Patents Examined by Kahsay T. Habte
  • Hydroxylation of ?-dicarbonyls with zirconium catalysts
    Patent number: 8258345
    Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: September 4, 2012
    Assignee: E I du Pont de Nemours and Company
    Inventor: Albert Loren Casalnuovo
  • 7, 8 and 9-substituted tetracycline compounds
    Patent number: 8252777
    Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: August 28, 2012
    Assignee: Trustees of Tufts College
    Inventors: Mark L. Nelson, Darrell J. Koza, Glen Rennie
  • Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof
    Patent number: 8242113
    Abstract: Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: August 14, 2012
    Assignee: Legochem Biosciences, Inc.
    Inventors: Young Lag Cho, Sang Eun Chae, Sung Yoon Baek, Yeon Ok Kim, Seong Jin Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Phosphorus-containing benzoxazines and preparing method thereof
    Patent number: 8242266
    Abstract: The Phosphorus-containing bisphenols and preparing method thereof are disclosed. A method for producing the phosphorus-containing bisphenol of the formula (1) includes reacting compounds respectively defined by a formula (a), (b), (c) and an acid catalyst to yield compounds of phosphorus-containing bisphenol.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: August 14, 2012
    Assignees: National Chunghsing University, Chang Chun Plastics Co., Ltd
    Inventors: Ching-Hsuan Lin, Chia-Wei Chang, Tsung-Li Lin, Kuen-Yuan Hwang, An-Pang Tu, Fang-Hsien Su
  • Polymorphs of efavirenz
    Patent number: 8242267
    Abstract: The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.
    Type: Grant
    Filed: July 1, 2011
    Date of Patent: August 14, 2012
    Assignee: Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
  • Cyclic inhibitors of 11?-hydroxysteroid dehydrogenase 1
    Patent number: 8242111
    Abstract: This invention relates to novel compounds of a structural formula selected from: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals, e.g., diabetes mellitus and obesity. Values for the variables in the structural formulas are provided herein. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: August 14, 2012
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Katerina Leftheris, Colin M. Tice, Yuanjie Ye, Suresh B. Singh
  • 5,6-dihydro-1H-pyridin-2-one compounds
    Patent number: 8236948
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: August 7, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich
  • Benzimidazoledihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, and pharmaceutical compositions comprising same
    Patent number: 8232272
    Abstract: The present invention relates to novel benzimidazole-dihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, to processes for the preparation thereof and to the use thereof in therapy, especially for the treatment of diabetes.
    Type: Grant
    Filed: October 13, 2008
    Date of Patent: July 31, 2012
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Gerard Botton, Caroline Leriche, Annick Arbellot de Vacqueur, Annick Audet, Johannes Gleitz
  • Process for preparing acyl amide compounds
    Patent number: 8222408
    Abstract: A process for preparing acyl amide compounds is described, in which a recrystallized o-nitrophenoxy carbonyl compound is hydrogenated with hydrogen gas in the presence of a nickel sponge metal catalyst with ring closure to form a benzoxazine, which is then reacted with an acyl halide to give the corresponding acyl amide compound.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: July 17, 2012
    Assignee: SALTIGO GmbH
    Inventors: Matthias Boll, Burkhard Koch
  • [1,2,4]Thiadiazin-3-yl acetic acid compound and methods of making the acetic acid compound
    Patent number: 8222404
    Abstract: The invention is directed to a [7-methanesulfonylamino-methyl)-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-3-yl]-acetic acid compound and to methods of making the same.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: July 17, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Peter Dragovich, Douglas Eric Murphy
  • Chemical compounds
    Patent number: 8217034
    Abstract: The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: July 10, 2012
    Assignees: Shionogi & Co., Ltd., GlaxoSmithKline LLC
    Inventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
  • Prodrugs of 2,4-pyrimidinediamine compounds and their uses
    Patent number: 8211889
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: July 3, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Thomas Sun, Valentino J. Stella
  • Thiadiazinone derivatives
    Patent number: 8211886
    Abstract: Compounds of the formula (I), which are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed for the treatment of tumours.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: July 3, 2012
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Prodrugs of 2,4-pyrimidinediamine compounds and their uses
    Patent number: 8211888
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: July 3, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Chiral fused [1,2]imidazo[4,5-] ring compounds
    Patent number: 8207162
    Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: June 26, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: George W. Griesgraber, Sarah J. Slania
  • Compositions, synthesis, and methods of using piperazine based antipsychotic agents
    Patent number: 8207163
    Abstract: The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: June 26, 2012
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Substituted piperidines
    Patent number: 8202862
    Abstract: The invention relates to compounds of the formula to processes for the preparation thereof, and to the use thereof for treatment and/or prophylaxis of cardiovascular diseases and tumour diseases.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: June 19, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
  • Fused aminodihydrothiazine derivative
    Patent number: 8198269
    Abstract: A compound represented by the general formula: wherein Ring A is a C6-14 aryl group or the like, L is —NRLCO— or the like (wherein RL is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a C1-3 alkylene group or the like, Z is an oxygen atom or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: June 12, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Takafumi Motoki, Kunitoshi Takeda, Yoichi Kita, Mamoru Takaishi, Yuichi Suzuki, Tasuku Ishida
  • Colorimetric detection of cyanide with a chromogenic oxazine
    Patent number: 8198436
    Abstract: A chromogenic oxazine compound for the colorimetric detection of cyanide was designed. Indeed, the [1,3]oxazine ring of our compound opens to form a phenolate chromophore in response to cyanide. The heterocyclic com-pound may be comprised of fused benzooxazine and indoline rings: wherein R1 is an alkyl (e.g., methyl, ethyl, propyl, isopropyl, butyl, isobutyl), a substituted alkyl, a cycloalkyl (e.g., cyclopentyl, cyclohexyl), a substituted cycloalkyl, an aryl (e.g., phenyl), or a substituted aryl and R2 is a chromophore (e.g., nitroso, nitro, azo dyes). This quantitative chromogenic transformation permits the detection of micromolar concentrations of cyanide in water. Furthermore, our chromogenic oxazine is insensitive to the presence of large concentrations of fluoride, chloride, bromide or iodide anions, which are generally the principal interferents in the colorimetric detection of cyanide.
    Type: Grant
    Filed: September 1, 2006
    Date of Patent: June 12, 2012
    Assignee: The University of Miami
    Inventors: Francisco M. Raymo, Massimiliano Tomasulo
  • C-phenyl-substituted cyclic ketonols
    Patent number: 8193120
    Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols, to a plurality of processes for their preparation and to their use as pesticides as herbicides.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: June 5, 2012
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb