Patents Assigned to Institute of Cancer Research: Royal Cancer Hospital (The)
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Publication number: 20200095314Abstract: The present invention provides a method of treatment of prostate cancer, comprising administering a therapeutically effective amount of an inhibitor of IL-23 and/or an inhibitor of IL-23R to a mammalian patient in need thereof. The prostate cancer may be castration resistant prostate cancer (CRPC). The inhibitor may, for example, be an anti-IL-23 antibody, such as risankizumab, guselkumab or tildrakizumab. The method of treatment may further comprise administration of androgen deprivation therapy, such as enzalutamide. Also provided is a method of predicting the development of resistance to androgen deprivation therapy (ADT) in a prostate cancer in a mammalian patient and a related screening method.Type: ApplicationFiled: September 18, 2019Publication date: March 26, 2020Applicants: Fondazione per l'Istituto Oncologico di Ricerca (IOR), The Institute of Cancer Research: Royal Cancer HospitalInventors: Andrea Alimonti, Arianna Calcinotto, Johann de Bono
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Publication number: 20190152966Abstract: Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.Type: ApplicationFiled: February 17, 2017Publication date: May 23, 2019Applicant: THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITALInventors: Caroline SPRINGER, Richard MARAIS, Dan NICULES-CU-DUVAZ, Leo LEUNG, Deborah SMITHEN, Cedric CALLENS, Haoran TANG
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Patent number: 10167282Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as “TBAP compounds”) that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.Type: GrantFiled: June 29, 2017Date of Patent: January 1, 2019Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Caroline Joy Springer, Richard Marais, Romina Girotti, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Alfonso Zambon
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Patent number: 9820976Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.Type: GrantFiled: September 1, 2016Date of Patent: November 21, 2017Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Caroline Joy Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
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Patent number: 9725447Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as “TBAP compounds”) that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g. BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF. CRAF, etc.Type: GrantFiled: November 25, 2014Date of Patent: August 8, 2017Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Caroline Joy Springer, Richard Marais, Romina Girotti, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Alfonso Zambon
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Patent number: 9708317Abstract: The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.Type: GrantFiled: November 25, 2014Date of Patent: July 18, 2017Assignees: Cancer Research Technology Limited, Oxy Scientific Limited, The Institute of Cancer Research: Royal Cancer HospitalInventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
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Patent number: 9611223Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.Type: GrantFiled: September 11, 2014Date of Patent: April 4, 2017Assignee: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliott, Dan Niculescu-Duvaz, Roderick Alan Porter, Rehan Aqil, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Anna Hopkins, Ashley Nicholas Jarvis, Trevor Robert Perrior, Philip Alan Skone, Rebekah Elisabeth Key
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Patent number: 9550764Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof for use in the treatment of cancer:Type: GrantFiled: August 22, 2013Date of Patent: January 24, 2017Assignee: The Institute of Cancer Research: Royal Cancer HospitalInventors: Keith Jones, Matthew David Cheeseman, Spyridon Linardopoulos, Amir Faisal, Olivier Remi Barbeau, Andrew Kalusa
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Patent number: 9540372Abstract: The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g.,B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.Type: GrantFiled: September 14, 2015Date of Patent: January 10, 2017Assignees: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE), CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
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Publication number: 20160355510Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as “TBAP compounds”) that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g. BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF. CRAF, etc.Type: ApplicationFiled: November 25, 2014Publication date: December 8, 2016Applicants: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE), INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Caroline Joy SPRINGER, Richard MARAIS, Romina GIROTTI, Dan NICULESCU-DUVAZ, Ion NICULESCU-DUVAZ, Alfonso ZAMBON
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Patent number: 9512486Abstract: Aspects of the invention relate to methods of treatment, and to kits and systems for the same including materials for determining that an individual is susceptible to cancer and if warranted treating the patient of cancer or initiating a monitoring strategy and/or taking a preventive action. Therapeutic and preventive interventions include, treating the patient with a PARR inhibitors and/or laprascopic oophorectomy. The invention also relates to systems and methods of genotyping an individual, and to methods of identifying a patent with a higher than normal likelihood of developing cancer and/or genetically related individuals or groups at heighten risk for developing cancer, particularly ovarian cancer.Type: GrantFiled: August 6, 2013Date of Patent: December 6, 2016Assignee: The Institute of Cancer Research: Royal Cancer HospitalInventor: Sabera Nazneen Rahman
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Patent number: 9439893Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.Type: GrantFiled: July 30, 2015Date of Patent: September 13, 2016Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Caroline Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
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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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Publication number: 20160221953Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.Type: ApplicationFiled: September 11, 2014Publication date: August 4, 2016Applicant: Institute of Cancer Research Royal Cancer Hospital (THE)Inventors: Alan ASHWORTH, Christopher James LORD, Richard James Rowland ELLIOT, Dan NICULESCU-DUVAZ, Roderick Alan PORTER, Rehan AQIL, Raymond John BOFFEY, Melanie Jayne BAYFORD, Stuart FIRTH-CLARK, Anna HOPKINS, Ashley Nicholas JARVIS, Trevor Robert PERRIOR, Philip Alan SKONE, Rebekah Elisabeth KEY
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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: 9193689Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.Type: GrantFiled: March 7, 2013Date of Patent: November 24, 2015Assignee: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
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Patent number: 9155737Abstract: The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.Type: GrantFiled: November 17, 2014Date of Patent: October 13, 2015Assignees: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE), CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
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Patent number: 9120789Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.Type: GrantFiled: July 15, 2014Date of Patent: September 1, 2015Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)Inventors: Caroline Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
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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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Patent number: D801526Type: GrantFiled: March 30, 2016Date of Patent: October 31, 2017Assignees: Sussex Development Services LLP, The Institute of Cancer Research: Royal Cancer Hospital LimitedInventor: Lee Bulbrook