Patents Assigned to Universita Degli Studi di Urbino
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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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Patent number: 9428557Abstract: Tat protein produced in bulk culture is inactive when induced at conventional optical densities but can be obtained in biologically active form when induced during the logarithmic growth phase.Type: GrantFiled: February 6, 2009Date of Patent: August 30, 2016Assignees: ISTITUTO SUPERIORE DI SANITA, UNIVERSITA DEGLI STUDI DI URBINOInventors: Barbara Ensoli, Mauro Magnani
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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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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: 9145381Abstract: The present invention relates to compounds having general formula (I), i.e. poly-alkyl-bis-maltolic molecules and in particular to derivates of [(3-hydroxy-4-pyron-2-yl)methyl]-amine and pharmaceutically acceptable salts thereof, and to the use thereof as anti-neoplastic drugs, in particular, for the preparation of a medicament for the treatment of neoplastic diseases.Type: GrantFiled: November 27, 2009Date of Patent: September 29, 2015Assignee: Universita' Degli Studi Di UrbinoInventors: Mirco Fanelli, Vieri Fusi
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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: 20120035255Abstract: The present invention relates to compounds having general formula (I), i.e. poly-alkyl-bis-maltolic molecules and in particular to derivates of [(3-hydroxy-4-pyron-2-yl)methyl]-amine and pharmaceutically acceptable salts thereof, and to the use thereof as anti-neoplastic drugs, in particular, for the preparation of a medicament for the treatment of neoplastic diseases.Type: ApplicationFiled: November 27, 2009Publication date: February 9, 2012Applicant: Universita' Degli Studi Di UrbinoInventors: Mirco Fanelli, Vieri Fusi
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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
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Publication number: 20100267836Abstract: 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 theType: ApplicationFiled: January 12, 2007Publication date: October 21, 2010Applicants: UNIVERSITA DEGLI STUDI DI MILANO, UNIVERSITA DEGLI STUDI DI URBINO, MCGILL UNIVERSITY, UNIVERSITA DEGLI STUDI DI PARMAInventors: Gabriella Gobbi, Marco Mor, Silvia Rivara, Franco Fraschini, Giorgio Tarzia, Annalida Bedini, Gilberto Spadoni, Valeria Lucini
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Patent number: 7645788Abstract: Use of the tetramerous derivative of indole-3-carbinol having formula I for preparing a medicinal having anti-carcinogenic activity, and method of synthesis of the tetramerous derivative having formula I, in which indole-3-carbinol is reacted with an oxidizing agent so as to cause a polymeric oxidation of indole-3-carbinol.Type: GrantFiled: June 5, 2002Date of Patent: January 12, 2010Assignee: Universita' Degli Studi Di UrbinoInventors: Mauro Magnani, Chiara Fiorucci, Paolino Filippone, Giorgio Brandi, Mirko Paiardini
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Publication number: 20090082435Abstract: Methods, compositions, and compounds for inhibiting monoacyglycerol lipase, and for treating pain, for modulating stress-induced analgesia or for treating stress-induced disorders in mammals are provided.Type: ApplicationFiled: April 26, 2006Publication date: March 26, 2009Applicants: The Regents of the University of California, The University of Georgia Research, Universita Degli Studi Di Urbino, Univestia Degli Studi Di ParmaInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia, Andrea Hohmann
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Patent number: 7176201Abstract: 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: October 7, 2003Date of Patent: February 13, 2007Assignees: 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