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).
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Publication number: 20230000871Abstract: 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: ApplicationFiled: October 29, 2020Publication date: January 5, 2023Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco CASUSCELLI, Teresa DISINGRINI, Paola MAGNAGHI, Stefano NUVOLONI, Paolo ORSINI
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Publication number: 20220363636Abstract: 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: ApplicationFiled: July 13, 2022Publication date: November 17, 2022Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
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Patent number: 11420940Abstract: 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: GrantFiled: September 11, 2020Date of Patent: August 23, 2022Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
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Publication number: 20220144813Abstract: 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: ApplicationFiled: June 21, 2021Publication date: May 12, 2022Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 11047217Abstract: 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: GrantFiled: March 21, 2018Date of Patent: June 29, 2021Assignee: FORE S.R.L.Inventor: Paolo Orsini
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Publication number: 20200407314Abstract: 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: ApplicationFiled: September 11, 2020Publication date: December 31, 2020Applicant: NERVIANO MEDICAL SCIENCES S.r.lInventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
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Publication number: 20200377487Abstract: 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: ApplicationFiled: December 12, 2019Publication date: December 3, 2020Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 10800739Abstract: 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: GrantFiled: July 2, 2019Date of Patent: October 13, 2020Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
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Patent number: 10556913Abstract: 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: GrantFiled: November 1, 2018Date of Patent: February 11, 2020Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Daniele Donati, Paolo Orsini
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Publication number: 20200032628Abstract: 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: ApplicationFiled: March 21, 2018Publication date: January 30, 2020Inventor: Paolo ORSINI
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Publication number: 20190330151Abstract: 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: ApplicationFiled: July 2, 2019Publication date: October 31, 2019Applicant: NERVIANO MEDICAL SCIENCES S.r.lInventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
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Patent number: 10385018Abstract: 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: GrantFiled: October 23, 2013Date of Patent: August 20, 2019Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
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Publication number: 20190241546Abstract: 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: ApplicationFiled: September 19, 2018Publication date: August 8, 2019Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 10266547Abstract: 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: GrantFiled: September 16, 2014Date of Patent: April 23, 2019Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Michele Caruso, Paolo Orsini
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Publication number: 20190071451Abstract: 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: ApplicationFiled: November 1, 2018Publication date: March 7, 2019Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo BERIA, Michele CARUSO, Daniele DONATI, Paolo ORSINI
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Patent number: 10174048Abstract: 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: GrantFiled: July 12, 2016Date of Patent: January 8, 2019Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Daniele Donati, Paolo Orsini
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Patent number: 10081622Abstract: 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: GrantFiled: February 22, 2017Date of Patent: September 25, 2018Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 10071074Abstract: 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: GrantFiled: November 23, 2016Date of Patent: September 11, 2018Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
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Publication number: 20180215768Abstract: 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: ApplicationFiled: July 12, 2016Publication date: August 2, 2018Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo BERIA, Michele CARUSO, Daniele DONATI, Paolo ORSINI
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Publication number: 20170158677Abstract: 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: ApplicationFiled: February 22, 2017Publication date: June 8, 2017Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni