Patents by Inventor Edward Giles
Edward Giles 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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Patent number: 11136338Abstract: The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably. Alzheimer's disease.Type: GrantFiled: April 22, 2020Date of Patent: October 5, 2021Assignee: LIFEARCInventors: Jon James Winter-Holt, Edward Giles Mciver, Martin Ambler, Stephen Lewis, Joanne Osborne, Kayleigh Webb-Smith
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Patent number: 10918645Abstract: Provided are a substituted tricyclic heterocyclic compound of formula I or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt, ester or a prodrug thereof, a pharmaceutical composition including the same and uses thereof. The substituted tricyclic heterocyclic compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be used for treating a disorder caused by at least one of cancer and neurodegenerative diseases. Further the compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be also used for preventing or treating a disorder caused by, associated with or accompanied by any abnormal kinase activity.Type: GrantFiled: June 13, 2017Date of Patent: February 16, 2021Assignees: LIFEARC, SUZHOU YABAO PHARMACEUTICAL R&D CO., LTD.Inventors: Yan Xia, Edward Giles McIver, Yang Song, Yuanyuan Xu, Lin Zhu, Chunjun Chu, Ling Wu, Miao Liu, Justin Stephen Bryans
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Publication number: 20200317639Abstract: The invention provides new polymorphs of N-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 31, 2017Publication date: October 8, 2020Inventors: David Malcolm CROWE, Melvyn Edward GILES
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Publication number: 20200247822Abstract: The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably. Alzheimer's disease.Type: ApplicationFiled: April 22, 2020Publication date: August 6, 2020Inventors: Jon James Winter-Holt, Edward Giles Mciver, Martin Ambler, Stephen Lewis, Joanne Osborne, Kayleigh Webb-Smith
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Patent number: 10669284Abstract: The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.Type: GrantFiled: November 16, 2016Date of Patent: June 2, 2020Assignee: LIFEARCInventors: Jon James Winter-Holt, Edward Giles Mciver, Martin Ambler, Stephen Lewis, Joanne Osborne, Kayleigh Webb-Smith
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Patent number: 10604524Abstract: The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO—NR8R9, wherein R8 and R9 are each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more R12 groups, and said heterocycloalkyl is optionally substituted by R10 or R12; or R8 and R9 are linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from R10 and (CH2)mR12; R2 is selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more R12 groups; R3 is selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z1, Z2, Z3 and Z4 are all C; R4, R5, R6 and R7 are each independently selected from H, alkyl, CN, NO2, OH, alkoxy, NType: GrantFiled: November 16, 2016Date of Patent: March 31, 2020Assignee: LIFE ARCInventors: Jon James Winter-Holt, Edward Giles Mciver, Stephen Lewis, Joanne Osborne
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Publication number: 20190307763Abstract: Provided are a substituted tricyclic herteocyclic compound of formula I or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt, ester or a prodrug thereof, a pharmaceutical composition including the same and uses thereof. The substituted tricyclic herteocyclic compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be used for treating a disorder caused by at least one of cancer and neurodegenerative diseases. Further the compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be also used for preventing or treating a disorder caused by, associated with or accompanied by any abnormal kinase activity.Type: ApplicationFiled: June 13, 2017Publication date: October 10, 2019Applicants: LifeArc, Suzhou Yabao Pharmaceutical R&D Co., Ltd.Inventors: Yan XIA, Edward Giles MCIVER, Yang SONG, Yuanyuan XU, Lin ZHU, Chunjun CHU, Ling WU, Miao LIU, Justin Stephen BRYANS
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Publication number: 20180346483Abstract: The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.Type: ApplicationFiled: November 16, 2016Publication date: December 6, 2018Inventors: Jon James Winter-Holt, Edward Giles Mciver, Martin Ambler, Stephen Lewis, Joanne Osborne, Kayleigh Webb-Smith
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Publication number: 20180346469Abstract: The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO—NR8R9, wherein R8 and R9 are each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more R12 groups, and said heterocycloalkyl is optionally substituted by R10 or R12; or R8 and R9 are linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from R10 and (CH2)mR12; R2 is selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more R12 groups; R3 is selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z1, Z2, Z3 and Z4 are all C; R4, R5, R6 and R7 are each independently selected from H, alkyl, CN, NO2,OH, alkoxy, NHType: ApplicationFiled: November 16, 2016Publication date: December 6, 2018Inventors: Jon James Winter-Holt, Edward Giles Mciver, Stephen Lewis, Joanne Osborne
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Publication number: 20170320870Abstract: A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-hType: ApplicationFiled: April 3, 2017Publication date: November 9, 2017Inventors: Edward Giles MCIVER, Ela SMILJANIC, Denise Jamilla HARDING, Joanne HOUGH
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Patent number: 8569281Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.Type: GrantFiled: September 21, 2011Date of Patent: October 29, 2013Assignees: Medical Research Council Technology, Genentech, Inc.Inventors: Bryan K. Chan, Huifen Chen, Anthony Estrada, Daniel Shore, Zachary Sweeney, Edward Giles McIver
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Publication number: 20130267513Abstract: A compound of formula Ia or formula Ib, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; -0-C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; Q is CN, halogen, or is selected from C1-6-alkyl, C3-7-cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with one or more substituents A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl and halogen, wherein said C1-6-alkyl, Cz-B-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independType: ApplicationFiled: May 16, 2011Publication date: October 10, 2013Inventors: Brayn Chan, Anthony Estrada, Zachary Sweeney, Edward Giles Mciver, Stephen Lewis
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Publication number: 20120295883Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.Type: ApplicationFiled: September 21, 2011Publication date: November 22, 2012Applicants: GENENTECH, INC., MEDICAL RESEARCH COUNCIL TECHNOLOGYInventors: Bryan K. CHAN, Huifen CHEN, Anthony ESTRADA, Daniel SHORE, Zachary SWEENEY, Edward Giles MCIVER
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Patent number: 8203004Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.Type: GrantFiled: November 3, 2006Date of Patent: June 19, 2012Assignee: Merck, Sharp & Dohme LimitedInventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Mciver, Paul Joseph Oakley, Martin Richard Teall
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Publication number: 20120088753Abstract: The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is —NR7(CO)R11; R2 is aryl, heteroaryl, fused aryl-C3-6-heterocycloalkyl or fused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted; each R7 is selected from hydrogen, C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6alkyl-C3-7-cycloalkyl, C?-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease.Type: ApplicationFiled: March 4, 2010Publication date: April 12, 2012Applicant: MEDICAL RESEARCH COUNCIL TECHNOLOGYInventors: Edward Giles Mciver, Joanne HOUGH, Joanne Hough
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Publication number: 20100317646Abstract: A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-hType: ApplicationFiled: March 19, 2010Publication date: December 16, 2010Applicant: Medical Research Council TechnologyInventors: Edward Giles Mciver, Ela Smiljanic, Denise Jamilla Harding, Joanne Hough
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Patent number: 7700640Abstract: A process for making a compound of formula (I), said process comprising a) reacting a compound of formula (II) with: i) a compound of formula (III) by nucleophilic aromatic substitution of X2 and ii) a compound of formula (IV) for example by nucleophilic aromatic substitution b) where necessary, converting X1 to a carboxylic acid; and c) coupling of the carboxylic acid group to an appropriate heterocyclic amine; wherein all variables are as defined in the description.Type: GrantFiled: October 11, 2005Date of Patent: April 20, 2010Assignee: AstraZeneca ABInventors: Philip Cornwall, David Simon Ennis, Melvyn Edward Giles, Jacob Robert James Perkins, Shelly Louise Jenkin, Jeremy Stephen Parker, Bharti Patel
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Publication number: 20100056524Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, —NR4R5, —OR6, —NR7(CO)R6, —NR7(CO)NR4R5, —NR7SO2R6, —NR7COOR7, —CONR4R5, C3-6-heterocycloalkyl and wherein R4Type: ApplicationFiled: April 2, 2009Publication date: March 4, 2010Inventors: Edward Giles Mciver, Justin Stephen Bryans, Ela Smiljanic, Stephen John Lewis, Joanne Hough, Thomas Drake
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Publication number: 20100016308Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.Type: ApplicationFiled: November 3, 2006Publication date: January 21, 2010Inventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Meiver, Paul Joseph Oakley, Martin Richard Teall
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Patent number: 7442701Abstract: The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C—Ar2, with the proviso that when Y is N or CH then Z is C—Ar2, and with the further proviso that when Y is C—Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONType: GrantFiled: November 14, 2003Date of Patent: October 28, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, Gregory John Hollingworth, A. Brian Jones, Edward Giles McIver, Christopher Richard Moyes, Lauren Rogers