Patents Examined by Patricia L. Morris
  • 5-aryl-1H-pyrrole-3-carbonitrile and a pharmaceutical product using the same
    Patent number: 10538489
    Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: January 21, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomomi Ikemoto, Naohiro Fukuda
  • Crystal form of a potassium-competitive acid blocker and preparation method thereof
    Patent number: 10538506
    Abstract: The present invention relates to a crystal form of a potassium-competitive acid blocker, that is, 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrole-3-yl]-N-methyl methylamine fumaric acid salt (which is briefly referred to as a formula I) and a preparation method thereof. An X-ray powder diffraction characteristic peak thereof is shown in FIG. 1. The crystal form that is represented by formula I, provided in the present invention, is stable, reproducible, and is suitable for drug development.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: January 21, 2020
    Assignee: Jiangsu Hansoh Pharmaceutical Group Co., Ltd.
    Inventors: Hongwei Tang, Changan Sun, Ruijun Wang, Hengli Yuan
  • Antimicrobial prochelators to target drug-resistant bacteria and methods of making and using the same
    Patent number: 10533018
    Abstract: The present disclosure provides antibacterial prodrugs and methods of making and using the same.
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: January 14, 2020
    Assignee: Duke University
    Inventors: Katherine J. Franz, David M. Besse, Patrick C. Seed
  • Solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
    Patent number: 10532047
    Abstract: The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.
    Type: Grant
    Filed: May 16, 2019
    Date of Patent: January 14, 2020
    Assignee: FORMA Therapeutics, Inc.
    Inventor: George P. Luke
  • Crystalline forms of an androgen receptor modulator
    Patent number: 10526310
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3,4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: April 15, 2019
    Date of Patent: January 7, 2020
    Assignees: Aragon Pharmaceuticals Inc., Sloan Kettering Institute for Cancer Research
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
  • Antifungal compound process
    Patent number: 10513505
    Abstract: The present invention relates to a process for preparing a compound of 5 or 5*, or a mixture thereof, and/or a compound of 14 or 14*, or a mixture thereof, that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compounds 7, 7* and 11, 11* and substituted derivatives thereof.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: December 24, 2019
    Assignee: NQP 1598, LTD.
    Inventors: David Dale Wirth, Christopher M. Yates, William J. Hoekstra
  • Processes for the preparation of apalutamide and intermediates thereof
    Patent number: 10513504
    Abstract: The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1).
    Type: Grant
    Filed: March 6, 2019
    Date of Patent: December 24, 2019
    Assignee: Apotex Inc.
    Inventors: Prabhudas Bodhuri, Alfredo Paul Ceccarelli, Michael R. Emmett, Avedis Karadeolian, Fabio E. S. Souza, Gamini Weeratunga, Boris Gorin
  • Benzimidazole derivates useful as inhibitors of mammalian histone deacetylase activity
    Patent number: 10512634
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound. The compound is useful in therapy, for the treatment of disorders mediated by HDAC6, such as autoimmune disorders, neurodegenerative disorders and hyperproliferative disorders, such as cancer.
    Type: Grant
    Filed: May 11, 2015
    Date of Patent: December 24, 2019
    Assignee: KANCERA AB
    Inventors: Johan Schultz, Jan Vågberg, Elisabeth Olsson, Katarina Färnegårdh, Mattias Jönsson, Kristin Hammer, Lars Krüger
  • Nicotine salts, co-crystals, and salt co-crystal complexes
    Patent number: 10508096
    Abstract: The invention provides certain nicotine salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, certain nicotine salt-co-crystals are described, including nicotine and two different coformers. The invention further provides methods of preparation and characterization of nicotine salts, co-crystals, and salt co-crystals. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: December 17, 2019
    Assignee: R.J. Reynolds Tobacco Company
    Inventors: Gary M. Dull, Susana del Rio Gancedo, Judit Galcera Julia
  • Processes for the preparation of ivacaftor
    Patent number: 10501419
    Abstract: The present invention provides processes for the preparation of ivacaftor using novel intermediates and a process for its preparation.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: December 10, 2019
    Assignee: Laurus Labs Limited
    Inventors: Suresh Thatipally, Venkata Krishna Reddy, Venkata Lakshmi Narasimha Rao Dammalapati, Satyanarayana Chava
  • Therapeutic agents for the treatment of HBV infection
    Patent number: 10501456
    Abstract: The disclosure includes compounds of Formula (I) wherein Z1, Z2, Z3, X, R1, R2, R3, R4, R5, R6, and R7 are defined herein. Also disclosed is a method for treating HBV infection.
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: December 10, 2019
    Assignee: Newave Pharmaceutical Inc.
    Inventors: Yi Chen, Yan Lou
  • HPK1 inhibitors and methods of using same
    Patent number: 10501474
    Abstract: Thienopyridinone compounds of Formula (I) and pharmaceutically acceptable salts thereof are described. In these compounds, one of X1; X2, and X3 is S and the other two are each independently CR, wherein R and all other variables are as defined herein. The compounds are shown to inhibit HPK1 kinase activity and to have in vivo antitumor activity. The compounds can be effectively combined with pharmaceutically acceptable carriers and also with other immunomodulatory approaches, such as checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).
    Type: Grant
    Filed: June 23, 2016
    Date of Patent: December 10, 2019
    Assignee: University Health Network
    Inventors: Peter Brent Sampson, Narendra Kumar B. Patel, Heinz W. Pauls, Sze-Wan Li, Grace Ng, Radoslaw Laufer, Yong Liu, Yunhui Lang
  • Tetrahydroisoquinoline derived PRMT5-inhibitors
    Patent number: 10494376
    Abstract: A compound of formula I wherein: n is 1 or 2: p is 0 or 1; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: December 3, 2019
    Assignee: CTXT PTY. LTD.
    Inventors: Ylva Elisabet Bergman, Richard Charles Foitzik, Benjamin Joseph Morrow, Michelle Ang Camerino, Scott Raymond Walker, H. Rachel Lagiakos, John Feutrill, Graeme Irvine Stevenson, Paul Anthony Stupple
  • Crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate, compositions and methods of use thereof
    Patent number: 10494361
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: December 3, 2019
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Enantiopure haptens for nicotine vaccine development
    Patent number: 10487141
    Abstract: The invention provides chiral haptens (?)-3?-AmNic and (?)-N4N for use in generating antibodies in a patient specific for (?)-nicotine. The haptens can be conjugated to suitable carrier proteins and administered as an antigenic mixture, optionally comprising adjuvant(s), to a patient suffering from nicotine or tobacco addiction or habituation.
    Type: Grant
    Filed: December 10, 2018
    Date of Patent: November 26, 2019
    Assignee: The Scripps Research Institute
    Inventors: Kim D. Janda, Jonathan W. Lockner
  • Cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof
    Patent number: 10487058
    Abstract: A cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof, wherein the structural formula of the compound is as follows: An application of the compound or its pharmaceutically acceptable salts, hydrates, solvates, or prodrugs in preparing a drug for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes is provided. A drug composition includes the cyclopropyl unsaturated quinoline compound or the pharmaceutically acceptable salts, hydrates, solvates, or prodrugs thereof. The compound series has favorable foreground in preparing drugs for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes.
    Type: Grant
    Filed: April 23, 2019
    Date of Patent: November 26, 2019
    Assignee: Guangdong Moltech Pharma Co. Ltd.
    Inventor: Yingjie Lai
  • Crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate, compositions and methods of use thereof
    Patent number: 10487069
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate are also disclosed.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: November 26, 2019
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Methods of preparing hydroxylamine derivatives useful in the preparation of anti-infective agents
    Patent number: 10472345
    Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: November 12, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Xu, Dongfang Meng
  • Nicotine salts, co-crystals, and salt co-crystal complexes
    Patent number: 10464917
    Abstract: The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: November 5, 2019
    Assignee: R.J. Reynolds Tobacco Company
    Inventors: Gary M. Dull, Andrew Carr, Emma Sharp
  • Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate
    Patent number: 10442829
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: October 15, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson