Patents by Inventor Alexandros Makriyannis

Alexandros Makriyannis 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).

  • Patent number: 11964956
    Abstract: Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.
    Type: Grant
    Filed: December 11, 2020
    Date of Patent: April 23, 2024
    Assignee: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Ganeshsingh A. Thakur, Rishi Sharma, Shashank Kulkarni
  • Patent number: 11939325
    Abstract: A process of manufacturing biologically active compounds, their analogs, pharmaceutically acceptable salts, solvates, polymorphs, isotopic variants, and intermediates thereof. Notably, the compounds of the formula IA, 1B, 1C. 1D. 1E, 1F and IG for which novel processes have been disclosed, selectively act on the cannabinoid receptors, and with high affinity. The processes for the preparation of the compounds enable the syntheses of cannabinoid modulators on a large-scale that are eco-friendly and economically viable. Additionally, the processes disclosed enable the synthesis of cannabinoid modulators with high purity and in high yield for their use in making drug substance and drug products.
    Type: Grant
    Filed: July 26, 2021
    Date of Patent: March 26, 2024
    Assignee: MAKScientific, LLC
    Inventors: Alexandros Makriyannis, Kiran Vemuri
  • Patent number: 11746113
    Abstract: Novel cannabinoid ligands represented by the general formulas I, II, and III and methods for preparation and use within which one or more of a fluorescent ligand, nitroxide spin label, metal chelate, biotin moiety, or group with enhanced polarity may be incorporated. The compounds can bind to and modulate the cannabinoid CB1 and CB2 receptors and thereby considered specific ligands for these receptors. Some of the disclosed compounds that bind to cannabinoid CB1 and CB2 receptors can exhibit tight or irreversible binding characteristics for these receptors. Due to the presence of the imaging/diagnostic and/or therapeutic functional groups including fluorescent groups, nitroxide spin labels, metal chelates, biotin moieties, and groups with enhanced polarity, the disclosed compounds may be useful as imaging/diagnostic tools and/or therapeutic agents.
    Type: Grant
    Filed: March 18, 2021
    Date of Patent: September 5, 2023
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Christos Iliopoulos Tsoutsouvas, Shashank Kulkarni, Lipin Ji
  • Publication number: 20230234928
    Abstract: Several biological targets have been implicated in the pathogenesis of lung, liver, renal and prostrate fibrotic proliferative diseases. While cannabinoid receptor-mediated signaling has emerged as a novel signaling pathway regulating fibrogenesis and inflammation, the present invention relates generally to biologically active compounds capable of interacting with one or more biological targets including the CB1 and/or the CB2 cannabinoid receptors, and comprise of neutral antagonists, neutral-peripheral antagonists, peripheral antagonists/inverse-agonists, compounds with mixed properties including CB1 antagonist/CB2 agonist properties, and allosteric properties for treating fibrosis of the liver, lung, kidney and the prostrate, and inflammatory conditions, including benign prostatic hyperplasia.
    Type: Application
    Filed: July 27, 2021
    Publication date: July 27, 2023
    Inventors: Alexandros Makriyannis, Kiran Vemuri
  • Publication number: 20220033393
    Abstract: The present invention relates to novel compounds that can act as antidotes for treating “Acute Cannabinoid Overdose” produced by classical cannabinoids such as ?9-tetrahydrocannabinol (THC) and several synthetic psychoactive cannabinoids (SPCs). The cannabis constituent THC exerts its psychotropic effects via CB1 receptor activation and SPCs mimic the effects of THC with higher potency and severe neurotoxicity. Compounds disclosed in this invention, their enantiomers, diastereomers, geometric isomers, racemates, tautomers, rotamers, atropisomers, metabolites, N-oxides, salts, solvates, hydrates, isotopic variations and their polymorphic forms can be therapeutically useful in an emergency setting for counteracting the intoxicating effects of acute THC ingestion and SPC overdose. Also, aspects of the invention are concerned with pyrazoles, imidazoles, triazoles, thiazoles, oxazoles, dihydropyrazoles, pyrrolidinones, azetidines, oxyazetidines and azaspiro[3.
    Type: Application
    Filed: August 2, 2021
    Publication date: February 3, 2022
    Inventors: Alexandros Makriyannis, Kiran Vemuri
  • Publication number: 20220024910
    Abstract: A process of manufacturing biologically active compounds, their analogs, pharmaceutically acceptable salts, solvates, polymorphs, isotopic variants, and intermediates thereof. Notably, the compounds of the formula IA, 1B, 1C. 1D. 1E, 1F and IG for which novel processes have been disclosed, selectively act on the cannabinoid receptors, and with high affinity. The processes for the preparation of the compounds enable the syntheses of cannabinoid modulators on a large-scale that are eco-friendly and economically viable. Additionally, the processes disclosed enable the synthesis of cannabinoid modulators with high purity and in high yield for their use in making drug substance and drug products.
    Type: Application
    Filed: July 26, 2021
    Publication date: January 27, 2022
    Inventors: Alexandros Makriyannis, Kiran Vemuri
  • Patent number: 11214578
    Abstract: Disclosed are compounds of general formulas I-III that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL.
    Type: Grant
    Filed: January 16, 2020
    Date of Patent: January 4, 2022
    Assignee: Northeastern University
    Inventors: Alexandros Makriyannis, Vidyanand G. Shukla, Shakiru O. Alapafuja
  • Publication number: 20210300937
    Abstract: Novel cannabinoid ligands represented by the general formulas I, II, and III and methods for preparation and use within which one or more of a fluorescent ligand, nitroxide spin label, metal chelate, biotin moiety, or group with enhanced polarity may be incorporated. The compounds can bind to and modulate the cannabinoid CB1 and CB2 receptors and thereby considered specific ligands for these receptors. Some of the disclosed compounds that bind to cannabinoid CB1 and CB2 receptors can exhibit tight or irreversible binding characteristics for these receptors. Due to the presence of the imaging/diagnostic and/or therapeutic functional groups including fluorescent groups, nitroxide spin labels, metal chelates, biotin moieties, and groups with enhanced polarity, the disclosed compounds may be useful as imaging/diagnostic tools and/or therapeutic agents.
    Type: Application
    Filed: March 18, 2021
    Publication date: September 30, 2021
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Christos Iliopoulos Tsoutsouvas, Shashank Kulkarni, Lipin Ji
  • Publication number: 20210101878
    Abstract: Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.
    Type: Application
    Filed: December 11, 2020
    Publication date: April 8, 2021
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Ganeshsingh A. Thakur, Rishi Sharma, Shashank Kulkarni
  • Patent number: 10968206
    Abstract: The present technology relates to novel cannabinergic nitrate esters and related analogs, process of preparation, pharmaceutical compositions and their methods of use as medicaments, pharmacological tools and/or biomarkers. The novel cannabinergic nitrate ester compounds provide medicaments useful in treating a variety of diseases and medical disorders.
    Type: Grant
    Filed: January 4, 2019
    Date of Patent: April 6, 2021
    Assignee: Northeastern University
    Inventors: Alexandros Makriyannis, Venkata Kiran Vemuri
  • Patent number: 10882838
    Abstract: Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.
    Type: Grant
    Filed: January 7, 2019
    Date of Patent: January 5, 2021
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Alexandros Makriyannis, Ganeshsingh A. Thakur, Rishi Sharma
  • Patent number: 10689357
    Abstract: Disclosed herein are compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof. Values for the variables in Structural Formula I are described herein. The compounds can be used to modulate (e.g., inhibit) N-acylethanolamine hydrolyzing acid amidase (NAAA) and thereby treat a variety of diseases, disorders and conditions mediated by NAAA, such as a gastrointestinal motility disorder, irritable bowel syndrome, an inflammatory bowel disorder, neuroinflammation, nicotine addiction, cancer, opioid dependence, analgesia, chemotherapy-induced neuropathic pain and pain. Also disclosed herein are compositions and methods including compounds of Structural Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 8, 2019
    Date of Patent: June 23, 2020
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Michael S. Malamas, Alexandros Makriyannis, Shrouq I. Farah, Alexander M. Zvonok, Shakiru Olajire Alapafuja
  • Patent number: 10662159
    Abstract: Provided herein are compounds and pharmaceutical compositions for selectively inhibiting serine hydrolase a/b-hydrolase domain 6 (ABHD6) and dually inhibiting ABHD6 and monoacylglycerol lipase (MGL). The compounds and pharmaceutical compositions disclosed herein are useful for treating a number of therapeutic conditions related to cannabinergic receptor function such as pain, inflammation, neuropathy, neurodegenerative diseases, anxiety disorders, motor function disorder, metabolic disorder, glaucoma and chemotherapy-induced nausea and vomiting and cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: May 26, 2020
    Assignee: MAKSCIENTIFIC, LLC
    Inventors: Alexandros Makriyannis, Michael Malamas, Manjunath Lamani, Shrouq I. Farah
  • Publication number: 20200148696
    Abstract: Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylgly-cerol lipase (MAGL) or dual FAAH/MAGL.
    Type: Application
    Filed: January 16, 2020
    Publication date: May 14, 2020
    Inventors: Alexandros Makriyannis, Vidyanand G. Shukla, Shakiru O. Alapafuja
  • Patent number: 10640494
    Abstract: A compound is represented as Formula I, a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof: Compounds of Formula I are inhibitors of N-acylethanolamine hydrolyzing acid amidase (NAAA).
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: May 5, 2020
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Michael Malamas, Alexandros Makriyannis, Kumara Vadivel Subramanian, Kyle M. Whitten, Nikolai M. Zvonok, Jay Matthew West, Michael McCormack, Spiro Pavlopoulos
  • Patent number: 10570146
    Abstract: Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL. More particularly, compounds of formula II have utility in a variety of therapeutic uses such as treatment of pain, inflammation, neuropathy, or appetite disorder.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: February 25, 2020
    Assignee: Northeastern University
    Inventors: Alexandros Makriyannis, Vidyanand G Shukla, Shakiru O Alapafuja
  • Publication number: 20190345132
    Abstract: Disclosed herein are compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof. Values for the variables in Structural Formula I are described herein. The compounds can be used to modulate (e.g., inhibit) N-acylethanolamine hydrolyzing acid amidase (NAAA) and thereby treat a variety of diseases, disorders and conditions mediated by NAAA, such as a gastrointestinal motility disorder, irritable bowel syndrome, an inflammatory bowel disorder, neuroinflammation, nicotine addiction, cancer, opioid dependence, analgesia, chemotherapy-induced neuropathic pain and pain. Also disclosed herein are compositions and methods including compounds of Structural Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 8, 2019
    Publication date: November 14, 2019
    Inventors: Michael S. Malamas, Alexandros Makriyannis, Shrouq I. Farah, Alexander M. Zvonok, Shakiru Olajire Alapafuja
  • Publication number: 20190225596
    Abstract: The present technology relates to novel cannabinergic nitrate esters and related analogs, process of preparation, pharmaceutical compositions and their methods of use as medicaments, pharmacological tools and/or biomarkers. The novel cannabinergic nitrate ester compounds provide medicaments useful in treating a variety of diseases and medical disorders.
    Type: Application
    Filed: January 4, 2019
    Publication date: July 25, 2019
    Inventors: Alexandros Makriyannis, Venkata Kiran Vemuri
  • Publication number: 20190185443
    Abstract: Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.
    Type: Application
    Filed: January 7, 2019
    Publication date: June 20, 2019
    Inventors: Alexandros Makriyannis, Ganeshsingh A. Thakur, Rishi Sharma
  • Publication number: 20190152917
    Abstract: Provided herein are compounds and pharmaceutical compositions for selectively inhibiting serine hydrolase a/b-hydrolase domain 6 (ABHD6) and dually inhibiting ABHD6 and monoacylglycerol lipase (MGL). The compounds and pharmaceutical compositions disclosed herein are useful for treating a number of therapeutic conditions related to cannabinergic receptor function such as pain, inflammation, neuropathy, neurodegenerative diseases, anxiety disorders, motor function disorder, metabolic disorder, glaucoma and chemotherapy-induced nausea and vomiting and cancer.
    Type: Application
    Filed: November 21, 2018
    Publication date: May 23, 2019
    Inventors: Michael Malamas, Alexandros Makriyannis, Manjunath Lamani, Shrouq I. Farah