Patents by Inventor Stefano Crosignani

Stefano Crosignani 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).

  • Method for the Production of Thiocarbamate Derivatives A2AR Inhibitors
    Publication number: 20230407352
    Abstract: The present disclosure relates to synthesis of enantiomerically rich key drug intermediates as a means for manufacturing of thiocarbamate derivatives as A2A adenosine receptor (A2AR) inhibitors. More particularly, the present disclosure provides a viable efficient technology using enzymatic biotransformation process which utilizes cheaper substrate for production of high value key intermediates for A2AR inhibitors.
    Type: Application
    Filed: October 29, 2021
    Publication date: December 21, 2023
    Applicant: iTeos Belgium SA
    Inventors: Xuecheng Jiao, Michael Deligny, Stefano Crosignani, Xiangjun Jiang
  • 2-Oxo-Thiazole Derivatives as A2A Inhibitors and Compounds for Use in the Treatment of Cancers
    Publication number: 20230159564
    Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: September 21, 2022
    Publication date: May 25, 2023
    Inventors: Stefano Crosignani, Bruno Gomes, Erica Houthuys
  • THIOCARBAMATE DERIVATIVES AS A2A INHIBITORS, PHARMACEUTICAL COMPOSITION THEREOF AND COMBINATIONS WITH ANTICANCER AGENTS
    Publication number: 20230121530
    Abstract: The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-?-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers. The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.
    Type: Application
    Filed: June 1, 2022
    Publication date: April 20, 2023
    Inventors: Stefano Crosignani, Erica Joke Katelijne Heleen Houthuys, Reece Gerrad Marillier, Chiara Martinoli, Oliver De Henau, Gregory Driessens
  • NON BRAIN PENETRANT A2A INHIBITORS AND METHODS FOR USE IN THE TREATMENT OF CANCERS
    Publication number: 20230098694
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention further relates to the use of the compounds of Formula (I) as A2A inhibitors. The invention also relates to the use of the compounds of Formula (I) for the treatment and/or prevention of proliferative disorders, including cancers.
    Type: Application
    Filed: July 18, 2022
    Publication date: March 30, 2023
    Inventor: Stefano CROSIGNANI
  • Non brain penetrant A2A inhibitors and methods for use in the treatment of cancers
    Patent number: 11427594
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention further relates to the use of the compounds of Formula (I) as A2A inhibitors. The invention also relates to the use of the compounds of Formula (I) for the treatment and/or prevention of proliferative disorders, including cancers.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: August 30, 2022
    Assignee: ITEOS BELGIUM SA
    Inventor: Stefano Crosignani
  • Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
    Patent number: 11376255
    Abstract: The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-?-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers. The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.
    Type: Grant
    Filed: September 9, 2020
    Date of Patent: July 5, 2022
    Assignee: iTeos Belgium SA
    Inventors: Stefano Crosignani, Erica Joke Katelijne Heleen Houthuys, Reece Gerrad Marillier, Chiara Martinoli, Oliver De Henau, Gregory Driessens
  • USE OF AN INHIBITOR OF AN ENT FAMILY TRANSPORTER IN THE TREATMENT OF CANCER AND COMBINATION THEREOF WITH AN ADENOSINE RECEPTOR ANTAGONIST
    Publication number: 20210338672
    Abstract: The present invention relates to the use of an inhibitor of an ENT family transporter for the treatment of cancer. The invention further relates to the combined use of such inhibitor of an ENT family transporter with an adenosine receptor antagonist, for the treatment of cancer. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination.
    Type: Application
    Filed: September 27, 2019
    Publication date: November 4, 2021
    Inventors: Stefano CROSIGNANI, Erica Joke Katelijne Heleen HOUTHUYS, Oliver DE HENAU
  • 2-OXO-THIAZOLE DERIVATIVES AS A2A INHIBITORS AND COMPOUNDS FOR USE IN THE TREATMENT OF CANCERS
    Publication number: 20210198281
    Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: August 14, 2020
    Publication date: July 1, 2021
    Inventors: Stefano Crosignani, Bruno Gomes, Erica Houthuys
  • 2-oxo-thiazole derivatives as A2A inhibitors and compounds for use in the treatment of cancers
    Patent number: 10995101
    Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: May 4, 2021
    Assignee: iTeos Therapeutics SA
    Inventors: Stefano Crosignani, Bruno Gomes, Erica Houthuys
  • Combinations comprising a pyrrolidine-2,5-dione IDO1 inhibitor and an anti-body
    Patent number: 10945994
    Abstract: Combinations of an IDO1 inhibitor (e.g., a 3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione compound), with an anti-PD1 antibody or anti-PD-L1 antibody, and an anti-4-1BB antibody, as selected anti-cancer or anti-viral agents are provided. Also provided are use of these combinations for the treatment and/or prevention of cancer and endometriosis.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: March 16, 2021
    Assignees: Pfizer Inc., iTEOS THERAPEUTICS
    Inventors: Manfred Kraus, Sandra Cauwenberghs, Stefano Crosignani, Gregory Driessens
  • THIOCARBAMATE DERIVATIVES AS A2A INHIBITORS, PHARMACEUTICAL COMPOSITION THEREOF AND COMBINATIONS WITH ANTICANCER AGENTS
    Publication number: 20210069196
    Abstract: The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-?-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers. The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.
    Type: Application
    Filed: September 9, 2020
    Publication date: March 11, 2021
    Inventors: Stefano Crosignani, Paul Dickinson, Marcel de Matas, Erica Joke Katelijne Heleen Houthuys, Reece Gerrad Marillier, Chiara Martinoli, Olivier De Henau, Gregory Driessens
  • NON BRAIN PENETRANT A2A INHIBITORS AND METHODS FOR USE IN THE TREATMENT OF CANCERS
    Publication number: 20200102319
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention further relates to the use of the compounds of Formula (I) as A2A inhibitors. The invention also relates to the use of the compounds of Formula (I) for the treatment and/or prevention of proliferative disorders, including cancers.
    Type: Application
    Filed: September 26, 2019
    Publication date: April 2, 2020
    Inventor: Stefano CROSIGNANI
  • 3-indol substituted derivatives, pharmaceutical compositions and methods for use
    Patent number: 10544095
    Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: January 28, 2020
    Assignees: Pfizer Inc., iTeos Therapeutics
    Inventors: Sacha Ninkovic, Michael Raymond Collins, Stefano Crosignani, Andreas Maderna, Indrawan James McAlpine, Stephanie Anne Scales, Martin Wythes
  • 2-Oxo-Thiazole Derivatives as A2A Inhibitors and Compounds for Use in the Treatment of Cancers
    Publication number: 20190276473
    Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: March 14, 2019
    Publication date: September 12, 2019
    Inventors: Stefano Crosignani, Bruno Gomes, Erica Houthuys
  • Treatment method utilizing pyrrolidine-2, 5-dione derivatives as IDO1 inhibitors
    Patent number: 10398679
    Abstract: Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: September 3, 2019
    Assignee: ITEOS THERAPEUTICS
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Gregory Driessens, Frederik Deroose
  • NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
    Publication number: 20180222862
    Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: August 4, 2016
    Publication date: August 9, 2018
    Inventors: Sacha Ninkovic, Michael Raymond Collins, Stefano Crosignani, Andreas Maderna, Indrawan James McAlpine, Stephanie Anne Scales, Martin Wythes
  • TREATMENT METHOD UTILIZING PYRROLIDINE-2, 5-DIONE DERIVATIVES AS IDO1 INHIBITORS
    Publication number: 20180214415
    Abstract: Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.
    Type: Application
    Filed: March 23, 2018
    Publication date: August 2, 2018
    Inventors: Stefano CROSIGNANI, Sandra CAUWENBERGHS, Gregory DRIESSENS, Frederik DEROOSE
  • COMBINATIONS COMPRISING A PYRROLIDINE-2,5-DIONE IDO1 INHIBITOR AND AN ANTI-BODY
    Publication number: 20180125817
    Abstract: Combinations of an IDO1 inhibitor (e.g., a 3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione compound), with an anti-PD1 antibody or anti-PD-L1 antibody, and an anti-4-1BB antibody, as selected anti-cancer or anti-viral agents are provided. Also provided are use of these combinations for the treatment and/or prevention of cancer and endometriosis.
    Type: Application
    Filed: May 12, 2016
    Publication date: May 10, 2018
    Inventors: Manfred Kraus, Sandra Cauwenberghs, Stefano Crosignani, Gregory Driessens
  • Pyrrolidine-2, 5-dione derivatives, pharmaceutical compositions and methods for use as IDO1 inhibitors
    Patent number: 9949951
    Abstract: Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: April 24, 2018
    Assignee: ITEOS THERAPEUTICS
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Gregory Driessens, Frederik Deroose
  • 3-indol substituted derivatives, pharmaceutical compositions and methods for use
    Patent number: 9873690
    Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: January 23, 2018
    Assignees: Pfizer Inc, iTeos Therapeutics
    Inventors: Sacha Ninkovic, Stefano Crosignani, Indrawan James McAlpine, Michael Raymond Collins, Stephanie Anne Scales, Andreas Maderna, Martin Wythes