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).
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Publication number: 20220041538Abstract: 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: ApplicationFiled: December 11, 2019Publication date: February 10, 2022Applicant: EMERALD HEALTH PHARMACEUTICALS INCInventors: Eduardo MUÑOZ BLANCO, Giovanni APPENDINO
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Patent number: 10766855Abstract: 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: GrantFiled: October 3, 2017Date of Patent: September 8, 2020Assignee: VIVACELL BIOTECHNOLOGY ESPAÑA, S.L.Inventors: Eduardo Munoz Blanco, Alberto Minassi, Maria Luz Bellido Cabello De Alba, Giovanni Appendino
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Publication number: 20190367447Abstract: 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: ApplicationFiled: October 3, 2017Publication date: December 5, 2019Inventors: Eduardo MUNOZ BLANCO, Alberto MINASSI, Maria Luz BELLIDO CABELLO DE ALBA, Giovanni APPENDINO
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Patent number: 9802880Abstract: 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: GrantFiled: February 12, 2015Date of Patent: October 31, 2017Inventors: Giovanni Appendino, María Luz Bellido Cabello De Alba, Eduardo Muñoz Blanco
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Publication number: 20170247308Abstract: 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: ApplicationFiled: February 12, 2015Publication date: August 31, 2017Applicant: VIVACELL BIOTECHNOLOGY ESPAÑA S.L.Inventors: Giovanni APPENDINO, María Luz BELLIDO CABELLO DE ALBA, Eduardo MUÑOZ BLANCO
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Patent number: 9701618Abstract: 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: GrantFiled: April 16, 2014Date of Patent: July 11, 2017Inventors: Giovanni Appendino, María Luz Bellido Cabello De Alba, Eduardo Muñoz Blanco
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Publication number: 20170044092Abstract: 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: ApplicationFiled: April 16, 2014Publication date: February 16, 2017Inventors: Giovanni APPENDINO, María Luz BELLIDO CABELLO DE ALBA, Eduardo MUÑOZ BLANCO
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Patent number: 9416083Abstract: 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: GrantFiled: October 26, 2015Date of Patent: August 16, 2016Assignee: INDENA S.P.A.Inventors: Maria Luz Bellido Cabello De Alba, Giovanni Appendino, Alberto Pagani, Eduardo Munoz Blanco
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Publication number: 20160039733Abstract: 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: ApplicationFiled: October 26, 2015Publication date: February 11, 2016Inventors: Maria Luz Bellido Cabello De Alba, Giovanni Appendino, Alberto Pagani, Eduardo Munoz Blanco
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Publication number: 20140243551Abstract: 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: ApplicationFiled: October 2, 2012Publication date: August 28, 2014Inventors: Maria Luz Bellido Cabello De Alba, Giovanni Appendino, Alberto Pagani, Eduardo Munoz Blanco
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Patent number: 8772349Abstract: 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: GrantFiled: March 26, 2010Date of Patent: July 8, 2014Assignee: Vivacell Biotechnology Espana, S.L.Inventors: Eduardo Muñoz Blanco, Giovanni Appendino, María Luz Bellido Cabello De Alba
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Patent number: 8673578Abstract: 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: GrantFiled: October 27, 2010Date of Patent: March 18, 2014Assignee: Deutsches Institut für Ernahrungsforschung Potsdam-RehbrückeInventors: Giovanni Appendino, Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof
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Patent number: 8524465Abstract: 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: GrantFiled: August 13, 2012Date of Patent: September 3, 2013Assignee: Deutsches Institut fuer Ernaehrungsforschung Potsdam-RehbrueckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Publication number: 20130158126Abstract: 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: ApplicationFiled: March 26, 2010Publication date: June 20, 2013Applicant: VIVACELL BIOTECHNOLOGY ESPAÑA, S.L.Inventors: Eduardo Muñoz Blanco, Giovanni Appendino, María Luz Bellido Cabello De Alba
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Publication number: 20120309703Abstract: 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: ApplicationFiled: August 13, 2012Publication date: December 6, 2012Applicant: Deutsches Institut Fuer Ernaehrungsforschung Potsdam-RehbrueckeInventors: Maik BEHRENS, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Patent number: 8309314Abstract: 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: GrantFiled: March 31, 2008Date of Patent: November 13, 2012Assignee: Deutsches Institut Fuer Ernaehrungsforschung Potsdam-RehbrueckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Publication number: 20120283324Abstract: 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: ApplicationFiled: October 27, 2010Publication date: November 8, 2012Applicant: DEUTSCHES INSTITUT FUR EMAHRUNGSFORSCHUNG POTSDAM-REHBRUCKEInventors: Giovanni Appendino, Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof
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Patent number: 8043823Abstract: 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: GrantFiled: March 31, 2008Date of Patent: October 25, 2011Assignee: Deutsches Institut fuer ErnaehrungsforschungInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino, Valeria D'Auria
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Publication number: 20100222437Abstract: 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: ApplicationFiled: September 29, 2008Publication date: September 2, 2010Applicant: Vivacell Biotechnology Espana, S.L.Inventors: Eduardo Munoz Blanco, Giovanni Appendino, Bernd L. Fiebich, Giampaolo Grassi
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Publication number: 20100184796Abstract: 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: ApplicationFiled: March 31, 2008Publication date: July 22, 2010Applicant: DEUTSCHES INSTITUT FÜR ERNÄHRUNGSFORSCHUNG POTSDAM-REHBRÜCKEInventors: Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof, Giovanni Appendino, Valeria D' Auria