Hetero Ring Is Five-membered Consisting Of One Nitrogen And Four Carbons (e.g., Halopyrrolidines, Etc.) Patents (Class 548/400)
  • Patent number: 8592419
    Abstract: The invention provides the compounds of formula (): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: November 26, 2013
    Assignee: MUSC Foundation for Research Development
    Inventors: Alicja Bielawska, Yusuf A. Hannun, James Norris, Zdzislaw M. Szulc, Jian-yun Dong, Jacek Bielawski, David A. Schwartz, David H. Holman, Ahmed M. El-Zawahry, John McKillop
  • Patent number: 8585779
    Abstract: The invention relates to a composition for dyeing keratin fibers, and in particular human keratin fibers such as the hair, comprising at least one 2-pyrrolidone functionalized in the 4 position with a carboxylic acid or amide radical, and at least one hydrophobic direct dye or a pigment; a dyeing process using this composition. Similarly, the invention relates to the use of the said pyrrolidone combined with a direct dye or a pigment for dyeing keratin fibers, and especially to the use of the said pyrrolidone for improving the color uptake onto the fibers of direct dyes that are sparingly soluble or insoluble in aqueous-alcoholic supports. The invention also relates to novel pyrrolidone derivatives. The present invention makes it possible in particular to obtain direct dyeing on keratin fibers that is fast, resistant to washing, chromatic and powerful.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: November 19, 2013
    Assignee: L'Oreal
    Inventors: Stéphane Sabelle, Madeleine Leduc
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8552122
    Abstract: Disclosed is a method of preparing terminally functionalized telechelic polymers using a cationic living polymer product or a terminal tert-chloride chain end of a carbocationic quasiliving polymer product, which comprises quenching the polymer product with a functionalized N-substituted pyrrole to thereby introduce the functionalized N-substituted pyrrole at the terminal reactive polymer chain end(s). A method is also disclosed whereby the N-substituent may be derivatized to a basic amine containing functional group. Also disclosed are the terminal functionalized polyisobuyl N-substituted pyrrole compounds where the polyisobutyl group is substituted at the 2 and 3 position of the N-substituted pyrrole.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: October 8, 2013
    Assignees: The University of Southern Mississippi, Chevron Oronite Company LLC
    Inventors: Robson F. Storey, Casey D. Stokes, James J. Harrison, Nemesio Martinez-Castro
  • Patent number: 8530461
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
  • Patent number: 8507537
    Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: October 13, 2007
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
  • Patent number: 8501937
    Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethlamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: August 6, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Dennis J. Hlasta, Mark J. Schulz
  • Publication number: 20130180591
    Abstract: The present invention relates to electrolyte formulations comprising at least one imidazolium fluorotricyanoborate or pyrrolidinium fluorotricyanoborate and their use in an electrochemical and/or optoelectronic device such as a photovoltaic cell, a light emitting device, an electrochromic or photo-electrochromic device, an electrochemical sensor and/or biosensor, preferably their use in a dye or quantum dot sensitized solar cell.
    Type: Application
    Filed: September 1, 2011
    Publication date: July 18, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Kentaro Kawata, Nikolai Mykola Ignatyev, Michael Schulte, Hiroki Yoshizaki
  • Patent number: 8481579
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: July 9, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
  • Patent number: 8476336
    Abstract: The invention relates to an ophthalmologic composition including a dye of the general formula I in which R1=substituted or unsubstituted hydrocarbon radical, R2=substituted or unsubstituted hydrocarbon radical with at least one polymerizable double bond, R3?H or substituted or unsubstituted hydrocarbon radical, R4?H, electron-withdrawing substituent or substituted or unsubstituted hydrocarbon radical and X?O, S, NH or NR5, wherein R5 is a substituted and/or unsubstituted hydrocarbon radical. Moreover, the invention relates to another ophthalmologic composition and an ophthalmologic lens.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 2, 2013
    Assignee: Acri.Tec GmbH
    Inventor: Juergen Nachbaur
  • Patent number: 8455665
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: June 4, 2013
    Assignee: Theravance, Inc.
    Inventors: Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
  • Publication number: 20130137744
    Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Applicant: Sunovion Pharmaceutical Inc.
    Inventor: Sunovion Pharmaceutical Inc.
  • Patent number: 8445695
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: May 21, 2013
    Assignees: North Carolina State University, ZettaCore, Inc.
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Patent number: 8445525
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: May 21, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Patent number: 8435968
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: May 7, 2013
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Patent number: 8426636
    Abstract: A sterically bulky stabilizer that is associated non-covalently with a benzimidazolone pigment. The sterically bulky stabilizer compound includes an aromatic acid derivative, and the presence of the sterically bulky stabilizer limits an extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: April 23, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Patent number: 8426587
    Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: (I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: April 23, 2013
    Assignee: Pharmaxis Ltd.
    Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
  • Patent number: 8426630
    Abstract: A multi-step method for the continuous synthesis of ibuprofen or a synthetic precursor of ibuprofen is provided that does not require any intermediate purification or isolation steps and uses reagents compatible with downstream reactions. According to some embodiments, a method is provided wherein isobutylbenzene and a propionyl compound may be converted into a first product in a first Friedel Crafts acylation reaction. The first product may then be converted into a second product in a 1,2-aryl migration reaction. Finally, the second product may be converted into ibuprofen in a hydrolysis reaction. The present invention also provides a method wherein only the first and second reaction steps or only the second and third reaction steps are performed. An apparatus is also provided having two or more microreactors and two or more junctions in particular arrangements for the synthesis of ibuprofen or a synthetic precursor of ibuprofen.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: April 23, 2013
    Assignee: Florida State University Research Foundation
    Inventors: D. Tyler McQuade, Andrew Bogdan, Sarah Lihoa Poe
  • Patent number: 8420830
    Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: April 16, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Peter W. Glunz, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata, Luciano Mueller
  • Patent number: 8415499
    Abstract: Dyes for a dye-sensitized solar cell are provided. The dyes for a dye-sensitized solar cell have a structure of wherein each of X and Y independently comprises a substituent, comprising a substituted or unsubstituted aromatic hydrocarbon group, a substituted or unsubstituted aromatic heterocyclic group, and combinations thereof, and at least one of the X and Y comprises an aromatic group which are substituted a pyrene derivative substituted with an alkyl group or an aryl group, and Z comprises a substituted or unsubstituted aromatic hydrocarbon group, a substituted or unsubstituted heterocyclic group, a vinyl group, and a substituted or unsubstituted polyvinyl group, and A comprises an acid functional group.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: April 9, 2013
    Assignee: LG Display Co., Ltd.
    Inventors: Jinok Hwang, Seongkee Park, Sunghoon Joo
  • Patent number: 8372840
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, R4, R5, X1, and j are defined herein. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: February 12, 2013
    Assignee: Xention Limited
    Inventors: Richard John Hamlyn, Mushtaq Mulla, Derek Edward John, Simon Mark Jones, Basil Hartzoulakis, David Madge, John Ford
  • Patent number: 8367844
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: February 5, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
  • Patent number: 8362274
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: January 29, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8357709
    Abstract: The present invention is directed to 2,4-disubstituted pyrrolidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: January 22, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, John D. Schreier
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Patent number: 8329921
    Abstract: This invention relates to a catalyst compound comprising a combination of a cyclic alkyl amino carbene ligand and a benzylidene both attached to a Group 8 metal, preferably ruthenium atom. This invention also relates to a process to make linear alpha-olefins comprising contacting a feed material and an optional alkene (such as ethylene) with the catalyst described above, wherein the feed material is a triacylglyceride, fatty acid, fatty acid alkyl ester, and/or fatty acid ester, typically derived from seed oil (e.g., biodiesel).
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: December 11, 2012
    Assignee: Exxonmobil Chemical Patents Inc.
    Inventors: John R. Hagadorn, Matthew W. Holtcamp, Matthew S. Bedoya
  • Patent number: 8324258
    Abstract: The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: December 4, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Gina Ney
  • Patent number: 8318760
    Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
  • Patent number: 8314140
    Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: November 20, 2012
    Assignee: Antibe Therapeutics Inc.
    Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
  • Patent number: 8304447
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: November 6, 2012
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Patent number: 8303936
    Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared (NIR) spectral range. The NIR is highly sensitive for tumor detection and tracking. The application discloses targeting a tumor-enriched cell surface receptor with a ligand-conjugated fluorescent probe, which specifically allows detection of the tumor relative to the negligible animal autofluorescence.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: November 6, 2012
    Assignee: Li-Cor, Inc.
    Inventors: Daniel R. Draney, Ananda G. Lugade, Narasimhachari Narayanan, Joy Kovar, D. Michael Olive
  • Patent number: 8288529
    Abstract: A method of making a compound of Formula I? comprises reacting a compound of the formula DLCHO, with a compound of the formula to produce the compound of Formula I?. Methods of using the compounds are also described, particularly as intermediates for the synthesis of porphyrin rods, which porphyrin rods are in turn useful for (among other things) the production of molecular memory devices.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: October 16, 2012
    Assignee: North Carolina State University
    Inventors: Jonathan S. Lindsey, Lianhe Yu, Patchanita Thamyongkit, Anil D. Bhise
  • Patent number: 8288399
    Abstract: Method for treating Alzheimer's disease, Parkinson's disease, Huntington's chorea or Pick's disease by administering to a patient a compound of formula (I) wherein R1 represents hydrogen; R2 represents hydrogen, a C1-C6 alkyl group or C3-C6 cycloalkyl group; A represents nitrogen; D represents a methylene group, a methyl methylene group, a halogen atom substituted methylene group or a halogen substituted methyl methylene group; E represents CH2, CHR3 wherein R3 represents a C1-C6 alkyl group, CH or a carbon atom substituted by a C1-C6 alkyl group; Arom represents aryl, aryl having from 1 to 3 identical or different substituent groups selected from halogen, C1-C6 alkyl, and C1-C6 alkyloxy, heteroaryl or heteroaryl having from 1 to 3 substituent groups, selected from halogen, C1-C6 alkyl and C1-C6 alkyloxy. The part represented by is a single bond or double bond.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: October 16, 2012
    Assignee: BTG International Limited
    Inventors: Tomiichiro Oda, Shigeko Uryu, Shinya Tokuhiro
  • Patent number: 8278439
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: October 2, 2012
    Assignees: North Carolina State University, ZettaCore, Inc.
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Patent number: 8273786
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: September 25, 2012
    Assignee: Theravance, Inc.
    Inventors: Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
  • Patent number: 8258171
    Abstract: A compound represented by the following general formula (I): wherein R1 represents an amino group which may be substituted with one or two alkyl groups; R2, R3, R4 and R5 independently represent an alkyl group; and R6 and R7 independently represent a monocarboxyalkyl group, a salt thereof, or an ester thereof, which is useful as a pH-sensitive fluorescent probe which emits intense fluorescence in an acidic region.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: September 4, 2012
    Assignee: The University of Tokyo
    Inventors: Tetsuo Nagano, Yasuteru Urano, Daisuke Asanuma
  • Patent number: 8258138
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives wherein R1, R2, R3, X1, and A are defined herein. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: September 4, 2012
    Assignee: Xention Limited
    Inventors: Derek Edward John, Mushtaq Mulla, Richard John Hamlyn, Simon Mark Jones, Derek Roland Pollard, Basil Hartzoulakis, Helen Payne, David Madge, John Ford
  • Publication number: 20120220635
    Abstract: The present invention relates to aromatic compounds of the formula (I) and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
    Type: Application
    Filed: February 27, 2012
    Publication date: August 30, 2012
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
  • Patent number: 8252833
    Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1 R2 R3, R4, R5, R6, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Grant
    Filed: February 1, 2007
    Date of Patent: August 28, 2012
    Assignee: Glaxo Group Limited
    Inventors: Andrew Billinton, Nicholas Maughan Clayton, Gerard Martin Paul Giblin, Mark Patrick Healy
  • Publication number: 20120215005
    Abstract: The present invention relates to diionic liquid salts of dicationic or dianionic molecules, as well as solvents comprising diionic liquids and the use of diionic liquids as the stationary phase in a gas chromatographic column.
    Type: Application
    Filed: April 19, 2012
    Publication date: August 23, 2012
    Applicant: SIGMA-ALDRICH CO. LLC
    Inventors: Daniel W. Armstrong, Jared Anderson
  • Patent number: 8242150
    Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.
    Type: Grant
    Filed: June 9, 2008
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
  • Patent number: 8227500
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: July 24, 2012
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Patent number: 8222425
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: July 17, 2012
    Assignee: Novartis AG
    Inventors: Shawn D. Britt, Lech Andrzej Ciszewski, Jiping Fu, Subramanian Karur, Yugang Liu, Peichao Lu, David Thomas Parker, Mahavir Prashad, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng
  • Patent number: 8212055
    Abstract: A method of making chlorins comprises the steps of reacting (e.g. condensing) a dipyrrin western half intermediate with an eastern half intermediate to form a tetrahydrobilene, and then cyclizing the tetrahydrobilene to form a chlorin. Intermediates including tetrahydrobilenes useful in such reactions are also described.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: July 3, 2012
    Assignee: North Carolina State University
    Inventors: Jonathan S. Lindsey, Masahiko Taniguchi, Doyoung Ra, Guoning Mo, Thiagarajan Balasubramanian
  • Patent number: 8193235
    Abstract: The present invention embraces compositions and methods for establishing and maintaining stem cells and inhibiting stem cell differentiation using a selective Protein Kinase C (PKC) inhibitor.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: June 5, 2012
    Assignee: University of Kansas
    Inventors: Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
  • Patent number: 8178077
    Abstract: The present invention provides novel target proteins and target genes for drug discovery, and the means that enable the development of novel drugs using the same. More particularly, the present invention provides NCS proteins and genes thereof; screening methods for drug (for example, anti-central nervous disease drug); agents for regulating disease (for example, central nervous disease); production methods of a drug derivative; a complex comprising a drug and NCS protein, and a method of producing the complex; a kits comprising a drug or a salt thereof; determination methods for the onset or risk of onset of a specified disease, determination methods for susceptibility to a drug, and determination kits used for the determination methods; and the like.
    Type: Grant
    Filed: October 19, 2005
    Date of Patent: May 15, 2012
    Assignee: Reverse Proteomics Research Institute Co., Ltd.
    Inventors: Tadakazu Yamauchi, Hideaki Sueoka, Kouichi Tsuchiya, Katsuhisa Murayama, Ken Horiuchi, Kazuo Komiya, Morikazu Kito, Takeshi Tsutsumi, Yuko Isono, Yorimasa Suwa
  • Patent number: 8163787
    Abstract: A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: April 24, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Kazunobu Kira, Shinsuke Hirota, Hiroshi Azuma, Tadashi Nagakura, Tatsuo Horizoe, Kimiyo Tabata, Kazutomi Kusano, Takao Omae, Atsushi Inoue
  • Patent number: 8153818
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: April 10, 2012
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
  • Patent number: 8148545
    Abstract: The present invention discloses processes for producing ?-nitrocarbonyl and ?-dicarbonyl compounds, which can be precursors in the synthesis of pyrrole compounds. A process for producing pyrroles such as 2,5-dimethylpyrrole, and structurally similar pyrrole compounds, is also disclosed.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: April 3, 2012
    Assignee: Chevron Phillips Chemical Company LP
    Inventors: Hu Yang, Eduardo J. Baralt
  • Patent number: 8148443
    Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?xHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1, 2 or 3, or anions selected from the group of [(Rf1SO2)2N]? anions or anions selected from the group of [BFWRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: April 3, 2012
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Nikolai (Mykola) Ignatyev, German Bissky, Helge Willner