Patents Examined by Erich A. Leeser
  • GPR35 modulators
    Patent number: 11053251
    Abstract: Described herein are GPR35 modulators and methods of using these compounds in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: January 23, 2020
    Date of Patent: July 6, 2021
    Assignee: Prometheus Biosciences, Inc.
    Inventor: Robert Higuchi
  • Crystalline (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, compositions and methods of use thereof
    Patent number: 11053199
    Abstract: Provided herein are crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate. Pharmaceutical compositions comprising crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate are also disclosed.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: July 6, 2021
    Assignees: Celgene Corporation, Abide Therapeutics, Inc.
    Inventors: Lianfeng Huang, Nancy Tsou, Nicole Suzanne White, Jun Xu, Qun Zhang
  • Inhibitors of hepatitis C virus replication
    Patent number: 11053243
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: March 25, 2020
    Date of Patent: July 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soil, Bin Zhong, Jian Zhu
  • Spiropiperidine derivatives
    Patent number: 11046707
    Abstract: Described herein are spiropiperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described spiropiperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described spiropiperidine compounds and synthetic intermediates that are useful in those syntheses.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: June 29, 2021
    Assignee: 89BIO LTD
    Inventors: Robert L. Hudkins, David B. Whitman, Craig A. Zificsak, Allison L. Zulli, Melody McWherter
  • Fused 1,4-diazepines as BET bromodomain inhibitors
    Patent number: 11046709
    Abstract: The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.
    Type: Grant
    Filed: February 2, 2018
    Date of Patent: June 29, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jiantao Hu, Fuming Xu
  • Pyruvate kinase activators for use in treating blood disorders
    Patent number: 11040036
    Abstract: Described herein are compounds that activate pyruvate kinase, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I) wherein R1, R2, Ra, Rb, Rj, Rk, and Q are as defined herein.
    Type: Grant
    Filed: November 19, 2020
    Date of Patent: June 22, 2021
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Giovanni Cianchetta, Tao Liu, Anil Kumar Padyana, Zhihua Sui, Zhenwei Cai, Dawei Cui, Jingjing Ji
  • Methods of treating cancer
    Patent number: 11040040
    Abstract: Provided herein are, inter alia, methods of treating a cancer tumor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an adenosine A2A receptor antagonist, wherein the subject comprises an elevated level of CD8+ tumor infiltrating lymphocytes relative to a control, the subject comprises an elevated level of T-effector gene signature relative to a control, the subject comprises an increased cancer tumor T cell receptor diversity or blood T cell receptor diversity relative to a control, the cancer tumor comprises an elevated level of PD-L1 relative to a control, and/or the cancer tumor or the blood of the subject comprises an elevated level of CD73 relative to a control. Further provided are, inter alia, methods for determining whether a subject is likely to, is, or has responded to anti-cancer therapy comprising an A2A receptor antagonist.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: June 22, 2021
    Assignee: Corvus Pharmaceuticals, Inc.
    Inventors: Andrew Hotson, Richard A. Miller, Ian Mccaffery, Stephen Willingham
  • Carboxamide-pyrimidine derivatives as SHP2 antagonists
    Patent number: 11033547
    Abstract: The invention relates to carboxamide-pyrimidine derivatives of the general formula I, or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
    Type: Grant
    Filed: March 9, 2020
    Date of Patent: June 15, 2021
    Assignee: Merck Patent GmbH
    Inventors: Catherine Jorand-LeBrun, Roch Boivin, Igor Mochalkin, Theresa Johnson, Nina Linde, Doreen Musch, Deepak Kumar
  • Modulators of BTK proteolysis and methods of use
    Patent number: 11028088
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: June 8, 2021
    Assignee: Yale University
    Inventors: Craig M. Crews, Saul Jaime-Figueroa, Momar Toure
  • Preparative scale conversion of gonyautoxins to neosaxitoxin
    Patent number: 11028094
    Abstract: A method of preparing neosaxitoxin in quantities of a purity sufficient to allow the compound to be used as an active pharmaceutical ingredient (API) is described. The method includes the reductive desulfonation of an unresolved mixture of gonyautoxin 1 (GTX1) and gonyautoxin 4 (GTX4).
    Type: Grant
    Filed: September 11, 2020
    Date of Patent: June 8, 2021
    Inventors: Andrew Ian Selwood, Roelof Van Ginkel, Craig Alan Waugh
  • CD73 inhibitors
    Patent number: 11028074
    Abstract: The present invention provides 5-[5]-[2-cycloalkyl]-6-pyridazin-3-yl]-1H-pyrimidine-2,4-dione compounds, or pharmaceutically acceptable salts thereof, that inhibit the activity of CD73 and are useful in treating cancer.
    Type: Grant
    Filed: February 22, 2019
    Date of Patent: June 8, 2021
    Assignee: Eli Lilly and Company
    Inventors: Robert Dean Dally, Maria Cristina Garcia Paredes, Lawrence Joseph Heinz, II, Jennifer Marie Howell, Frank George Njoroge, Yan Wang, Genshi Zhao
  • Compositions and methods for inhibiting arginase activity
    Patent number: 11021495
    Abstract: The disclosure relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the disclosure. Also provided herein are methods of treating cancer with the arginase inhibitors of the disclosure.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: June 1, 2021
    Assignee: Calithera Biosciences, Inc.
    Inventors: Eric B. Sjogren, Jim Li, Lijing Chen, Roland J. Billedeau, Timothy F. Stanton, Michael Van Zandt, Darren Whitehouse, Gunnar E. Jagdmann, Jr., Lene Raunkjær Petersen
  • Triazolopyrimidine, triazolopyridine compounds, and the composition thereof for treating PRC2-mediated diseases
    Patent number: 11013745
    Abstract: The present invention provides a compound represented by formula I, pharmaceutically acceptable salts, enantiomers, diastereomers or racemates thereof, the preparation method thereof, the pharmaceutical composition comprising the same, and the use thereof in the preparation of a medicament for treating a disease or condition mediated by EED and/or PRC2. The compound of the present invention can be used treating PRC2-mediated diseases or conditions.
    Type: Grant
    Filed: August 29, 2018
    Date of Patent: May 25, 2021
    Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU SUPLEAD LIFE SCIENCES CO., LTD.
    Inventors: Bing Zhou, Cheng Luo, Yaxi Yang, Yuanyuan Zhang, Daohai Du, Hualiang Jiang, Gang Qiao, Xinjun Wang
  • Inhibitors of cancer invasion, attachment, and/or metastasis
    Patent number: 11008325
    Abstract: Provided herein are, inter alia, compositions that bind to a PDZ1 domain of MDA-9/Syntenin (syndecan binding protein: SDCBP), thereby inhibiting MDA-9/Syntenin activity, and methods of use of same. The compositions and methods provided herein are useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: May 18, 2021
    Assignees: VIRGINIA COMMONWEALTH UNIVERSITY, SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Paul B. Fisher, Maurizio Pellecchia, Swadesh K. Das, Timothy P. Kegelman, Bainan Wu, Surya K. De, Jun Wei, Mitchell E. Menezes, Luni Emdad
  • TRAF 6 inhibitors
    Patent number: 11001591
    Abstract: The invention relates to compounds which are suitable for the treatment of cancer, an immune disease, Parkinson's disease, Cardiac Hypertrophy or Type-2 diabetes and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds.
    Type: Grant
    Filed: March 9, 2020
    Date of Patent: May 11, 2021
    Assignee: HELMHOLTZ ZENTRUM MUENCHEN—DEUTSCHES FORSCHUNGSZENTRUM FÜR GESUNDHEIT UND UMWELT (GMBH)
    Inventors: Kamyar Hadian, Jara Kerstin Brenke, Oliver Plettenburg, Gerrit Juerjens
  • Pyrimidinone derivatives as SHP2 antagonists
    Patent number: 11001561
    Abstract: The invention relates to pyrimidinone derivatives of the general Formula I, or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
    Type: Grant
    Filed: April 8, 2020
    Date of Patent: May 11, 2021
    Assignee: Merck Patent GmbH
    Inventors: Catherine Jorand-Lebrun, Roch Boivin, Theresa Johnson, Yanping Wang, Yufang Xiao, Xiaoling Chen, Nina Linde, Doreen Musch, Deepak Kumar
  • 2-oxo-thiazole derivatives as A2A inhibitors and compounds for use in the treatment of cancers
    Patent number: 10995101
    Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: May 4, 2021
    Assignee: iTeos Therapeutics SA
    Inventors: Stefano Crosignani, Bruno Gomes, Erica Houthuys
  • Organic electroluminescent compound and organic electroluminescent device comprising the same
    Patent number: 10991889
    Abstract: The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. An organic electroluminescent device having a low driving voltage, a high luminous efficiency and/or excellent color coordinates can be provided by comprising the organic electroluminescent compound according to the present disclosure.
    Type: Grant
    Filed: July 19, 2018
    Date of Patent: April 27, 2021
    Assignee: Rohm and Haas Electronic Materials Korea Ltd.
    Inventors: Hyun Kim, Doo-Hyeon Moon, Sang-Hee Cho, Sung-Wook Cho
  • Pyrazolo[1,5a]pyrimidine derivatives as IRAK4 modulators
    Patent number: 10988478
    Abstract: Compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
    Type: Grant
    Filed: January 29, 2020
    Date of Patent: April 27, 2021
    Assignee: Genentech, Inc.
    Inventors: Marian C. Bryan, Alberto Gobbi, James Richard Kiefer, Jr., Aleksandr Kolesnikov, Alan G. Olivero, Joy Drobnick, Jun Liang, Naomi Rajapaksa, Chudi Ndubaku, Jianwen Feng
  • Pyrrolotriazinones and imidazotriazinones as ubiquitin-specific protease 7 inhibitors
    Patent number: 10981915
    Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, R6, X1, X2, m, and n are described herein.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: April 20, 2021
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell