Patents by Inventor Graham Wyatt
Graham Wyatt 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: 20160250187Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: January 29, 2016Publication date: September 1, 2016Applicants: Astex Therapeutics Ltd, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio BERDINI, Gordon SAXTY, Marinus Leendert VERDONK, Steven John WOODHEAD, Paul Graham WYATT, Robert George BOYLE, Hannah Fiona SORE, David Winter WALKER, Ian COLLINS, Robert DOWNHAM, Robin Arthur Ellis CARR
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Patent number: 9283226Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: GrantFiled: February 14, 2014Date of Patent: March 15, 2016Assignees: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Patent number: 9051278Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: GrantFiled: May 19, 2014Date of Patent: June 9, 2015Assignee: ASTEX THERAPEUTICS, LTD.Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
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Patent number: 9006430Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of theType: GrantFiled: June 20, 2014Date of Patent: April 14, 2015Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, David Winter Walker, Steven John Woodhead, Paul Graham Wyatt, Alastair Donald, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca
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Publication number: 20140371213Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: May 19, 2014Publication date: December 18, 2014Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20140303177Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of theType: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Valerio BERDINI, Robert George BOYLE, Gordon SAXTY, David Winter WALKER, Steven John WOODHEAD, Paul Graham WYATT, Alastair DONALD, John CALDWELL, Ian COLLINS, Tatiana Faria DA FONSECA
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Publication number: 20140271662Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: February 14, 2014Publication date: September 18, 2014Applicants: Astex Therapeutics Ltd, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer HospitalInventors: Valerio BERDINI, Gordon SAXTY, Marinus Leendert VERDONK, Steven John WOODHEAD, Paul Graham WYATT, Robert George BOYLE, Hannah Fiona SORE, David Winter WALKER, Ian COLLINS, Robert DOWNHAM, Robin Arthur Ellis CARR
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Patent number: 8809336Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of theType: GrantFiled: September 4, 2013Date of Patent: August 19, 2014Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, David Winter Walker, Steven John Woodhead, Paul Graham Wyatt, Alastair Donald, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca
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Patent number: 8779147Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.Type: GrantFiled: November 4, 2011Date of Patent: July 15, 2014Assignee: Astex Therapeutics, Ltd.Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
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Patent number: 8778936Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: GrantFiled: December 19, 2011Date of Patent: July 15, 2014Assignee: Astex Therapeutics LimitedInventors: Valerio Berdini, Maria Grazia Carr, Adrian Liam Gill, Steven Howard, Eva Figueroa Navarro, Gary Trewartha, David Charles Rees, Mladen Vinkovic, Paul Graham Wyatt
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Publication number: 20140107137Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of theType: ApplicationFiled: September 4, 2013Publication date: April 17, 2014Inventors: Valerio BERDINI, Robert George BOYLE, Gordon SAXTY, David Winter WALKER, Steven John WOODHEAD, Paul Graham WYATT, Alistair DONALD, John CALDWELL, Ian COLLINS, Tatiana Faria DA FONSECA
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Patent number: 8691806Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.Type: GrantFiled: June 28, 2012Date of Patent: April 8, 2014Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Publication number: 20140010892Abstract: The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Aurora kinases and are therefore useful to treat cancer and viral diseases.Type: ApplicationFiled: May 24, 2013Publication date: January 9, 2014Applicant: Astex Therapeutics LimitedInventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Eva Figueroa NAVARRO, Adrian Liam GILL, Steven HOWARD, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Patent number: 8546407Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (Ic) or salts, tautomers or N-oxides thereof.Type: GrantFiled: October 25, 2005Date of Patent: October 1, 2013Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, David Winter Walker, Steven John Woodhead, Paul Graham Wyatt, Alastair Donald, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca
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Patent number: 8541579Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 14, 2012Date of Patent: September 24, 2013Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Richard Jonathan Hatley, Deirdre Mary Bernadette Hickey, John Liddle, David George Hubert Livermore, Andrew McMurtrie Mason, Neil Derek Miller, Fabrizio Nerozzi, Steven Leslie Sollis, Anna Katrin Szardenings, Paul Graham Wyatt
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Patent number: 8404718Abstract: The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4—; A is a bond, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from fluorine, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g.Type: GrantFiled: April 1, 2010Date of Patent: March 26, 2013Assignee: Astex Therapeutics LimitedInventors: Jayne Elizabeth Curry, John Francis Lyons, Matthew Simon Squires, Neil Thomas Thompson, Kyla Merriom Thompson, Paul Graham Wyatt
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Patent number: 8367673Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 27, 2009Date of Patent: February 5, 2013Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Richard Jonathan Hatley, Deirdre Mary Bernadette Hickey, John Liddle, David George Hubert Livermore, Andrew McMurtrie Mason, Neil Derek Miller, Fabrizio Nerozzi, Steven Leslie Sollis, Anna Katrin Szardenings, Paul Graham Wyatt
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Publication number: 20130005702Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.Type: ApplicationFiled: June 28, 2012Publication date: January 3, 2013Applicants: Astex Therapeutics Limited, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer HospitalInventors: Valerio BERDINI, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Patent number: 8293767Abstract: The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.Type: GrantFiled: July 22, 2011Date of Patent: October 23, 2012Assignee: Astex Therapeutics LimitedInventors: Paul Graham Wyatt, David Charles Rees, Mladen Vinkovic, Gary Trewartha
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Publication number: 20120213791Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.Type: ApplicationFiled: November 4, 2011Publication date: August 23, 2012Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT