Patents Examined by Jeffrey H Murray
  • Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof
    Patent number: 10980816
    Abstract: The present invention relates to compounds of formula (1): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
    Type: Grant
    Filed: June 29, 2020
    Date of Patent: April 20, 2021
    Assignee: Sanofi
    Inventors: Jean-Christophe Carry, Fabienne Chatreaux, Stephanie Deprets, Olivier Duclos, Vincent Leroy, Sergio Mallart, Dominique Melon-Manguer, Maria Mendez-Perez, Fabrice Vergne
  • Substituted fused pyrazole compounds and their use as LRRK2 inhibitors
    Patent number: 10975081
    Abstract: Disclosed are substituted fused pyrazoles, for example substituted indazoles, that inhibit LRRK2 kinase activity, pharmaceutical compositions containing them and their use in the treatment of Parkinson's disease.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: April 13, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Xiao Ding, Yun Jin, Qian Liu, Feng Ren, Yingxia Sang, Luigi Piero Stasi, Zehong Wan, Hailong Wang, Weiqiang Xing, Yang Zhan, Baowei Zhao
  • Inhibitor of FLT3 kinase and use thereof
    Patent number: 10975082
    Abstract: The present invention provides a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. The present invention also provides a pharmaceutical composition comprising the compound of formula (I), as well as the use and method for preventing or treating FLT3-related conditions, especially conditions related to mutant FLT3 kinase (particularly, FLT3/ITD mutant kinase).
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: April 13, 2021
    Assignee: PRECEDO PHARMACEUTICALS CO., LTD
    Inventors: Qingsong Liu, Jing Liu, Xixiang Li, Aoli Wang, Ziping Qi, Hong Wu, Jiaxin Wu, Wenchao Wang, Chen Hu, Cheng Chen, Li Wang, Beilei Wang
  • 4-aminoquinazolinyl compounds as prolyl hydroxylase inhibitors
    Patent number: 10975062
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: April 13, 2021
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • JAK inhibitors and uses thereof
    Patent number: 10973913
    Abstract: The present invention provides methods for treating pruritus in a subject in need thereof comprising administering a therapeutically effective amount of a JAK inhibitor. Also provided are methods of intranasal administration of JAK inhibitors for use in treating pruritus.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: April 13, 2021
    Assignee: Washington University
    Inventor: Brian Kim
  • Crystalline forms of a Bruton's tyrosine kinase inhibitor
    Patent number: 10961251
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: November 18, 2020
    Date of Patent: March 30, 2021
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
    Patent number: 10947222
    Abstract: The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: March 16, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Thomas H. Graham, Jinlong Jiang, Fa-Xiang Ding, Clare Tudge
  • Certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor
    Patent number: 10946014
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: March 16, 2021
    Assignee: Hutchison Medipharma Limited
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • Forms of a PI3K delta selective inhibitor for use in pharmaceutical formulations
    Patent number: 10947244
    Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: March 16, 2021
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventor: Swaroop K. Vakkalanka
  • Heterocyclic compounds and uses thereof
    Patent number: 10941162
    Abstract: Trisubstituted bicyclic heterocyclic compounds (e.g., pyridopyrimidinones) and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: March 1, 2019
    Date of Patent: March 9, 2021
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Martin R. Tremblay
  • Methods and compositions for treatment of Zika virus infection
    Patent number: 10933066
    Abstract: Disclosed are 9-deazaaadenine derivatives of the general formula (I) and pharmaceutically acceptable salts thereof, wherein A is OH or NH2, and B is H or NH2. Methods for treating and/or suppressing a Zika virus infection with the compounds disclosed are also provided. Pharmaceutical compositions comprising the disclosed compounds are also provided. Such pharmaceutical compositions may optionally contain one or more additional active agents.
    Type: Grant
    Filed: November 22, 2019
    Date of Patent: March 2, 2021
    Assignee: Biocryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pravin L. Kotian, Shanta Bantia
  • Compounds and compositions for inhibiting the activity of SHP2
    Patent number: 10934285
    Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, R1, R2 and R3 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: March 2, 2021
    Assignee: NOVARTIS AG
    Inventors: Zhuoliang Chen, Jorge Garcia Fortanet, Rajesh Karki, Matthew J. Lamarche, Dyuti Majumdar, Lawrence Blas Perez, Martin Sendzik, Troy Douglas Smith, Fan Yang, Bing Yu
  • Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors
    Patent number: 10934299
    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 m, n, X1, X2, R1-R5, R5? and R6 are described herein.
    Type: Grant
    Filed: July 19, 2019
    Date of Patent: March 2, 2021
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, Darby Rye Schmidt, David Joseph Guerin, Justin Andrew Caravella, R. Bruce Diebold, Anna Ericsson, David R. Lancia, Jr.
  • Solid pharmaceutical compositions comprising biopterin derivatives and uses of such compositions
    Patent number: 10925877
    Abstract: Compositions comprising derivatives of biopterin, useful for the treatment of traumatic brain injury, non-traumatic brain injury, elevated cranial pressure, and secondary brain injury.
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: February 23, 2021
    Assignee: VASOPHARM GMBH
    Inventors: Peter Scheurer, Frank Tegtmeier, Reinhard Schinzel
  • Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
    Patent number: 10927130
    Abstract: The disclosure 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?, X1, X2, X3, n, and m are described herein.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: February 23, 2021
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell
  • CDK inhibitors
    Patent number: 10927120
    Abstract: Compounds of Formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: May 13, 2020
    Date of Patent: February 23, 2021
    Assignee: GI Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay Copeland Strum
  • Adenine derivatives which are useful in the treatment of allergic diseases or other inflammatory conditions
    Patent number: 10919894
    Abstract: Compounds of formula (I): wherein: R1 is butoxy or methylbutoxy; R2 is a group having the structure: where n is an integer having a value of five; Het is a six-membered saturated heterocycle containing five carbon atoms and one nitrogen atom, wherein Het is attached to the —(CH2)n— moiety at the carbon 4 position of the heterocycle; and R3 is hydrogen; or pharmaceutically acceptable salts thereof; and their use as vaccine adjuvants and in the treatment of various disorders.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: February 16, 2021
    Assignee: GLAXOSMITHKLINE BIOLOGICALS SA
    Inventors: Helene G. Bazin-Lee, Yufeng Li
  • Preparation and uses of pyrimidinone derivatives
    Patent number: 10919896
    Abstract: The present invention relates to compounds of formula (I), and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity: wherein X, R1, R2, and n are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: February 16, 2021
    Assignee: Cancer Research Technology Limited
    Inventors: Emma L. Carswell, Mark David Charles, Anne Cochi, Benjamin J. Dugan, Chukuemeka Tennyson Ekwuru, Fred Elustondo, Katherine M. Fowler, Frederic Georges Marie Leroux, Nathaniel J. T. Monck, Gregory R. Ott, Jonathan R. Roffey, Gurwinder Sidhu, Neil Tremayne
  • Broad spectrum antiviral compounds
    Patent number: 10919922
    Abstract: Antiviral compounds comprising prodrugs with differing side chains derived from a tyrosine substance in the form of a tyrosine amide in which the amide substituent side chain is an alkyl ether, thioether, or alkene. Embodiments of the compounds have a range of effective lipophilicity values allowing variation in aqueous solubility, oral bioavailability, cell permeability and in vivo activation properties. The embodiments have promoieties derived from a single amino acid, which are expected to have low toxicity. The features described above also make possible a novel “precision medicine” approach to treatment of viral infections, whereby the prodrug variations can be exploited to match optimal activation of the prodrug to a given patient or strain of virus.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: February 16, 2021
    Assignee: University of Southern California
    Inventors: Charles E. McKenna, Boris A. Kashemirov, Jaijun Fan, Jinglei Lyu
  • Diketopiperazine salts for drug delivery and related methods
    Patent number: 10912821
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: February 9, 2021
    Assignee: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson