Patents Examined by Bruck Kifle
  • Patent number: 10842779
    Abstract: The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as ?-lactamase inhibitors and/or as antibacterial agents.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: November 24, 2020
    Assignee: MUTABILIS
    Inventors: Julie Brias, Sophie Chasset, Francis Chevreuil, Nicolas Lecointe, Benoit Ledoussal, Frédéric Le Strat, Julien Barbion
  • Patent number: 10844077
    Abstract: The present disclosure provides thiazolyl-containing compounds of Formula (I), (II), or (III). The compounds described herein may be able to inhibit protein kinases (e.g. Src family kinases (e.g. hemopoietic cell kinase (HCK)), Bruton's tyrosine kinase (BTK)) and may be useful in treating and/or preventing proliferative diseases (e.g. myelodysplasia, leukemia, lymphoma, (e.g. Waldenström's macroglobulinemia)) and in inducing apoptosis in a cell (e.g. malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: November 24, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Sara Jean Buhrlage, Steven P. Treon, Hwan Geun Choi, Yuan Xiong, Guang Yang
  • Patent number: 10836757
    Abstract: Provided herein are novel polymorphic forms of metopimazine mesylate. These polymorphic forms are useful in methods, compositions, and kits for the treatment of an enteric nervous system disorder.
    Type: Grant
    Filed: April 2, 2020
    Date of Patent: November 17, 2020
    Assignee: NEUROGASTRX, INC.
    Inventor: Shu Yu
  • Patent number: 10815242
    Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a ?5-containing GABAA receptor agonist (e.g.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: October 27, 2020
    Assignee: AgeneBio, Inc.
    Inventors: Belew Mekonnen, John A. Butera, Jianxing Huang
  • Patent number: 10814010
    Abstract: In one aspect, the present disclosure provides a compound of the formula: In another aspect, the present disclosure also provides methods of preparing the compound disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compound disclosed herein. Additionally, methods of treating cancer with the compound disclosed herein are described.
    Type: Grant
    Filed: March 25, 2019
    Date of Patent: October 27, 2020
    Assignees: The Board of Regents, The University of Texas System, Pohang University of Science and Technology
    Inventors: Jiyong Lee, Hyun-Suk Lim, Maria Castaneda
  • Patent number: 10807951
    Abstract: Provided herein, inter alia, are methods and compounds for inhibiting mTORC1 and for treating diseases associated with mTORC1 activity.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: October 20, 2020
    Inventors: Daniel K. Nomura, Roberto Zoncu, Allison M. Roberts, Kelvin F. Cho, Yik Sham Clive Chung, Hijai Shin, Benjamin Croze
  • Patent number: 10800778
    Abstract: The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts are useful in combination with beta-lactam antibiotics, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3, R4, R5 and R6 are described herein.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: October 13, 2020
    Assignee: Entasis Therapeutics Limited
    Inventors: Janelle Comita-Prevoir, Thomas Francois Durand-Reville, Lise Gauthier, John O'Donnell, Jan Romero, Ruben Tommasi, Jeroen Cunera Verheijen, Frank Wu, Xiaoyun Wu, Jing Zhang
  • Patent number: 10799595
    Abstract: A compound of formula (I): (I) and its conjugates.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: October 13, 2020
    Assignee: MedImmune Limited
    Inventors: Philip Wilson Howard, Stephen John Gregson
  • Patent number: 10793554
    Abstract: The present disclosure reports solid forms of (4-(2-fluoro-4-(1-methyl-1H- benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone:
    Type: Grant
    Filed: October 29, 2019
    Date of Patent: October 6, 2020
    Assignee: Forma Therapeutics, Inc.
    Inventors: George P. Luke, Stephen Hubbs, Matthew W. Martin, Robert Wenslow, Yawei Shi, Jun Huang
  • Patent number: 10793572
    Abstract: Disclosed are novel compounds useful in the treatment of multiple sclerosis and other autoimmune diseases. The present invention describes compounds of formula (I) wherein: R1 is selected from H and CH3 R2 is selected from H, C4H9 alkyl, C6H13 alkyl and C3H6-phenyl, said phenyl optionally substituted by OH or OCH3, (1R,2S,5S)-5-methylcyclopent-3-ene-1,2-diol X is O or S Y is C, N or S.
    Type: Grant
    Filed: September 29, 2015
    Date of Patent: October 6, 2020
    Inventors: John Michael Southern, Stephen J. Connon
  • Patent number: 10787417
    Abstract: The present invention relates to a process for purifying caprolactam from solutions of crude caprolactam by a direct treatment with one or more alkaline compounds of polyvalent metals, preferably bivalent and trivalent, without resorting to organic solvent extraction as used in the usual purification process. A further subject of the present invention is a facility devoid of a unit for organic solvent extraction and designed to carry out the caprolactam purification process described herein.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: September 29, 2020
    Assignee: AquafilSLO d.o.o.
    Inventors: Anacleto Dal Moro, Michele Cecchetto, Denis Jahic, Vid Margon
  • Patent number: 10787461
    Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Grant
    Filed: September 13, 2019
    Date of Patent: September 29, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, David Waller, Hwan Guen Choi, Jinhua Wang, Xianming Deng
  • Patent number: 10787463
    Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
    Type: Grant
    Filed: June 6, 2019
    Date of Patent: September 29, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Baudouin Gérard, Manami Shizuka, Michael Louis Miller, Richard A. Silva
  • Patent number: 10787445
    Abstract: The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
    Type: Grant
    Filed: June 12, 2019
    Date of Patent: September 29, 2020
    Assignee: Midwestern University
    Inventors: Mark Jon Olsen, John-Michael Thomas
  • Patent number: 10781174
    Abstract: The present disclosure relates to N-alkylaryl-5-oxyaryl-octadihydrocyclopent[c]pyrrole negative allosteric modulators of NR2B receptors useful in the treatment of neurological diseases having the Formula I: where R1, R2, L1, L2, X, Y, and Y? are described therein.
    Type: Grant
    Filed: January 23, 2019
    Date of Patent: September 22, 2020
    Inventors: David R. Anderson, Robert A. Volkmann, Frank S. Menniti
  • Patent number: 10772962
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: September 15, 2020
    Inventors: Yimin Qian, Hanqing Dong, Jing Wang, Michael Berlin, Andrew P. Crew, Craig M. Crews
  • Patent number: 10758524
    Abstract: The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises piperlongumine (PL) or derivative thereof. The selective killing of senescent cells may delay aging and/or treat age-related disorders.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: September 1, 2020
    Assignee: BioVentures, LLC
    Inventors: Guangrong Zheng, Daohong Zhou, Xingui Liu, Yingying Wang, Jianhui Chang, Wei Feng, Lijian Shao, Yi Luo
  • Patent number: 10759785
    Abstract: The invention relates to compounds of general formula (I): wherein R1, R2, R3, R10 and X? are as defined herein. The compounds are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: September 1, 2020
    Assignee: Enterprise Therapeutics Limited
    Inventors: Clive McCarthy, Jonathan David Hargrave, Duncan Alexander Hay, Thomas Beauregard Schofield, Naomi Went
  • Patent number: 10751341
    Abstract: The invention provides substituted pyrrolo[1,2-a]pyrimidines and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]pyrimidines compounds described herein include substituted 2,4-dimethyl-N-phenylpyrrolo[1,2-a]pyrimidine-8-carboxamide compounds and variants thereof.
    Type: Grant
    Filed: June 26, 2019
    Date of Patent: August 25, 2020
    Assignee: Lysosomal Therapeutics Inc.
    Inventors: Renato T. Skerlj, Peter T. Lansbury, Andrew C. Good, Elyse Marie Josee Bourque, Richard B. Silverman, Dimitri Krainc, Jianbin Zheng
  • Patent number: 10751339
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: August 25, 2020
    Inventors: Ning Xi, Liang Wang, Xuejin Feng, Min Liao