Patents Examined by Douglas M Willis
  • Patent number: 10781171
    Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: September 22, 2020
    Assignee: Epics Therapeutics
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Patent number: 10774077
    Abstract: The invention relates to a compound comprising the following general formula (1): and said compound for use as a medicament, in particular for use in the treatment psychiatric or neurological disorders and inflammation, in particular neuroinflammation: (formula 1) wherein each of R1, R2 and R3 are selected independently from each other from alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, or heteroaryl.
    Type: Grant
    Filed: August 21, 2019
    Date of Patent: September 15, 2020
    Assignee: UNIVERSITAT BERN
    Inventors: Jean-Louis Reymond, Simon Nicolussi, Jurg Gertsch
  • Patent number: 10774056
    Abstract: Provided herein are substituted piperazine compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Grant
    Filed: July 10, 2019
    Date of Patent: September 15, 2020
    Assignee: REGENACY PHARMACEUTICALS, INC.
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 10766895
    Abstract: Disclosed is a preparation method for a Palbociclib free base crystal form A as shown in Formula I, comprising the following steps: treating a Palbociclib free base and/or a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 35 to 100?C. to obtain a Palbociclib free base crystal form A, the water solvent being water or mixed solvent obtained by water and an organic solvent capable of being mixed and disclosed in the water. Also disclosed is a preparation method for a Palbociclib free base crystal form B, comprising the following steps: treating a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 0 to 20° C. to obtain a Palbociclib free crystal form B, the water solvent being water or a mixed solvent obtained by water and an organic solvent capable of being mixed and dissolved in the water. The method is safe and convenient in operation and low in pollution, and facilitates industrial production.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: September 8, 2020
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., SHANGHAI SYNCORES TECHNOLOGIES INC. LTD.
    Inventors: Haisheng Fan, Xiaowen Guo, Luning Huang, Hong Gu
  • Patent number: 10766899
    Abstract: Provided are methods of preparing compounds of Formula 201:
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: September 8, 2020
    Assignee: CYTOKINETICS, INCORPORATED
    Inventors: Bradley P. Morgan, David J. Morgans, Jr., Alex Muci
  • Patent number: 10766922
    Abstract: A compound and pharmaceutically acceptable salts thereof for treating cancer, having a structure represented by the following formula (I) or formula (II): in which X and Y each individually represent: R1, R2, R3, R4, and R5 individually represents hydrogen atom, acyl having 20 or less carbon atoms, alkyl having 20 or less carbon atoms, alkanoyl having 20 or less carbon atoms, aroyl having 20 or less carbon atoms, aryl having 20 or less carbon atoms, aralkyl having 20 or less carbon atoms, sulfonyl having 20 or less carbon atoms, phosphonyl having 20 or less carbon atoms, or haloacyl having 20 or less carbon atoms.
    Type: Grant
    Filed: May 28, 2019
    Date of Patent: September 8, 2020
    Assignee: AQUAVAN TECHNOLOGY CO., LTD.
    Inventors: Kuo-Tang Tseng, Hsin Ju Wang, Wen-Hung Chen
  • Patent number: 10759751
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: September 1, 2020
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Patent number: 10758529
    Abstract: Methods for inhibiting the activity of Clostridium difficile in a subject comprises administering to the subject in need thereof, a therapeutically effective amount of azaquinone or a pharmaceutical composition consisting of clofazimine or a clofazimine analogue, azaquinone, and at least one pharmaceutically acceptable excipient. Pharmaceutical compositions comprising a therapeutically effective amount of azaquinone or consisting of clofazimine or a clofazimine analogue, azaquinone, and at least one pharmaceutically acceptable excipient are provided for treating Clostridium difficile infection and diseases or symptoms associated therewith.
    Type: Grant
    Filed: August 21, 2019
    Date of Patent: September 1, 2020
    Assignee: KamTek, Inc.
    Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
  • Patent number: 10759743
    Abstract: Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
    Type: Grant
    Filed: October 19, 2017
    Date of Patent: September 1, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Jin-Quan Yu
  • Patent number: 10745387
    Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: August 18, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Gregg F. Keaney, John Wang, Baudouin Gerard, Kenzo Arai, Xiang Liu, Guo Zhu Zheng, Kazunobu Kira, Parcharee Tivitmahaisoon, Sudeep Prajapati, Nicholas C. Gearhart, Yoshihiko Kotake, Satoshi Nagao, Regina Mikie Kanada Sonobe, Masayuki Miyano, Norio Murai, Silvia Buonamici, Lihua Yu, Eunice Sun Park, Betty Chan, Peter G. Smith, Michael P. Thomas, Ermira Pazolli, Kian Huat Lim, Atsushi Endo, Arani Chanda
  • Patent number: 10745381
    Abstract: The present invention relates to indoline-based compounds that inhibit Rho-associated protein kinase (ROCK) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.
    Type: Grant
    Filed: November 6, 2019
    Date of Patent: August 18, 2020
    Assignee: Cervello Therapeutics, LLC.
    Inventors: Matthew Randolph Lee, Anthony Joseph Varano, Jr.
  • Patent number: 10738031
    Abstract: This invention relates to compounds of formula (I), a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar1 and Ar2 have meanings given in the description.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: August 11, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec
  • Patent number: 10738046
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: August 11, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jason W. Brown, Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Holger Monenschein, Holly Reichard, Kristin Schleicher, Huikai Sun, Todd Macklin
  • Patent number: 10722481
    Abstract: The present disclosure relates to a method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (II): wherein R1, R2, R3, X and Y are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt. More particularly, the present disclosure relates to a method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (I): wherein R2, R3, and X, are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: July 28, 2020
    Assignee: BASF AS
    Inventor: Hilde Steineger
  • Patent number: 10717721
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: July 21, 2020
    Assignee: Helsinn Healthcare SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Patent number: 10711011
    Abstract: The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: July 14, 2020
    Assignee: BUGWORKS RESEARCH, INC.
    Inventors: Shahul Hameed Peer Mohamed, Nagakumar Bharatham, Nainesh Katagihallimath, Sreevalli Sharma, Radha Nandishaiah
  • Patent number: 10711018
    Abstract: A process can prepare an isocyanurate compound by hydrosilylation. The compound is a tris[3-(trialkoxysilyl)propyl] isocyanurate, a tris[3-(alkyldialkoxysilyl)propyl] isocyanurate, and/or a tris[3-(dialkylalkoxysilyl)propyl] isocyanurate, The process includes (A) preparing a mixture of at least one carboxylic acid, a platinum catalyst, and 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione; (B) heating the mixture to a temperature in the range of 40 to 140° C.; (C) adding at least one H-silane among a hydrotrialkoxysilane, a hydroalkyldialkoxysilane, and a hydrodialkylalkoxysilane to the mixture; (D) adding at least one alcohol to the mixture prepared in step (C); and (E) isolating the isocyanurate compound.
    Type: Grant
    Filed: April 11, 2019
    Date of Patent: July 14, 2020
    Assignee: Evonik Operations GmbH
    Inventors: Philipp Albert, Eckhard Just
  • Patent number: 10702521
    Abstract: The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: July 7, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventor: Katherine Louisa Widdowson
  • Patent number: 10703769
    Abstract: A process can prepare an isocyanurate compound by hydrosilylation. The compound is a tris[3-(trialkoxysilyl)propyl] isocyanurate, a tris[3-(alkyldialkoxysilyl)propyl] isocyanurate, and/or a tris[3-(dialkylalkoxysilyl)propyl] isocyanurate, The process includes (A) preparing a mixture of at least one carboxylic acid, a platinum catalyst, and 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione; (B) heating the mixture to a temperature in the range of 40 to 140° C.; (C) adding at least one H-silane among a hydrotrialkoxysilane, a hydroalkyldialkoxysilane, and a hydrodialkylalkoxysilane to the mixture; (D) adding at least one alcohol to the mixture prepared in step (C); and (E) isolating the isocyanurate compound.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: July 7, 2020
    Assignee: Evonik Operations GmbH
    Inventors: Philipp Albert, Eckhard Just
  • Patent number: 10696641
    Abstract: Disclosed are novel bis(aminophenylphenol) ligands and transition metal compounds derived therefrom. Also disclosed are methods of making the ligands and transition metal compounds.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: June 30, 2020
    Assignee: Univation Technologies, LLC
    Inventors: Catherine Anne Faler, Kevin P. Ramirez