Patents by Inventor Victor J. Hruby

Victor J. Hruby 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).

  • Publication number: 20220143196
    Abstract: Ligand-drug conjugates for targeted melanoma therapies are disclosed herein. A ligand is conjugated to a cytotoxic cancer drug through a cleavage linker. The ligand can bind to an overexpressed receptor on a cancer cell, resulting in selectivity. This allows the drug to enter a cancer cell selectively and release the drug within that specific cancer cell. Such therapies provide selectivity to melanoma through a ligand that targets the MC1R receptor, which is highly expressed in 80% of malignant melanomas. The ligand-drug conjugates can be used to deliver a wide range of cytotoxic cancer drugs selective to melanoma cells which may solve the drug resistance problem of melanoma in current therapies.
    Type: Application
    Filed: January 19, 2022
    Publication date: May 12, 2022
    Inventors: Minying Cai, Victor J. Hruby, Yang Zhou
  • Publication number: 20220024978
    Abstract: The present invention relates generally to a compound having both agonist activity at opioid receptor(s) and antagonist activity at NK1 receptor, and methods for producing and using the same. This combination of activities provides several synergistic and/or beneficial effects such as enhanced potency in analgesic effect and reduction or inhibition of tolerance.
    Type: Application
    Filed: October 12, 2021
    Publication date: January 27, 2022
    Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Victor J. Hruby, Aswini K. Giri
  • Patent number: 11230568
    Abstract: The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: January 25, 2022
    Assignees: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC., INTEZYNE TECHNOLOGIES INC., ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA, BOARD OF REGENTS, UNTVERSITY OF TEXAS SYSTEM
    Inventors: Robert J. Gillies, David L. Morse, Natalie M. Barkey, Kevin N. Sill, Josef Vagner, Narges K. Tafreshi, Jonathan L. Sessler, Christian Preihs, Victor J. Hruby
  • Patent number: 11141452
    Abstract: A compound for treatment of pain comprising a single multivalent/multifunctional ligand with agonist activity at opioid receptors and with antagonist activity at NK-1 receptors, joined by a linker. Also disclosed is a pharmaceutical compound comprising the above compound in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: October 12, 2021
    Assignee: Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Victor J. Hruby, Aswini K. Giri
  • Patent number: 11124542
    Abstract: Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Zaa10]-R2. R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)nCH3, or —CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COOH, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: September 21, 2021
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Victor J. Hruby, Minying Cai
  • Publication number: 20210196782
    Abstract: Opioid receptor ligands (ORLs) that are multifunctional having agonist activity at mu opioid receptor (MOR), agonist activity at delta opioid receptor (DOR), and antagonist (or partial agonist) activity at kappa opioid receptor (KOR) are for the treatment of pain. The ORLs comprise peptide portions that are analogs derived from enkephalins, endomorphins, or [DArg2, Lys4]-dermorphine (DALDA), as well as tail portions that comprise a lipophilic molecule such as a 4-anilidopiperidine moiety.
    Type: Application
    Filed: March 10, 2021
    Publication date: July 1, 2021
    Inventors: Yeon Sun Lee, Victor J. Hruby, Frank Porreca
  • Publication number: 20200277331
    Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described herein. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand according to the following: in a pharmaceutically acceptable carrier is administered to the subject. Xaa can be Cha or Pro. The MC5R peptide is a selective MC5R antagonist, and administration thereof to the subject can treat the depressive or anxiety disorder with clinical improvement observed in a relatively short time.
    Type: Application
    Filed: May 18, 2020
    Publication date: September 3, 2020
    Inventors: Victor J. Hruby, Minying Cai, Caurnel Morgan
  • Publication number: 20200222380
    Abstract: The present invention provides using a substituted 1-arylalkyl-4-acylaminopiperidine compound of Formula I: to treat various clinical conditions including, but not limited to, hemorrhagic shock, nicotine withdrawal symptoms, gastrointestinal side effects of opioids, cancer therapy, epithelial wounds, herpes zoster infection, or opioid-induced pruritus. In compound of Formula I, R1 is C1-10 alkyl, C1-10 haloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R2 is C1-6 alkylene; Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(?O)—X1, wherein X1 is —OR3 or —NR4R5, where each of R3, R4 and R5 is H or C1-10 alkyl.
    Type: Application
    Filed: March 25, 2020
    Publication date: July 16, 2020
    Applicant: Arizona Board of Regents on Behalf of the University of Arizona, a body corporate
    Inventors: Ruben S. Vardanyan, Victor J. Hruby
  • Patent number: 10653743
    Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising compound PG-20N in a pharmaceutically acceptable carrier is described. According to another embodiment, the subject disclosure features method of treating a depressive disorder or an anxiety disorder in a subject in need of such treatment. The method may comprise administering to the subject a therapeutically effective amount of a composition comprising PG-20N.
    Type: Grant
    Filed: October 17, 2016
    Date of Patent: May 19, 2020
    Assignees: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA, THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Victor J. Hruby, Minying Cai, Caurnel Morgan
  • Patent number: 10617681
    Abstract: The present invention provides a compound of the formula: wherein ring Z is a 5-, 6- or 7-membered ring; R1 is C1-10 alkyl, C1-10 haloalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heteroaralkyl; R2 is C1-10 alkylene; and Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(?O)—X1, wherein X1 is —OR3 or —NR4R5, where each of R3, R4 and R5 is H or C1-10 alkyl. The present invention also provides a method for using compound of Formula I to treat a wide variety of clinical conditions.
    Type: Grant
    Filed: December 31, 2018
    Date of Patent: April 14, 2020
    Assignee: Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Ruben S. Vardanyan, Victor J. Hruby
  • Patent number: 10550157
    Abstract: Compositions and methods of treating a central nervous system (CNS) disorder or mood disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand in a pharmaceutically acceptable carrier is administered to the subject. The MCSR peptide ligand is a selective MCSR antagonist, in which administration thereof to the subject can treat the CNS disorder or mood disorder with clinical improvement observed in a relatively short time.
    Type: Grant
    Filed: October 17, 2016
    Date of Patent: February 4, 2020
    Assignee: ARIZONA BOARD OF REGENT ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Victor J. Hruby, Minying Cai, Horst Kessler
  • Publication number: 20200002376
    Abstract: The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.
    Type: Application
    Filed: June 24, 2019
    Publication date: January 2, 2020
    Inventors: ROBERT J. GILLIES, DAVID L. MORSE, NATALIE M. BARKEY, KEVIN N. SILL, JOSEF VAGNER, NARGES K. TAFRESHI, JONATHAN L. SESSLER, CHRISTIAN PREIHS, VICTOR J. HRUBY
  • Publication number: 20190309022
    Abstract: Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Zaa10]-R2. R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)nCH3, or —CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COON, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.
    Type: Application
    Filed: June 4, 2019
    Publication date: October 10, 2019
    Inventors: Victor J. Hruby, Minying Cai
  • Patent number: 10428115
    Abstract: Described are Dynorphin A analog compounds and uses thereof for treating pain in humans and lower animals by administering to a human or lower animal in need of treatment. The compounds interact with the bradykinin receptor to relieve pain. Preferred compounds are amphipathic [Des-Arg7]-dynorphin A peptide analogs and specific cyclic dynorphin A peptide analogs.
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: October 1, 2019
    Assignee: Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Yeon Sun Lee, Victor J. Hruby, Frank Porreca, Josephine Lai
  • Publication number: 20190255142
    Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand according to SEQ NO. 1: in a pharmaceutically acceptable carrier is administered to the subject. Xaa can be Cha or Pro. The MC5R peptide is a selective MC5R antagonist, and administration thereof to the subject can treat the depressive or anxiety disorder with clinical improvement observed in a relatively short time.
    Type: Application
    Filed: October 17, 2016
    Publication date: August 22, 2019
    Inventors: Victor J. Hruby, Minying Cai
  • Publication number: 20190233487
    Abstract: Peptide analogues of ?-amyloid and methods of using said analogues for neuroprotection are described herein. The ?-amyloid peptide analogues have a sequence that is at least 50% identical to an N-terminal ?-amyloid core fragment. A pharmaceutical composition of the ?-amyloid peptide analogues in a pharmaceutically acceptable carrier can be administered to a subject for neuromodulation. The ?-amyloid peptide analogues, while lacking neurotoxicity, effectively provides for protective activity against ?-amyloid toxicity.
    Type: Application
    Filed: August 15, 2017
    Publication date: August 1, 2019
    Inventors: Robert A. Nichols, Kelly Forest, Victor J. Hruby
  • Patent number: 10329326
    Abstract: The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: June 25, 2019
    Assignees: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA, BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM, H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC., INTEZYNE TECHNOLOGIES INC.
    Inventors: Robert J. Gillies, David L. Morse, Natalie M. Barkey, Kevin N. Sill, Josef Vagner, Narges K. Tafreshi, Jonathan L. Sessler, Christian Preihs, Victor J. Hruby
  • Publication number: 20190177371
    Abstract: A backbone N-methylation approach on SHU9119, a non-selective cyclic peptide antagonist at hMC3R and hMC4R. Systematic N-methylated derivatives of SHU9119, with all possible backbone N-methylation combinations have been synthesized and examined for their binding and functional activities towards melanocortin receptor subtypes 1, 3, 4 and 5 (hMCRs). Several N-methylated analogues, which have selective and potent agonists or antagonists activity for the hMC1R or hMC5R or selective antagonist activity for the hMC3R, are discovered from the library. The selective hMC1R ligands show strong binding for human melanoma cells. The first universal antagonist for all subtypes of hMCRs will be of critical importance to modulate the melanocortin system with endogenous agonists.
    Type: Application
    Filed: February 21, 2019
    Publication date: June 13, 2019
    Inventors: Minying Cai, Victor J. Hruby
  • Publication number: 20190134018
    Abstract: The present invention provides a compound of the formula: wherein ring Z is a 5-, 6- or 7-membered ring; R1 is C1-10 alkyl, C1-10 haloalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heteroaralkyl; R2 is C1-10 alkylene; and Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(?O)—X1, wherein X1 is —OR3 or —NR4R5, where each of R3, R4 and R5 is H or C1-10 alkyl. The present invention also provides a method for using compound of Formula I to treat a wide variety of clinical conditions.
    Type: Application
    Filed: December 31, 2018
    Publication date: May 9, 2019
    Applicant: Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Ruben S. Vardanyan, Victor J. Hruby
  • Patent number: 10188704
    Abstract: A gamma-melanocyte stimulating hormone (?-MSH) derivative having improved stability, selectivity and bioavailabilty. The ?-MSH derivative is selective for the melanocortin-1 receptor (MC1 R) and is deliverable to skin cells via topical or transdermal delivery. The ?-MSH derivative is made up of naturally occurring amino acids for stimulating melanin from within for photoprotection of human skin against ultraviolet radiation damage.
    Type: Grant
    Filed: May 18, 2016
    Date of Patent: January 29, 2019
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Victor J. Hruby, Minying Cai