Patents Examined by Bruck Kifle
  • Patent number: 10894793
    Abstract: The present invention relates to bicyclic pyridine, pyrazine, and pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: January 19, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Claude Berthelot, Laurence Anne Mevellec, Patrick Rene Angibaud, Sophie Coupa, Christophe Gabriel Marcel Demestre, Lieven Meerpoel, Guillaume Jean Maurice Mercey, Christophe Meyer, Elisabeth Therese Jeanne Pasquter, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Olivier Alexis Georges Querolle
  • Patent number: 10894796
    Abstract: The present invention provides methods of preparing a MK2 inhibitor, and intermediates related thereto.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: January 19, 2021
    Assignee: Celgene CAR LLC
    Inventors: Gregg Brian Feigelson, Maryll E. Geherty, Richard Martin Heid, Jr., Mohit Kothare, Hon-Wah Man, Alexander L. Ruchelman, John F. Traverse, Kelvin Hin-Yeong Yong, Chengmin Zhang
  • Patent number: 10889592
    Abstract: The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: (I), where R1, R2, R3, R4, R4?, R5, R6, X, and n are described herein.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: January 12, 2021
    Assignee: VALO EARLY DISCOVERY, INC.
    Inventors: David Joseph Guerin, Kenneth W. Bair, Justin A. Caravella, Stephanos Ioannidis, Jr., David R. Lancia, Jr., Hongbin Li, Steven Mischke, Pui Yee Ng, David Richard, Shawn E. R. Schiller, Tatiana Shelekhin, Zhongguo Wang
  • Patent number: 10882867
    Abstract: The present invention provides solid forms of an MK2 inhibitor, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: January 5, 2021
    Assignee: Celgene CAR LLC
    Inventors: Jianxin Han, Lianfeng Huang, Uday Jain, Ying Li, John Malona, Kevin Molter, Chittari Pabba, Alexander L. Ruchelman, Jean Xu, Daozhong Zou
  • Patent number: 10882862
    Abstract: The invention relates to stable, isotopically labeled compounds for use in mass spectrometry analysis for quantifying methotrexate in a sample. Exemplary compounds include isotopically labeled variants of methotrexate.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: January 5, 2021
    Assignee: Micromass UK Limited
    Inventors: Donald Peter Cooper, Billy J. Molloy
  • Patent number: 10882865
    Abstract: Disclosed are new small molecules having a pyrrolopyrimidine core structure and the uses thereof for modulating glucocerebrosidase activity. Also disclosed are pharmaceutical compositions comprising the small molecules which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurological diseases and disorders such as Gaucher's disease and Parkinson's disease. The small molecules may be utilized to generate activated glucocerebrosidase. The activated glucocerebrosidase thusly generated can be administered in enzyme replacement therapy and/or utilized in screening assays for new small molecules that bind to the activated glucocerebrosidase and/or modulate the activity of the activated glucocerebrosidase.
    Type: Grant
    Filed: August 29, 2019
    Date of Patent: January 5, 2021
    Assignee: Northwestern University
    Inventors: Dimitri Krainc, Richard B. Silverman, Jianbin Zheng
  • Patent number: 10870625
    Abstract: The disclosure provides compounds of the formula I and the pharmaceutically acceptable salts thereof. The variables, e.g. R1, R2, R3, R4, A, B, J, V, W, M, J and Ar are defined herein. The disclosure also provides pharmaceutical compositions comprising a compound or salt of formula I and a pharmaceutically acceptable carrier, methods of inhibiting dihydrofolate reductase (DHFR) in vitro or in vivo with a compound or salt of formula I, and methods of treating a bacterial infections, fungal infections, and protozoal infections with a compound or salt of formula I. A compound or salt of formula I can be the first and only active ingredient used in a pharmaceutical composition or method of this disclosure or may be combined with one or more additional active ingredients that are not compounds or salts of formula I.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: December 22, 2020
    Assignee: UNIVERSITY OF CONNECTICUT
    Inventors: Dennis Wright, Amy C. Anderson, Eric Scocchera, Narendran Gummudipundi Dayanandan, Santosh Keshipeddy, Stephanie Reeve, Michael N. Lombardo, Michael Henry Cynamon
  • Patent number: 10870657
    Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: December 22, 2020
    Assignee: SHY Therapeutics LLC
    Inventors: Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds
  • Patent number: 10870661
    Abstract: The present invention provides a novel compound having antiviral activity, especially HIV replication inhibitory activity and a medicament containing the same. The compound represented by the formula: wherein A3 is CR3A, CR3AR3B, N or NR3C; R3A, R3B, R4A and R4B are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted non-aromatic carbocyclyl; R3C is a hydrogen atom, substituted or unsubstituted alkyl, or substituted or unsubstituted non-aromatic carbocyclyl; ring T1 is substituted or unsubstituted nitrogen-containing non-aromatic heterocycle; R1 is a hydrogen atom, halogen, cyano, or substituted or unsubstituted alkyl; R2 is each independently substituted or unsubstituted alkyl or the like: n is 1 or 2; R3 is substituted or unsubstituted aromatic carbocyclyl or the like; R4 is a hydrogen atom or a carboxy protecting group.
    Type: Grant
    Filed: October 28, 2019
    Date of Patent: December 22, 2020
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshinori Tamura, Shuichi Sugiyama, Akira Matsumura, Toshiyuki Akiyama, Yutaka Tomida
  • Patent number: 10865213
    Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.
    Type: Grant
    Filed: October 22, 2018
    Date of Patent: December 15, 2020
    Assignee: Massachusetts Institute of Technology
    Inventors: Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
  • Patent number: 10865215
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: December 15, 2020
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Brian C. Shook, In Jong Kim, Thomas P. Blaisdell, Jianming Yu, Joseph Panarese, Yat Sun Or
  • Patent number: 10865204
    Abstract: The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: December 15, 2020
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski, Baishan Jiang, Eric Wang
  • Patent number: 10865205
    Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: December 15, 2020
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
  • Patent number: 10851070
    Abstract: The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors.
    Type: Grant
    Filed: November 14, 2019
    Date of Patent: December 1, 2020
    Assignee: Enata Pharmaceuticals, Inc.
    Inventors: Andrew Hague, Matthew Ronsheim
  • Patent number: 10851117
    Abstract: The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
    Type: Grant
    Filed: November 11, 2019
    Date of Patent: December 1, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Michael Reardon, Richard A. Silva
  • Patent number: 10851058
    Abstract: Provided herein are compounds and methods for inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: December 1, 2020
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Shripad Bhagwat, Gregory Luedtke, Alexander Bridges
  • Patent number: 10844078
    Abstract: The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: November 24, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Baudouin Gérard, Richard A. Silva, Michael Louis Miller, Manami Shizuka
  • 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: 10844055
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: March 1, 2019
    Date of Patent: November 24, 2020
    Assignee: NOVARTIS AG
    Inventors: Guillaume Barbe, Gregory Raymond Bebernitz, Sicong Geng, Hatice Belgin Gulgeze Efthymiou, Lv Liao, Fupeng Ma, Ruowei Mo, David Thomas Parker, Yunshan Peng, Stefan Peukert, Ken Yamada, Kayo Yasoshima, Nichola Smith