Patents Assigned to Heptares Therapeutics Limited
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Patent number: 11208396Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and 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 p; q; X1; X2; Y; R1; R2; R3; R4; R5 and R6 are as defined herein.Type: GrantFiled: November 2, 2016Date of Patent: December 28, 2021Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Benjamin Gerald Tehan
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Patent number: 11091456Abstract: 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: GrantFiled: May 21, 2019Date of Patent: August 17, 2021Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Patent number: 11014880Abstract: 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: GrantFiled: June 2, 2020Date of Patent: May 25, 2021Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Publication number: 20210148939Abstract: A method of producing a conformational specific binding partner of a GPCR, the method comprising: a) providing a mutant GPCR of a parent GPCR, wherein the mutant GPCR has increased stability in a particular conformation relative to the parent GPCR; b) providing a test compound; c) determining whether the test compound binds to the mutant GPCR when residing in a particular conformation; and d) isolating a test compound that binds to the mutant GPCR when residing in the particular formation. Methods of producing GPCRs with increased stability relative to a parent GPCR are also disclosed.Type: ApplicationFiled: November 30, 2020Publication date: May 20, 2021Applicant: Heptares Therapeutics LimitedInventors: Malcolm Peter Weir, Richard Henderson, Christopher Gordon Tate, Francesca Magnani, Maria Josefa Serrano-Vega, Yoko Shibata, Antony Johannes Warne
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Patent number: 10995072Abstract: The present application relates to certain substituted imidazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions.Type: GrantFiled: December 27, 2019Date of Patent: May 4, 2021Assignee: Heptares Therapeutics LimitedInventors: John Graham Cumming, Frank Xinhe Wu, Karl Henrik Edman, Hongming Chen, Dean Gordon Brown, Roland Werner Burli, Shawn Donald Johnstone, Giles Albert Brown, Benjamin Gerald Tehan, Barry John Teobald, Miles Stuart Congreve
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Patent number: 10988455Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whicType: GrantFiled: October 16, 2018Date of Patent: April 27, 2021Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Patent number: 10981889Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.Type: GrantFiled: February 3, 2020Date of Patent: April 20, 2021Assignee: Heptares Therapeutics LimitedInventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Aves, Benjamin Gerald Tehan
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Patent number: 10973832Abstract: 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 I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.Type: GrantFiled: September 4, 2019Date of Patent: April 13, 2021Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
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Patent number: 10961225Abstract: 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: GrantFiled: June 17, 2020Date of Patent: March 30, 2021Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
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Publication number: 20210061882Abstract: The invention relates to mutant G-protein coupled receptors with increased conformational stability, and methods of use thereof. In some aspects, polynucleotides encoding the mutant G-protein coupled receptors are provided. In some aspects, host cells comprising the polynucleotides are provided. In some aspects, the invention relates to crystallized forms of the mutant G-protein coupled receptors, and methods of preparing the same.Type: ApplicationFiled: May 11, 2020Publication date: March 4, 2021Applicant: Heptares Therapeutics LimitedInventors: Richard Henderson, Christopher Gordon Tate, Francesca Magnani, Maria Josefa Serrano-Vega, Yoko Shibata, Antony Johannes Warne, Malcolm Peter Weir
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Patent number: 10888561Abstract: 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: GrantFiled: April 8, 2019Date of Patent: January 12, 2021Assignee: Heptares Therapeutics LimitedInventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
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Patent number: 10858352Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and 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 where X1; X2; X3; X4; R1 R2 and R4 are as defined herein.Type: GrantFiled: June 24, 2019Date of Patent: December 8, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Barry John Teobald, Benjamin Gerald Tehan
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Patent number: 10787447Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and 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 where Y, R1, R2 and R4 are as defined herein.Type: GrantFiled: June 24, 2019Date of Patent: September 29, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Barry John Teobald, Benjamin Gerald Tehan
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Patent number: 10766945Abstract: The invention provides a fusion protein comprising, from N-terminus to C-terminus: a) a first portion of a Family B G-protein coupled receptor (GPCR) that comprises transmembrane helix (TM)-1, TM2 and TM3 of the GPCR; b) a stable protein domain; and c) a second portion of the GPCR comprising TM4, TM5, TM6 and TM7 of the GPCR. The invention also provides a method of crystallising a GPCR comprising providing the fusion protein of the invention and crystallising it to obtain crystals.Type: GrantFiled: September 20, 2018Date of Patent: September 8, 2020Assignee: Heptares Therapeutics LimitedInventors: Seyed Ali Jazayeri-Dezfuly, Fiona Hamilton Marshall
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Patent number: 10759751Abstract: 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: GrantFiled: March 7, 2019Date of Patent: September 1, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Patent number: 10752610Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and 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 (1) wherein X1; X2; R1 and R4 are as defined herein.Type: GrantFiled: May 14, 2019Date of Patent: August 25, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Benjamin Gerald Tehan, Barry John Teobald
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Patent number: 10738287Abstract: The invention provides a mutant of a parent heterotrimeric G protein alpha (G?) subunit, which mutant (i) lacks at least one helix of the helical domain of the parent G? subunit; (ii) is capable of binding to a GPCR in the absence of a heterotrimeric G protein beta (G?) subunit and a heterotrimeric G protein gamma (G?) subunit; and (iii) has an amino acid sequence that contains one or more mutations compared to the amino acid sequence of the parent heterotrimeric G? subunit, which mutations are selected from a deletion, a substitution and an insertion.Type: GrantFiled: January 27, 2017Date of Patent: August 11, 2020Assignee: Heptares Therapeutics LimitedInventors: Byron Carpenter, Andrew Leslie, Rony Nehmé, Christopher Gordon Tate, Antony Warne
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Patent number: 10738029Abstract: 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: GrantFiled: August 3, 2016Date of Patent: August 11, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Cansfield, Mark Pickworth, Benjamin Gerald Tehan, Barry John Teobald
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Patent number: 10695321Abstract: The invention relates to a novel use of the antimuscarinic agent glycopyrrolate, for example the salt glycopyrronium bromide. In particular, the invention relates to glycopyrrolate for use as a heart rate lowering agent and more particularly, but not exclusively, for use in patients suffering from respiratory conditions such as chronic obstructive pulmonary disease.Type: GrantFiled: January 31, 2016Date of Patent: June 30, 2020Assignee: HEPTARES THERAPEUTICS LIMITEDInventors: Susan Snape, Robert Tansley
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Patent number: 10689368Abstract: 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: GrantFiled: July 1, 2019Date of Patent: June 23, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald