Patents Examined by Golam M M Shameem
  • Cyclopropylboronic compounds, preparation process thereof and use thereof
    Patent number: 9527798
    Abstract: Cyclopropylboronic compounds, the preparation process thereof and the use thereof.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: December 27, 2016
    Assignee: DIVERCHIM
    Inventors: Peter Oosting, Emmanuel Thomas, Rukiye Pamuk, Benoit Folleas, Jean-Louis Brayer, Benoit De Carne Carnavalet, Christophe Meyer, Janine Cossy
  • Oxidation of alcohol compounds via mesostructured VPO catalysts
    Patent number: 9522898
    Abstract: The present invention concerns a process for the production of an aldehyde compound by an oxidation reaction of an alcohol compound in the presence of a mesostructured vanadium phosphorus mixed oxide catalyst, at a temperature comprised between 50° C. and 200° C., in presence of an oxidant. The reaction medium may also comprise a solvent.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: December 20, 2016
    Assignees: RHODIA OPERATIONS, CENTRE NATIONAL DE LA RECHERECHE SCIENTIFIQUE
    Inventors: Jean-Marc Clacens, Floryan Decampo, Fabien Grasset, Benjamin Katryniok, Franck Dumeignil, Sebastien Paul, Veronique Rataj
  • Method for preparing an important intermediate of linagliptin
    Patent number: 9522915
    Abstract: The present invention discloses an improved process for preparing an important intermediate of linagliptin. In particular, disclosed are a process for preparing a compound V which is an important intermediate of linagliptin and has the structure V, and an industrial process of preparing linagliptin having excellent chemical and optical purities, which is an inhibitor of dipeptidyl peptidase-4 (DPP-IV), from the compound V. The process employs a phase-transfer catalyst, is high in yield, easy and simple to handle, environmentally friendly, suitable for industrial mass production, and can be implemented by a “one-pot process”.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: December 20, 2016
    Assignee: 2Y-CHEM, LTD.
    Inventors: Yanfeng Zhou, Yong Liu, Xuezhang Wang, Xungui He, Yuan Wang
  • Aadenosine receptor antagonists
    Patent number: 9522916
    Abstract: This invention relates to compounds of formula (I), Wherein R1-R4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: December 20, 2016
    Inventor: Constance Neely Wilson
  • Substituted Isoquinolin-1(2H)-one compounds, compositions, and methods thereof
    Patent number: 9522146
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: December 20, 2016
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yi)prop-2-en-1-one
    Patent number: 9518043
    Abstract: The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: December 13, 2016
    Assignee: Hanmi Pharm. Co., Ltd.
    Inventors: Keuk Chan Bang, Jae Hyuk Jung, Young Ho Moon
  • Bioderived based plasticizers
    Patent number: 9518167
    Abstract: A bioderived based plasticizer is produced by reacting a bioderived diol (and/or a bioderived alcohol) and a bioderived carboxylic acid in the presence of N,N?-dicyclohexylcarbodiimide (DCC), wherein the bioderived carboxylic acid includes a hydrolyzed oil. The bioderived carboxylic acid (e.g., linoleic acid, ?-linolenic acid, oleic acid, and mixtures thereof) may be produced by hydrolyzing a triglyceride, such as canola oil, linseed oil, soybean oil, and mixtures thereof. In one embodiment of the present invention, a bioderived based plasticizer is produced by reacting 2,5-bis-(hydroxymethyl)furan and ?-linolenic acid in the presence of DCC. In some embodiments of the present invention, the bioderived based plasticizer is blended into one or more polymers.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: December 13, 2016
    Assignee: International Business Machines Corporation
    Inventors: Dylan J. Boday, Joseph Kuczynski, Jason T. Wertz, Jing Zhang
  • 2-cycloalkyl resorcinol cannabinergic ligands
    Patent number: 9517989
    Abstract: The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid receptors and thus, they are specific ligands for these receptors. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: December 13, 2016
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Alexandros Makriyannis, Marsha R. D'Souza, Shama Bajaj, Spyridon P. Nikas, Ganeshsingh A. Thakur
  • Process for synthesis of ezetimibe and intermediates used in said process
    Patent number: 9518014
    Abstract: A process for the production of ezetimibe and intermediates used in said process are disclosed. A kind of Morita-Baylis-Hillman adduct can be altered to chiral carboxylic acid derivatives of ?-arylamino ?-methylene with high activity and selectivity by means of ally lamination reaction, and the above carboxylic acid derivatives of ?-arylamino ?-methylene can be altered to the chiral intermediates of ezetimibe by means of simple conversion and further synthesized into the chiral drug ezetimibe. The synthesis route introduces chirality through the use of a chiral catalysis method, thereby avoiding the use of the chiral auxiliary oxazolidinone; and the route is economical and eco-friendly.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: December 13, 2016
    Assignee: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
    Inventors: Kuiling Ding, Xiaoming Wang, Zheng Wang
  • Method for producing ethylene oxide
    Patent number: 9518036
    Abstract: [Problem] To provide a novel technology by which energy efficiency can be further improved in a process for producing ethylene oxide.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: December 13, 2016
    Assignee: NIPPON SHOKUBAI CO., LTD.
    Inventors: Akimasa Watanabe, Takahiro Takinami, Noriji Morikawa
  • Phenyl and benzodioxinyl substituted indazoles derivatives
    Patent number: 9512110
    Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: December 6, 2016
    Assignees: AstraZeneca AB, Bayer Pharma Aktiengesellschaft
    Inventors: Markus Berger, Hartmut Rehwinkel, Jan Dahmen, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Tomas Klingstedt, Matti Lepistö, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
  • NMDA receptor modulators and uses thereof
    Patent number: 9512133
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: December 6, 2016
    Assignee: Northwestern University
    Inventors: M. Amin Khan, Joseph Moskal, Paul Wood
  • Purine derivatives as CB2 receptor agonists
    Patent number: 9505762
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: November 29, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Stefanie Bendels, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch
  • Thienopyranones as kinase and epigenetic inhibitors
    Patent number: 9505780
    Abstract: The invention relates to methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infaction, atheroscleosis, Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder including by modulating biological processes by the inhibition of PI3 kinase and/or bromodomain protein binding to substrates composing the administration of a compound(s) of Formula I-IX (or pharmaceutically acceptable salts thereof) as defined herein.
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: November 29, 2016
    Assignee: SignalRx Pharmaceuticals, Inc.
    Inventors: Donald L. Durden, Guillermo A. Morales, Joseph R. Garlich
  • Oxidation process for preparing 3-formyl-cephem derivatives
    Patent number: 9499566
    Abstract: The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.
    Type: Grant
    Filed: April 7, 2015
    Date of Patent: November 22, 2016
    Assignee: Basilea Pharmaceutica International
    Inventor: Ivan Joseph Maria Vervest
  • Substituted prolines / piperidines as orexin receptor antagonists
    Patent number: 9499517
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: November 22, 2016
    Assignee: Eolas Therapeutics, Inc.
    Inventors: Theodore M. Kamenecka, Yuanjun He, William Nguyen, Rong Jiang, Xinyi Song, Robert Jason Herr, Qin Jiang
  • Pro-drug compounds
    Patent number: 9499510
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: wherein Z1, Z2, and Z3, Q, R2, A, and R1 are as defined in the claims.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: November 22, 2016
    Assignee: Proximagen Limited
    Inventors: Edward Savory, Martyn Pritchard, Mike Ashwood
  • Phosphatidylalkanols and compositions thereof
    Patent number: 9499572
    Abstract: The present invention discloses a composition comprising a compound of formula I and a deuterated solvent. The deuterated solvent is miscible with water in any proportion at a temperature of 20 to 25° C. and comprises less than 5% residual 1H-isotopes. The concentration of the compound of formula I may advantageously be determined by 1H-QNMR. Methods of production of the composition and salts of compounds of formula I, as well as related analogs and novel reagents and intermediates for the production thereof, are also described.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: November 22, 2016
    Assignee: Pethmark AB
    Inventors: David Wensbo Posaric, Karl-Erik Berquist
  • Therapeutic compounds and compositions
    Patent number: 9499532
    Abstract: The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: November 22, 2016
    Assignee: eXIthera Pharmaceuticals Inc.
    Inventors: Robert A. Chrusciel, Robert C. Gadwood, Neil J. Hayward, Michael J. Melnick, Manuel A. Navia, Toni J. Poel, Frans L. Stassen, Catherine A. Stewart
  • Process for the synthesis of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine
    Patent number: 9493409
    Abstract: The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: November 15, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventor: Borut Zupancic