Patents Examined by Zinna N. Davis
  • Pharmaceutical composition
    Patent number: 7538125
    Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.
    Type: Grant
    Filed: September 20, 2006
    Date of Patent: May 26, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Vanilloid receptor modulators
    Patent number: 7538121
    Abstract: Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, P, X, Y, q, r ans s 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 13, 2003
    Date of Patent: May 26, 2009
    Assignee: Glaxo Group Limited
    Inventors: Gregor James MacDonald, Darren Jason Mitchell, Harshad Kantilal Rami, Mervyn Thompson, Susan Marie Westaway
  • Compounds having 4-pyridylalkylthio group as substituent
    Patent number: 7534802
    Abstract: A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a pharmaceutical. Compound represented by the following general formula [I] or salts thereof are useful as therapeutic agents for diseases in which angiogenesis or augmentation of vascular permeability is involved. In the formula, ring “A” is a benzene ring or an aromatic five- or six-memberd heterocycle which can be fused with a cycloalkane ring, “B” is alkylene, R1 and R2, the same or different, are H, OH, substituted or unsubstituted alkoxy and the like, X and Y, the same or different, are group(s) selected from H, halogen, OH, substituted or unsubstituted alkoxy and the like respectively, p is 0, 1 or 2, and q is 0 or 1.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: May 19, 2009
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
  • Preparation of olmesartan medoxomil
    Patent number: 7528258
    Abstract: The present invention provides a process for preparing olmesartan medoxomil.
    Type: Grant
    Filed: September 2, 2005
    Date of Patent: May 5, 2009
    Assignee: Teva Pharmaceutical Industries Ltd
    Inventors: Lilach Hedvati, Gideon Pilarsky
  • Urea derivatives having vanilloid receptor antagonist activity
    Patent number: 7528150
    Abstract: According to the invention there are provided compounds of formula (I) wherein R1, p, P, n, s, r, W, P?, t, R2 and q are as defined in the specification, processes for preparing them and their use in therapy.
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: May 5, 2009
    Assignee: Glaxo Group Limited
    Inventors: Gregor James MacDonald, Harshad Kantilal Rami, Mervyn Thompson
  • Substituted 1-pyrrolo[2,3-b]pyridines and preparation thereof
    Patent number: 7528146
    Abstract: The invention relates to novel substituted 1H-pyrrolo[2,3-b]pyridines of the general formula (I) to processes for their preparation and to intermediates therefor.
    Type: Grant
    Filed: December 9, 2005
    Date of Patent: May 5, 2009
    Assignee: LANXESS Deutschland GmbH
    Inventors: Wolfgang Ebenbeck, Perez Santiago Figueroa, Hartmut Schirok
  • Process for the preparation of nicotinaldehydes
    Patent number: 7528256
    Abstract: The invention relates to a process for the preparation of nicotinaldehydes by reduction of the corresponding nicotinic acid morpholinamides.
    Type: Grant
    Filed: March 27, 2004
    Date of Patent: May 5, 2009
    Assignee: Merck Patent GmbH
    Inventors: Heinz-Hermann Bokel, Mike Brandner, Ludwig Gantzert, Ralf Knierieme
  • Process for the preparation of a hydrate of an anthranilic acid derivative
    Patent number: 7524861
    Abstract: A hydrate of an acid addition bis-salt of an anthranilic acid derivative is produced by a process which comprises: (a) combining, in any order, the anthranalic acid derivative, a pharmaceutically acceptable organic solvent, an excess of water and a pharmaceutically acceptable strong acid to form a mixture; (b) warming the mixture until a clear solution forms; (c) filtering the solution while it is warm, to yield a filtrate; and (d) recovering the hydrate as defined above from the filtrate. The hydrate has a defined number of moles of water of crystallization and possesses better storage stability and dissolution characteristics than conventionally produced hydrates of such acid addition bis-salts.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: April 28, 2009
    Inventors: David Frank Hayman, Michael Wright
  • Biaryloxymethylarenecarboxylic acids as glycogen synthase activators
    Patent number: 7524870
    Abstract: The present invention relates to compounds of formula (I) wherein Ar, Ar2, R2, R3, R4, m, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
    Type: Grant
    Filed: November 21, 2005
    Date of Patent: April 28, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Gillespie, Robert Alan Goodnow, Jr., Jefferson Wright Tilley
  • Compounds that stimulate glucose utilization and methods of use
    Patent number: 7524885
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, I, m and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: April 28, 2009
    Assignee: The Governors of the University of Alberta
    Inventors: Gary D. Lopaschuk, John C Vederas, Jason R. Dyck
  • Process for producing 5-(2?-pyridyl)-2-pyridone derivative
    Patent number: 7524967
    Abstract: The present invention provides a method of industrially and advantageously producing a 5-(2?-pyridyl)-2-pyridone derivative. The present invention relates to a production method of a 5-(2?-pyridyl)-2-pyridone derivative represented by the formula (VI), which includes reacting a pyridine derivative of the formula (I) with a brominating agent to give a 5-bromopyridine derivative of the formula (II), reacting the obtained 5-bromopyridine derivative with a metallizing agent to give an organometallic compound of the formula (III), reacting the obtained organometallic compound with a 2-sulfonylpyridine derivative of the formula (IV) to give a 6-alkoxy-3,2?-bipyridine derivative of the formula (V) and hydrolyzing the obtained 6-alkoxy-3,2?-bipyridine derivative: wherein each symbol is as defined in the Description.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: April 28, 2009
    Assignees: Kuraray Co., Ltd., Eisai R & D Management Co., Ltd.
    Inventors: Kenichi Koyakumaru, Yoshimi Fukunaga, Youichi Satake
  • Manufacturing process for facial tris-cyclometallated complexes
    Patent number: 7517984
    Abstract: A process for forming a facial tris-cyclometallated iridium or rhodium complex isomer comprises heating an original composition containing (a) a meridional isomer of a tris-cyclometallated iridium or rhodium complex in (b) an organic hydrocarbon solvent, a halogenated hydrocarbon solvent, or a combination thereof, to a reaction temperature of least 150° C. for a time sufficient to form a product containing the facial isomer in an increased ratio to meridional isomer compared to the original composition. The process is simple and efficient and provides improved purity.
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: April 14, 2009
    Assignee: Eastman Kodak Company
    Inventor: Shouquan Huo
  • Bichalcophenes and their prodrugs as antiprotozoal agents
    Patent number: 7517893
    Abstract: Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: April 14, 2009
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: Richard R. Tidwell, David W. Boykin, Chad Stephens, Mohamed A. Ismail, W. David Wilson, Reto Brun, Karl Werbovetz
  • Nicotinamide derivatives useful as p38 inhibitors
    Patent number: 7514456
    Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: April 7, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Nicola Mary Aston, Paul Bamborough, Ann Louise Walker
  • Inhibitors against complex II of electron transport system
    Patent number: 7514455
    Abstract: An electron transport system complex II inhibitor comprising 2-pyridinol derivative represented by the general formula [I] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or its tautomer 2-pyridone derivative represented by the general formula [II] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or salt thereof as an active ingredient. The compound inhibits the complex II strongly with nM order activity. Consequently, 2-pyridinol derivative or its tautomer, 2-pyridone derivative, are useful as the complex II inhibitor.
    Type: Grant
    Filed: June 10, 2002
    Date of Patent: April 7, 2009
    Assignee: The Kitasato Institute
    Inventors: Satoshi Omura, Kazuro Shiomi, Hiroshi Tomoda, Rokuro Masuma, Kiyoshi Kita
  • Inhibitors of ?-lactamase
    Patent number: 7514556
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: April 7, 2009
    Assignee: Methylgene Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Diamine calcium channel blockers
    Patent number: 7511077
    Abstract: Aromatic derivatives of aliphatic diamines are effective in ameliorating conditions characterized by unwanted calcium ion channel activity, especially T-type and N-type channels. These conditions include, for example, stroke and pain.
    Type: Grant
    Filed: February 8, 2006
    Date of Patent: March 31, 2009
    Assignee: Neuromed Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Terrance P. Snutch, Francesco Belardetti
  • Opiate intermediates and methods of synthesis
    Patent number: 7511060
    Abstract: Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: March 31, 2009
    Assignee: Mallinckrodt Inc.
    Inventors: Peter Xianqi Wang, Frank W. Moser
  • Triazole compounds
    Patent number: 7511042
    Abstract: Disclosed are compounds of formula (I) Where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines and are thus useful for treating cytokine mediated diseases. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 1, 2004
    Date of Patent: March 31, 2009
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Derek Cogan, Daniel R. Goldberg, Abdelhakim Hammach, Matthew Russell Netherton, Ronald A. Aungst
  • Substituted aryl-amine derivatives and methods of use
    Patent number: 7507748
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II wherein R, R1 and R2 for each formula are defined herein. The invention further includes analogs, prodrugs and pharmaceutically acceptable salts and derivatives of Formulas I and II, as well as pharmaceutical compositions, medicaments and methods thereof for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: July 19, 2005
    Date of Patent: March 24, 2009
    Assignee: Amgen Inc.
    Inventor: Chester Chenguang Yuan