Patents Examined by Brenda Coleman
  • Chiral disulfonimides
    Patent number: 9079869
    Abstract: Chiral disulfonimides having the formula I to III, wherein at least one of the groups A and B in the compound of formula I, C and D of the compound in formula II, and E and F of the compound in formula III is a chiral group, or E and F together form a chiral backbone, X is C, Si, O, N or S, and n is 0, 1, 2, 3, 4, 5 or 6, where n is >1 only if X is C, and G is as defined herein, and to the organic salts, metal salts and metal complexes thereof, are suited as NMR shift reagents and as reagents for racemate splitting, and also as chiral Brønsted acid catalysts or chiral Lewis acid catalysts for activating ketones, aldehydes and alkenes, and also as catalysts in the organic synthesis.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: July 14, 2015
    Assignee: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Benjamin List, Frank Lay, Pilar Garcia Garcia
  • Polymorph of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzylcarbamoyl)-L-proline--dimethylamide
    Patent number: 9079881
    Abstract: The invention provides a new polymorph of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzyl-carbamoyl)-L-proline-N,N-dimethylamide, pharmaceutical compositions containing it and its use in therapy.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: July 14, 2015
    Assignee: Vantia Limited
    Inventors: Kjellström Henrik Johan, Johansson Erik Björn, Vilhelmsen Thomas
  • Treatment of age-related macular degeneration
    Patent number: 9072749
    Abstract: Methods and compounds are disclosed for treating dry age-related macular degeneration, and preventing or delaying the onset of wet age-related macular degeneration.
    Type: Grant
    Filed: November 30, 2009
    Date of Patent: July 7, 2015
    Inventors: Joseph Weinstock, Sarah Jane Paikowsky
  • Tosylate salt of cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4, 10-dihydro-3H-2,3,4,9-tetrabenzo[f]azulene-9-carbonyl)-2-fluorobenzylamide
    Patent number: 9073928
    Abstract: The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: July 7, 2015
    Assignee: Vantia Limited
    Inventors: Andrzej Roman Batt, Rachel Louisa Charlotte Handy, Michael Bryan Roe, Valerie Elizabeth Peal, Timothy John Kenhardt Gibs, David Raymond Churchley
  • 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
    Patent number: 9067924
    Abstract: The present invention relates to 1,4 Thiazepines/Sulfones of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: June 30, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Hans Hilpert, Mark Rogers-Evans, Didier Rombach
  • Preparation method of rocuronium
    Patent number: 9067965
    Abstract: A method for preparing rocuronium is disclosed. 2?-(4-Morpholinyl)-16?-(1-pyrrolidinyl)-5?-androstan-3?-ol-17?-acetate is used as a starting material and is directly reacted with 3-bromopropene at ambient temperature to produce rocuronium.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: June 30, 2015
    Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd.
    Inventors: Zhiwen Zeng, Wenling Zhang, Peng Wang, Xini Zhang
  • Substituted glycinamides, process for their manufacture and use thereof as medicaments
    Patent number: 9062034
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: June 23, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
  • Phosphate esters of noribogaine
    Patent number: 9051343
    Abstract: Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: June 9, 2015
    Assignee: DEMERX, INC.
    Inventors: Richard D. Gless, Jr., Robert M. Moriarty
  • Processes for the preparation of 5-HTreceptor agonists
    Patent number: 9045431
    Abstract: Processes and intermediates for preparing salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and pharmaceutically acceptable solvates and hydrates thereof, that are useful for, inter alia, weight management.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: June 2, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Anna Shifrina
  • Production method for isoquinoline derivatives and salts thereof
    Patent number: 9045460
    Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 2, 2015
    Assignee: KOWA CO., LTD.
    Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Substituted noribogaine
    Patent number: 9045481
    Abstract: This invention relates noribogaine derivatives, compositions and methods of use thereof.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: June 2, 2015
    Assignee: DEMERX, INC.
    Inventors: Deborah C. Mash, Richard D. Gless, Jr., Robert M. Moriarty
  • 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
    Patent number: 9045468
    Abstract: The compounds of the present invention are represented by the following 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives having formula (I): where the carbon atom designated * is in the R or S configuration when n is 1 and the substituents X and R1-R7 are as defined herein.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: June 2, 2015
    Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Peter R. Guzzo, Shuang Liu, Kristen N. Ryan, Bruce F. Molino, Russell DeOrazio, Richard E. Olson, John E. Macor
  • Antifungal 5,6-dihydro-4H-pyrrolo[1,2-?][1,4]-benzodiazepines and 6H-pyrrolo[1,2-?][1,4]benzodiazepines substituted with benzene derivatives
    Patent number: 9040523
    Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines of Formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: May 26, 2015
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit
  • Antifungal 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]-benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with bicycle benzene derivatives
    Patent number: 9040524
    Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with bicyclic benzene derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: May 26, 2015
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit
  • Chemical compounds
    Patent number: 9040518
    Abstract: Compounds of Formula I and methods for treating metabolic disorders are disclosed.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: May 26, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Christopher Joseph Aquino, Jon Loren Collins, David John Cowan, Yulin Wu
  • Pyrazolopyrimidines as metabotropic glutamate 5 receptor antagonists
    Patent number: 9029360
    Abstract: This invention relates to novel pyrazolopyrimidines and their use as metabotropic glutamate 5 receptor antagonists (mGlu5 receptor antagonists), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of mGlu5 receptor mediated disorders.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: May 12, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Heiner Ebel, Doris Riether, Bernd Wellenzohn
  • Benzodiazepine bromodomain inhibitor
    Patent number: 9023842
    Abstract: The present invention relates to a benzodiazepine compound of formula (I), processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: May 5, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Romain Luc Marie Gosmini, Olivier Mirguet
  • Method for purifying rocuronium bromide
    Patent number: 9024013
    Abstract: Provided is a method for purifying rocuronium bromide, which comprises: formulating crude rocuronium bromide to be purified into an aqueous solution, distilling off excess residue solvents at reduced pressure, absorbing by adding active carbon or silica gel, then filtrating, quick freezing the filtrate into ice, and then lyophilizing to obtain rocuronium bromide.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: May 5, 2015
    Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd
    Inventors: Zhiwen Zeng, Peng Wang, Wenling Zhang, Xini Zhang
  • Process for preparing tolvaptan intermediates
    Patent number: 9024015
    Abstract: The present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: May 5, 2015
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Maruthi Janakiram Reddy, Bandi Vamsi Krishna
  • Gabaergic receptor subtype selective ligands and their uses
    Patent number: 9006233
    Abstract: Described herein are ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: April 14, 2015
    Assignee: UWM Research Foundation, Inc.
    Inventors: James M. Cook, Terry S. Clayton, Hiteshkumar D. Jain, Sundari K. Rallipalli, Yun Teng Johnson, Jie Yang, Michael Ming-jin Poe, Ojas A. Namjoshi, Zhi-jian Wang