Patents by Inventor Dan Niculescu-Duvaz

Dan Niculescu-Duvaz 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: 11608330
    Abstract: 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: Grant
    Filed: April 2, 2021
    Date of Patent: March 21, 2023
    Assignee: THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
    Inventors: Caroline Springer, Richard Marais, Dan Niculescu-Duvaz, Leo Leung, Deborah Smithen, Cedric Callens, Haoran Tang
  • Publication number: 20220372028
    Abstract: 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: Application
    Filed: April 2, 2021
    Publication date: November 24, 2022
    Inventors: Caroline SPRINGER, Richard MARAIS, Dan NICULESCU-DUVAZ, Leo LEUNG, Deborah SMITHEN, Cedric CALLENS, 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: 20220017516
    Abstract: The disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, Formula (I) as defined herein. Compounds according to Formula I are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.
    Type: Application
    Filed: November 15, 2019
    Publication date: January 20, 2022
    Inventors: Mohammed ALJARAH, Dan NICULESCU-DUVAZ, Leo LEUNG, Deborah SMITHEN, Michael BROWN, Lawrence Christopher DAVIES, Caroline SPRINGER
  • Publication number: 20210238179
    Abstract: The disclosure relates to compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein X1 and X5 is each selected from CR1 or N; X2, X3 and X4 is each selected from CR1, CR2 or N, provided at least one of X2, X3 and X4 is CR2 and provided only one of X1, X2, X3, X4 and X5 can be N. R1, R2, R3, R4, R5, L1, L2 and L3 are as defined herein. Compounds according to Formula (I) are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.
    Type: Application
    Filed: June 5, 2019
    Publication date: August 5, 2021
    Inventors: Leo LEUNG, Kiri NORTH, Deborah SMITHEN, Mohammed ALJARAH, Michael BROWN, Ben AYERS, Dan NICULESCU-DUVAZ, Caroline SPRINGER
  • Patent number: 10995088
    Abstract: 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: Grant
    Filed: June 22, 2020
    Date of Patent: May 4, 2021
    Assignee: THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
    Inventors: Caroline Springer, Richard Marais, Dan Niculescu-Duvaz, Leo Leung, Deborah Smithen, Cedric Callens, Haoran Tang
  • Publication number: 20210040078
    Abstract: 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: Application
    Filed: June 22, 2020
    Publication date: February 11, 2021
    Inventors: Caroline SPRINGER, Richard MARAIS, Dan NICULESCU-DUVAZ, Leo LEUNG, Deborah SMITHEN, Cedric CALLENS, 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: 10807974
    Abstract: 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: Grant
    Filed: February 17, 2017
    Date of Patent: October 20, 2020
    Assignee: The Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Caroline Springer, Richard Marais, Dan Niculescu-Duvaz, Leo Leung, Deborah Smithen, Cedric Callens, 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: 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
  • 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
  • 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
  • Patent number: 9611223
    Abstract: 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: Grant
    Filed: September 11, 2014
    Date of Patent: April 4, 2017
    Assignee: 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
  • 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