Patents Examined by Golam M. Shameem
  • Patent number: 10975084
    Abstract: The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
    Type: Grant
    Filed: October 6, 2017
    Date of Patent: April 13, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Umar Faruk Mansoor, Christian Fischer, Phieng Siliphaivanh, Luis Torres, Hakan Gunaydin, David L. Sloman
  • Patent number: 10975027
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Grant
    Filed: June 30, 2020
    Date of Patent: April 13, 2021
    Inventor: Thomas Daly
  • Patent number: 10960007
    Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: March 30, 2021
    Inventors: István Borza, Viktor Román, János Éles, Zsuzsa Hadady, József Huszár
  • Patent number: 10961202
    Abstract: Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: March 30, 2021
    Inventors: Matthew Disney, Timothy Allen Blizzard, Suzanne Rzuczek, John Ndungu, Joseph Vacca, Andy Jennings, Alexei Pushechnikov
  • Patent number: 10954260
    Abstract: Organometallic compounds comprising a chloroquinoline moiety and uses of the compounds. The compounds are, for example, manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety. The compounds can be used in, for example, methods of inhibiting cell growth.
    Type: Grant
    Filed: August 5, 2019
    Date of Patent: March 23, 2021
    Assignee: University of Vermont and State Agricultural College
    Inventors: William E. Geiger, Kevin Lam, Jon E. Ramsey, Claire F. Verschraegen
  • Patent number: 10954194
    Abstract: The invention relates to a method of treating a subject who has cancer or a non-malignant tumor, the method comprising administering a therapeutically effective amount of a 18-20 member bi-polycyclic compound to the subject.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: March 23, 2021
    Assignees: Haro Pharmaceuticals Inc., The Royal Institution for the Advancement of Learning/ McGill University, Universite De Montreal
    Inventors: David Bettoun, Eduardo Martinez, James Gleason, Sylvie Mader, Shuo Xing
  • Patent number: 10947186
    Abstract: The present invention refers to a process for a Rh-catalyzed Anti-Markovnikov hydrocyanation of terminal alkynes which process discloses, for the first time, the highly stereo- and regio-selective hydrocyanation of terminal alkynes to furnish E-configured alkenyl nitriles and the catalyst used in the present process.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: March 16, 2021
    Inventors: Tobias Ritter, Fei Ye
  • Patent number: 10947176
    Abstract: Provided herein are compounds, compositions and method of using thereof to treat or prevent malaria.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: March 16, 2021
    Inventors: Wil Joseph Andahazy, Arnab K. Chatterjee, Case W. McNamara, Federico C. Beasley, Anders Mikal Eliasen, Hank Michael James Petrassi, Jason T. Roland, Timothy Wells, Olga Vladimirovna Zatolochnaya, Fei Zhou, Peter G. Schultz, Anil Kumar Gupta
  • Patent number: 10945988
    Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.
    Type: Grant
    Filed: September 14, 2019
    Date of Patent: March 16, 2021
    Inventors: Marlene Michelle Dressman, Louis William Licamele, Mihael H. Polymeropoulos
  • Patent number: 10947206
    Abstract: Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
    Type: Grant
    Filed: April 15, 2018
    Date of Patent: March 16, 2021
    Assignees: ImmuneSensor Therapeutics, Inc., The Board of Regents of the University of Texas System
    Inventors: Boyu Zhong, Lijun Sun, Heping Shi, Jing Li, Chuo Chen, Zhijian Chen
  • Patent number: 10941169
    Abstract: An object of the present invention is to provide crystal of a cyclic phosphonic acid sodium salt (2ccPA) with high purity and excellent storage stability and a method for producing the crystal.
    Type: Grant
    Filed: May 19, 2020
    Date of Patent: March 9, 2021
    Inventors: Hiroaki Yuasa, Hiroki Okazaki
  • Patent number: 10941134
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: March 9, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 10933037
    Abstract: The present disclosure provides certain N-Acylethanolamide derivatives, and uses relating thereto.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: March 2, 2021
    Inventor: Andrew D. Levin
  • Patent number: 10933071
    Abstract: Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.
    Type: Grant
    Filed: November 25, 2019
    Date of Patent: March 2, 2021
    Assignee: Board of Regents of the University of Nebraska
    Inventors: Dong Wang, Fang Yuan, Zhenshan Jia, Xiaobei Wang
  • Patent number: 10934296
    Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: March 2, 2021
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Adrianus Petrus Antonius de Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
  • Patent number: 10934305
    Abstract: The disclosure provides compounds of Formulae (I)-(IX). The disclosed compounds are capable of inhibiting a mammalian SHMT. Compounds of the disclosure have numerous uses, such as for treatment of cancer or autoimmune disorders.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: March 2, 2021
    Assignee: The Trustees of Princeton University
    Inventors: Joshua D. Rabinowitz, Hahn Kim, Gregory S. Ducker, Jonathan M. Ghergurovich
  • Patent number: 10919850
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: February 16, 2021
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Patent number: 10919900
    Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.
    Type: Grant
    Filed: September 13, 2019
    Date of Patent: February 16, 2021
    Assignee: Magenta Therapeutics Inc.
    Inventor: Arthur Glenn Romero
  • Patent number: 10918642
    Abstract: The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: February 16, 2021
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Simona Bindi, Davide Carenzi, Ilaria Motto, Maurizio Pulici
  • Patent number: 10913715
    Abstract: The present invention provides a novel crystalline form I of hydrochloride, a crystalline form II of hydrochloride, a crystalline form of succinate, a crystalline form of tartrate, a crystalline form I of fumarate and a crystalline form II of fumarate of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine. The above-described novel crystalline forms have high solubility in water and excellent stability under moisture-proof conditions and high-humidity exposure conditions, and thus can be pharmaceutically used.
    Type: Grant
    Filed: December 18, 2019
    Date of Patent: February 9, 2021
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Aeri Kim, Kwan Hyung Cho