Patents Examined by Fiona T. Powers
  • Patent number: 8455497
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Patent number: 8436153
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: May 7, 2013
    Assignee: Biosearch Technologies, Inc.
    Inventors: Tim Carter, Mark Reddington
  • Patent number: 8415348
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: April 9, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
  • Patent number: 8410135
    Abstract: The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders. Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: April 2, 2013
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Hendrik C. Wals, Bernard J. Van Vliet, Mahmut Yildirim
  • Patent number: 8394971
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: January 20, 2010
    Date of Patent: March 12, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Patent number: 8394815
    Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: March 12, 2013
    Assignee: Lorus Therapeutics Inc.
    Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
  • Patent number: 8389500
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
  • Patent number: 8383841
    Abstract: Fluorescent phenyl xanthene dyes are described that comprise any fluorescein, rhodamine or rhodol comprising a particular C9 phenyl ring. One or both of the ortho groups on the lower C9 phenyl ring is ortho substituted with a group selected from alkyl, heteroalkyl, alkoxy, halo, haloalkyl, amino, mercapto, alkylthio, cyano, isocyano, cyanato, mercaptocyanato, nitroso, nitro, azido, sulfeno, sulfinyl, and sulfino. In one embodiment, halo and/or hydroxy groups are used. Optimal dyes contain a lower C9 phenyl ring in which both ortho groups are the same and the lower ring exhibits some form a symmetry relative to an imaginary axis running from the phenyl rings point of attachment to the remainder of the xanthene dye through a point para to the point of attachment. The phenyl xanthene dyes may be activated. Furthermore, the phenyl xanthene dyes may be conjugated to one or more substances including other dyes.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: February 26, 2013
    Assignee: Applied Biosystems, LLC
    Inventors: Joe Y. L. Lam, Steven M. Menchen, Ruiming Zou, Scott C. Benson
  • Patent number: 8377910
    Abstract: The invention relates to sphingosine derivative compounds, like D-erythro-sphingosine 1-phosphate (S1P), to be used as immunomodulators in a microbicidal treatment of infections derived from bacteria and specifically Mycobacterium tuberculosis. Such compounds are characterized in that they stimulate macrophagic Phospholipase D (PLD) (FIG. 1). The invention further relates to pharmaceutical compositions containing sphingosine derivative compounds and diagnostic methods for the preparation thereof. Further objects of the invention are methods of inducing or restoring the microbicidal activity in vitro of macrophages for monitoring the efficiency of phagocytosis and degradation processes performed by the same and assay methods suitable to evaluate therapeutic effectiveness of candidate microbicides.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: February 19, 2013
    Assignee: Universita Degli Studi di Roma “Tor Vergata”
    Inventors: Maurizio Fraziano, Sanjay Kumar Garg, Antonio Ciaramella, Giovanni Auricchio, Elisabetta Volpe, Angelo Martino, Patrizia Morena Baldihi, Paolo De Vito, Domenico Galati, Vittorio Colizzi
  • Patent number: 8378136
    Abstract: The subject of the present invention is a process for preparing acrolein by dehydration of glycerol in the presence of a catalyst system comprising oxygen, phosphorus and at least one metal chosen from vanadium, boron or aluminium. The process is preferably carried out in the gas phase in the presence of oxygen starting from aqueous solutions of glycerol.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: February 19, 2013
    Assignee: Arkema France
    Inventor: Jean-Luc Dubois
  • Patent number: 8378083
    Abstract: This invention relates to bis-azo colorants for use as bluing agents, laundry care compositions comprising bis-azo colorants that may serve as bluing agents, processes for making such bluing agents and laundry care compositions and methods of using the same. The bluing agents are generally comprised of at least two components: at least one chromophore component and at least one polymeric component. These bluing agents are advantageous in providing a whitening effect to fabrics, while not building up over time and causing undesirable blue discoloration to the treated fabrics.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: February 19, 2013
    Assignee: Milliken & Company
    Inventors: Robert L. Mahaffey, Jr., Xiaoyong Michael Hong, Eduardo Torres, Dominick J Valenti, Gregory S Miracle
  • Patent number: 8377641
    Abstract: Disclosed is a group of azo quencher compositions useful as fluorescence quenchers having the general structure of formula 1, methods of making or using the compositions, and kits comprising the composition.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: February 19, 2013
    Assignee: Integrated DNA Technologies, Inc.
    Inventors: Andrei Laikhter, Mark Aaron Behlke, Joseph Walder, Kevin William Roberts, Yawfui Yong
  • Patent number: 8377911
    Abstract: A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: February 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Lin Yan
  • Patent number: 8372822
    Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: February 12, 2013
    Assignee: Pliva Hrvatska D.O.O.
    Inventors: Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
  • Patent number: 8373002
    Abstract: Organic compounds containing at least one site of ethylenic unsaturation are catalytically hydrocyanated and the medium of hydrocyanation is separated into desired linear organic compounds containing at least one nitrile function, e.g., 3-pentenenitrile, and undesired nitrile by-products, e.g., methylglutaronitrile, and the undesired nitrile by-products are hydrodenitrogenated into ammonia and at least one hydrocarbon compound under an absolute hydrogen pressure ranging from 0.1 to 10 MPa at a temperature ranging from 200° to 500° C. and in the presence of a hydrodenitrogenation catalyst.
    Type: Grant
    Filed: January 12, 2009
    Date of Patent: February 12, 2013
    Assignees: Rhodia Operations, Centre National de la Recherche Scientifique
    Inventors: Philippe Marion, Amélie Hynaux, Dorothée Laurenti, Christophe Geantet
  • Patent number: 8367857
    Abstract: To provide a novel method for producing an isothiocyanate compound having a carboxyl group(s) from the corresponding amino compound having a carboxyl group(s). A method for producing an isothiocyanate compound which has a carboxyl group(s) and is represented by the formula (2). And the method comprises reacting an amino compound which has a carboxyl group(s) and is represented by the formula (1) (wherein A is e.g. a C6-14 aromatic hydrocarbon group or a C1-12 saturated hydrocarbon group, and B is e.g. a single bond, a C6-14 aromatic hydrocarbon group or a C1-12 saturated hydrocarbon group), in a solvent, with carbon disulfide (CS2) and then with a halogen as a simple substance.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: February 5, 2013
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Satoshi Nakano, Daisuke Saito
  • Patent number: 8367847
    Abstract: Methods for the preparation of the high intensity sweetener, monatin, 3-(1-amino-1,3-dicarboxy-3-hydroxy-but-4-yl)indole, its salts and internal condensation products thereof, including methods applicable to the large-scale production of monatin are described.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: February 5, 2013
    Assignee: Cargill, Incorporated
    Inventors: Subash Buddoo, Amanda Louise Rousseau, Gregory E. R. Gordon
  • Patent number: 8367812
    Abstract: The synthesis of purified functionalized organosilicon compounds containing at least one active azo group having formula (I): [(G0)3SiO1/2]m[(G0)2SiO2/2]n[G0SiO3/2]o[SiO4/2]p[(G2)a(G1)a?(Z—CO—HN?NH—CO-A)SiO(3-a-a?)/2] entails providing at least one hydrazino (—HN—NH—) precursor (II) of the compound (I) and oxidizing the precursor (II) into an azo group specific to the compound (I) with the aid of an oxidizing system comprising at least one oxidant (Ox) and at least one base (B), wherein 1) Ox is selected from among the oxidants that can oxidize a hydrazine function into an azo function, with or without the exclusion of N-bromosuccinimide (NBS), 2) and/or Ox (optionally B) is/are employed in stoichiometric quantities in relation to the precursor (II); 3) and/or the organosilicon compounds (I) thus prepared are subjected to a purification post-treatment to eliminate any unwanted residues of the base B used, with the proviso that, when NBS is not excluded, characteristic (1) is combined with characteristic (2) a
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: February 5, 2013
    Assignee: Rhodia Chimie
    Inventor: Sébastien Sterin
  • Patent number: 8367664
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: January 23, 2007
    Date of Patent: February 5, 2013
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Patent number: 8362278
    Abstract: The present invention discloses processes for producing substituted pyrrole compounds, such as 2,5-disubstituted pyrroles. Synthetic processes which directly convert substituted furan compounds to substituted pyrrole compounds, via a reaction of the substituted furan compound with ammonia and/or an ammonium salt in the presence of a catalyst, also are described.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: January 29, 2013
    Assignee: Chevron Phillips Chemical Company LP
    Inventors: Bruce E. Kreischer, Orson L. Sydora, Steven Hutchinson, Eduardo J. Baralt, Ron D. Knudsen