Sulfur Or Halogen Containing Patents (Class 536/122)
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Patent number: 11534469Abstract: Provided herein is a substance for use in a therapeutic method for stimulating cells in the human immune system, a method for producing this substance, and a method of use of the substance for stimulating cells of the human immune system in treating various diseases involving immune system disorders.Type: GrantFiled: August 25, 2020Date of Patent: December 27, 2022Assignee: Vita Motus AGInventors: Aleksandr Abramov, Alisa Petkevic, Vadim Pospelov
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Patent number: 10864225Abstract: A SGLT2 inhibitor or a pharmaceutically acceptable form thereof is provided for use in the treatment and/or prevention of a metabolic disorder of an equine animal. In particular, a SGLT2 inhibitor or a pharmaceutically acceptable form thereof is provided for use in the treatment and/or prevention of insulin resistance, hyperinsulinemia, impaired glucose tolerance, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, obesity, and/or regional adiposity in an equine animal.Type: GrantFiled: November 28, 2016Date of Patent: December 15, 2020Inventors: Dania Birte Reiche, Laura Johnston, Nicole Mohren
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Patent number: 10857247Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: GrantFiled: August 29, 2019Date of Patent: December 8, 2020Assignee: The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Patent number: 10842892Abstract: The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comprising a radioisotope (e.g., 18F). Various embodiments of the invention may be useful as sensors, diagnostic tools, and the like. In some cases, methods for evaluating perfusion, including myocardial perfusion, are provided. Synthetic methods of the invention have also been incorporated into an automated synthesis unit to prepare and purify imaging agents that comprise a radioisotope. In some embodiments, the present invention provides a novel methods and systems comprising imaging agent 1, including methods of imaging in a subject comprising administering a composition comprising imaging agent 1 to a subject by injection, infusion, or any other known method, and imaging the area of the subject wherein the event of interest is located.Type: GrantFiled: February 21, 2018Date of Patent: November 24, 2020Assignee: Lantheus Medical Imaging, Inc.Inventors: James F. Castner, Enrico Mongeau, Dianne D. Zdankiewicz, Robert W. Siegler, Richard R. Cesati
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Patent number: 10633396Abstract: The present invention claims UV detectable (?>210 nm) potassium [18F]fluoride diaryl- and aryl-fused [2.2.2]cryptate complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species.Type: GrantFiled: June 22, 2018Date of Patent: April 28, 2020Inventors: Yousry M. A. Naguib, Ashraf Naguib, Ahmed Naguib
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Patent number: 10308664Abstract: The present invention claims complexing [18F] fluoride anion with diaryl and aryl fused-[2.2.2]cryptand to form [18F] fluoride diaryl and aryl fused-cryptate complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species.Type: GrantFiled: August 19, 2012Date of Patent: June 4, 2019Inventors: Yousry M. A. Naguib, Ashraf Naguib, Ahmed Naguib
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Patent number: 10053474Abstract: The present invention features compounds effective in inhibiting active against Hepatitis C virus (“HCV”) polymerase. The invention also features processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: May 5, 2017Date of Patent: August 21, 2018Assignee: AbbVie Inc.Inventors: Jaclyn Chau, Hui-Ju J. Chen, David A. DeGoey, John Hartung, Nathan Ide, Vikram Kalthod, Allan C. Krueger, Yi-Yin Ku, Tongmei Li, John T. Randolph, Rolf Wagner, Geoff T. Halvorsen, Christopher C. Marvin, Eric Voight, Brian S. Brown, Steven R. Martinez, Anurupa Shrestha, Howard R. Heyman
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Patent number: 10052395Abstract: The present invention claims UV detectable (?>210 nm) potassium [18F]fluoride diaryl- and aryl-fused [2.2.2]cryptate complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species.Type: GrantFiled: May 30, 2017Date of Patent: August 21, 2018Inventors: Yousry Naguib, Ashraf Naguib, Ahmed Naguib
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Patent number: 9315799Abstract: The present invention provides a process for preparing an isotope-containing phosphate compound easily. The process for preparing an isotope-containing phosphate compound according to the present invention includes the step of: oxidizing a trivalent phosphorus compound with an oxidizing agent containing an isotope to synthesize a pentavalent phosphate compound to which the isotope has been introduced. The present invention preferably is applied to the synthesis of nucleic acids such as DNA and RNA, for example. The isotope preferably is a stable isotope. The oxidizing agent preferably is H218O, 3H-1,2-benzodithiol 3-one 1,1-dioxide having 34S, or a diisopropylethylamine-borane complex having 10B, for example.Type: GrantFiled: May 7, 2012Date of Patent: April 19, 2016Assignee: BONAC CorporationInventors: Tomohiro Hamasaki, Tadaaki Ohgi
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Patent number: 9035044Abstract: The present invention is directed to L-proline and citric acid co-crystals of (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, pharmaceutical compositions containing said co-crystals and their use in the treatment glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X.Type: GrantFiled: May 8, 2012Date of Patent: May 19, 2015Assignee: Janssen Pharmaceutica NVInventors: Minh Nguyen, Edwin A. Collier
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Publication number: 20150133777Abstract: The invention disclosed herein discloses selected ribose isomers that are useful as PET probes (e.g. [18F]-2-fluoro-2-deoxy-arabinose). These PET probes are useful, for example, in methods designed to monitor physiological processes including ribose metabolism and/or to selectively observe certain tissue/organs in vivo. The invention disclosed herein further provides methods for making and using such probes.Type: ApplicationFiled: May 9, 2013Publication date: May 14, 2015Inventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
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Publication number: 20150133650Abstract: The invention relates to a device for the preparation of radiochemical compounds. It is provided that the device comprises at least a reaction module, a dosing module, and a storage module, wherein the reaction module has at least one reaction vessel having a closable opening through which substances needed for the preparation of a predetermined radiochemical compound can be introduced into the reaction vessel of the reaction module and through which the prepared radiochemical compound can be removed from the reaction vessel of the reaction module; the dosing module has at least one pipetting head which can be moved relative to the storage module and the reaction module and in x, y, and z directions and also has at least one dosing unit; and at least one reservoir for one of the substances needed for the preparation of the respective radiochemical compound is formed in the storage module.Type: ApplicationFiled: January 8, 2015Publication date: May 14, 2015Applicants: GESIM-GESELLSCHAFT FUER SILIZIUM-MIKROSYSTEME MBH, ABX ADVANCED BIOCHEMICAL COMPOUNDS GMBHInventors: Marco MUELLER, Steffen HOWITZ
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Patent number: 9024009Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.Type: GrantFiled: September 9, 2008Date of Patent: May 5, 2015Assignees: Janssen Pharmaceutica N.V., Mitsubishi Tanabe Pharma CorporationInventors: Ahmed F. Abdel-Magid, Maureen Chislom, Steven Mehrman, Lorraine Scott, Kenneth M. Wells, Fan Zhang-Plasket, Sumihiro Nomura, Mitsuya Hongu, Yuichi Koga
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Publication number: 20150119355Abstract: There is provided a composition comprising a polysaccharide obtainable from the microalgae, Prasinococcus capsulatus and strains related to P. capsulatus for use prophylactically and/or therapeutically in the treatment of disorders of the immune system, for example in psoriasis and dermatological conditions, internal immune system disorders, in particular gut inflammatory conditions and respiratory conditions. Further, there is provided derivatives of a polysaccharide obtainable from the microalgae, Prasinococcus capsulatus or an algal strain related to P. capsulatus and the use of such derivatives prophylactically and/or therapeutically in the treatment of disorders of the immune system.Type: ApplicationFiled: May 13, 2013Publication date: April 30, 2015Inventors: Charles Daniel Bavington, Claire Moss
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Patent number: 9012412Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein A, R1, R2, R3, R4, and R5 are as defined herein, useful as dual SGLT1/SGLT2 inhibitors.Type: GrantFiled: March 7, 2014Date of Patent: April 21, 2015Assignee: Janssen Pharmaceutica NVInventors: Micheal Gaul, Gee-Hong Kuo, Guozhang Xu, Bao-Ping Zhao
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Patent number: 9012413Abstract: The invention relates to FGF receptor-activating N-acyl octasaccharides having Formula (I), wherein: R1 is an O-alkyl group optionally replaced by one or more aryl or cycloalkyl groups, R2 is an OSO3? or hydroxyl group, R3 is an alkyl, cycloalkyl, or alkyl-cycloalkyl group, R4 is a disaccharide having Formula (II), R6 is a disaccharide having Formula (III), and R8 is a disaccharide having Formula (IV), where R5, R7, and R9 are OSO3? or hydroxyl groups. The invention further relates to the preparation of said octasaccharides and to the therapeutic use thereof.Type: GrantFiled: February 9, 2012Date of Patent: April 21, 2015Assignee: SanofiInventors: Pierre Alexandre Driguez, Philippe Duchaussoy, Pierre Fons, Corentin Herbert, Gilbert Lassalle
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Patent number: 9006187Abstract: The present invention relates to a novel compound with thiophene ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The prevention also provides a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating metabolic disorders, particularly diabetes.Type: GrantFiled: September 9, 2011Date of Patent: April 14, 2015Assignee: Green Cross CorporationInventors: Jinhwa Lee, Kwang-Seop Song, Suk Ho Lee
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Patent number: 8999941Abstract: The present invention provides amorphous forms and the crystalline complexes of SGLT2 inhibitors as a novel material, in particular in pharmaceutically acceptable form. The crystalline forms of SGLT2 inhibitor canagliflozin are designated as Forms CS1, CS2, CS3, CS4 and CS5.Type: GrantFiled: October 30, 2012Date of Patent: April 7, 2015Assignee: ScinoPharm Taiwan, Ltd.Inventors: Julian Paul Henschke, Meng-Fen Ho, Shu-Ping Chen, Yung-Fa Chen
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Patent number: 8981079Abstract: A chlorinating agent such as a chloroiminium species is used to remove or neutralize tertiary acetamide present as a contaminant in a tertiary formamide solvent. Tertiary formamide solvent purified or treated in this manner can be used as a reaction vehicle for the chlorination of sucrose-6-acylates, thereby improving the yields of the desired sucralose-6-acylate (an intermediate in the production of sucralose).Type: GrantFiled: June 18, 2010Date of Patent: March 17, 2015Assignee: Tate & Lyle Technology LimitedInventors: James Edwin Wiley, Jr., Mohamad R. Jaber
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Patent number: 8962822Abstract: The present invention provides a modified polyuronic acid represented by formula (1) or a salt thereof which is excellent in surface activity: wherein R1 is a hydrogen atom, a hydrocarbon group having 1 to 40 carbon atoms or the like; X is an oxygen atom, a sulfur atom or a —NH— group, with the proviso that a ratio value of [m/(m+n)] is from 0.3 to 1.0, and a plurality of the R1 groups being present in a molecule of the modified polyuronic acid or the salt thereof may be the same or different from each other but all of the R1 groups are not hydrogen atoms at the same time.Type: GrantFiled: October 14, 2011Date of Patent: February 24, 2015Assignee: Kao CorporationInventors: Kouji Ohsaki, Kazuaki Sato, Yuri Okutani
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Patent number: 8962823Abstract: This invention concerns the first environmentally benign heterogeneous modification of polysaccharide-based material in native solid state by thiol-ene “click chemistry”. The direct reaction of a thiol with an un-activated double or triple bond by thiol-ene and thiol-enyne click modification is thermally or photochemically catalyzed and is completely metal-free and allows for a highly modular approach to modifications of fibers and fiber-based materials.Type: GrantFiled: January 19, 2011Date of Patent: February 24, 2015Assignee: Organoclick ABInventors: Armando Cordova, Jonas Hafren
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Patent number: 8957033Abstract: Disclosed is a compound of formula I, or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer or racemic mixture thereof, wherein R1 and R2 are each independently hydrogen, —OH, alkyl, —CF3, —OCHF2, —OCF3 or halogen; R3 is cycloalkyl, —OCH2CF3, —OCH2CHF2, —OCH2CH2F or —OCH2CH3; R4 is hydrogen, —OH, —O aryl, —OCH2 aryl, alkyl, cycloalkyl, —CF3, —OCHF2, —OCF3, —OCH2CF3, —OCH2CHF2, —OCH2CH2F or halogen; A is —CX1X2, wherein X1 and X2 are each independently H, F and Cl, and when both X1 and X2 are H, R3 is not —OCH2CH3. The compound has an activity of inhibitors of sodium-dependent glucose transport protein. Also disclosed is a method for preparing the compound, a pharmaceutical composition comprising the compound, use of the compound and pharmaceutical composition thereof in preparing medicaments of SGLT2 inhibitors and treating related diseases.Type: GrantFiled: February 20, 2012Date of Patent: February 17, 2015Assignee: Beijing Prelude Pharm. SCI. & Tech. Co., Ltd.Inventor: Michael Wang
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Publication number: 20150038689Abstract: Provided are methods for the efficient stereoselective formation of glycosidic bonds, without recourse to prosthetic or directing groups.Type: ApplicationFiled: July 29, 2014Publication date: February 5, 2015Inventors: Clay S. Bennett, John P. Issa, Dina Lloyd
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Patent number: 8940325Abstract: The present invention relates to the use of at least one compound selected among the synthetic polysulphated oligosaccharides having 1 to 4 ose units and to the salts and complexes thereof as cleaning agents for a wound. The invention can be used in particular for preparing bandages intended for cleaning wounds.Type: GrantFiled: February 16, 2011Date of Patent: January 27, 2015Assignee: Laboratories UrgoInventors: Laurent Apert, Christelle Laurensou, Dominque Nicot
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Publication number: 20150018541Abstract: The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-?-D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed.Type: ApplicationFiled: April 22, 2014Publication date: January 15, 2015Applicants: GE HEALTHCARE AS, GE HEALTHCARE LIMITEDInventors: Torild WICKSTROM, DIRK-JAN IN'T VELD, NIGEL JOHN OSBORN, JULIAN GRIGG, ANTHONY WILSON
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Publication number: 20150011003Abstract: A medium which comprises a fibroblast growth factor (FGF), and a sulfated compound or a pharmaceutically acceptable salt thereof at a concentration which promotes the growth of a stem cell in the presence of FGF, is useful for culturing stem cells.Type: ApplicationFiled: September 26, 2014Publication date: January 8, 2015Applicant: AJINOMOTO CO., INC.Inventors: Yoko KURIYAMA, Nao SUGIMOTO, Manabu KITAZAWA, Satoru OKAMOTO, Sho SENDA, Ikue HARATA, Satoru OHASHI
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Patent number: 8884003Abstract: A process for chlorinating polysaccharides or oligosaccharides, which comprises A) dissolving a polysaccharide or oligosaccharide in a solvent system which comprises at least one ionic liquid and B) reacting the polysaccharides or oligosaccharides with a chlorinating agent.Type: GrantFiled: January 11, 2011Date of Patent: November 11, 2014Assignee: BASF SEInventors: Mari Granström, Werner Mormann, Petra Frank
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Publication number: 20140316130Abstract: This invention relates to the miniaturisation of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).Type: ApplicationFiled: April 15, 2014Publication date: October 23, 2014Applicant: HAMMERSMITH IMANET LIMITEDInventors: FRANK BRADY, SAJINDER KAUR LUTHRA, JAMES MILLAR GILLIES, NICHOLAS TOBY JEFFREY
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Patent number: 8853387Abstract: The present invention is directed to sulfated oligosaccharides having 4, 5 or 6 saccharidic units and wherein a glycosidic bond between two saccharide units is substituted by a C—C bond, and wherein the sulfation degree expressed as percentage of OH groups substituted by a OSO3? group is comprised between 50 and 100%. The sulfated oligosaccharides according to the invention are useful as a drug, in particular in the treatment of angiogenesis, metastasis, and inflammation.Type: GrantFiled: July 9, 2009Date of Patent: October 7, 2014Assignee: Istituto di Ricerche Chimiche e Biochimiche “G. Ronzoni”Inventors: Giangiacomo Torri, Elena Vismara, Israel Vlodavsky, Annamaria Naggi
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Publication number: 20140296506Abstract: A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.Type: ApplicationFiled: June 9, 2014Publication date: October 2, 2014Inventors: Sumihiro NOMURA, Eiji KAWANISHI, Kiichiro UETA
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Publication number: 20140256657Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein A, R1, R2, R3, R4, and R5 are as defined herein, useful as dual SGLT1/SGLT2 inhibitors.Type: ApplicationFiled: March 7, 2014Publication date: September 11, 2014Applicant: Janssen Pharmaceutica NVInventors: Micheal Gaul, Gee-Hong Kuo, Guozhang Xu, Bao-Ping Zhao
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Patent number: 8829182Abstract: A particulate SAE-CD composition is provided. The SAE-CD composition has an advantageous combination of physical properties not found in known solid forms of SAE-CD. In particular, the SAE-CD composition possesses an advantageous physicochemical and morphological property profile such that it can be tailored to particular uses. The SAE-CD composition of the invention has improved flow and dissolution performance as compared to known compositions of SAE-CD.Type: GrantFiled: March 11, 2013Date of Patent: September 9, 2014Assignee: Cydex Pharmaceuticals, Inc.Inventors: James D. Pipkin, Gerold L. Mosher, Douglas B. Hecker
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Publication number: 20140243517Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: ApplicationFiled: May 1, 2014Publication date: August 28, 2014Applicant: AstraZeneca ABInventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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Publication number: 20140243283Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.Type: ApplicationFiled: December 18, 2013Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Yeeman K. Ramtohul, Sanjoy Kumar Das, Caroline Cadilhac, Thumkunta Jagadeeswar Reddy, Louis Vaillancourt, Michel Gallant, Bingcan Liu, Evelyne Dietrich, Frederic Vallee, Julien Martel, Carl Poisson
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Publication number: 20140235848Abstract: A method that can be used to make a precursor of L-fucose from D-glucose that includes the steps of a) making a compound of formula (1) from D-glucose, formula (1) wherein R1 is acyloxy, and Q is a group (a), (b), (c) or (d), formula (a), (b), (c) or (d) or wherein R1 is OH, and Q is a group (e), (f) or (g); formula (e), (f) or (g) wherein R2 is acyloxy and R3 is a sulphonyl leaving group; and b) producing 6-deoxy-L-talose from the compound of formula (1) formed in step a), wherein the moiety is a highly lipophilic protecting group; compounds according to formula (1), and use of a compound according to formula (1) are provided.Type: ApplicationFiled: September 28, 2012Publication date: August 21, 2014Applicant: Glycom A/SInventors: Julien BOUTET, Nikolay KHANZHIN, Filippo BONACCORSI, Gyula DEKANY
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Patent number: 8809300Abstract: Disclosed is a depolymerized glycosaminoglycan from Thelenota ananas (dTHG), weight average molecular weight of which is about 8000˜20000 Da, and monosaccharide components of which are acetylgalactosamine (GalNAc), glucuronic acid (GlcUA), fucose (Fuc) or their sulfates (expressed as —OSO3?), in which molar ratio of GalNAc:GlcUA:Fuc:—OSO3? is about 1:(1±0.3):(1±0.3):(3.5±0.5). Said dTHG is a potent endogenous inhibitor of factor X, which has good anticoagulant and antithrombotic activity, and can be used for the prevention and/or treatment of thrombotic diseases. Also provided is a method for preparing said dTHG, which comprises steps of 1) extracting and obtaining fucosylated glycosaminoglycan (THG) from the body wall of Thelenota ananas; 2) depolymerizing THG to obtain dTHG by method of peroxide depolymerization or method of peroxide depolymerization catalyzed by catalyst of the fourth period transition metal ions; 3) removing impurities with lower and/or higher molecular weight in dTHG.Type: GrantFiled: October 25, 2010Date of Patent: August 19, 2014Assignee: Shenzhen Neptunus Pharmaceutical Co., Ltd.Inventors: Jinhua Zhao, Hui Kang, Mingyi Wu, Weizhen Zeng, Zi Li, Yuan Gao, Jing Cui, Zhiguo Wang, Hanlin Feng, Lin Yu
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Patent number: 8802842Abstract: The invention relates to a method for the preparation for a crystalline form of 1-chloro-4-(?-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. In addition the invention relates to a crystalline form obtainable by this method, to a pharmaceutical composition and to the use thereof for preparing medicaments.Type: GrantFiled: September 28, 2010Date of Patent: August 12, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Weber, Svenja Renner, Tobias Fiedler, Simone Orlich
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Patent number: 8802637Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.Type: GrantFiled: September 30, 2013Date of Patent: August 12, 2014Assignee: Theracos, Inc.Inventors: Yuanwei Chen, Huawei Cheng, Shengbin Li, Yuelin Wu, Yan Feng, Binhua Lv, Binhua Xu, Brian Seed, Michael J. Hadd, Yanli Song, Jiyan Du, Congna Wang, Jacques Y. Roberge
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Publication number: 20140216304Abstract: This invention is directed to a process for preparing an additive for cementitious materials, in particular an admixture for paste, grout, mortar and concrete applications as well as a cement additive for cement production by grinding, from a sugar-based material. The process comprises a step of the sugar-based material being subjected to a sulfonation treatment.Type: ApplicationFiled: May 17, 2011Publication date: August 7, 2014Applicant: CONSTRUCTION RESEARCH & TECHNOLOGY GMBHInventors: Xiaohui Hou, Tomomi Sugiyama, Jan Kluegge, Akira Ohta
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Patent number: 8796446Abstract: A method of removing a carboxylic acid from a liquid including a tertiary amide solvent includes: forming an extraction medium including an acid-extracting tin species and an extraction solvent that is immiscible with the tertiary amide solvent; subsequently contacting the liquid with the extraction medium, forming a phase including a de-acidified tertiary amide solvent and a phase including the extraction solvent; and removing the phase including the extraction solvent, to afford a liquid including the de-acidified tertiary amide solvent. The acid-extracting tin species is one or more tin species obtained by reaction of a di(hydrocarbyl) tin oxide with less than one equivalent of a carboxylic acid, or tin species obtainable by reaction of a 1,3-diacyloxy-1,1,3,3-tetra-(hydrocarbyl)distannoxane with an aqueous base. A method of preparing a sucralose-6-acylate includes uses the foregoing method to remove a carboxylic acid from a liquid including a tertiary amide solvent and the sucralose-6-acylate.Type: GrantFiled: May 3, 2012Date of Patent: August 5, 2014Assignee: Tate & Lyle Technology LimitedInventors: David T. Coleman, Edward Micinski, James Edwin Wiley, Jr., Thomas A. Eilers, David A. Dentel
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Patent number: 8785403Abstract: A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.Type: GrantFiled: June 12, 2012Date of Patent: July 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Sumihiro Nomura, Eiji Kawanishi, Kiichiro Ueta
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Publication number: 20140199727Abstract: The present invention concerns compounds of the following formula (I) or a pharmaceutically acceptable salt thereof, a stereoisomer or a mixture of stereoisomers in any proportion, in particular a mixture of enantiomers, and particularly a racemate mixture, in which R represents H, OH or OR19, as well as processes for preparing these compounds and their use as inducer for the transcription of genes under control of the lac promoter.Type: ApplicationFiled: August 8, 2012Publication date: July 17, 2014Applicant: TFCHEMInventors: Geraldine Deliencourt-Godefroy, Hyacinthe Fillon
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Publication number: 20140187768Abstract: Disclosed is a method for chlorinating a carbohydrate or a derivative thereof to produce a polychlorinated carbohydrate or a derivative thereof, such as sucralose, the method involves (i) reacting the carbohydrate or derivative thereof with a chlorinating agent to obtain a reaction mixture comprising said polychlorinated carbohydrate or derivative thereof and at least one under-chlorinated carbohydrate or derivative thereof, (ii) returning the at least one under-chlorinated carbohydrate or derivative thereof to a chlorinating step and further chlorinating the at least one under-chlorinated carbohydrate or derivative thereof to obtain the desired polychlorinated carbohydrate or derivative thereof; and (iii) optionally repeating steps (i) and (ii) “n” times where n?1. The polychlorinated carbohydrate or a derivative thereof is obtained in high yields.Type: ApplicationFiled: March 5, 2014Publication date: July 3, 2014Applicant: Lexington Pharmaceuticals Laboratories, LLCInventors: William Randal ERICKSON, Stephen Craig FIELDS
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Patent number: 8748595Abstract: Methods for purifying fucoidan in extracts from brown seaweed are disclosed. In particular, methods of purifying fucoidan in the extract to remove heavy metal ions, bacterial and endotoxin contaminants, and other impurities are disclosed. The methods include the use of a chelating agent, selective precipitation, and filtration.Type: GrantFiled: February 1, 2008Date of Patent: June 10, 2014Assignees: Baxter International Inc., Baxter Healthcare S.A.Inventors: Patrick N. Shaklee, Jennifer Bahr-Davidson, Srinivasa Prasad, Kirk Johnson
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Publication number: 20140154200Abstract: The present invention relates to a non-cellulosic polysaccharide derivative: i) having a mean average molecular weight (Mw) from about 100,000 g/mol, preferably from about 150,000 g/mol and more preferably from about 200,000 g/mole to about 2,000,000 g/mol, preferably to about 1,800,000 g/mol and more preferably to about 1,400,000 g/mole; and ii) containing at least one cationic group, with a cationic degree of substitution (DScat.)extraction, from about 0.20 to about 0.30.Type: ApplicationFiled: July 20, 2012Publication date: June 5, 2014Applicant: RHODIA OPERATIONSInventors: Gilda Lizarraga, Delphine Mechineau, Dominique Lemos, Caroline Mabille
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Patent number: 8729255Abstract: Disclosed is a method of chlorinating a carbohydrate or derivative thereof, for example, a sucrose-6-ester at the 4,1?, and 6? positions, with irreversible removal of HCl formed during the reaction to form the chlorinated carbohydrate or derivative thereof, for example, a 4,1?,6?-trichloro-4,1?,6?-trideoxy-6-O-ester of galactosucrose (TGS-6E). The irreversible removal of HCl can be carried out by an irreversible physical process and/or an irreversible chemical process. Sucralose, an artificial sweetener, can be prepared by deesterification of the TGS-6E. The chlorination reaction takes place at low temperatures and the desired chlorinated product is obtained in high yields and in high purities.Type: GrantFiled: March 14, 2013Date of Patent: May 20, 2014Assignee: Lexington Pharmaceuticals Laboratories, LLCInventors: William Randal Erickson, Stephen Craig Fields
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Patent number: 8722633Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: April 12, 2012Date of Patent: May 13, 2014Assignee: Novartis AGInventors: Gregory Raymond Bebernitz, Mark Gary Bock
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Publication number: 20140128595Abstract: The present invention provides processes for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.Type: ApplicationFiled: November 7, 2012Publication date: May 8, 2014Applicant: ScinoPharm Taiwan, LTD.Inventors: Julian Paul Henschke, Chen-Wei Lin, Ping-Yu Wu, Chi-Nung Hsiao, Jyh-Hsiung Liao, Tsung-Yu Hsiao
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Publication number: 20140121180Abstract: The invention relates to a sucrose octasulfate of magnesium, having general formula I, the preparation method thereof and the use of same in the pharmaceutical and/or cosmetic field, wherein 0?n?4, n is an integer and Y represents OH, Cl, Br, I, NO3, C6H5O7, CH3CO2, CF3CO2 or —OCH3.Type: ApplicationFiled: May 31, 2012Publication date: May 1, 2014Applicant: PIERRE FABRE DERMO-COSMETIQUEInventors: Séverine Jeulin, Hélène Hernandez-Pigeon, Luc Aguilar
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Publication number: 20140011754Abstract: Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.Type: ApplicationFiled: June 13, 2011Publication date: January 9, 2014Applicant: Theracos, Inc.Inventors: Ge Xu, Binhua Lv, Brian Seed, Jacques Y. Roberge