Patents by Inventor Mark Pickworth

Mark Pickworth has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • SARS-COV-2 MPRO INHIBITOR COMPOUNDS
    Publication number: 20240083845
    Abstract: The disclosures herein relate to compounds of Formula (1?): or a salt thereof, wherein A, Q, X, Z, L, R2, R3 and R9 are defined herein, and their use in the treatment of SARS-CoV-2 and related viruses and disorders associated with SARS-CoV-2: Mpro.
    Type: Application
    Filed: December 20, 2021
    Publication date: March 14, 2024
    Applicant: HEPTARES THERAPEUTICS LIMITED
    Inventors: Miles Stuart CONGREVE, John Andrew CHRISTOPHER, Mark PICKWORTH, Chris DE GRAAF, Alicia Perez HIGUERUELO, Jonathan Stephen MASON, Santosh S. KULKARNI
  • Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists
    Patent number: 11834407
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
    Type: Grant
    Filed: May 3, 2021
    Date of Patent: December 5, 2023
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • MEDIUM- OR MACRO-CYCLIC BENZYL-SUBSTITUTED HETEROCYCLE DERIVATIVES AND THEIR USES AS OREXIN-2 RECEPTOR AGONISTS
    Publication number: 20230331720
    Abstract: The present disclosure relates to compounds of Formula (I?): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating orexin-2 receptor activity and may be used in the treatment of disorders in which orexin-2 receptor activity is implicated, such as narcolepsy, a hypersomnia disorder, a neurodegenerative disorder, a symptom of a rare genetic disorder, a mental health disorder, a metabolic syndrome, osteoporosis, cardiac failure, coma, or facilitating emergence from anaesthesia.
    Type: Application
    Filed: September 3, 2021
    Publication date: October 19, 2023
    Inventors: Bruce LEFKER, Gordon SAXTY, Karl GIBSON, Mark PICKWORTH, Matthew SPENDIFF, Miles Stuart CONGREVE, Paul HUMPHRIES
  • H4 ANTAGONIST COMPOUNDS
    Publication number: 20230167094
    Abstract: The disclosure herein relates to azetidinylpyrimidin-2-amine derivatives, their use as Histamine H4 receptor antagonists and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with H4 receptors.
    Type: Application
    Filed: April 22, 2021
    Publication date: June 1, 2023
    Applicant: Heptares Therapeutics Limited
    Inventors: Miles Stuart CONGREVE, Charlotte FIELDHOUSE, Nigel Alan SWAIN, Mark PICKWORTH, Duncan Robert HANNAH
  • MUSCARINIC AGONISTS
    Publication number: 20230002354
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.
    Type: Application
    Filed: February 15, 2022
    Publication date: January 5, 2023
    Inventors: Giles Albert Brown, Julie Cansfield, Mark Pickworth, Benjamin Gerald Tehan, Barry John Teobald
  • SUBSTITUTED CYCLOHEXANES AS MUSCARINIC M1 RECEPTOR AND/OR M4 RECEPTOR AGONISTS
    Publication number: 20220213034
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
    Type: Application
    Filed: May 3, 2021
    Publication date: July 7, 2022
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Muscarinic agonists
    Patent number: 11324738
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1a or a salt thereof, wherein n, p, Q, R1, R2, R3, R9 and R4 are as defined herein.
    Type: Grant
    Filed: December 27, 2019
    Date of Patent: May 10, 2022
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan
  • Muscarinic agonists
    Patent number: 11254656
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.
    Type: Grant
    Filed: July 29, 2020
    Date of Patent: February 22, 2022
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Mark Pickworth, Benjamin Gerald Tehan, Barry John Teobald
  • MUSCARINIC RECEPTOR AGONISTS
    Publication number: 20220048928
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2, R3 and R4 are as defined herein.
    Type: Application
    Filed: June 11, 2021
    Publication date: February 17, 2022
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
  • QUINOLINONE AND BENZOXAZINE DERIVATIVES AS MUSCARINIC M1 AND/OR M4 RECEPTOR AGONISTS
    Publication number: 20220017504
    Abstract: This invention related to compounds having activity as muscarinic M1 or M1 and M4 receptor agonists which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (I) where X1; X2; X3; X4; Y; Z; n, R1 and R2 are defined herein.
    Type: Application
    Filed: December 9, 2019
    Publication date: January 20, 2022
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Benjamin Gerald Tehan, Mark Pickworth
  • PYRAZOLE DERIVATIVES AS H4 ANTAGONIST COMPOUNDS
    Publication number: 20210300906
    Abstract: The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein A; X; n; R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with H4 receptors.
    Type: Application
    Filed: October 21, 2019
    Publication date: September 30, 2021
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Barry John Teobald, Charlotte Fieldhouse, Nigel Alan Swain, Mark Pickworth, Giovanni Bottegoni
  • Muscarinic agonists
    Patent number: 11091456
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1a) or a salt thereof, wherein p, q, r, s, Q, R3 and R4 are as defined herein.
    Type: Grant
    Filed: May 21, 2019
    Date of Patent: August 17, 2021
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • CGRP RECEPTOR ANTAGONISTS
    Publication number: 20210213011
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Application
    Filed: December 31, 2020
    Publication date: July 15, 2021
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Muscarinic receptor agonists
    Patent number: 11034704
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: June 15, 2021
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
  • Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists
    Patent number: 11014880
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
    Type: Grant
    Filed: June 2, 2020
    Date of Patent: May 25, 2021
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Bicyclic AZA compounds as muscarinic M1 receptor and/or M4 receptor
    Patent number: 10961225
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: June 17, 2020
    Date of Patent: March 30, 2021
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • CGRP receptor antagonists
    Patent number: 10888561
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: January 12, 2021
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • MUSCARINIC AGONISTS
    Publication number: 20200354339
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.
    Type: Application
    Filed: July 29, 2020
    Publication date: November 12, 2020
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Mark Pickworth, Benjamin Gerald Tehan, Barry John Teobald
  • BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AND/OR M4 RECEPTOR
    Publication number: 20200325118
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Application
    Filed: June 17, 2020
    Publication date: October 15, 2020
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • SUBSTITUTED CYCLOHEXANES AS MUSCARINIC M1 RECEPTOR AND/OR M4 RECEPTOR AGONISTS
    Publication number: 20200290963
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
    Type: Application
    Filed: June 2, 2020
    Publication date: September 17, 2020
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan