Patents Examined by Nizal Chandrakumar
  • Patent number: 10501418
    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
    Type: Grant
    Filed: February 16, 2015
    Date of Patent: December 10, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Patent number: 9975877
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: May 22, 2018
    Inventor: Robert Murray McKinnell
  • Patent number: 9969717
    Abstract: The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are each as defined in the description, by conversion of compounds of the general formula (IV) in the presence of a palladium catalyst and carbon monoxide. The present invention likewise relates to compounds of the general formula (IV).
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: May 15, 2018
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Himmler, Sergii Pazenok, Frank Volz, Norbert Lui
  • Patent number: 9944652
    Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: April 17, 2018
    Inventors: Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
  • Patent number: 9943507
    Abstract: Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: April 17, 2018
    Assignees: Memorial Sloan-Kettering Cancer Center, The Rockefeller University
    Inventors: Marilyn D. Resh, Joseph Fraser Glickman, Elissaveta Petrova, Ouathek Ouerfelli
  • Patent number: 9938260
    Abstract: The invention relates to activators of soluble guanylate cyclase and their use in pharmaceutical compositions, primarily topically administered ophthalmic compositions. The pharmaceutical compositions are useful for reducing intraocular pressure in animals of the mammalian species.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: April 10, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Nerina Dodic, Anne Marie Jeanne Bouillot
  • Patent number: 9932310
    Abstract: Disclosed herein, inter alia, are compositions and methods for inhibiting DNA2.
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: April 3, 2018
    Assignees: City of Hope, California Institute of Technology
    Inventors: Binghui Shen, Judith Campbell, Li Zheng, Hongzhi Li, David Horne, Jun Xie, Kenneth Karanja
  • Patent number: 9926315
    Abstract: The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: March 27, 2018
    Assignee: Flatley Discovery Lab, LLC
    Inventors: Bridget M. Cole, Richard A. Nugent, Paul T. Smith, Jr.
  • Patent number: 9913471
    Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH—O— or —CH?C—CH2—O—; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C?O, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and
    Type: Grant
    Filed: November 28, 2016
    Date of Patent: March 13, 2018
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Patent number: 9914702
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: March 13, 2018
    Assignees: Bionomics Limited, Merck Patent GmbH
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 9908882
    Abstract: A process for preparing halogenated azaindole compounds makes use of stable reagents including a brominating reagent, a boroxine and a sulfonic anhydride to enhance the selectivity and yield of the final product. In addition, the process is associated with various other advantages, including the ability to recycle reagents, cost reduction, and improved manufacturability.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: March 6, 2018
    Inventors: Michael S. Bultman, Benjamin Cohen, Francisco Gonzalez-Bobes, Matthew R. Hickey
  • Patent number: 9907763
    Abstract: The present invention relates to a method of treating or preventing the visual function loss in optic nerve in a subject after crush injury by using 4-(Phenylsulfanyl)butane-2-one (4-PSB-2). The present invention has the ability of enhancing the protection effect of RGCs, preserving the visual function in optic nerve after crush injury, recovering the visual function loss, attenuating apoptosis in optic nerve after injury, and inhibiting the inflammatory responses in optic nerves after ON injury.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: March 6, 2018
    Inventors: Shun-Ping Huang, Jyh-Horng Sheu, Zhi-Hong Wen, Rong-Kung Tsai
  • Patent number: 9907805
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: March 6, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
  • Patent number: 9895347
    Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: February 20, 2018
    Assignee: Galapagos NV
    Inventors: Steven Emiel Van Der Plas, Hans Kelgtermans, Sébastien Jean Jacques Cédric Dropsit Montovert, Sébastien Laurent Xavier Martina, Martin James Inglis Andrews
  • Patent number: 9889114
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: June 13, 2016
    Date of Patent: February 13, 2018
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Patent number: 9884833
    Abstract: The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide disulfate and crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide monosulfate. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms. In one embodiment, the crystalline compound is (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: February 6, 2018
    Assignee: PharmatrophiX, Inc.
    Inventors: Rajgopal Munigeti, Frank M. Longo
  • Patent number: 9867816
    Abstract: Methods of treatment of multiple sclerosis (MS) with PPAR? agonists, and in particular with the compound of formula (I) known as INT131:
    Type: Grant
    Filed: January 10, 2017
    Date of Patent: January 16, 2018
    Assignee: InteKrin Therapeutics, Inc.
    Inventor: David Weinstein
  • Patent number: 9850254
    Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: December 26, 2017
    Assignee: Sandoz AG
    Inventors: Fabio E. S. Souza, Alena Rudolph, Dino Alberico, Robert Jordan, Ming Pan, Boris Gorin
  • Patent number: 9845321
    Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: December 19, 2017
    Assignee: Janssen Sciences Ireland UC
    Inventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
  • Patent number: 9834514
    Abstract: The present disclosure describes a method to treat conditions, including bacterial infections and cancer, using a photosensitive compound that, upon exposure to white light, can be activated. The photosensitive compound can also interact synergistically with antibiotics used concomitantly to kill drug-resistant bacteria. The photosensitive compounds can also be used to inhibit the proliferation of cancer cells.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: December 5, 2017
    Inventors: Snezna Rogelj, Liliya Frolova, Alexander Kornienko, Leslie D. Edwards, Cody Champion, Kailee Zingler, Danielle Nicole Turner