Patents Examined by E Crane
  • Phosphonate nucleosides useful as active ingredients in pharmaceutical compositions for the treatment of viral infections, and intermediates for their production
    Patent number: 9249177
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: February 2, 2016
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Pyrazole derivatives
    Patent number: 9249172
    Abstract: Disclosed are pyrazole compounds of general formula (I), wherein R, R1, Rc, Rd, Re, Rf, X, Y, Z, A and B are as defined in the application. These compounds are active as inhibitors of poly(ADP-ribose)polymerase (PARP) and are useful in methods for treating diseases or conditions mediated by PARP, including breast cancer and malignant melanoma.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: February 2, 2016
    Assignees: HANDE PHARMA LIMITED, HANDE STARLAKE BIOSCIENXE CO., LTD.
    Inventors: Chenxi Li, Weisheng Shen, Yang Fang, Xiaoyong Le
  • Composition containing iridoids and uses thereof
    Patent number: 9233116
    Abstract: Composition containing iridoids such as morroniside and loganin, the use thereof in preparing medicaments for preventing and treating neurologic demyelinating diseases, and the method thereof in treating diseases related to neurologic demyelinating lesions are disclosed by the present application.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: January 12, 2016
    Assignee: XUANWU HOSPITAL OF CAPITAL MEDICAL UNIVERSITY
    Inventors: Lin Li, Linlin Yin, Lan Zhang, Wen Wang, Ruyi Zhang
  • Uridine di- or tri-phosphate derivatives and uses thereof
    Patent number: 9221868
    Abstract: The disclosure provides particular uridine di- and tri-phosphate compounds of Formula I, and pharmaceutical compositions thereof. The definitions of variables such as R, Y, B, m, Z1, Z2, and Z3 are as provided in the disclosure. These compounds are useful for treatment of diseases, disorders and conditions modulated by P2Y6 receptors, and particularly for lowering intraocular pressure and thereby treating ocular hypertension and/or glaucoma.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: December 29, 2015
    Assignees: BAR-ILAN UNIVERSITY, UNIVERSIDAD COMPLUTENSE DE MADRID
    Inventors: Bilha Fischer, Jesus Jeronimo Pintor, Shay Elyahu, Tamar Ginsburg-Shmuel
  • Polynucleotide capture materials, and methods of using same
    Patent number: 9217143
    Abstract: Disclosed are methods for isolating polynucleotides (e.g., RNA and DNA) from a cell-containing sample. The disclosed methods employ polyamidoamine (PAMAM) dendrimer molecules bound to the surface of binding particles to capture and isolate the polynucleotides from the samples. The polynucleotides are released from the binding particles by contacting the binding particles with a release solution having a basic pH.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: December 22, 2015
    Assignee: HANDYLAB, INC.
    Inventors: Sundaresh N. Brahmasandra, Elizabeth Craig
  • Nucleotide analogue, method of synthesis of nucleotide analogue, use of nucleotide analogue, antiviral pro-nucleotide, pharmaceutical composition
    Patent number: 9206209
    Abstract: An exemplary emboidment is related to a pharmaceutical composition of the class of nucleotide analogues and antiviral pro-nucleotides useful in partial or complete inhibition of human immunodeficiency virus (HIV). An exemplary embodiment is expressed in the formula (XVI): where X stands for N3 and B stands for thymidine-1-yl, or X stands for H and B stands for uracil-1-yl or adenin-1-yl or hypoxanthin-1-yl.A method of synthesis of the nucleotide analogue using a phosphorylating agent for synthesis of the nucleotide analogue is provided.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: December 8, 2015
    Assignees: INSTYTUT CHEMII BIOORGANICZNEJ PAN, NARODOWY INSTYTUT LEKOW
    Inventors: Adam Kraszewski, Joanna Romanowska, Michal Sobkowski, Agnieszka Szymanska-Michalak, Jacek Stawinski, Jerzy Boryski, Andrzej Lipniacki, Andrzej Piasek
  • Monomers and oligonucleotides comprising cycloaddition adduct(s)
    Patent number: 9198972
    Abstract: The invention features compounds of formula (V) or (XII). In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: December 1, 2015
    Assignee: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Narayanannair K. Jayaprakash, Kallanthottahil G. Rajeev, Michael E. Jung
  • Methods of myocardial perfusion imaging
    Patent number: 9163057
    Abstract: The present invention provides a method of myocardial perfusion imaging using reduced doses of (1-{9-[(4S,2R,3R,5R)3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: October 20, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Brent K. Blackburn, Zhenhai Gao
  • Crystalline forms of an antiviral benzimidazole compound
    Patent number: 9163052
    Abstract: The invention relates to crystalline forms of 5,6-dichloro-2-(isopropylamino)-1-?-L-ribofuranosyl-1H-benzimidazole, pharmaceutical compositions comprising the same, processes for preparing the same, and their use in medical therapy.
    Type: Grant
    Filed: January 25, 2011
    Date of Patent: October 20, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Bobby Neal Glover, Lian-Feng Huang, Robert William Lancaster, Stacey Todd Long, Michele Catherine Rizzolio, Eric Allen Schmitt, Barry Riddle Sickles
  • Dosing methods for treating disease
    Patent number: 9161946
    Abstract: The invention relates to a method for treating disease such as viral infections, tumors, and cancers, comprising administering a TLR7 agonist or TLR7 agonist prodrug according to a cyclical dosing schedule having a dosing period and a resting period. For example, the method encompasses treating disease with: 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one Tosylate according to a dosing schedule of every-other-day or a dosing schedule of three consecutive days of dosing followed by four consecutive days of not dosing.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: October 20, 2015
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: James Appleman, Joyce Tan, Simon Fletcher
  • Modified 5? diphosphate nucleosides and oligomeric compounds prepared therefrom
    Patent number: 9156873
    Abstract: Provided herein are modified 5? diphosphate nucleosides and oligomeric compounds prepared therefrom. More particularly, modified 5? diphosphate nucleosides are provided that can be further modified at the 2? and 5? positions. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The oligomeric compounds are also expected to be useful as primers and probes in diagnostic applications.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: October 13, 2015
    Assignees: Isis Pharmaceuticals, Inc., Alnylam Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Muthiah Manoharan, Eric E. Swayze, Kallanthottathil G. Rajeev, Ivan Zlatev
  • Use of adenosine Areceptor agonists for treatment of neuropathic pain
    Patent number: 9132131
    Abstract: A method of treating neuropathic pain in a subject is provided. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutically effective amount of an A3AR agonist, optionally further including administering an analgesic.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: September 15, 2015
    Assignee: Saint Louis University
    Inventor: Daniela Salvemini
  • 5? modified nucleosides and oligomeric compounds prepared therefrom
    Patent number: 9127033
    Abstract: The present invention provides 5? modified nucleosides and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides having at least one 5?-substituent and an optional 2? substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: September 8, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
  • Synthesis of nucleosides
    Patent number: 9109000
    Abstract: A process for the preparation of nucleosides, derivatives and analogues thereof by coupling reaction of a protected suitable nitrogeneous purine or pyrimidine base, a derivative or analogue thereof and a protected suitable sugar in the presence of SnCl4 comprising the removal of SnCl4 by adding DMSO directly into the reaction mixture is described. Preferably said process is used for the preparation of antiviral and antitumor agents having a nucleoside or nucleoside-like structure, still more preferably for the preparation of azacytidine, decitabine, chlorfarabine, cladribine, mizoribine. A residual tin content lower than 300 ppm is obtained with said process.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: August 18, 2015
    Assignee: FARMABIOS, S.p.A.
    Inventors: Claudio Gianluca Pozzoli, Valentina Canevari, Marco Brusasca, Lorenzo Menna, Matteo Curti
  • Compositions and methods for treating and preventing dermatoses
    Patent number: 9084788
    Abstract: The invention encompasses protectant agents including uracil or a metabolite thereof that effectively treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Specifically, and surprisingly, the compositions of the invention including uracil or a metabolite thereof are effective for treating various dermatoses including atopic dermatitis, irritant contact dermatitis, radiation-induced dermatitis, dry skin dermatitis, papulopustular rashes, xerosis, pruitus, actinic keratosis, and genital warts.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: July 21, 2015
    Assignee: Asymmetric Therapeutics, LLC
    Inventor: John P. Ford
  • Method for deblocking of labeled oligonucleotides
    Patent number: 9085797
    Abstract: The invention relates to a process for deblocking substantially a blocked, detectably labeled oligonucleotide by contacting the blocked detectably labeled oligonucleotide with an effective amount of a nucleophilic amino compound under conditions that result in substantial deblocking of the oligonucleotide, thereby giving the substantially deblocked oligonucleotide.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: July 21, 2015
    Assignee: Life Technologies Corporation
    Inventors: Gulilat Gebeyehu, Richard Pires
  • Process for preparing an A2A-adenosine receptor agonist and its polymorphs
    Patent number: 9085601
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: July 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein, Robert Seemayer, Travis Lemons
  • CDK-inhibiting pyrrolopyrimidine carboxamide derivative or pharmaceutically acceptable salt thereof, and pharmaceutical composition containing the same as active ingredient for preventing or treating hepatocellular carcinoma
    Patent number: 9062088
    Abstract: The present invention relates to a CDK-inhibiting pyrrolopyrimidine carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating liver cell cancer. Compositions comprising a pyrrolopyrimidine carboxamide derivative of the present invention suppress the cell growth of SNU-354 cell, which is a liver cancer stem cell in humans, by inhibiting CDK1 and CDK2, and induces cell apoptosis of the cell by inhibiting CDK7 and CDK 7. Such compositions are useful for preventing or treating liver cell cancer.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: June 23, 2015
    Assignee: SNU R&DB Foundation
    Inventors: Seung Ki Lee, Byeong Moon Kim, Seung Ju Cho, Young Jong Kim
  • Minor groove binder phosphoramidites and methods of use
    Patent number: 9056887
    Abstract: Minor groove binder phosphoramidites having the formula M-L-PA, wherein M is a minor groove binder comprising a protected heteroaromatic amine, L is a linker, and PA is a phosphoramidite group, have been synthesized. Preferred methods of synthesis include synthesizing a minor groove binder intermediate containing a transiently protected hydroxyl group, protecting heteroaromatic amines of the corresponding minor groove binder intermediate as carbamate intermediates, reacting the carbamate intermediate to remove the transient protecting group to yield carbamate-protected minor groove binder agent as an intermediate with a free hydroxyl group, and converting the intermediate with a free hydroxyl group to the desired minor groove binder phosphoramidite. These minor groove binder phosphoramidites are useful in the preparation of oligonucleotide conjugates, particularly those for use as probes and primers.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: June 16, 2015
    Assignee: Elitech Holding B.V.
    Inventors: Alexei Vorobiev, Eugeny A. Lukhtanov
  • N-pyrazole Areceptor agonists
    Patent number: 9045519
    Abstract: The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compound to stimulate mammalian coronary vasodilatation for imaging the heart.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: June 2, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli