Patents by Inventor Daniele Piomelli
Daniele Piomelli 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: 20160194296Abstract: The invention provides compounds of Formula (I) or pharmaceutically acceptable salts thereof wherein Ar?, R1, R2, R3, R4, X, Y are as defined in the description of invention, as multi-target directed ligands (MTDLs) that are at the same time inhibitors of the fatty acid amide hydrolase (FAAH) enzyme and modulators of the D3 dopamine receptor (D3DR), their methods of preparation, formulations and therapeutic applications thereof.Type: ApplicationFiled: July 10, 2014Publication date: July 7, 2016Inventors: Giovanni BOTTEGONI, Alessio DE SIMONE, Gian Filippo RUDA, Andrea CAVALLI, Tiziano BANDIERA, Daniele PIOMELLI
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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: 20160068482Abstract: 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, Tiziano Bandiera, Fabio Bertozzi, Andrea Nuzzi, Annalisa Fiasella, Stefano Ponzano, Chiara Pagliuca, Angelo Mario Reggiani
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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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Publication number: 20150203447Abstract: Multitarget inhibitors of the enzymes Fatty Acid Amide Hydrolase (FAAH), Cyclooxygenase-1 (COX-1) and/or Cyclooxygenase-2 (COX-2) having a specific carbamate moiety on the meta or ortho position of the A ring of a substituted biphenyl core and having an halogen in the ortho position of the B ring of the biphenyl core. Also concerns the therapeutical application of the multitarget inhibitors, in particular, in the prevention and treatment of cancer.Type: ApplicationFiled: August 1, 2013Publication date: July 23, 2015Applicants: Fondazione Istituti Italiano di Tecnologia, The Regents of the University of California, Alma Mater Studiorum-Universitá di BolognaInventors: Marco De Vivo, Rita Scarpelli, Andrea Cavalli, Marco Migliore, Daniele Piomelli, Damien Habrant, Angelo Favia
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Publication number: 20150148387Abstract: Methamphetamine is a highly addictive psychostimulant that causes profound damage to the brain and other body organs. Post mortem studies of human tissues have linked the use of this drug to diseases associated with aging, such as coronary atherosclerosis, but the molecular mechanism underlying these findings remains unknown. We report now that methamphetamine accelerates cellular senescence in vitro and activates transcription of genes involved in cell-cycle control and inflammation in vivo by stimulating production of the sphingolipid messenger ceramide. This pathogenic cascade is triggered by reactive oxygen species, generated through methamphetamine metabolism via cytochrome P450-2D6, which recruit nuclear factor (NF)-KB to induce expression of enzymes in the de novo pathway of ceramide biosynthesis. Inhibitors of ceramide formation prevent methamphetamine-induced senescence and attenuate systemic inflammation and health deterioration in rats self-administering the drug.Type: ApplicationFiled: September 30, 2014Publication date: May 28, 2015Inventors: Daniele Piomelli, Giuseppe Astarita, Agnesa Avanesian, Andrea Cavalli
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Publication number: 20150111892Abstract: The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.Type: ApplicationFiled: May 27, 2013Publication date: April 23, 2015Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
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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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Publication number: 20140163034Abstract: Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicants: IIT-Istituto Italiano di Tecnologia, The Regents of the University of CaliforniaInventors: Daniele Piomelli, Jin Fu, Giovanni Bottegoni, Andrea Cavalli, Tiziano Bandiera
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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: 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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Patent number: 7897598Abstract: Analogs that inhibit the transport of anandamide across cell membranes. The inhibitors are amide and ester analogs of anandamide having a tail portion X that is a fatty acid chain remnant, a central portion Y that is an amide or ester radical and a head portion Z that is selected from a variety of groups including hydrogen, alkyl, hydroxy alkyl, aryl, hydroxy aryl, heterocyclic and hydroxy heterocyclic radicals. The disclosed analogs have potential pharmaceutical uses as drugs for treating a variety of diseases and afflictions, including cardiovascular diseases and blood pressure disorders.Type: GrantFiled: June 6, 1999Date of Patent: March 1, 2011Inventors: Alexandros Makriyannis, Sonyuan Lin, Daniele Piomelli
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Publication number: 20100311711Abstract: 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: October 10, 2008Publication date: December 9, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
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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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Publication number: 20090048337Abstract: Fatty acid amide hydrolase inhibitors of the Formula: I.Type: ApplicationFiled: July 28, 2006Publication date: February 19, 2009Applicants: The Regents of the University of California, Universita Degli Studi Du UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Publication number: 20090005447Abstract: Methods, pharmaceutical compositions, and compounds for reducing body weight, modulating body lipid metabolism, and reducing food intake in mammals are provided. The compounds of the invention include fatty acid ethanolamide compounds, homologues and analogs of which the prototype is the endogenous fatty acid ethanolamide, oleoylethanolamide.Type: ApplicationFiled: June 16, 2008Publication date: January 1, 2009Applicant: The Regents of the University of CaliforniaInventors: Daniele Piomelli, Fernando Rodriguez de Fonseca