Patents by Inventor Alfonso Zambon

Alfonso Zambon 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).

  • Patent number: 12060360
    Abstract: This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.
    Type: Grant
    Filed: April 4, 2022
    Date of Patent: August 13, 2024
    Assignee: The Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Richard Marais, Caroline Springer, Dan Niculescu-Duvaz, Natalie Miller, Mohammed Aljarah, Alfonso Zambon, Leo Leung, Deborah Smithen, Michael Brown, Haoran Tang
  • Publication number: 20220289757
    Abstract: This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.
    Type: Application
    Filed: April 4, 2022
    Publication date: September 15, 2022
    Inventors: Richard Marais, Caroline Springer, Dan Niculescu-Duvaz, Natalie Miller, Mohammed Aljarah, Alfonso Zambon, Leo Leung, Deborah Smithen, Michael Brown, Haoran Tang
  • Patent number: 11325915
    Abstract: This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: May 10, 2022
    Assignee: The Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Richard Marais, Caroline Springer, Dan Niculescu-Duvaz, Natalie Miller, Mohammed Aljarah, Alfonso Zambon, Leo Leung, Deborah Smithen, Michael Brown, Haoran Tang
  • Publication number: 20200331922
    Abstract: This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.
    Type: Application
    Filed: October 12, 2018
    Publication date: October 22, 2020
    Inventors: Richard Marais, Caroline Springer, Dan Niculescu-Duvaz, Natalie Miller, Mohammed Aljarah, Alfonso Zambon, Leo Leung, Deborah Smithen, Michael Brown, Haoran Tang
  • Patent number: 10167282
    Abstract: 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: Grant
    Filed: June 29, 2017
    Date of Patent: January 1, 2019
    Assignees: 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
  • Patent number: 10100053
    Abstract: 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: Grant
    Filed: June 28, 2017
    Date of Patent: October 16, 2018
    Assignees: Cancer Research Technology Limited, Institute of Cancer Research: Royal Cancer Hosp. (The)
    Inventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
  • Patent number: 9820976
    Abstract: 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: Grant
    Filed: September 1, 2016
    Date of Patent: November 21, 2017
    Assignees: 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
  • Publication number: 20170298066
    Abstract: 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: Application
    Filed: June 29, 2017
    Publication date: October 19, 2017
    Inventors: Caroline Joy SPRINGER, Richard MARAIS, Romina GIROTTI, Dan NICULESCU-DUVAZ, Ion NICULESCU-DUVAZ, Alfonso ZAMBON
  • Publication number: 20170298065
    Abstract: 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]phenyflurea.
    Type: Application
    Filed: June 28, 2017
    Publication date: October 19, 2017
    Inventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
  • Patent number: 9725447
    Abstract: 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: Grant
    Filed: November 25, 2014
    Date of Patent: August 8, 2017
    Assignees: 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
  • Patent number: 9708317
    Abstract: 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: Grant
    Filed: November 25, 2014
    Date of Patent: July 18, 2017
    Assignees: Cancer Research Technology Limited, Oxy Scientific Limited, The Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
  • Publication number: 20170079963
    Abstract: 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: Application
    Filed: September 1, 2016
    Publication date: March 23, 2017
    Inventors: Caroline Joy SPRINGER, Ion NICULESCU-DUVAZ, Richard MARAIS, Dan NICULESCU-DUVAZ, Alfonso ZAMBON, Delphine MENARD
  • Patent number: 9540372
    Abstract: 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: Grant
    Filed: September 14, 2015
    Date of Patent: January 10, 2017
    Assignees: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE), CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
  • Publication number: 20160355510
    Abstract: 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: Application
    Filed: November 25, 2014
    Publication date: December 8, 2016
    Applicants: 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
  • Publication number: 20160297814
    Abstract: 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: Application
    Filed: November 25, 2014
    Publication date: October 13, 2016
    Inventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
  • Patent number: 9439893
    Abstract: 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: Grant
    Filed: July 30, 2015
    Date of Patent: September 13, 2016
    Assignees: 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
  • Publication number: 20160030405
    Abstract: 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: Application
    Filed: July 30, 2015
    Publication date: February 4, 2016
    Inventors: Caroline SPRINGER, Ion NICULESCU-DUVAZ, Richard MARAIS, Dan NICULESCU-DUVAZ, Alfonso ZAMBON, Delphine MENARD
  • Publication number: 20160002230
    Abstract: 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: Application
    Filed: September 14, 2015
    Publication date: January 7, 2016
    Inventors: Caroline Joy SPRINGER, Dan NICULESCU-DUVAZ, Ion NICULESCU-DUVAZ, Richard MARAIS, Bartholomeus Marinus Josephus Marie SUIJKERBUIJK, Alfonso ZAMBON, Arnaud NOURRY, Delphine MENARD
  • Patent number: 9155737
    Abstract: 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: Grant
    Filed: November 17, 2014
    Date of Patent: October 13, 2015
    Assignees: INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE), CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
  • Patent number: 9120789
    Abstract: 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: Grant
    Filed: July 15, 2014
    Date of Patent: September 1, 2015
    Assignees: 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