Patents Assigned to Heptares Therapeutics Limited
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Patent number: 10174101Abstract: 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 crystallizing a GPCR comprising providing the fusion protein of the invention and crystallizing it to obtain crystals.Type: GrantFiled: August 9, 2012Date of Patent: January 8, 2019Assignee: Heptares Therapeutics LimitedInventors: Seyed Ali Jazayeri-Dezfuly, Fiona Hamilton Marshall
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Patent number: 10167272Abstract: 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: February 1, 2018Date of Patent: January 1, 2019Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Patent number: 10166226Abstract: The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 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: January 29, 2018Date of Patent: January 1, 2019Assignee: 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: 10167284Abstract: This invention relates to compounds that are agonists of the muscarinic M1 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 provided are of formula where p, q, r, s, X, Z, Y, R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: March 21, 2016Date of Patent: January 1, 2019Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
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Patent number: 10126313Abstract: 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: GrantFiled: January 6, 2016Date of Patent: November 13, 2018Assignee: 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: 10112923Abstract: 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 carbocylic 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, whichType: GrantFiled: November 4, 2016Date of Patent: October 30, 2018Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Patent number: 10030012Abstract: The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.Type: GrantFiled: March 10, 2017Date of Patent: July 24, 2018Assignee: Heptares Therapeutics LimitedInventors: David Livermore, Kathryn White, Miles Congreve, Giles Brown, Michael O'Brien
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Patent number: 10030035Abstract: 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: GrantFiled: March 19, 2015Date of Patent: July 24, 2018Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
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Patent number: 9975890Abstract: This invention relates to compounds (Formula (1)) 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 R1-R5, X1, X2 and p are as defined herein.Type: GrantFiled: May 15, 2017Date of Patent: May 22, 2018Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Publication number: 20180086814Abstract: 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: September 26, 2017Publication date: March 29, 2018Applicant: 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: 9925178Abstract: The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 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: May 5, 2017Date of Patent: March 27, 2018Assignee: 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: 9926297Abstract: 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: May 10, 2017Date of Patent: March 27, 2018Assignee: 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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Patent number: 9907805Abstract: 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: February 17, 2017Date of Patent: March 6, 2018Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
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Patent number: 9850237Abstract: The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.Type: GrantFiled: January 18, 2017Date of Patent: December 26, 2017Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, John Andrew Christopher, Benjamin Gerald Tehan, Sukhbinder Singh Klair, Sarah Joanne Aves
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Patent number: 9808457Abstract: 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: October 28, 2016Date of Patent: November 7, 2017Assignee: 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: 9802935Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2 and R3 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: October 28, 2016Date of Patent: October 31, 2017Assignee: 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: 9758506Abstract: 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: August 3, 2016Date of Patent: September 12, 2017Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Patent number: 9688660Abstract: The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 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: October 28, 2016Date of Patent: June 27, 2017Assignee: 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: 9676745Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined here, 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: July 17, 2014Date of Patent: June 13, 2017Assignee: Heptares Therapeutics LimitedInventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Aves, Benjamin Gerald Tehan
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Patent number: 9669013Abstract: This invention relates to compounds (Formula (1)) 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 R1-R5, X1, X2 and p are as defined herein.Type: GrantFiled: January 15, 2016Date of Patent: June 6, 2017Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan