Patents by Inventor Giorgio Tarzia
Giorgio Tarzia 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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Patent number: 10363237Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.Type: GrantFiled: March 16, 2016Date of Patent: July 30, 2019Assignees: The Regents of the University of California, Universita Degli Studi Di Urbino “Carlo Bo”, Universita Degli Studi Di ParmaInventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
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Patent number: 9908848Abstract: Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.Type: GrantFiled: September 14, 2015Date of Patent: March 6, 2018Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Tecnologia, Universita Degli Studi di Urbino “Carlo Bo”, Universita Degli Studi di ParmaInventors: Daniele Piomelli, Marco Mor, Giorgio Tarzia, Fabio Bertozzi, Andrea Nuzzi, Annalisa Fiasella, Tiziano Bandiera, Angelo Mario Reggiani
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Patent number: 9828338Abstract: Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.Type: GrantFiled: September 14, 2015Date of Patent: November 28, 2017Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Technologia, Universita Degli Studi di Urbino “Carlo Bo”, Universita Degli Studi di ParmaInventors: Daniele Piomelli, Tiziano Bandiera, Fabio Bertozzi, Andrea Nuzzi, Annalisa Fiasella, Stefano Ponzano, Chiara Pagliuca, Angelo Mario Reggiani, Marco Mor, Giorgio Tarzia
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Patent number: 9745255Abstract: The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.Type: GrantFiled: February 18, 2014Date of Patent: August 29, 2017Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Technologia, Universita Degli Studi di Urbino “Carlo Bo”, Universita Degli Studi di ParmaInventors: Daniele Piomelli, Guillermo Moreno-Sanz, Tiziano Bandiera, Marco Mor, Giorgio Tarzia
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Publication number: 20160256432Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.Type: ApplicationFiled: March 16, 2016Publication date: September 8, 2016Inventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
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Publication number: 20160235707Abstract: The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.Type: ApplicationFiled: April 25, 2016Publication date: August 18, 2016Inventors: Daniele Piomelli, Tiziano Bandiera, Marco Mor, Giorgio Tarzia, Fabio Bertozzi, Stefano Ponzano
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Patent number: 9353075Abstract: The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.Type: GrantFiled: November 21, 2012Date of Patent: May 31, 2016Assignees: The Regents of the University of California, Fondazione Istituto Italiano Di Technologia, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino “Carlo Bo”Inventors: Daniele Piomelli, Tiziano Bandiera, Marco Mor, Giorgio Tarzia, Fabio Bertozzi, Stefano Ponzano
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Patent number: 9321743Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.Type: GrantFiled: May 20, 2013Date of Patent: April 26, 2016Assignees: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino “Carlo Bo”Inventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
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Publication number: 20160068483Abstract: Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.Type: ApplicationFiled: September 14, 2015Publication date: March 10, 2016Inventors: Daniele Piomelli, Marco Mor, Giorgio Tarzia, Fabio Bertozzi, Andrea Nuzzi, Annalisa Fiasella, Tiziano Bandiera, Angelo Mario Reggiani
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Publication number: 20160002244Abstract: The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.Type: ApplicationFiled: August 10, 2015Publication date: January 7, 2016Inventors: Walter CABRI, Patrizia MINETTI, Giovanni PIERSANTI, Giorgio TARZIA
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Patent number: 9187413Abstract: Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof.Type: GrantFiled: July 22, 2011Date of Patent: November 17, 2015Assignees: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di UrbinoInventors: Daniele Piomelli, Jason R. Clapper, Guillermo Moreno-Sanz, Andrea Duranti, Giovanna Guiducci, Marco Mor, Giorgio Tarzia
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Patent number: 9133197Abstract: The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.Type: GrantFiled: March 18, 2010Date of Patent: September 15, 2015Assignee: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Walter Cabri, Patrizia Minetti, Giovanni Piersanti, Giorgio Tarzia
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Publication number: 20150045442Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C6 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which theType: ApplicationFiled: June 13, 2014Publication date: February 12, 2015Inventors: Gabriella GOBBI, Marco MOR, Silvia RIVARA, Franco FRASCHINI, Giorgio TARZIA, Annalida BEDINI, Gilberto SPADONI, Valeria LUCINI
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Publication number: 20140288170Abstract: The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.Type: ApplicationFiled: February 18, 2014Publication date: September 25, 2014Applicants: The Regents of the University of California, Universita Degli Studi di Parma, Universita Degli Studi di Urbino "Carlo Bo", Fondazione Istituto Italiano di TecnologiaInventors: Daniele Piomelli, Guillermo Moreno-Sanz, Tiziano Bandiera, Marco Mor, Giorgio Tarzia
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Patent number: 8791163Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which thType: GrantFiled: January 12, 2007Date of Patent: July 29, 2014Assignees: McGill University, Universita Degli Studi di Parma, Universita Degli Studi di Milano, Universita Degli Studi di UrbinoInventors: Gabriella Gobbi, Marco Mor, Silvia Rivara, Franco Fraschini, Giorgio Tarzia, Annalida Bedini, Gilberto Spadoni, Valeria Lucini
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Publication number: 20140094508Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.Type: ApplicationFiled: May 20, 2013Publication date: April 3, 2014Applicants: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino "Carlo Bo"Inventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
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Publication number: 20130217764Abstract: Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof.Type: ApplicationFiled: July 22, 2011Publication date: August 22, 2013Inventors: Daniele Piomelli, Jason R. Clapper, Guillermo Moreno-Sanz, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia, Todd A. Ostomel
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Publication number: 20120053191Abstract: The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.Type: ApplicationFiled: March 18, 2010Publication date: March 1, 2012Inventors: Walter Cabri, Patrizia Minetti, Giovanni Piersanti, Giorgio Tarzia
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Publication number: 20120010283Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: ApplicationFiled: August 16, 2011Publication date: January 12, 2012Applicants: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Patent number: 8003693Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: GrantFiled: July 28, 2006Date of Patent: August 23, 2011Assignees: The Regents of the University of California, Universita Degli Studi di Urbino, Universita Degl Studi di ParmaInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia