Patents Examined by Sagar Patel
  • Patent number: 10723727
    Abstract: The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: July 28, 2020
    Assignee: Pfizer Inc.
    Inventors: Chakrapani Subramanyam, Lawrence N. Tumey, Longfei Xie, Carolyn Leverett, Beth C. Vetelino, Sai Chetan K. Sukuru, Sarah Hudson, Venkata Ramana Doppalapudi, Abhijit S. Bhat
  • Patent number: 10703744
    Abstract: A process for the preparation of luliconazole and salts thereof is disclosed.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: July 7, 2020
    Assignee: GLENMARK LIFE SCIENCES LIMITED
    Inventors: Shekhar Bhaksar Bhirud, Kumar Hari Bhushan, Sunil Sudhakar Zhope, Shailesh Govind Ghadigaonkar, Pardeep Singh, Shekhar Ashok Deshmukh, Prem Chand
  • Patent number: 10703732
    Abstract: Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: July 7, 2020
    Assignees: OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.
    Inventors: Teruhiko Ishikawa, Morita Iwami
  • Patent number: 10703742
    Abstract: The present application relates to a novel and improved process for preparing 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives of the formula (I) in which R1A and R1B are independently selected from the group consisting of hydrogen, fluorine, chlorine, methyl, monofluoromethyl, difluoromethyl, trifluoromethyl, ethyl, methoxy, difluoromethoxy and trifluoromethoxy, to novel precursors for preparation thereof, and to the preparation and use of the crystalline polymorph I of (5-(4-chlorophenyl)-2-({1-(3-chlorophenyl)-5-[(1S)-1-hydroxyethyl]-1H-1,2,4-triazol-3-yl}methyl)-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I-A-1).
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: July 7, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Heiko Schirmer, Philipp Rubenbauer, Hans-Christian Militzer, Marie-Pierre Collin-Kröpelin, Frank Süßmeier, Kersten Matthias Gericke, Thomas Neubauer, Chantal Fürstner
  • Patent number: 10703718
    Abstract: Disclosed herein are compositions and methods for treating cancer, FLT3-AML, and CML.
    Type: Grant
    Filed: February 9, 2018
    Date of Patent: July 7, 2020
    Assignee: CITY OF HOPE
    Inventors: Sangkil Nam, David Horne, Jun Xie
  • Patent number: 10703698
    Abstract: Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: July 7, 2020
    Assignees: The Board of Trustees of the University of Illinois, Board of Regents of the University of Texas System
    Inventors: John A. Katzenellenbogen, Benita Katzenellenbogen, Sung Hoon Kim, Zeynep Madak-Erdogan, Philip Shaul
  • Patent number: 10689382
    Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
    Type: Grant
    Filed: November 7, 2019
    Date of Patent: June 23, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
  • Patent number: 10669425
    Abstract: A one-pot synthesis for preparing an aqueous reactive black mixture includes a) dissolving 2-[(4-aminophenyl)sulfonyl]ethanesulfonic acid (vinyl sulphone parabase ester) in water; b) diazotizing the dissolved vinyl sulphone parabase ester using excess nitrous acid or using excess nitrite and an acid, resulting in a diazonium salt and remaining nitrous acid; c) quenching the remaining nitrous acid with sulfamic acid; d) coupling the diazonium salt of step c) with 4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid (H-acid) until the reaction is complete, resulting in Reactive Black 5 (RB 5) and remaining diazonium salt, e) coupling the remaining diazonium salt with 7-acetamido-4-hydroxy-2-naphthalenesulfonic acid (acetyl-J-acid) until the reaction is complete resulting in Reactive Orange 78 (RO 78); and f) obtaining the aqueous reactive black mixture.
    Type: Grant
    Filed: May 1, 2018
    Date of Patent: June 2, 2020
    Assignee: SPGPrints B.V.
    Inventors: Dennis Manuel Vriezema, Sigrid Elisabeth Kleine, Martin Jan Smallegange
  • Patent number: 10669263
    Abstract: 2-(5-{1-[2-(Difluoromethoxy)-6-fluorobenzyl]-2-methyl-1H-benzimidazol-6-yl}pyrimidin-2-yl)propan-2-ol, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: June 2, 2020
    Assignee: UCB Biopharma SRL
    Inventor: Jag Paul Heer
  • Patent number: 10669261
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments, in particular for treating cardiovascular disorders.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: June 2, 2020
    Assignee: Bristl-Myers Squibb Company
    Inventors: Michael C. Myers, R. Michael Lawrence, Donna M. Bilder, Wei Meng, Zulan Pi, Robert Paul Brigance, Heather Finlay
  • Patent number: 10662153
    Abstract: Thin molecules, compounds producible by cleaving bilirubin at its methylene site in the center of the molecule, methods of making the same, and methods of using the same, are described.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: May 26, 2020
    Assignee: The University of Toledo
    Inventors: Terry D. Hinds, Jr., David E. Stec, Christopher J. Trabbic
  • Patent number: 10662218
    Abstract: Described herein, inter alia, are compositions and methods for treating or preventing obesity and using the same.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: May 26, 2020
    Inventors: Ralph Mazitschek, Yanbing Ding, Kaisheng Shen
  • Patent number: 10662184
    Abstract: This invention is directed to methods of preparing benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.
    Type: Grant
    Filed: February 28, 2019
    Date of Patent: May 26, 2020
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Jean-Christophe Andrez, Kristen Nicole Burford, Sultan Chowdhury, Charles Jay Cohen, Christoph Martin Dehnhardt, Robert Joseph Devita, James Roy Empfield, Thilo Focken, Michael Edward Grimwood, Syed Abid Hasan, James Philip Johnson, Jr., Alla Yurevna Zenova
  • Patent number: 10660789
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Grant
    Filed: February 28, 2019
    Date of Patent: May 26, 2020
    Assignee: RICHTER GEDEON NYRT.
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Patent number: 10654783
    Abstract: Described herein are polymorphic forms of 1,6-dibromo-1,6-dideoxy-dulcitol (dibromo dulcitol or DBD), which is a known antitumor agent. Also described are methods of making these new crystalline polymorphic forms as well as methods of using these polymorphic forms to treat cancer.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: May 19, 2020
    Assignee: Targent, LLC
    Inventors: Stefano Luca Giaffreda, Elena Dichiarante
  • Patent number: 10647664
    Abstract: Disclosed are compounds of formulae: (I), and (II) and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R21, R22, R23, R34, R37, R33, R39, D, Q, Y, X, X1, X3, and X4 are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
    Type: Grant
    Filed: August 18, 2014
    Date of Patent: May 12, 2020
    Assignees: Duke University, University of North Carolina
    Inventors: Pei Zhou, Eric J. Toone, Robert A. Nicholas
  • Patent number: 10640472
    Abstract: The invention provides novel compounds having the general formula (I) wherein RA, RB, RC, RC1 and W are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 2, 2018
    Date of Patent: May 5, 2020
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jerome Hert, Daniel Hunziker, Holger Kuehne, Thomas Luebbers, Rainer E. Martin, Patrizio Mattei, Werner Neidhart, Hans Richter, Markus Rudolph, Emmanuel Pinard
  • Patent number: 10626123
    Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: April 21, 2020
    Assignee: H. Lundbeck A/S
    Inventors: Carla De Faveri, Florian Anton Martin Huber
  • Patent number: 10618876
    Abstract: Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: April 14, 2020
    Assignees: OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.
    Inventors: Teruhiko Ishikawa, Morita Iwami
  • Patent number: 10604508
    Abstract: The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: March 31, 2020
    Assignee: CrystalGenomics, Inc.
    Inventors: Yong Rae Hong, Jeong Eun Na, Im Sook Min, Hyun Ju Cha, Sool Ki Kwon, Seonggu Ro, Joong Myung Cho