgroup,'}], 'Rrepresents'}{'sub': '2', 'claim-text': a hydrogen atom or', 'a substituted or unsubstituted branched or straight alkyl group, or', 'a substituted or unsubstituted branched or straight alkoxy group, 'Rrepresents'}{'sub': '3', 'claim-text': a substituted or unsubstituted branched or straight alkyl group or', 'a substituted or unsubstituted branched or straight alkoxy group,, 'Rrepresents'}{'sub': '4', 'claim-text': a hydrogen atom or', 'a halogen atom or', 'a substituted or unsubstituted branched or straight alkoxy group, or', 'a substituted or unsubstituted branched or straight alkyl group or', 'a aryl group or', {'sub': 2', '2', 'n+2, 'a CHF group, or a CHFgroup or —CnFgroup avec n=1 à 10, or'}], 'Rrepresents'}{'sub': '5', 'claim-text': [{'sub': a', 'a', '1', '4, 'a SORgroup with Rselected from a substituted or unsubstituted branched or straight-(C-C) alkyl group or a substituted or unsubstituted aryl group, or'}, 'a OH group, or', {'sub': a', 'd', 'a', 'd', 'a', 'd, '—PRnor a —P(O)Rnwith Rand Rindependently selected from a substituted or unsubstituted branched or straight alkyl group or a substituted or unsubstituted aryl group,'}], 'Rrepresents'}{'sub': '6', 'claim-text': a hydrogen atom,', 'a halogen atom or', {'sub': 1', '4, 'a substituted or unsubstituted branched or straight-(C-C) alkyl group or'}, {'sub': 1', '4, 'a ...

Hydrogenated Rubber with Improved Performance in TPE Compositions

New hydrogenated styrenic block copolymers, in particular styrene-ethylene/butylene-styrene copolymers (SEBS copolymers), with improved performance in thermoplastic elastomer compositions (TPE compositions), process for preparing said hydrogenated styrenic block copolymers, reprocessable TPE-S compositions made thereof, method for producing an article from said reprocessable TPE-S compositions and articles made of said reprocessable TPE-S compositions, in particular suitable for medical applications. 1. A hydrogenated styrenic block copolymer , wherein the copolymer is radial , has a molecular weight , expressed as Mpeak , between 300 ,000 and 475 ,000 g/mol , a vinyl content of between 60% and 69% , has a styrene content of 25% to 40% , a viscosity , expressed as Brookfield viscosity at 5% by weight in toluene , of less than 40 cps , and has a general formula [A-B]X , wherein A is a block based on aromatic vinyl monomers which are a styrene derivative having 8 to 20 carbon atoms , B is a block based on conjugated diene monomers having 4 to 10 carbon atoms , n>2 and X is a coupling agent residue , wherein the coupling agent is silicon tetrachloride SiCl.2. The hydrogenated styrenic block copolymer according to claim 1 , wherein it has a molecular weight claim 1 , expressed as Mpeak claim 1 , of between 400 claim 1 ,000 to 450 claim 1 ,000.3. (canceled)4. The hydrogenated styrenic block copolymer according to claim 1 , wherein it has a viscosity claim 1 , expressed as Brookfield viscosity at 5% by weight in toluene claim 1 , of 34 cps or less.5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. A TPE-S composition claim 1 , wherein it comprises:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) at least one hydrogenated styrenic block copolymer as defined in ;'}b) at least a thermoplastic resin; andc) at least a plasticizer agent.10. The TPE-S composition according to claim 9 , wherein the plasticizer/hydrogenated styrenic block copolymer weight ratio is equal ...

PROCESS FOR PRODUCING HYDROGENATED PETROLEUM RESIN

A near-infrared absorption spectrum of a hydrogenated compound (hydrogenated petroleum resin) in a form of a molten resin from which a hydrogenation solvent is separated in a hydrogenation solvent removing step is measured to calculate an aromatic content ratio and a softening point as physical property values of the hydrogenated compound based on analytical curve data. At least one of a temperature, pressure, reaction time and hydrogen content in a hydrogenating portion is controlled such that a difference between the aromatic content ratio and the bromine number measured in the near-infrared spectrometry and an aromatic content ratio and bromine number of a target hydrogenated petroleum resin pellet becomes small. At least one of a temperature and pressure in a thin-film evaporator is controlled such that a difference between a softening point measured in the near-infrared spectrometry and a softening point of the target hydrogenated petroleum resin pellet becomes small. 1. A method for producing a hydrogenated petroleum resin , comprising:measuring a near-infrared absorption spectrum of a molten resin from which a hydrogenation solvent is separated; andcontrolling a process for producing hydrogenated petroleum resin pellets based on a result of the measurement.2. The method of claim 1 , whereinin controlling the process for producing the hydrogenated petroleum resin pellets, the result of the measurement indicates a physical property value of at least one of an aromatic content ratio and a bromine number of the molten resin, andat least one of a temperature, a pressure, a reaction time and a hydrogen content of a hydrogenation reaction is controlled such that a difference between the physical property value of the molten resin and a physical property value of a target hydrogenated petroleum resin pellet becomes small.3. The method of claim 1 , whereinin controlling the process for producing the hydrogenated petroleum resin pellets, the result of the measurement ...

DEVICE FOR THE SYNTHESIS OF A RADIOTRACER, FACILITY COMPRISING SUCH A DEVICE, AND METHOD FOR PRODUCING A RADIOTRACER BY MEANS OF SUCH A DEVICE

Disclosed is a device for the synthesis of a radiotracer, including a universal confined enclosure designed for the insertion of a specific synthesis cassette of the radiotracer and the removal of same. The synthesis cassette includes a synthesis module designed to receive reagents and a radioisotope for the synthesis of the radiotracer. An inner connector plate includes at least one inlet, designed to be connected to a radioisotope admission and also to the inlet of the cassette, and an outlet, designed to be connected to a syringe to be filled with the radiotracer and also to the outlet of the cassette. Such a synthesis device can be installed in a facility including, in a confined room, as well as such devices normally arranged in a storage area, a synthesis station, a radioisotope admission, at least one window for communication to the outside, and a manipulator robot. 11. A device () for synthesizing a radioactive tracer from a radioisotope comprising:{'b': 10', '17', '13', '30, 'A universal confined chamber () comprising an internal connector plate () and in which is provided an access door () configured for insertion therein of a cassette () for specific synthesis of the radioactive tracer and for its removal therefrom,'}{'b': 30', '30, 'The cassette () for synthesis of the radioactive tracer, which comprises reagents and a synthesis module, the synthesis module comprising a reaction cell and being configured to receive the reagents and the radioisotope for synthesizing the radioactive tracer, the synthesis module being fluidically connected to an entry of the cassette that is configured for conveying the radioisotope into the reaction cell and an exit from the cassette configured for delivering the radioactive tracer out of the cassette (),'}{'b': '17', 'The internal connector plate (), comprising at least one entry, configured to connect the entry of the cassette to an ingress of the radioisotope, and an exit, configured to be connected to the exit of the ...

Labelled Quinoxaline Derivatives as Multimodal Radiopharmaceuticals and Their Precursors

The present invention relates to the compound of formula (I), in which R1 represents Sn(R), B(OH), B(OR), a halogen atom, NO, a radionuclide or a —N(R)group, where R is a (C-C) alkyl group, R2 represents a hydrogen atom or a (C-C)alkyl group, R3 represents: a —(CHCHO)—(CH)—X group, or a —(CHCHO)—(CH)—Y group with Y representing a —C═C—H, a —Nor a —Ar—(CH)—(OCHCH)—X group, and X represents a halogen atom, a radionuclide or a —OSOR′ group, where R′ is a CF, CH, t-Bu, Ph, p-NOPh, p-BrPh or p-CHPh group, and their addition salts with pharmaceutically acceptable acids, The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT or PET imaging and in therapy of melanoma, via targeted radionuclide therapy. 2. Compound of formula (I) according to claim 1 , wherein R2 is an ethyl group.3. Compound of formula (I) according to claim 1 , wherein nis 2.4. Compound of formula (I) according to claim 1 , wherein R1 is a iodine atom claim 1 , a radionuclide or Sn(R) claim 1 , where R is a (C-C) alkyl group claim 1 , and more particularly R1 is a iodine atom.7. Compound of formula (Ia) according to claim 6 , wherein nvaries between 3 and 7 and nis 2.8. Compound of formula (Ia) according to claim 6 , wherein R1 represents a iodine atom claim 6 , a radionuclide or Sn(R) claim 6 , where R is a (C-C)alkyl group claim 6 , and more particularly R1 represents a iodine atom or an optionally labelled iodine atom claim 6 , and X represents an optionally labelled fluorine atom or a —OSOR′ group claim 6 , where R′ is a CF claim 6 , a t-Bu or a CHgroup claim 6 , and more particularly a CHgroup.12. A radiolabelled compound according to claim 1 , wherein said radiolabelling occurs by means of a radionuclide which is a radioisotope chosen from iodine-123 claim 1 , iodine-124 claim 1 , iodine-125 claim 1 , iodine-131 claim 1 , bromine-75 claim 1 , bromine-76 claim 1 , bromine-77 claim 1 , fluorine-18 claim 1 , astatine-210 ...

DYNAMICALLY CROSSLINKED THERMOPLASTIC MATERIAL PROCESS

A method for making a thermoplastic material includes: (a) introducing into an extruder an elastomer composition including an ethylenically unsaturated elastomer polymer, a first free radical initiator, and a second free radical initiator; (b) in a first zone of the extruder, heating and partially crosslinking the elastomer composition at a first crosslinking temperature to form a thermoplastic, partially crosslinked elastomer composition; (c) introducing into the extruder in a second zone downstream of the first zone a thermoplastic polymer composition; (d) mixing and heating the thermoplastic polymer composition and the thermoplastic, partially crosslinked elastomer composition to a second crosslinking temperature higher than the first crosslinking temperature, wherein the thermoplastic polymer composition is liquid at the second crosslinking temperature; and (e) mixing and further crosslinking the elastomer composition to form a thermoplastic material having a dispersed phase of the crosslinked elastomer composition in the thermoplastic polymer composition. 1. A method for making a thermoplastic material , comprising:(a) introducing into an extruder an elastomer composition comprising an ethylenically unsaturated elastomer polymer and at least a first free radical initiator and a second free radical initiator;(b) in a first zone of the extruder, heating and partially crosslinking the elastomer composition at a first crosslinking temperature to form a thermoplastic, partially crosslinked elastomer composition;(c) introducing into the extruder in a second zone downstream of the first zone a thermoplastic polymer composition;(d) mixing and heating the thermoplastic polymer composition and the thermoplastic, partially crosslinked elastomer composition to a second crosslinking temperature higher than the first crosslinking temperature, wherein the thermoplastic polymer composition is liquid at the second crosslinking temperature; and(e) mixing and further crosslinking ...

PATTERN-FORMING METHOD AND COMPOSITION

A pattern-forming method includes applying a first composition on a surface layer of a substrate to form a first coating film. The surface layer includes a first region which includes a metal atom, and a second region which includes a silicon atom. The first coating film is heated. A portion other than a portion formed on the first region or a portion other than a portion formed on the second region of the first coating film heated is removed, thereby forming a first lamination portion. A second composition is applied on the substrate on which the first lamination portion is formed to form a second coating film. The second coating film is heated or exposed. A portion other than a portion formed on the first lamination portion of the second coating film heated or exposed is removed, thereby forming a second lamination portion. 1. A pattern-forming method comprising:applying a first composition on a surface layer of a substrate to form a first coating film, the surface layer comprising a first region which comprises a metal atom, and a second region which comprises a silicon atom;heating the first coating film;removing a portion other than a portion formed on the first region or a portion other than a portion formed on the second region of the first coating film heated, thereby forming a first lamination portion;applying a second composition on the substrate on which the first lamination portion is formed to form a second coating film;heating or exposing the second coating film; andremoving a portion other than a portion formed on the first lamination portion of the second coating film heated or exposed, thereby forming a second lamination portion,wherein the first composition comprises: a first polymer; and a solvent, the first polymer comprising: a first structural unit which comprises an acid-labile group; and a functional group which selectively bonds to a metal atom or an Si—OH bond, andthe second composition comprises: a second polymer comprising the first ...

APPARATUS AND METHOD FOR SYNTHESIZING F-18 LABELED RADIOACTIVE PHARMACEUTICALS

The present invention relates to an apparatus for synthesizing F-18 labeled radioactive pharmaceutical. The apparatus for synthesizing F-18 labeled radioactive pharmaceutical includes an F-18 radioactive isotope supplier, a reagent supplier, a polymer precursor cartridge, a first heating unit, a polymer compound cartridge, a synthesizing container, a second heating unit, a water liquid container, a transmitting gas supplier, a cleansing liquid supplier, a connection tube, a plurality of control valves, and a controller. 1. An apparatus for synthesizing F-18 labeled radioactive pharmaceutical comprising:an F-18 radioactive isotope supplier which supplies F-18 radioactive isotope;a reagent supplier which supplies reagent reacting with the F-18 radioactive isotope;a polymer precursor cartridge which is filled with polymer precursor and collects the F-18 radioactive isotope and causes a labeling reaction;a first heating unit which selectively heats the polymer precursor cartridge;a polymer compound cartridge which is filled with polymer compound and separates polar compound and nonpolar compound from each other;a synthesizing container which causes hydrolysis reaction of produced intermediate compound;a second heating unit which selectively heats the synthesizing container;a waste liquid container which contains fluid which is discarded after having been used for synthesis;a collecting container which collects a final synthesized product;a transmitting gas supplier which supplies transmitting gas;a cleansing liquid supplier which supplies a cleansing liquid;a connection tube which connects the F-18 radioactive isotope supplier, the reagent supplier, the polymer precursor cartridge, the polymer compound cartridge, the synthesizing container, the waste liquid container, the collection container, the transmitting gas supplier, and the cleansing liquid supplier together;a plurality of control valves which are disposed at predetermined positions of the connection tube to ...

Novel Chiral Alfa-Amino Tertiary Boronic Esters

The present disclosure relates to a novel, highly efficient and enantiospecific borylation method to synthesize a wide range of enantiopure alfa-amino tertiary boronic esters, and novel alfa-amino tertiary boronic acids and esters prepared by the method. More specifically, highly enantiospecific borylation of configurationally stable α-N-Boc substituted tertiary organolithium species and HBpin has been developed to synthesize various alfa-amino tertiary boronic esters through the formation of a new C—B bond with excellent enantiopurities. 2. The method of claim 1 , wherein R claim 1 , Rand Rare each individually different straight or branched optionally substituted C-Calkyl group claim 1 , optionally substituted C-Ccycloalkyl group claim 1 , optionally substituted C-Ccycloalkenyl group claim 1 , straight or branched optionally substituted C-Calkenyl group claim 1 , straight or branched optionally substituted C-Calkynyl group claim 1 , optionally substituted C-Caryl claim 1 , optionally substituted C-Cheteroaryl with one or more O claim 1 , N claim 1 , or S claim 1 , wherein Rand R claim 1 , Rand R claim 1 , or Rand Rmay jointly form an optionally substituted C-Csaturated or non-saturated ring claim 1 , or form an optionally substituted C-Csaturated or non-saturated heterocyclic ring.3. The method of claim 1 , wherein B(OR)(OR)Ris B(OMe) claim 1 , catecholborane claim 1 , or 4 claim 1 ,4 claim 1 ,5 claim 1 ,5-tetramethyl-1 claim 1 ,3 claim 1 ,2-dioxaborolane (HBpin) claim 1 , 2-methoxy-4 claim 1 ,4 claim 1 ,5 claim 1 ,5-tetramethyl-1 claim 1 ,3 claim 1 ,2-dioxaborolane (MeO-Bpin).4. The method of claim 1 , wherein the NPG is a nitrogen protecting group that has a carbonyl (C═O) group claim 1 , a sulfinyl group ((S═O) claim 1 , or a sulfonyl (—SO)— group directly attached to the nitrogen to be protected.5. The method of claim 1 , wherein the NPG is tert-butyloxycarbonyl (Boc) or CON(Pr).6. The method of claim 1 , wherein LiRis lithium diisopropylamide (LDA) claim 1 , ...

HYDROPHILIC COATING METHOD FOR CONTACT LENS SURFACE

The present invention provides a hydrophilic coating method for contact lens surface, firstly performing a hydration procedure S to form a hydrated polymer from a non-hydrated polymer, then sequentially contacting the hydrated polymer with a first solution and a second solution containing a high molecular compound at a specific temperature between 50° C. and 70° C. to complete a first hydration process S and a second hydration process S A contact lens obtained according to the above procedures has a contact angle ranging from about 30° to 65°, and proteins and lipids are not easily deposited on a surface of the contact lens thereby providing the user with good comfort when wearing. 1. A hydrophilic coating method for contact lens surface , comprising following steps of:{'b': '1', 'performing a hydration procedure S to form a hydrated polymer from a non-hydrated polymer;'}{'b': '2', 'performing a first hydration process S for contacting the hydrated polymer with a first solution at a first temperature for a first treatment time, the first solution comprising at least one composition selected from a group consisting of polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyethylene glycol (PEG) and the combination thereof; and'}{'b': '3', 'performing a second hydration process S for contacting the hydrated polymer with a second solution at a second temperature for a second treatment time, the second solution comprising at least one composition selected from a group consisting of polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycols and the combination thereof;'}wherein the first temperature and the second temperature are between 50° C. and 70° C. independently.2. The hydrophilic coating method for contact lens surface of claim 1 , wherein the first temperature and the second temperature are between 55° C. and 65° C. independently.3. The hydrophilic coating method for contact lens surface of claim 1 , wherein each of the first solution and the second solution ...

Resin composition and use of same

The present invention is a laminated glass [H] which uses, as an intermediate film, a sheet [G] that is formed from a resin composition [F] that is prepared by blending a total amount of 0.001 to 2.0 parts by weight of a metal oxide particulate and/or a near infrared-absorbing pigment having a function of shielding infrared ray, into 100 parts by weight of a specific hydrogenated block copolymer [D] and/or a modified hydrogenated block copolymer [E]. The present invention provides a laminated glass which has excellent infrared shielding function, moisture resistance and heat resistance.

Deuterated cftr potentiators

This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.

MEDICAL INSTRUMENT, FLUORINE-CONTAINING CYCLIC OLEFIN POLYMER, FLUORINE-CONTAINING CYCLIC OLEFIN POLYMER COMPOSITION, AND CELL CULTURE METHOD

Medical instrument including a substrate using a fluorine-containing cyclic olefin polymer containing a structural unit represented by General Formula (1), in which the substrate has one surface where the substrate comes into contact with cells, and the substrate is provided with a convex-concave structure on the one surface, a ratio (L1/L2) of a width (L1) between convexities formed by the convex-concave structure and a maximum diameter (L2) of inoculated cells per cell in the cells is 1 to 300, and the cells do not adhere to or attach to the one surface provided with the convex-concave structure and the medical instrument promotes cell proliferation. 2. The medical instrument according to claim 1 ,wherein the L1/L2 is 1 to 100.3. The medical instrument according to claim 1 ,wherein a width between convexities of the convex-concave structure is 10 μm to 1,000 μm.4. The medical instrument according to claim 1 ,wherein the one surface has a water contact angle of 70° to 160°.5. The medical instrument according to claim 1 ,wherein the one surface is formed by a fluorine-containing cyclic olefin polymer composition including the fluorine-containing cyclic olefin polymer, a photocurable compound, and a photo-curing initiator.6. The medical instrument according to claim 5 ,wherein a mass ratio (fluorine-containing cyclic olefin polymer/photocurable compound) of the fluorine-containing cyclic olefin polymer and the photocurable compound in the fluorine-containing cyclic olefin polymer composition is from 99.9/0.1 to 50/50.7. The medical instrument according to claim 1 , which is used for culturing cells in contact with the one surface.8. The medical instrument according to claim 7 ,wherein the cultured cells from the cells float and proliferate while forming a group of growing cells selected from cell sheets, spheroids, or colonies.9. The medical instrument according to claim 7 ,wherein a group of growing cells is liberated by a buffer solution and detached from the one ...

ANALOGS OF FEXARAMINE AND METHODS OF MAKING AND USING

Novel compounds having a formula 1. A method of treating atherosclerosis in a subject , the method comprising administering to the subject an effective amount of an intestinally-selective , non-bile acid FXR agonist.3. The method of claim 2 , wherein Land Ltogether form a pi-bond.4. The method of claim 2 , wherein Ris deuterium.5. The method of claim 3 , wherein Ror Ror both are halogen.6. The method of claim 5 , wherein Ror Ror both are F.9. The method of claim 2 , wherein Rcomprises a nitrogen-containing heteroaryl ring.10. The method of claim 9 , wherein Ris selected from pyridine claim 9 , pyrazole claim 9 , pyrrole claim 9 , imidazole claim 9 , oxazole claim 9 , isoxazole claim 9 , thiazole claim 9 , isothiazole claim 9 , triazole claim 9 , pyrimidine claim 9 , pyrazine claim 9 , triazine claim 9 , benzopyrazole claim 9 , benzimidazole claim 9 , indole claim 9 , quinoline claim 9 , indazole claim 9 , purine claim 9 , quinoxaline claim 9 , or acridine.12. The method of claim 11 , wherein Z is N; R claim 11 , R claim 11 , Rand Rare all H; Ris methyl; or a combination thereof.14. The method of claim 13 , wherein Rand Rare both methyl.17. The method of claim 1 , wherein administering the FXR agonist comprises administering the FXR agonist to a gastrointestinal tract of the subject.18. The method of claim 1 , wherein the FXR agonist is administered orally.19. The method of claim 1 , wherein the FXR agonist is selected frommethyl (E)-3-(3-(N-(4-(1-methyl-1H-indazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl) acrylate;methyl (E)-3-(3-((1R,2S,4S)—N-(4-(1-methyl-1H-indazol-5-yl)benzyl)bicyclo[2.2.1]heptane-2-carboxamido)phenyl)acrylate;methyl (E)-3-(3-(1-methyl-N-(4-(1-methyl-1H-indazol-5-yl)benzyl)piperidine-4-carboxamido)phenyl)acrylate;methyl (E)-3-(5-(N-((1-methyl-1H-benzo[f]indazol-8-yl)methyl)cyclohexanecarboxamido)pyridin-3-yl) acrylate;methyl (E)-3-(3-fluoro-5-((1S,2R,4R)—N-((1-methyl-1H-benzo[f]indazol-8-yl)methyl)bicyclo[2.2.1]heptane-2-carboxamido)phenyl) ...

METALLACYCLOPENTADIENE INITIATORS FOR CYCLIC POLYMER SYNTHESIS FROM ALKYNES

Provided herein are complexes for polymerization of linear alkynes to cyclic poly(alkynes), and methods of making and using same. For example, provided herein are compounds of formula (I) or formula (IV):

Coated superabsorbent polymer particles and processes therefore

Superabsorbent material, comprising first superabsorbent polymers, coated with second clay-crosslinked superabsorbent polymers, said second clay-crosslinked superabsorbent polymers being obtainable by the step of polymerization of a solution/dispersion of polymerizable compounds and clay particles, to obtain said second superabsorbent polymers, crosslinked by said clay particles, of a weight average largest particle dimension of less than 800 nm.

METHOD FOR PREPARING DEUTERATED IMIDAZOLE DIKETONE COMPOUND

A method for preparation of deuterated imidazole diketone compounds includes the following steps: (1) using compound of formula (I) and compounds of formula (II) as starting material, compounds of formula (III) can be obtained by a substitution reaction; (2) Compounds of formula (IV) can be prepared by esterification of carboxyl in compounds of formula (III); (3) Cyclization of compounds of formula (IV) and compound of formula (V) provides compounds of formula (VI); (4) Compounds of formula (VI) are deesterificated and react to produce compounds of formula (VII); (5) using compounds of formula (VII) and compounds of formula (VIII) as starting material, the deuterated imidazole diketone compounds of formula (IX) are obtained by the condensation reaction of amide. 2. The method according to claim 1 , characterized in that Rand Rare both methyl.3. The method according to claim 1 , characterized in that R claim 1 , Rand Rare all deuterium.4. The method according to claim 1 , characterized in that R is methyl.5. The method according to claim 1 , characterized in that in step (1) claim 1 , the reaction temperature is 40-120° C.6. The method according to claim 1 , characterized in that in step (2) claim 1 , the reaction temperature is −10-60° C.7. The method according to claim 1 , characterized in that in step (3) claim 1 , the reaction temperature is 40-90° C.8. The method according to claim 1 , characterized in that in step (4) claim 1 , the reaction temperature is −10-70° C.9. The method according to claim 1 , characterized in that in step (5) claim 1 , the reaction temperature is −10-40° C.10. The method according to claim 1 , characterized in that in the cyclization of step (3) claim 1 , solvents are dimethyl sulfoxide or the mixture of dimethyl sulfoxide and isopropyl acetate claim 1 , in which the volume ratio of dimethyl sulfoxide and isopropyl acetate is 50:1-1:10.11. The method according to claim 10 , characterized in that the volume ratio of dimethyl sulfoxide ...

METHOD FOR PREPARING ANTHRAQUINONE-FUNCTIONALIZED POLY(VINYLIDENE FLUORIDE) MEMBRANE

This present disclosure relates to a method for preparation of polyvinylidene fluoride membrane with functional anthraquinones. The method is carried out according, to the following steps: step 1: preparing 2-(1-hydroxy-3-butene)-1,4,5,8-tetramethoxyl naphthalene; step 2: preparing polyvinylidene fluoride-aromatic ether copolymers: polyvinylidene fluoride was used as the initiator, 2-(1-hydroxy-3-butene) -1,4,5,8-tetramethoxynaphthalene was the monomer, N,N-dimethylformamide was solvent, cuprous chloride/Me6TREN was the catalytic, polyvinylidene fluoride-aromatic ether copolymer was synthesized by atomic transfer radical polymerization; step 3: reducing the polyvinylidene fluoride-aromatic ether copolymer to quinone by demethoxy oxidation; step 4: using the product of step 3 and N, N-dimethylformamide a film-forming reagents, then scraping into a membrane. Further, the anthraquinone which fixed in the polyvinylidene fluoride membrane would not fall off. 1. A method for preparation of polyvinylidene fluoride membrane with functional anthraquinones , the method comprising:step 1: preparing 2-(1-hydroxy-3-butene)-1,4,5,8-tetramethoxyl naphthalene;step 2: preparing polyvinylidene fluoride-aromatic ether copolymers: polyvinylidene fluoride was used as the initiator, 2-(1-hydroxy-3-butene) -1,4,5,8-tetramethoxynaphthalene was the monomer, N,N-dimethylformamide was solvent, cuprous chloride/Me6TREN was the catalytic, polyvinylidene fluoride-aromatic ether copolymer was synthesized by atomic transfer radical polymerization;step 3: reducing the polyvinylidene fluoride-aromatic ether copolymer to quinone by demethoxy oxidation;step 4: using the product of step 3 and N,N-dimethylformamide as film-forming reagents, then scraping into a membrane.2. The method of claim 1 , wherein the method of preparing 2-(1-hydroxy-3-butene) -1 claim 1 ,4 claim 1 ,5 claim 1 ,8-tetramethoxyl naphthalene from step 1 comprises steps of:step 1a). preparing 1,4,5,8-tetramethoxynaphthalene:adding ...