Patents by Inventor Giovanni Appendino

Giovanni Appendino 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).

  • Publication number: 20220041538
    Abstract: A compound of formula I or a pharmaceutical salt thereof of formula II, as well as a process to obtain said compound and a process to obtain said salt. Additionally, disclosed is the use of said compound of formula I or said pharmaceutical salt thereof of formula II as a medicament, in particular as a peroxisome proliferator-activated receptor gamma (PPAR?) agonist, for use in the treatment or prevention of a disease responsive to PPAR? agonists. Also disclosed is a pharmaceutical composition comprising said compound or said salt, as well as a method of treating or preventing a disease with said compound of formula I or said salt thereof of formula II, or with a composition comprising said compound or said salt.
    Type: Application
    Filed: December 11, 2019
    Publication date: February 10, 2022
    Applicant: EMERALD HEALTH PHARMACEUTICALS INC
    Inventors: Eduardo MUÑOZ BLANCO, Giovanni APPENDINO
  • Patent number: 10766855
    Abstract: Triterpenoid derivatives and compositions comprising said triterpenoids derivatives of Formula (I) are described, wherein R?—C(O)NHOH. Said triterpenoids and compositions show capacity to bind PHD2, stabilize HIF-1? and HIF-2? proteins, activate the HIF pathway in different cell types, induce angiogenesis in human endothelial vascular cell, show neuroprotective activity in vitro and in vivo, antidiabetic activity and reduce the levels of lipids in vivo, and increase the plasma levels of Erythropoietin in vivo. The triterpenoid derivatives described act also in a selective manner and do not induce Nrf2 activation, NF-?B inhibition, STAT3 inhibition, and TGR5 activation, which are known activities of the natural triterpenoid precursors.
    Type: Grant
    Filed: October 3, 2017
    Date of Patent: September 8, 2020
    Assignee: VIVACELL BIOTECHNOLOGY ESPAÑA, S.L.
    Inventors: Eduardo Munoz Blanco, Alberto Minassi, Maria Luz Bellido Cabello De Alba, Giovanni Appendino
  • Publication number: 20190367447
    Abstract: Triterpenoid derivatives and compositions comprising said triterpenoids derivatives of Formula (I) are described, wherein R?—C(O)NHOH. Said triterpenoids and compositions show capacity to bind PHD2, stabilize HIF-1? and HIF-2? proteins, activate the HIF pathway in different cell types, induce angiogenesis in human endothelial vascular cell, show neuroprotective activity in vitro and in vivo, antidiabetic activity and reduce the levels of lipids in vivo, and increase the plasma levels of Erythropoietin in vivo. The triterpenoid derivatives described act also in a selective manner and do not induce Nrf2 activation, NF-?B inhibition, STAT3 inhibition, and TGR5 activation, which are known activities of the natural triterpenoid precursors.
    Type: Application
    Filed: October 3, 2017
    Publication date: December 5, 2019
    Inventors: Eduardo MUNOZ BLANCO, Alberto MINASSI, Maria Luz BELLIDO CABELLO DE ALBA, Giovanni APPENDINO
  • Patent number: 9802880
    Abstract: The present invention relates to novel cannabigerol quinone derivatives of formula (I) wherein R is the carbon atom of a linear or branched group, represented by: aryl, alkenyl, alkynyl or alcoxycarbonil groups; or wherein R is the nitrogen atom of a linear or branched group, represented by: alkylamino, arylamino, alkenylamino or alkynylamino groups; or, alternatively, R represents a bond between 2 molecules of formula (I) forming a dimer. The invention also relates to the use of any of the compounds of formula (I) as medicaments in therapy, particularly for treating PPARg-related diseases due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: October 31, 2017
    Inventors: Giovanni Appendino, María Luz Bellido Cabello De Alba, Eduardo Muñoz Blanco
  • Publication number: 20170247308
    Abstract: The present invention relates to novel cannabigerol quinone derivatives of formula (I) wherein R is the carbon atom of a linear or branched group, represented by: aryl, alkenyl, alkynyl or alcoxycarbonil groups; or wherein R is the nitrogen atom of a linear or branched group, represented by: alkylamino, arylamino, alkenylamino or alkynylamino groups; or, alternatively, R represents a bond between 2 molecules of formula (I) forming a dimer. The invention also relates to the use of any of the compounds of formula (I) as medicaments in therapy, particularly for treating PPARg-related diseases due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds.
    Type: Application
    Filed: February 12, 2015
    Publication date: August 31, 2017
    Applicant: VIVACELL BIOTECHNOLOGY ESPAÑA S.L.
    Inventors: Giovanni APPENDINO, María Luz BELLIDO CABELLO DE ALBA, Eduardo MUÑOZ BLANCO
  • Patent number: 9701618
    Abstract: The present invention relates to novel cannabidiol quinone derivatives of formula (I) (I) wherein R is the carbon atom of a, linear or branched group, represented by: alkyl, aryl, alkenyl, alkynyl, acyl or alkoxycarbonyl groups; or wherein R is the nitrogen atom of a, linear or branched group represented by: alkylamine, arylamine, alkenylamine or alkynylamine groups. The invention also relates to the use of any of the compounds of formula (I) as medicaments in therapy, particularly for treating diseases and conditions responsive to PPARg modulation due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: July 11, 2017
    Inventors: Giovanni Appendino, María Luz Bellido Cabello De Alba, Eduardo Muñoz Blanco
  • Publication number: 20170044092
    Abstract: The present invention relates to novel cannabidiol quinone derivatives of formula (I) (I) wherein R is the carbon atom of a, linear or branched group, represented by: alkyl, aryl, alkenyl, alkynyl, acyl or alkoxycarbonyl groups; or wherein R is the nitrogen atom of a, linear or branched group represented by: alkylamine, arylamine, alkenylamine or alkynylamine groups. The invention also relates to the use of any of the compounds of formula (I) as medicamentsin therapy, particularly for treating diseases and conditions responsive to PPARg modulation due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds.
    Type: Application
    Filed: April 16, 2014
    Publication date: February 16, 2017
    Inventors: Giovanni APPENDINO, María Luz BELLIDO CABELLO DE ALBA, Eduardo MUÑOZ BLANCO
  • Patent number: 9416083
    Abstract: The present invention relates to a new method for isolating ingenol (C20H28O5) from mixtures of diterpenoid esters and ingenol esters in a single step. Ingenol isolated by means of this method can be used as a precursor for the synthesis of biologically active ingenol derivatives, such as ingenol-3-angelate and ingenol-3-tigliate.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: August 16, 2016
    Assignee: INDENA S.P.A.
    Inventors: Maria Luz Bellido Cabello De Alba, Giovanni Appendino, Alberto Pagani, Eduardo Munoz Blanco
  • Publication number: 20160039733
    Abstract: The present invention relates to a new method for isolating ingenol (C20H28O5) from mixtures of diterpenoid esters and ingenol esters in a single step. Ingenol isolated by means of this method can be used as a precursor for the synthesis of biologically active ingenol derivatives, such as ingenol-3-angelate and ingenol-3-tigliate.
    Type: Application
    Filed: October 26, 2015
    Publication date: February 11, 2016
    Inventors: Maria Luz Bellido Cabello De Alba, Giovanni Appendino, Alberto Pagani, Eduardo Munoz Blanco
  • Publication number: 20140243551
    Abstract: The present invention relates to a new method for isolating ingenol (C20H28O5) from mixtures of diterpenoid esters and ingenol esters in a single step. Ingenol isolated by means of this method can be used as a precursor for the synthesis of biologically active ingenol derivatives, such as ingenol-3-angelate and ingenol-3-tigliate.
    Type: Application
    Filed: October 2, 2012
    Publication date: August 28, 2014
    Inventors: Maria Luz Bellido Cabello De Alba, Giovanni Appendino, Alberto Pagani, Eduardo Munoz Blanco
  • Patent number: 8772349
    Abstract: Cannabinoid quinone derivatives. The present invention refers to cannabinoid quinone derivatives to be used as medicaments, particularly as PPAR gamma (PPARg) agonists for treating diseases which etiology is based on an impaired PPARg function as transcription factor i.e. PPARg-related diseases.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: July 8, 2014
    Assignee: Vivacell Biotechnology Espana, S.L.
    Inventors: Eduardo Muñoz Blanco, Giovanni Appendino, María Luz Bellido Cabello De Alba
  • Patent number: 8673578
    Abstract: The present invention relates to antagonists and agonists of the human bitter-taste receptors hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and hTAS2R47. The invention also relates to methods for identifying further molecules that suppress or enhance bitter taste transduction or bitter taste response mediated by hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and/or hTAS2R47 and uses thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 18, 2014
    Assignee: Deutsches Institut für Ernahrungsforschung Potsdam-Rehbrücke
    Inventors: Giovanni Appendino, Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof
  • Patent number: 8524465
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: September 3, 2013
    Assignee: Deutsches Institut fuer Ernaehrungsforschung Potsdam-Rehbruecke
    Inventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
  • Publication number: 20130158126
    Abstract: Cannabinoid quinone derivatives. The present invention refers to cannabinoid quinone derivatives to be used as medicaments, particularly as PPAR gamma (PPARg) agonists for treating diseases which etiology is based on an impaired PPARg function as transcription factor i.e. PPARg-related diseases.
    Type: Application
    Filed: March 26, 2010
    Publication date: June 20, 2013
    Applicant: VIVACELL BIOTECHNOLOGY ESPAÑA, S.L.
    Inventors: Eduardo Muñoz Blanco, Giovanni Appendino, María Luz Bellido Cabello De Alba
  • Publication number: 20120309703
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.
    Type: Application
    Filed: August 13, 2012
    Publication date: December 6, 2012
    Applicant: Deutsches Institut Fuer Ernaehrungsforschung Potsdam-Rehbruecke
    Inventors: Maik BEHRENS, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
  • Patent number: 8309314
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: November 13, 2012
    Assignee: Deutsches Institut Fuer Ernaehrungsforschung Potsdam-Rehbruecke
    Inventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
  • Publication number: 20120283324
    Abstract: The present invention relates to antagonists and agonists of the human bitter-taste receptors hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and hTAS2R47. The invention also relates to methods for identifying further molecules that suppress or enhance bitter taste transduction or bitter taste response mediated by hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and/or hTAS2R47 and uses thereof.
    Type: Application
    Filed: October 27, 2010
    Publication date: November 8, 2012
    Applicant: DEUTSCHES INSTITUT FUR EMAHRUNGSFORSCHUNG POTSDAM-REHBRUCKE
    Inventors: Giovanni Appendino, Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof
  • Patent number: 8043823
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R46, hTAS2R47 and hTAS2R50 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R46, hTAS2R47 and hTAS2R50 bitter taste transduction or bitter taste response.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: October 25, 2011
    Assignee: Deutsches Institut fuer Ernaehrungsforschung
    Inventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino, Valeria D'Auria
  • Publication number: 20100222437
    Abstract: The invention relates to a composition comprising cannabidiol and Denbinobin and its use in medicine, for example, for the prevention and treatment of gastrointestinal inflammatory diseases and for the prevention and treatment of gastrointestinal cancers.
    Type: Application
    Filed: September 29, 2008
    Publication date: September 2, 2010
    Applicant: Vivacell Biotechnology Espana, S.L.
    Inventors: Eduardo Munoz Blanco, Giovanni Appendino, Bernd L. Fiebich, Giampaolo Grassi
  • Publication number: 20100184796
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R46, hTAS2R47 and hTAS2R50 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R46, hTAS2R47 and hTAS2R50 bitter taste transduction or bitter taste response.
    Type: Application
    Filed: March 31, 2008
    Publication date: July 22, 2010
    Applicant: DEUTSCHES INSTITUT FÜR ERNÄHRUNGSFORSCHUNG POTSDAM-REHBRÜCKE
    Inventors: Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof, Giovanni Appendino, Valeria D' Auria