Patents Examined by Laura Daniel
  • 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
  • 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
  • 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
  • Substituted azabicycles and use thereof
    Patent number: 9498480
    Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: November 22, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
  • 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
  • Valomaciclovir polymorphs
    Patent number: 9492456
    Abstract: The present invention relates to crystalline forms of valomaciclovir, processes for preparing crystalline forms of valomaciclovir, pharmaceutical compositions thereof and methods of using thereof.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: November 15, 2016
    Assignee: EPIPHANY BIOSCIENCES, INC.
    Inventors: Mike H. O'Neill, Gregory P. Butke
  • Wee1 degradation inhibitors
    Patent number: 9493464
    Abstract: The invention provides compounds that inhibit the degradation of Wee1. The compounds of the present invention are generally N-((1H-benzo[d]imidazol-2-yl)methyl)-9H-purin-6-amines. Compounds of the invention can be used for treatment of malconditions in patients for which inhibition of Wee1 is medically indicated, for example cancer, Alzheimer's, neurological disorders, psychiatric disorders, or inflammation-related disorders.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: November 15, 2016
    Assignee: The Scripps Research Institute
    Inventors: William R. Roush, Ronald Rahaim, Mathieu Bibian
  • Ganciclovir compositions and related methods
    Patent number: 9486530
    Abstract: Gancyclovir formulations that are ready-to-use, substantially particulate free, and stable upon storage are disclosed. Methods of manufacture and administration of such compositions are also provided.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: November 8, 2016
    Assignee: Exela Pharma Sciences, LLC
    Inventors: Sreerama Murthy Mallipeddi, Jonathan E. Sterling, Phanesh B. Koneru
  • Solid forms of tenofovir
    Patent number: 9487546
    Abstract: The present invention relates to solid forms of tenofovir and methods for preparation, use and isolation of such forms.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: November 8, 2016
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Paul Bernard Hurley, Olga Viktorovna Lapina, Bing Shi, Fang Wang, Zhi Xian Wang, Jacqueline Ching-See Woo
  • Process for preparing ceftaroline fosamil
    Patent number: 9481698
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: November 1, 2016
    Assignee: Sandoz AG
    Inventors: Hubert Sturm, Josef Wieser
  • ?-lactam compounds
    Patent number: 9469610
    Abstract: Novel methods for the production of enantiomerically pure (EP) ?-lactams by decomposition of ?-diazo-?-ketoamides.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: October 18, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Yvette S. Vaske, Maximillian E. Mahoney, Joseph P. Konopelski
  • Spirocyclic sulfones as gamma secretase inhibitors
    Patent number: 9464103
    Abstract: Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: October 11, 2016
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Dmitri Pissarnitski, Zhiqiang Zhao
  • Method for late introduction of the () hydroxyl group carbapenem ?-lactam antibiotic synthesis
    Patent number: 9458479
    Abstract: The presently disclosed subject matter demonstrates that ThnG and ThnQ enzymes encoded by the thienamycin gene cluster in Streptomyces cattleya oxidize the C-2 and C-6 moieties of carbapenems, respectively. ThnQ stereospecifically hydroxylates PS-5 giving N-acetyl thienamycin. ThnG catalyzes sequential desaturation and sulfoxidation of PS-5, giving PS-7 and its sulfoxide. The ThnG and ThnQ enzymes are relatively substrate selective, but give rise to the oxidative diversity of carbapenems produced by S. cattleya, and orthologues likely function similarly in allied streptomyces.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: October 4, 2016
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Craig Arthur Townsend, Micah Jeffrey Bodner, Ryan Martin Phelan, Michael Francis Freeman
  • Method of preparing intermediate of salmeterol
    Patent number: 9447067
    Abstract: A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: September 20, 2016
    Assignee: Amphastar Pahmaceuticals, Inc.
    Inventors: Yinhua Qiu, Zhengyuan Wu, Song Chen, Haoning Zhang
  • Method for treating glioblastomas and other tumors
    Patent number: 9440914
    Abstract: Methods of treating an astrocytoma with agents effective to inhibit microglia function are provided, as well as methods of enhancing the efficacy of brain tumor radiation therapy on an astrocytoma in a subject. Also provided are methods of treating other solid tumor types, and tumor cell invasion, with guanylhydrazone compounds.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: September 13, 2016
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Marc Symons
  • Process for the preparation of enantiomeric forms of 2,3-diaminopropionic acid derivatives
    Patent number: 9434696
    Abstract: The disclosure relates to a process for the preparation of the enantiomeric forms of 2,3-diaminopropionic acid derivatives of formula I, wherein R1, R2 and R3 are defined as in the disclosure, by racemate resolution. The separation of the racemate into its enantiomers takes place through formation of diastereomeric salts upon addition of an enantiomerically pure auxiliary, and subsequent separation by fractional crystallization.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: September 6, 2016
    Assignee: Sanofi
    Inventors: Claus-Dieter Graf, Joerg Rieke-Zapp
  • Prophylactic agent and/or therapeutic agent for diffuse large B-cell lymphoma
    Patent number: 9416131
    Abstract: To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-CLBCL) than the existing Btk inhibitor, and is excellent in safety. The present compound exhibits more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-DLBCL) patients, inter alia, ABC-DLBCL patients having CD79B wild-type gene background than the existing Btk inhibitor, and therefore, it can attain the object of the present invention.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: August 16, 2016
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Toshio Yoshizawa, Ryohei Kozaki
  • Anti-inflammatory compounds
    Patent number: 9403786
    Abstract: New clerodane compounds isolated from plant material from Dodonaea polyandra are disclosed. The compounds have anti-inflammatory activity. Pharmaceutical and cosmetic compositions containing the compounds, as well as methods of treating inflammation using the compounds, are also disclosed.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: August 2, 2016
    Assignees: University of South Australia, Chuulangun Aboriginal Corporation
    Inventors: Susan J. Semple, Bradley S. Simpson, Ross Allan McKinnon, David Claudie, Jacobus P. Gerber, Jiping Wang, George Moreton, Sr.
  • Compositions and methods for the treatment of inflammatory disorders
    Patent number: 9403826
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia, improves blood flow through peripheral blood vessels and therefore helps with blood circulation in the arms and legs (e.g.
    Type: Grant
    Filed: February 2, 2013
    Date of Patent: August 2, 2016
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula