Sulfur Or Halogen Containing Patents (Class 536/122)
  • Patent number: 10308664
    Abstract: 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: Grant
    Filed: August 19, 2012
    Date of Patent: June 4, 2019
    Inventors: Yousry M. A. Naguib, Ashraf Naguib, Ahmed Naguib
  • Patent number: 10052395
    Abstract: 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: Grant
    Filed: May 30, 2017
    Date of Patent: August 21, 2018
    Inventors: Yousry Naguib, Ashraf Naguib, Ahmed Naguib
  • Patent number: 10053474
    Abstract: 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: Grant
    Filed: May 5, 2017
    Date of Patent: August 21, 2018
    Assignee: 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
  • Patent number: 9315799
    Abstract: 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: Grant
    Filed: May 7, 2012
    Date of Patent: April 19, 2016
    Assignee: BONAC Corporation
    Inventors: Tomohiro Hamasaki, Tadaaki Ohgi
  • Patent number: 9035044
    Abstract: 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: Grant
    Filed: May 8, 2012
    Date of Patent: May 19, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Minh Nguyen, Edwin A. Collier
  • Publication number: 20150133650
    Abstract: 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: Application
    Filed: January 8, 2015
    Publication date: May 14, 2015
    Applicants: GESIM-GESELLSCHAFT FUER SILIZIUM-MIKROSYSTEME MBH, ABX ADVANCED BIOCHEMICAL COMPOUNDS GMBH
    Inventors: Marco MUELLER, Steffen HOWITZ
  • Publication number: 20150133777
    Abstract: 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: Application
    Filed: May 9, 2013
    Publication date: May 14, 2015
    Inventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
  • Patent number: 9024009
    Abstract: 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: Grant
    Filed: September 9, 2008
    Date of Patent: May 5, 2015
    Assignees: Janssen Pharmaceutica N.V., Mitsubishi Tanabe Pharma Corporation
    Inventors: Ahmed F. Abdel-Magid, Maureen Chislom, Steven Mehrman, Lorraine Scott, Kenneth M. Wells, Fan Zhang-Plasket, Sumihiro Nomura, Mitsuya Hongu, Yuichi Koga
  • Publication number: 20150119355
    Abstract: 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: Application
    Filed: May 13, 2013
    Publication date: April 30, 2015
    Inventors: Charles Daniel Bavington, Claire Moss
  • Patent number: 9012412
    Abstract: 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: Grant
    Filed: March 7, 2014
    Date of Patent: April 21, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Micheal Gaul, Gee-Hong Kuo, Guozhang Xu, Bao-Ping Zhao
  • Patent number: 9012413
    Abstract: 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: Grant
    Filed: February 9, 2012
    Date of Patent: April 21, 2015
    Assignee: Sanofi
    Inventors: Pierre Alexandre Driguez, Philippe Duchaussoy, Pierre Fons, Corentin Herbert, Gilbert Lassalle
  • Patent number: 9006187
    Abstract: 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: Grant
    Filed: September 9, 2011
    Date of Patent: April 14, 2015
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Kwang-Seop Song, Suk Ho Lee
  • Patent number: 8999941
    Abstract: 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: Grant
    Filed: October 30, 2012
    Date of Patent: April 7, 2015
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Julian Paul Henschke, Meng-Fen Ho, Shu-Ping Chen, Yung-Fa Chen
  • Patent number: 8981079
    Abstract: 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: Grant
    Filed: June 18, 2010
    Date of Patent: March 17, 2015
    Assignee: Tate & Lyle Technology Limited
    Inventors: James Edwin Wiley, Jr., Mohamad R. Jaber
  • Patent number: 8962822
    Abstract: 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: Grant
    Filed: October 14, 2011
    Date of Patent: February 24, 2015
    Assignee: Kao Corporation
    Inventors: Kouji Ohsaki, Kazuaki Sato, Yuri Okutani
  • Patent number: 8962823
    Abstract: 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: Grant
    Filed: January 19, 2011
    Date of Patent: February 24, 2015
    Assignee: Organoclick AB
    Inventors: Armando Cordova, Jonas Hafren
  • Patent number: 8957033
    Abstract: 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: Grant
    Filed: February 20, 2012
    Date of Patent: February 17, 2015
    Assignee: Beijing Prelude Pharm. SCI. & Tech. Co., Ltd.
    Inventor: Michael Wang
  • Publication number: 20150038689
    Abstract: Provided are methods for the efficient stereoselective formation of glycosidic bonds, without recourse to prosthetic or directing groups.
    Type: Application
    Filed: July 29, 2014
    Publication date: February 5, 2015
    Inventors: Clay S. Bennett, John P. Issa, Dina Lloyd
  • Patent number: 8940325
    Abstract: 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: Grant
    Filed: February 16, 2011
    Date of Patent: January 27, 2015
    Assignee: Laboratories Urgo
    Inventors: Laurent Apert, Christelle Laurensou, Dominque Nicot
  • Publication number: 20150018541
    Abstract: 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: Application
    Filed: April 22, 2014
    Publication date: January 15, 2015
    Applicants: GE HEALTHCARE AS, GE HEALTHCARE LIMITED
    Inventors: Torild WICKSTROM, DIRK-JAN IN'T VELD, NIGEL JOHN OSBORN, JULIAN GRIGG, ANTHONY WILSON
  • Publication number: 20150011003
    Abstract: 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: Application
    Filed: September 26, 2014
    Publication date: January 8, 2015
    Applicant: AJINOMOTO CO., INC.
    Inventors: Yoko KURIYAMA, Nao SUGIMOTO, Manabu KITAZAWA, Satoru OKAMOTO, Sho SENDA, Ikue HARATA, Satoru OHASHI
  • Patent number: 8884003
    Abstract: 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: Grant
    Filed: January 11, 2011
    Date of Patent: November 11, 2014
    Assignee: BASF SE
    Inventors: Mari Granström, Werner Mormann, Petra Frank
  • Publication number: 20140316130
    Abstract: 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: Application
    Filed: April 15, 2014
    Publication date: October 23, 2014
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: FRANK BRADY, SAJINDER KAUR LUTHRA, JAMES MILLAR GILLIES, NICHOLAS TOBY JEFFREY
  • Patent number: 8853387
    Abstract: 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: Grant
    Filed: July 9, 2009
    Date of Patent: October 7, 2014
    Assignee: Istituto di Ricerche Chimiche e Biochimiche “G. Ronzoni”
    Inventors: Giangiacomo Torri, Elena Vismara, Israel Vlodavsky, Annamaria Naggi
  • Publication number: 20140296506
    Abstract: 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: Application
    Filed: June 9, 2014
    Publication date: October 2, 2014
    Inventors: Sumihiro NOMURA, Eiji KAWANISHI, Kiichiro UETA
  • Publication number: 20140256657
    Abstract: 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: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Micheal Gaul, Gee-Hong Kuo, Guozhang Xu, Bao-Ping Zhao
  • Patent number: 8829182
    Abstract: 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: Grant
    Filed: March 11, 2013
    Date of Patent: September 9, 2014
    Assignee: Cydex Pharmaceuticals, Inc.
    Inventors: James D. Pipkin, Gerold L. Mosher, Douglas B. Hecker
  • Publication number: 20140243283
    Abstract: 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: Application
    Filed: December 18, 2013
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Publication number: 20140243517
    Abstract: 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: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: AstraZeneca AB
    Inventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
  • Publication number: 20140235848
    Abstract: 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: Application
    Filed: September 28, 2012
    Publication date: August 21, 2014
    Applicant: Glycom A/S
    Inventors: Julien BOUTET, Nikolay KHANZHIN, Filippo BONACCORSI, Gyula DEKANY
  • Patent number: 8809300
    Abstract: 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: Grant
    Filed: October 25, 2010
    Date of Patent: August 19, 2014
    Assignee: 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
  • Patent number: 8802842
    Abstract: 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: Grant
    Filed: September 28, 2010
    Date of Patent: August 12, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Weber, Svenja Renner, Tobias Fiedler, Simone Orlich
  • Patent number: 8802637
    Abstract: 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: Grant
    Filed: September 30, 2013
    Date of Patent: August 12, 2014
    Assignee: 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
  • Publication number: 20140216304
    Abstract: 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: Application
    Filed: May 17, 2011
    Publication date: August 7, 2014
    Applicant: CONSTRUCTION RESEARCH & TECHNOLOGY GMBH
    Inventors: Xiaohui Hou, Tomomi Sugiyama, Jan Kluegge, Akira Ohta
  • Patent number: 8796446
    Abstract: 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: Grant
    Filed: May 3, 2012
    Date of Patent: August 5, 2014
    Assignee: Tate & Lyle Technology Limited
    Inventors: David T. Coleman, Edward Micinski, James Edwin Wiley, Jr., Thomas A. Eilers, David A. Dentel
  • Patent number: 8785403
    Abstract: 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: Grant
    Filed: June 12, 2012
    Date of Patent: July 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Sumihiro Nomura, Eiji Kawanishi, Kiichiro Ueta
  • Publication number: 20140199727
    Abstract: 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: Application
    Filed: August 8, 2012
    Publication date: July 17, 2014
    Applicant: TFCHEM
    Inventors: Geraldine Deliencourt-Godefroy, Hyacinthe Fillon
  • Publication number: 20140187768
    Abstract: 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: Application
    Filed: March 5, 2014
    Publication date: July 3, 2014
    Applicant: Lexington Pharmaceuticals Laboratories, LLC
    Inventors: William Randal ERICKSON, Stephen Craig FIELDS
  • Patent number: 8748595
    Abstract: 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: Grant
    Filed: February 1, 2008
    Date of Patent: June 10, 2014
    Assignees: Baxter International Inc., Baxter Healthcare S.A.
    Inventors: Patrick N. Shaklee, Jennifer Bahr-Davidson, Srinivasa Prasad, Kirk Johnson
  • Publication number: 20140154200
    Abstract: 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: Application
    Filed: July 20, 2012
    Publication date: June 5, 2014
    Applicant: RHODIA OPERATIONS
    Inventors: Gilda Lizarraga, Delphine Mechineau, Dominique Lemos, Caroline Mabille
  • Patent number: 8729255
    Abstract: 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: Grant
    Filed: March 14, 2013
    Date of Patent: May 20, 2014
    Assignee: Lexington Pharmaceuticals Laboratories, LLC
    Inventors: William Randal Erickson, Stephen Craig Fields
  • Patent number: 8722633
    Abstract: 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: Grant
    Filed: April 12, 2012
    Date of Patent: May 13, 2014
    Assignee: Novartis AG
    Inventors: Gregory Raymond Bebernitz, Mark Gary Bock
  • Publication number: 20140128595
    Abstract: The present invention provides processes for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 8, 2014
    Applicant: ScinoPharm Taiwan, LTD.
    Inventors: Julian Paul Henschke, Chen-Wei Lin, Ping-Yu Wu, Chi-Nung Hsiao, Jyh-Hsiung Liao, Tsung-Yu Hsiao
  • Publication number: 20140121180
    Abstract: 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: Application
    Filed: May 31, 2012
    Publication date: May 1, 2014
    Applicant: PIERRE FABRE DERMO-COSMETIQUE
    Inventors: Séverine Jeulin, Hélène Hernandez-Pigeon, Luc Aguilar
  • Publication number: 20140011754
    Abstract: 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: Application
    Filed: June 13, 2011
    Publication date: January 9, 2014
    Applicant: Theracos, Inc.
    Inventors: Ge Xu, Binhua Lv, Brian Seed, Jacques Y. Roberge
  • Patent number: 8613318
    Abstract: The invention relates to an enhancing oil recovery method by injecting into a subterranean oil formation an aqueous flooding fluid comprising at least one injecting galactomannan polymer substituted by at least one sulfonation agent. The invention also relates to an flooding fluid having better injectivity properties than existing flooding fluids.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: December 24, 2013
    Assignee: IFP Energies Nouvelles
    Inventors: Marie-Pierre Labeau, Guillaume Degre, Rajesh Ranjan, Isabelle Henaut, René Tabary, Jean-François Argillier
  • Publication number: 20130324464
    Abstract: Disclosed are an aryl glycoside compound as represented by formula I or formular I?, a pharmaceutically acceptable salt thereof, optical isomer thereof or a prodrug thereof. The present invention relates to a method of preparing said aryl glycoside compound and the use thereof The aryl glycoside compound of the present invention has an excellent ability on inhibit SGLT activity, especially SGLT2 activity, and is diabetes-fighting medicine with great potential.
    Type: Application
    Filed: February 17, 2012
    Publication date: December 5, 2013
    Applicants: SHANGHAI CHEMPARTNER CO., LTD, SHANGHAI YINGLI SCIENCE AND TECHNOLOGY CO., LTD
    Inventors: Zusheng Xu, Su Qian
  • Publication number: 20130303467
    Abstract: The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
    Type: Application
    Filed: July 10, 2013
    Publication date: November 14, 2013
    Inventors: Jack Z. Gougoutas, Hildegard Lobinger, Srividya Ramakrishnan, Prashant P. Deshpande, Jeffrey T. Bien, Chiajen Lai, Chenchi Wang, Peter Riebel, John Anthony Grosso, Alexandra A. Nirschl, Janak Singh, John D. DiMarco
  • Patent number: 8557968
    Abstract: The invention concerns novel biotinylated hexadecasaccharides of general formula (I) wherein: Biot is a biotin derivative; R, R1 and R2, represent independently of one another a C1-C6 alkoxy or and —OSO3; R3 represents a C1-C6 alkoxy or an —OSO3, or R3 constitutes a —O—CH2— bridge; Pe represents a saccharide concatenation; as well as their pharmaceutically acceptable salts, and their use as medicines.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: October 15, 2013
    Assignee: Sanofi
    Inventors: Philippe Duchaussoy, Jean Pascal Herault, Jean Marc Herbert, Maurice Petitou, Pierre Savi
  • Publication number: 20130267694
    Abstract: Provided are methods of making compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides synthetic intermediates useful for preparing such compounds.
    Type: Application
    Filed: May 8, 2013
    Publication date: October 10, 2013
    Applicant: Theracos, Inc.
    Inventors: Baihua Xu, Binhua Lv, Ge Xu, Brian Seed, Jacques Y. Roberge