Patents by Inventor Paolo Orsini

Paolo Orsini 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: 11773064
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 13, 2022
    Date of Patent: October 3, 2023
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Publication number: 20230000871
    Abstract: The present invention relates to certain gem-disubstituted heterocyclic compounds, which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type (wt) enzyme. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: October 29, 2020
    Publication date: January 5, 2023
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco CASUSCELLI, Teresa DISINGRINI, Paola MAGNAGHI, Stefano NUVOLONI, Paolo ORSINI
  • Publication number: 20220363636
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: July 13, 2022
    Publication date: November 17, 2022
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Patent number: 11420940
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of in-flammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: September 11, 2020
    Date of Patent: August 23, 2022
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Publication number: 20220144813
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: June 21, 2021
    Publication date: May 12, 2022
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 11047217
    Abstract: An extraction systems in the oil sector, in particular to the equipment intended for the completion of the wells after their drilling; more in particular, the system relates to a safety valve for artificial lifting wells driven by reciprocating downhole rod pumps.
    Type: Grant
    Filed: March 21, 2018
    Date of Patent: June 29, 2021
    Assignee: FORE S.R.L.
    Inventor: Paolo Orsini
  • Publication number: 20200407314
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of in-flammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: September 11, 2020
    Publication date: December 31, 2020
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Publication number: 20200377487
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: December 12, 2019
    Publication date: December 3, 2020
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 10800739
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of in-flammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: October 13, 2020
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Patent number: 10556913
    Abstract: The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (Ia) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: February 11, 2020
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Daniele Donati, Paolo Orsini
  • Publication number: 20200032628
    Abstract: An extraction systems in the oil sector, in particular to the equipment intended for the completion of the wells after their drilling; more in particular, the system relates to a safety valve for artificial lifting wells driven by reciprocating downhole rod pumps.
    Type: Application
    Filed: March 21, 2018
    Publication date: January 30, 2020
    Inventor: Paolo ORSINI
  • Publication number: 20190330151
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of in-flammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: July 2, 2019
    Publication date: October 31, 2019
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Patent number: 10385018
    Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: August 20, 2019
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Publication number: 20190241546
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: September 19, 2018
    Publication date: August 8, 2019
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 10266547
    Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno[2,3-e]indole moiety tethered to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: April 23, 2019
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Michele Caruso, Paolo Orsini
  • Publication number: 20190071451
    Abstract: The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (la) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation.
    Type: Application
    Filed: November 1, 2018
    Publication date: March 7, 2019
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo BERIA, Michele CARUSO, Daniele DONATI, Paolo ORSINI
  • Patent number: 10174048
    Abstract: The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (Ia) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation.
    Type: Grant
    Filed: July 12, 2016
    Date of Patent: January 8, 2019
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Daniele Donati, Paolo Orsini
  • Patent number: 10081622
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: September 25, 2018
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 10071074
    Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: September 11, 2018
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
  • Publication number: 20180215768
    Abstract: The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (Ia) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation.
    Type: Application
    Filed: July 12, 2016
    Publication date: August 2, 2018
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo BERIA, Michele CARUSO, Daniele DONATI, Paolo ORSINI