Patents by Inventor Fiona Hamilton Marshall
Fiona Hamilton Marshall 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).
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Publication number: 20220218676Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 15, 2022Publication date: July 14, 2022Applicant: Merck Sharp & Dohme Corp.Inventors: Ashok Arasappan, Anthony S. Basile, Tjerk Johannes Helena Bueters, Michael F. Egan, Nancy Dohee Kim, Fiona Hamilton Marshall, Yuki Mukai, Arie Struyk, Jason Martin Uslaner
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Publication number: 20210015800Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGuR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGuR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 25, 2020Publication date: January 21, 2021Inventors: Ashok Arasappan, Anthony S. Basile, Tjerk Johannes Helena Bueters, Michael F. Eagan, Nancy Dohee Kim, Fiona Hamilton Marshall, Yuki Mukai, Arie Struyk, Jason Martin Uslaner
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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: 10458993Abstract: The invention provides an assay for assessing the conformational stability of a membrane protein, comprising: (a) providing a sample comprising a first population and a second population of a membrane protein; wherein the membrane protein in the first population is labelled with a donor label and the membrane protein in the second population is labelled with an acceptor label, or the membrane protein in the first population is labelled with an acceptor label and the membrane protein in the second population is labelled with a donor label, (b) exposing the first and second populations of the membrane protein to a stability modulating agent and/or condition, (c) and assessing aggregation between membrane proteins of the first and second populations by activating the donor label to permit a distance-dependent interaction with the acceptor label, which interaction produces a detectable signal.Type: GrantFiled: May 31, 2013Date of Patent: October 29, 2019Assignee: Heptares Therapeutics LimitedInventors: Fiona Hamilton Marshall, Seyed Ali Jazayeri-Dezfuly, Jayesh Chhotubhai Patel
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Publication number: 20190112355Abstract: 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: ApplicationFiled: September 20, 2018Publication date: April 18, 2019Applicant: Heptares Therapeutics LimitedInventors: Seyed Ali Jazayeri-Dezfuly, Fiona Hamilton Marshall
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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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Publication number: 20170145075Abstract: A method for producing a mutant G-protein coupled receptor (GPCR) with increased stability relative to a parent GPCR, the method comprising making one or more mutations in the amino acid sequence that defines a Class 1 parent GPCR, wherein (i) the one or more mutations are located within a window of i plus or minus 5 residues, where i is the position of amino acid residue 3.55 in the parent GPCR, and/or (ii) the one or more mutations are located within a window of i minus 2 to i residues, where i is the position of amino acid residue 5.63 in the parent GPCR, and/or (iii) the one or more mutations are located within a window of i minus 4 to i plus 1 residues, where i is the position of amino acid residue 7.42 in the parent GPCR, to provide one or more mutants of the parent GPCR with increased stability.Type: ApplicationFiled: June 29, 2016Publication date: May 25, 2017Applicant: Heptares Therapeutics LimitedInventors: Nathan Jacob Robertson, Fiona Hamilton Marshall
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Publication number: 20160327576Abstract: 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: January 6, 2016Publication date: November 10, 2016Inventors: Malcolm Peter Weir, Fiona Hamilton Marshall
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Patent number: 9260505Abstract: 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: April 17, 2014Date of Patent: February 16, 2016Assignee: Heptares Therapeutics LimitedInventors: Malcolm Peter Weir, Fiona Hamilton Marshall
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Publication number: 20150261911Abstract: The invention provides a method of predicting a three dimensional structural representation of a target protein of unknown structure, or part thereof, comprising: providing the coordinates of the human corticotropin-releasing factor receptor-1 (CRF1R) structure listed in Table A, Table B or Table C, optionally varied by a root mean square deviation of residue backbone atoms of not more than 4.383 ?, or selected coordinates thereof; and predicting the three-dimensional structural representation of the target protein, or part thereof, by modelling the structural representation on all or the selected coordinates of the CRF1R structure. The invention also provides the use of the CRF1R coordinates to select or design one or more binding partners of CRF1R.Type: ApplicationFiled: March 13, 2014Publication date: September 17, 2015Applicant: Heptares Therapeutics LimitedInventors: Andrea Bortolato, Kin Yip Cheng, Andrew Stephen Dore, Kaspar Hollenstein, Seyed Ali Jazayeri-Dezfuly, James Kean, Fiona Hamilton Marshall
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Publication number: 20150147822Abstract: The invention provides an assay for assessing the conformational stability of a membrane protein, comprising: (a) providing a sample comprising a first population and a second population of a membrane protein; wherein the membrane protein in the first population is labelled with a donor label and the membrane protein in the second population is labelled with an acceptor label, or the membrane protein in the first population is labelled with an acceptor label and the membrane protein in the second population is labelled with a donor label, (b) exposing the first and second populations of the membrane protein to a stability modulating agent and/or condition, (c) and assessing aggregation between membrane proteins of the first and second populations by activating the donor label to permit a distance-dependent interaction with the acceptor label, which interaction produces a detectable signal.Type: ApplicationFiled: May 31, 2013Publication date: May 28, 2015Applicant: Heptares Therapeutics LimitedInventors: Fiona Hamilton Marshall, Seyed Ali Jazayeri-Dezfuly, Jayesh Chhotubhai Patel
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Patent number: 8900591Abstract: There is provided a G protein coupled receptor (GPCR) or a polynucleotide encoding said GPCR for use as a vaccine. There is also provided methods of antagonizing or agonizing A GPCR in vivo comprising the administration of a GPCR or a polynucleotide encoding a GPCR to a subject. The invention further provides a GPCR for use in inhibiting an activity of a GPCR binding partner in a subject.Type: GrantFiled: August 5, 2011Date of Patent: December 2, 2014Assignee: Heptares Therapeutics LimitedInventors: Catherine Jane Hutchings, Malcolm Peter Weir, Fiona Hamilton Marshall
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Publication number: 20140315299Abstract: 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: ApplicationFiled: August 9, 2012Publication date: October 23, 2014Applicant: Heptares Therapeutics LimitedInventors: Seyed Ali Jazayeri-Dezfuly, Fiona Hamilton Marshall
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Publication number: 20140316116Abstract: 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: April 17, 2014Publication date: October 23, 2014Applicant: Heptares Therapeutics LimitedInventors: Malcolm Peter Weir, Fiona Hamilton Marshall
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Patent number: 8790933Abstract: 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 conformation. Methods of producing GPCRs with increased stability relative to a parent GPCR are also disclosed.Type: GrantFiled: December 19, 2008Date of Patent: July 29, 2014Assignee: Heptares Therapeutics LimitedInventors: Malcolm Peter Weir, Fiona Hamilton Marshall
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Patent number: 8703915Abstract: A method for producing a mutant G-protein coupled receptor (GPCR) with increased stability relative to a parent GPCR, the method comprising making one or more mutations in the amino acid sequence that defines a parent GPCR, wherein (i) the one or more mutations are located within a window of/plus or minus 5 residues, where/is the position of amino acid residue 2.46 in the parent GPCR when the parent GPCR is a Class 1 GPCR, or where/is the position of an equivalent amino acid residue in the parent GPCR when the parent GPCR is a Class 2 or 3 GPCR, and/or (ii) the one or more mutations are located within an amino acid sequence of transmembrane helix 7 in the parent GPCR which amino acid sequence interacts with the window of/plus or minus 5 residues, to provide one or more mutants of the parent GPCR with increased stability.Type: GrantFiled: June 22, 2010Date of Patent: April 22, 2014Assignee: Heptares Therapeutics LimitedInventors: Seyed Ali Jazayeri-Dezfuly, Guillaume Pierre Lebon, Fiona Hamilton Marshall, Christopher Gordon Tate, Nathan Robertson
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Publication number: 20140031525Abstract: A method for producing a mutant G-protein coupled receptor (GPCR) with increased stability relative to a parent GPCR, the method comprising making one or more mutations in the amino acid sequence that defines a Class 1 parent GPCR, wherein (i) the one or more mutations are located within a window of i plus or minus 5 residues, where i is the position of amino acid residue 3.55 in the parent GPCR, and/or (ii) the one or more mutations are located within a window of i minus 2 to i residues, where i is the position of amino acid residue 5.63 in the parent GPCR, and/or (iii) the one or more mutations are located within a window of i minus 4 to i plus 1 residues, where i is the position of amino acid residue 7.42 in the parent GPCR, to provide one or more mutants of the parent GPCR with increased stability.Type: ApplicationFiled: January 20, 2012Publication date: January 30, 2014Applicant: Heptares Therapeutics LimitedInventors: Nathan Jacob Robertson, Fiona Hamilton Marshall
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Publication number: 20130224238Abstract: There is provided a G protein coupled receptor (GPCR) or a polynucleotide encoding said GPCR for use as a vaccine. There is also provided methods of antagonising or agonising A GPCR in vivo comprising the administration of a GPCR or a polynucleotide encoding a GPCR to a subject. The invention further provides a GPCR for use in inhibiting an activity of a GPCR binding partner in a subject.Type: ApplicationFiled: August 5, 2011Publication date: August 29, 2013Applicant: HEPTARES THERAPEUTICS LIMITEDInventors: Catherine Jane Hutchings, Malcolm Peter Weir, Fiona Hamilton Marshall
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Publication number: 20120165507Abstract: A method for producing a mutant G-protein coupled receptor (GPCR) with increased stability relative to a parent GPCR, the method comprising making one or more mutations in the amino acid sequence that defines a parent GPCR, wherein (i) the one or more mutations are located within a window of / plus or minus 5 residues, where / is the position of amino acid residue 2.46 in the parent GPCR when the parent GPCR is a Class 1 GPCR, or where / is the position of an equivalent amino acid residue in the parent GPCR when the parent GPCR is a Class 2 or 3 GPCR, and/or (ii) the one or more mutations are located within an amino acid sequence of transmembrane helix 7 in the parent GPCR which amino acid sequence interacts with the window of / plus or minus 5 residues, to provide one or more mutants of the parent GPCR with increased stability.Type: ApplicationFiled: June 22, 2010Publication date: June 28, 2012Applicant: Heptares Therapeutics LimitedInventors: Seyed Ali Jazayeri-Dezfuly, Guillaume Pierre Lebon, Fiona Hamilton Marshall, Christopher Godon Tate, Nathan Robertson
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Publication number: 20110027910Abstract: 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 conformation. Methods of producing GPCRs with increased stability relative to a parent GPCR are also disclosed.Type: ApplicationFiled: December 19, 2008Publication date: February 3, 2011Inventors: Malcolm Peter Weir, Fiona Hamilton Marshall