Patents Examined by John Mabry
  • One pot process for producing 6-hydroxyl nal-opiate
    Patent number: 9012468
    Abstract: The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: April 21, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang
  • Camptothecin derivatives having anti-tumor activity
    Patent number: 9006439
    Abstract: Disclosed are novel camptothecin derivatives having anti-tumor activity (the basic structure thereof is as shown in the figure) and compositions of such compounds and use thereof. The compounds according to the present invention exhibit very good water solubility and stability, show good selectivity among drugs of the same category, and have a very high therapeutic index. Such compounds are promising as therapeutic agents for treating tumors.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: April 14, 2015
    Assignee: Ningbo Team Pharmaceutical Co., Ltd
    Inventors: Xiaoguang Lei, Xiuguo Zhang
  • Cannabinoid receptor modulators
    Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Cyclopropylamine derivatives useful as LSD1 inhibitors
    Patent number: 9006449
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: April 14, 2015
    Assignee: Oryzon Genomics, S.A.
    Inventors: Matthew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martinez, Nuria Valls Vidal
  • Substituted fused pyrimidinones and dihydropyrimidinones
    Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Processes for the preparation of 4?-[3-[4-(6-Fluoro-1 ,2-benzisoxazol-3-yl)piperidino]propoxy]-3?-methoxyacetophenone and intermediates thereof
    Patent number: 9000221
    Abstract: The present invention relates to processes for the preparation of 4?-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3?-methoxyacetophenone and intermediates thereof. The present invention also provides a process for purifying 4?-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3?-methoxyacetophenone to obtain the purity greater than about 98.0 area % to about 99.0 area % as measured by HPLC, preferably greater than about 99.0 area % to about 99.5 area %, more preferably greater about 99.5 area % to about 99.9 area %. individual impurities lower than about 0.15 area %, preferably lower than about 0.1% and total impurities lower than about 0.5 area % by HPLC.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: April 7, 2015
    Assignee: Symed Labs Limited
    Inventors: Dodda Mohan Rao, Pingili Krishna Reddy, Buthukuri Venkat Reddy
  • Bicyclic GPR119 modulators
    Patent number: 9000175
    Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
    Type: Grant
    Filed: November 24, 2011
    Date of Patent: April 7, 2015
    Assignee: Lupin Limited
    Inventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
  • Iodoarene derivative, method for manufacturing optically active spirolactone compound by using the same, and method for manufacturing optically active cycloadduct
    Patent number: 9000216
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: April 7, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Compounds for the treatment of addiction
    Patent number: 9000015
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Grant
    Filed: August 13, 2013
    Date of Patent: April 7, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Highly pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione and methods of preparing same
    Patent number: 9000005
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 7, 2015
    Assignee: ArQule, Inc.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Amide compound or salt thereof, biofilm inhibitor, biofilm remover and disinfectant containing the same
    Patent number: 9000190
    Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
    Type: Grant
    Filed: April 29, 2014
    Date of Patent: April 7, 2015
    Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.
    Inventors: Hiroaki Suga, Jun Igarashi
  • 4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics
    Patent number: 8993596
    Abstract: 4-(Azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: March 31, 2015
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Karine Bouquet, Sandrine Talano, Corinne Millois Barbuis
  • Synthesis of cyclometallated platinum(II) complexes
    Patent number: 8987451
    Abstract: A single-step method of making tetradentate platinum complexes is disclosed. The method advantageously allows the formation of a platinum complex in a single step, even with sterically hindered ligands, without the use of highly reactive intermediates. The compounds made by the disclosed method are useful in OLED applications.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: March 24, 2015
    Assignee: Universal Display Corporation
    Inventors: Jui-Yi Tsai, Gregg Kottas, Walter Yeager
  • 7-azaindole derivatives
    Patent number: 8981101
    Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: March 17, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
  • Use of novel coumarins as glutathione and thiol labels
    Patent number: 8981100
    Abstract: Fluorescent quinolizinocoumarin compounds substituted with electrophilic reactive groups that bind thiol compounds are described. The compounds are useful in detecting oxidative stress and processes associated therewith in live cells.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: March 17, 2015
    Assignee: Life Technologies Corporation
    Inventors: Hee Chol Kang, Kyle Gee, Iain Johnson, Michael Janes
  • Indenopyridine derivatives
    Patent number: 8975405
    Abstract: Disclosed is a compound of formula (I) and salts thereof. Also disclosed are methods of making the compound of formula (I) and the use of the compound as an intermediate for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: March 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bo Qu, Anjan Saha, Jolaine Savoie, Xudong Wei, Nathan K. Yee
  • Beta-lactamase inhibitors
    Patent number: 8969570
    Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: March 3, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
  • Calcium salt of pyrroloquinoline quinone
    Patent number: 8969563
    Abstract: An object of the present invention is to provide an industrially useful method for producing a calcium salt of pyrroloquinoline quinone, without using large amounts of organic solvents, and highly pure crystals produced thereby. According to the present invention, a highly pure calcium salt of pyrroloquinoline quinone can be produced by reacting an alkali metal salt of pyrroloquinoline quinone with a source of calcium ions.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 3, 2015
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Kazuto Ikemoto, Masahiko Nakano
  • Compounds for the inhibition of cellular proliferation
    Patent number: 8969573
    Abstract: Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: March 3, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Michael Chorev, Bertal Huseyin Aktas, Jose A. Halperin, Gerhard Wagner
  • Pyrazole compounds
    Patent number: 8962845
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: February 24, 2015
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Chun-Ping Chang, Yu-Sheng Chao