Patents Assigned to Astex Therapeutics
  • Combination of an FGFR inhibitor and a CMET inhibitor
    Patent number: 11918576
    Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.
    Type: Grant
    Filed: July 17, 2020
    Date of Patent: March 5, 2024
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Eleonora Jovcheva, Timothy Pietro Suren Perera
  • Bicyclic heterocycle compounds and their uses in therapy
    Patent number: 11866428
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: September 28, 2020
    Date of Patent: January 9, 2024
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • PHARMACEUTICAL COMPOSITIONS COMPRISING N-(3,5-DIMETHOXYPHENYL)-N'-(1-METHYLETHYL)-N-[3-(1-METHYL-1H-PYRAZOL-4-YL)QUINOXALIN-6-YL]ETHANE-1,2-DIAMINE
    Publication number: 20240000778
    Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g.
    Type: Application
    Filed: May 15, 2023
    Publication date: January 4, 2024
    Applicant: ASTEX THERAPEUTICS LTD
    Inventor: Diego Fernando Domenico BROGGINI
  • ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION AND PROCESS FOR MAKING THEM
    Publication number: 20230278989
    Abstract: The invention relates to processes for preparing isoindolin-1-one derivatives, and in particular processes for preparing (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid. The invention also relates to crystalline forms of the compound (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid and its salts.
    Type: Application
    Filed: January 25, 2023
    Publication date: September 7, 2023
    Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Steven HOWARD, Benjamin David CONS, Jeffrey David ST. DENIS, Charlotte Mary GRIFFITHS-JONES, Steven Douglas HISCOCK, Rhian Sara HOLVEY, Alan Richard BURNS, David COUSIN, Hannah Louise DEXTER, Guillaume François PARRA, John Paul WATTS, Robert JEWELL, Jennifer Ann STOCKWELL, Kim Louise HIRST, Isabelle Anne LEMASSON, David John NASH, James Daniel OSBORNE, Jonas Calleja PRIEDE, Nicholas Paul RICHARDS, Aaron Michael DUMAS, Brian Christopher BISHOP, David PARRY-JONES, Jeremy Peter SCOTT, Meenakshi Sundaram SHANMUGHAM, Peter Richard MULLENS, David Charles LATHBURY, Darren James DIXON, Matthew James GAUNT
  • BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
    Publication number: 20230227450
    Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: December 21, 2022
    Publication date: July 20, 2023
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Gianni CHESSARI, Christopher Norbert JOHNSON, Steven HOWARD, James Edward Harvey DAY, Ildiko Maria BUCK, Charlotte Mary GRIFFITHS-JONES, Gordon SAXTY, Emiliano TAMANINI, Nicola Elizabeth WILSHER
  • Pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine
    Patent number: 11684620
    Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g. cancer.
    Type: Grant
    Filed: December 17, 2020
    Date of Patent: June 27, 2023
    Assignee: ASTEX THERAPEUTICS LTD
    Inventor: Diego Fernando Domenico Broggini
  • Bicyclic heterocycle compounds and their uses in therapy
    Patent number: 11643410
    Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: December 7, 2021
    Date of Patent: May 9, 2023
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Gianni Chessari, Christopher Norbert Johnson, Steven Howard, James Edward Harvey Day, Ildiko Maria Buck, Charlotte Mary Griffiths-Jones, Gordon Saxty, Emiliano Tamanini, Nicola Elizabeth Wilsher
  • Isoindolinone inhibitors of the MDM2-P53 interaction and process for making them
    Patent number: 11603367
    Abstract: The invention relates to processes for preparing isoindolin-1-one derivatives, and in particular processes for preparing (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid. The invention also relates to crystalline forms of the compound (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid and its salts.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: March 14, 2023
    Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Steven Howard, Jeffrey David St. Denis, Charlotte Mary Griffiths-Jones, Steven Douglas Hiscock, Alan Richard Burns, David Cousin, Kim Louise Hirst, James Daniel Osborne, Jonas Calleja Priede, Aaron Michael Dumas, Brian Christopher Bishop, David Parry-Jones, Jeremy Peter Scott, Meenakshi Sundaram Shanmugham, Peter Richard Mullens, Darren James Dixon, Matthew James Gaunt
  • FGFR/PD-1 COMBINATION THERAPY FOR THE TREATMENT OF CANCER
    Publication number: 20230030983
    Abstract: Provided herein are combination therapies for the treatment of cancer. In particular, the disclosed methods are directed to treatment of cancer in a patient comprising administering an antibody that blocks the interaction between PD-1 and PD-L1 and an FGFR inhibitor, wherein the antibody that blocks the interaction between PD-1 and PD-L1 and the FGFR inhibitor are administered if one or more FGFR variants are present in a biological sample from the patient.
    Type: Application
    Filed: March 18, 2022
    Publication date: February 2, 2023
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Jayaprakash KARKERA, Suso Jesus PLATERO, Raluca VERONA, Matthew V. LORENZI
  • BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
    Publication number: 20220204503
    Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: December 7, 2021
    Publication date: June 30, 2022
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Gianni CHESSARI, Christopher Norbert JOHNSON, Steven HOWARD, James Edward Harvey DAY, Ildiko Maria BUCK, Charlotte Mary GRIFFITHS-JONES, Gordon SAXTY, Emiliano TAMANINI, Nicola Elizabeth WILSHER
  • PYRAZOLYL QUINOXALINE KINASE INHIBITORS
    Publication number: 20220135544
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 20, 2021
    Publication date: May 5, 2022
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Gordon SAXTY, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Christopher Norbert Johnson, Steven John Woodhead, Michael Reader, David Charles Rees, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Timothy Pietro Suren Perera, Ronaldus Arnodus Hendrika Joseph Gilissen, Berthold Wroblowski, Jean Fernand Armand Lacrampe, Alexandra Papanikos, Olivier Alexis Georges Querolle, Elisabeth Thérèse Jeanne Pasquier, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
  • ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY
    Publication number: 20220106287
    Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
    Type: Application
    Filed: April 12, 2021
    Publication date: April 7, 2022
    Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Gianni CHESSARI, Steven HOWARD, Ildiko Maria BUCK, Benjamin David CONS, Christopher Norbert JOHNSON, Rhian Sara HOLVEY, David Charles REES, Jeffrey David ST. DENIS, Emiliano TAMANINI, Bernard Thomas GOLDING, Ian Robert HARDCASTLE, Celine Florence CANO, Duncan Charles MILLER, Martin Edward Mäntylä NOBLE, Roger John GRIFFIN, James Daniel OSBORNE, Joanne PEACH, Arwel LEWIS, Kim Louise HIRST, Benjamin Paul WHITTAKER, David Wyn WATSON, Dale Robert MITCHELL
  • Isoindolinone inhibitors of the MDM2-P53 interaction having anticancer activity
    Patent number: 11261171
    Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
    Type: Grant
    Filed: November 12, 2019
    Date of Patent: March 1, 2022
    Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Gianni Chessari, Steven Howard, Ildiko Maria Buck, Benjamin David Cons, Christopher Norbert Johnson, Rhian Sara Holvey, David Charles Rees, Jeffrey David St. Denis, Emiliano Tamanini, Bernard Thomas Golding, Ian Robert Hardcastle, Celine Florence Cano, Duncan Charles Miller, Martin Edward Mäntylä Noble, Roger John Griffin, James Daniel Osborne, Joanne Peach, Arwel Lewis, Kim Louise Hirst, Benjamin Paul Whittaker, David Wyn Watson, Dale Robert Mitchell
  • Combination of isoindolinone derivatives with SGI-110
    Patent number: 11236047
    Abstract: The invention provides a combination comprising: (i) a compound of formula (Io): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims; and (ii) a compound which is SGI-110 or a tautomer or a solvate or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions containing the combinations and medical uses of the combinations.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: February 1, 2022
    Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Gianni Chessari, John Francis Lyons
  • Bicyclic heterocycle compounds and their uses in therapy
    Patent number: 11225476
    Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: February 19, 2020
    Date of Patent: January 18, 2022
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Gianni Chessari, Christopher Norbert Johnson, Steven Howard, James Edward Harvey Day, Ildiko Maria Buck, Charlotte Mary Griffiths-Jones, Gordon Saxty, Emiliano Tamanini, Nicola Elizabeth Wilsher
  • ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY
    Publication number: 20210276984
    Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
    Type: Application
    Filed: February 1, 2021
    Publication date: September 9, 2021
    Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Gianni CHESSARI, Steven HOWARD, Ildiko Maria BUCK, Benjamin David CONS, Christopher Norbert JOHNSON, Rhian Sara HOLVEY, David Charles REES, Jeffrey David ST. DENIS, Emiliano TAMANINI, Bernard Thomas GOLDING, Ian Robert HARDCASTLE, Celine Florence CANO, Duncan Charles MILLER, Martin Edward Mäntylä NOBLE, Roger John GRIFFIN, James Daniel OSBORNE, Joanne PEACH, Arwel LEWIS, Kim Louise HIRST, Benjamin Paul WHITTAKER, David Wyn WATSON, Dale Robert MITCHELL
  • Ether linked triazoles as NRF2 activators
    Patent number: 11059816
    Abstract: The present invention relates to ether-linked triazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: July 13, 2021
    Assignees: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED, ASTEX THERAPEUTICS LIMITED
    Inventors: Anthony William James Cooper, Nicole Cathleen Goodwin, Charlotte Mary Griffiths-Jones, Thomas Daniel Heightman, Jeffrey K. Kerns, Hendrika Maria Gerarda Willems, Hongxing Yan
  • PHARMACEUTICAL COMPOSITIONS COMPRISING N-(3,5-DIMETHOXYPHENYL)-N'-(1-METHYLETHYL)-N-[3-(1-METHYL-1H-PYRAZOL-4-YL)QUINOXALIN-6-YL]ETHANE-1,2-DIAMINE
    Publication number: 20210169877
    Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g.
    Type: Application
    Filed: December 17, 2020
    Publication date: June 10, 2021
    Applicant: ASTEX THERAPEUTICS LTD
    Inventor: Diego Fernando Domenico BROGGINI
  • BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
    Publication number: 20210122749
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: September 28, 2020
    Publication date: April 29, 2021
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne WOOLFORD, Steven HOWARD, Ildiko Maria BUCK, Gianni CHESSARI, Christopher Norbert JOHNSON, Emiliano TAMANINI, James Edward Harvey DAY, Elisabetta CHIARPARIN, Thomas Daniel HEIGHTMAN, Martyn FREDERICKSON, Charlotte Mary GRIFFITHS-JONES
  • Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity
    Patent number: 10981898
    Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
    Type: Grant
    Filed: August 8, 2019
    Date of Patent: April 20, 2021
    Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Gianni Chessari, Steven Howard, Ildiko Maria Buck, Benjamin David Cons, Christopher Norbert Johnson, Rhian Sara Holvey, David Charles Rees, Jeffrey David St. Denis, Emiliano Tamanini, Bernard Thomas Golding, Ian Robert Hardcastle, Celine Florence Cano, Duncan Charles Miller, Martin Edward Mäntylä Noble, Roger John Griffin, James Daniel Osborne, Joanne Peach, Arwel Lewis, Kim Louise Hirst, Benjamin Paul Whittaker, David Wyn Watson, Dale Robert Mitchell