Patents Examined by Sabiha N. Qazi
  • Neuroactive substituted cyclopent[]anthracenes as modulators for GABA type-A receptors
    Patent number: 9562026
    Abstract: The present disclosure is generally directed to neuroactive substituted cyclopent[a]anthracenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: February 7, 2017
    Assignee: WASHINGTON UNIVERSITY
    Inventor: Douglas Covey
  • Amphiphilic compounds
    Patent number: 9556217
    Abstract: Bringing membrane proteins into aqueous solution generally requires the use of detergents or other amphiphilic agents. The invention provides a new class of amphiphiles, each of which includes a multi-fused ring system as a lipophilic group. These new amphiphiles confer enhanced stability to a range of membrane proteins in solution relative to conventional detergents, leading to improved structural and functional stability of membrane proteins, including integral membrane proteins. Accordingly, the invention provides new amphiphiles for biochemical manipulations and characterization of membrane proteins. These amphiphiles display favorable behavior with membrane proteins and can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: January 31, 2017
    Assignees: Wisconsin Alumni Research Foundation, The Board of Trustees of the Leland Stanford Junior University
    Inventors: Samuel Helmer Gellman, Pil Seok Chae, Brian Kobilka, Soren Rasmussen
  • Solid mixtures based on sulfonylureas and adjuvants
    Patent number: 9538757
    Abstract: Solid mixtures comprising a) an active compound from the group consisting of the sulfonylureas, and b) an alkylpolyglucoside.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: January 10, 2017
    Assignee: BASF SE
    Inventors: Mathias Bratz, Karl-Friedrich Jäger
  • Method for monofluoromethylation of organic substrates to prepare biologically active organic compounds
    Patent number: 9540413
    Abstract: Described herein is a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for example, S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium tetrafluoroborate as monofluoromethylating reagent instead of bromofluoromethane.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: January 10, 2017
    Assignee: HOVIONE INTER LIMITED
    Inventor: Emilia Perpetua Tavares Leitao
  • Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
    Patent number: 9533995
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: January 3, 2017
    Assignee: Sanofi
    Inventors: Zhongli Gao, Daniel Hall, David Stefany
  • Synergistic microbicidal combinations
    Patent number: 9532571
    Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: January 3, 2017
    Assignee: Rohm and Haas Company
    Inventors: Megan Anne Diehl, Eileen Fleck Warwick
  • Steroid analogues for neuroprotection
    Patent number: 9527881
    Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: December 27, 2016
    Assignee: Emory University
    Inventors: Christopher Macnevin, Donald G. Stein, Dennis C. Liotta, Iqbal Sayeed, David B. Guthrie, Mark A. Lockwood, Michael G. Natchus
  • Methods for synthesizing substituted tetracycline compounds
    Patent number: 9522872
    Abstract: Methods of synthesizing substituted tetracycline compounds are provided.
    Type: Grant
    Filed: July 7, 2008
    Date of Patent: December 20, 2016
    Assignee: PARATEK PHARMACEUTICALS, INC.
    Inventors: Farzaneh Seyedi, Tadeusz Warchol, Mark Grier
  • Synergistic microbicidal combinations
    Patent number: 9497969
    Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: November 22, 2016
    Assignee: Rohm and Haas Company
    Inventors: Megan Anne Diehl, Eileen Fleck Warwick
  • Synergistic microbicidal combinations
    Patent number: 9497968
    Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: November 22, 2016
    Assignee: Rohm and Haas Company
    Inventors: Megan Anne Diehl, Eileen Fleck Warwick
  • Synergistic microbicidal combinations
    Patent number: 9491945
    Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: November 15, 2016
    Assignee: Rohm and Haas Company
    Inventors: Megan Anne Diehl, Eileen Fleck Warwick
  • Certain chemical entities, compositions, and methods
    Patent number: 9493503
    Abstract: Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: November 15, 2016
    Assignee: NeuPharma, Inc.
    Inventor: Xiangping Qian
  • 5,6-Dialkyl-7-aminotriazolopyrimidines, their preparation and their use for controlling harmful fungi, and compositions comprising these compounds
    Patent number: 9487519
    Abstract: 5,6-Dialkyl-7-aminotriazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl or alkoxyalkyl, where the aliphatic groups may be substituted as defined in the description; R2 is CHR3CH3, cyclopropyl, CH?CH2 or CH2CH?CH2; R3 is hydrogen, CH3 or CH2CH3; processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: November 8, 2016
    Assignee: BASF SE
    Inventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Matthias Niedenbrück, Maria Scherer, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
  • Low calcemic, highly antiproliferative, analogs of calcitriol
    Patent number: 9481646
    Abstract: The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: November 1, 2016
    Assignee: The Johns Hopkins University
    Inventors: Gary H. Posner, Kimberly S. Petersen, Lindsey C. Hess, Douglas T. Genna, Scott Borella
  • Synergistic microbicidal combinations
    Patent number: 9480258
    Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: November 1, 2016
    Assignee: Rohm and Haas Company
    Inventors: Megan Anne Diehl, Eileen Fleck Warwick
  • Synergistic microbicidal combinations
    Patent number: 9474280
    Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: October 25, 2016
    Assignee: Rohm and Haas Company
    Inventors: Megan Anne Diehl, Eileen Fleck Warwick
  • Substituted diketopiperazines and their use as oxytocin antagonists
    Patent number: 9452169
    Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: September 27, 2016
    Assignee: GLAXO GROUP LIMITED
    Inventor: John Liddle
  • Substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides, preparation and therapeutic use thereof
    Patent number: 9453023
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: September 27, 2016
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Arthropodicidal anthranilamides
    Patent number: 9445593
    Abstract: This invention provides a method for soil systemic control of an invertebrate pest by contacting the soil with a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.
    Type: Grant
    Filed: July 15, 2015
    Date of Patent: September 20, 2016
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
  • Androgen receptor down-regulating agents and uses thereof
    Patent number: 9439912
    Abstract: The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: September 13, 2016
    Assignee: University of Maryland, Baltimore
    Inventors: Vincent C. O. Njar, Lalji K. Gediya, Puranik Purushottamachar, Abhijit Godbole, Andrew Kwegyir-Afful, Tadas Vasaitis