Patents by Inventor Paul J. Hergenrother

Paul J. Hergenrother 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: 20210017165
    Abstract: Disclosed herein are antibacterial compounds that accumulate in Gram-negative bacteria, methods of preparing the compounds, and methods of using the compounds to inhibit or kill microbes, and methods of treating microbial infections, such as Gram-negative bacterial infections. Compounds selected for conversion to potential Gram-negative antibacterial compounds were identified based on compounds having low globularity and low flexibility. Amine substituents were then strategically added to the selected compounds to provide compounds having antibacterial activity against Gram-negative bacteria.
    Type: Application
    Filed: March 11, 2019
    Publication date: January 21, 2021
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Emily Jane GEDDES, Bryon Shane DROWN, Stephen E. MOTIKA, Erica Nicole PARKER
  • Patent number: 10888560
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: January 12, 2021
    Assignees: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc.
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Howard S. Roth, Theodore M. Tarasow
  • Publication number: 20210002286
    Abstract: New synthetic methods to provide access to previously unexplored functionality at the C8 position of imidazotetrazines. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM.
    Type: Application
    Filed: September 10, 2020
    Publication date: January 7, 2021
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Timothy M. Fan, Riley L. Svec
  • Patent number: 10874666
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: December 29, 2020
    Assignees: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc., The Johns Hopkins University
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Avadhut Joshi, Gregory J. Riggins, Theodore M. Tarasow
  • Patent number: 10800730
    Abstract: The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: October 13, 2020
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Robert W. Huigens, III, Karen C. Morrison, Robert W. Hicklin, II, Timothy A. Flood, Jr.
  • Publication number: 20200276189
    Abstract: The discovery of mutant or fusion kinases that drive oncogenesis, and the subsequent approval of specific inhibitors for these enzymes, has been instrumental in the management of some cancers. However, acquired resistance remains a significant problem in the clinic, limiting the long-term effectiveness of most of these drugs. Herein is demonstrated a strategy to overcome this resistance through drug-induced MEK cleavage (via direct procaspase-3 activation) combined with targeted kinase inhibition. This combination effect is shown to be general across diverse tumor histologies (melanoma, lung cancer, and leukemia) and driver mutations (mutant BRAF or EGFR, fusion kinases EML4-ALK and BCR-ABL). Caspase-3-mediated degradation of MEK kinases results in sustained pathway inhibition and substantially delayed or eliminated resistance in cancer cells in a manner superior to combinations with MEK inhibitors.
    Type: Application
    Filed: November 16, 2018
    Publication date: September 3, 2020
    Applicant: The Board of Teustrrs of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Jessie PEH, Matthew BOUDREAU
  • Publication number: 20200190029
    Abstract: A set of small molecules ER? biomodulators that kill therapy-resistant ER? positive breast, ovarian, and endometrial cancer cells. These small molecules have increased therapeutic potential because of an increased ability to kill therapy-resistant breast cancer cells compared to BHPI and other conventional therapies (endocrine therapies, tamoxifen and fulvestrant/ICI). The new compounds do not only inhibit proliferation of the cancer cells but actually kills them, which prevents reactivation of tumors years later.
    Type: Application
    Filed: February 26, 2020
    Publication date: June 18, 2020
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: David J. SHAPIRO, Paul J. Hergenrother, Matthew W. Boudreau
  • Publication number: 20200123173
    Abstract: Inhibitors of human topoisomerase II (Top2) are the backbone of numerous cancer chemotherapy regimens. Unfortunately, the onset of toxicity severely limits the utility of these powerful drugs. There is some conservation between human Top2 and bacterial homologues (DNA gyrase and TopoIV). Thus, the conversion of antibacterial topoisomerase inhibitors into antineoplastic agents is an intriguing strategy for anticancer compounds. Herein is described the conversion of deoxynybomycin (DNM), a natural product and DNA gyrase inhibitor with minimal cytotoxicity, into a compound that has anticancer activity. Detailed in vitro and cell culture experiments demonstrate that these compounds inhibit Top2 and also act upon topoisomerase I. Similar approaches are applicable to other classes of gyrase inhibitors and other antibacterial targets for discovery of new anticancer drugs.
    Type: Application
    Filed: June 21, 2018
    Publication date: April 23, 2020
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Paul J. HERGENROTHER, Andrew P. RILEY
  • Patent number: 10576096
    Abstract: The therapies described herein can be selectively lethal toward a variety of different cancer cell types and cancer conditions in a subject. The combination therapies described herein can be useful for the management, treatment, control, or adjunct treatment of diseases, where the selective legality is beneficial in chemotherapeutic therapy, particularly where the disease is accompanied by elevated levels of NQO1.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: March 3, 2020
    Assignees: The Board of Regents of the University of Texas System, The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Lifen Cao, Jinming Gao, Xiumei Huang, Xiuquan Luo, Xinpeng Ma, Zachary R. Moore, Elizabeth I. Parkinson
  • Patent number: 10525056
    Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: January 7, 2020
    Assignee: The Board of Trustees of the University of Illinois
    Inventor: Paul J. Hergenrother
  • Publication number: 20190358229
    Abstract: Compositions and methods for the induction of cancer cell death. The compositions and methods of using them include use of compositions in therapy for the treatment of cancer and for the selective induction of apoptosis in cancer cells. The drug combinations described herein can be synergistic and can have lower neurotoxicity effects than the same amounts of other compounds and combinations of compounds and can be effective when a particular cancer has become resistant to previously administered therapies.
    Type: Application
    Filed: June 10, 2019
    Publication date: November 28, 2019
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Jessie PEH
  • Patent number: 10350207
    Abstract: The invention provides compositions and methods for the induction of cancer cell death. The compositions and methods of using them include use of compositions in therapy for the treatment of cancer and for the selective induction of apoptosis in cancer cells. The drug combinations described herein can be synergistic and can have lower neurotoxicity effects than the same amounts of other compounds and combinations of compounds, and can be effective when a particular cancer has become resistant to previously administered therapies.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: July 16, 2019
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Jessie Peh
  • Publication number: 20190201394
    Abstract: Compositions and methods relating to induction of cell death such as in cancer cells are disclosed. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds in connection with modification of procaspases such as procaspase-3 are disclosed. In various embodiments, the compounds and compositions are capable of activation of procaspase-3.
    Type: Application
    Filed: December 21, 2018
    Publication date: July 4, 2019
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Karson S. Putt, Quinn P. Peterson, Valerie Fako
  • Publication number: 20190152891
    Abstract: The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.
    Type: Application
    Filed: September 20, 2018
    Publication date: May 23, 2019
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Robert W. Huigens, III, Karen C. Morrison, Robert W. Hicklin, II, Timothy A. Flood
  • Patent number: 10285986
    Abstract: Compositions comprising Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compositions are useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: May 14, 2019
    Assignees: The Board of Trustees of the University of Illinois, The Board of Regents of the University of Texas System
    Inventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Rahul Palchaudhuri, Elizabeth I. Parkinson
  • Publication number: 20190135821
    Abstract: Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
    Type: Application
    Filed: March 13, 2017
    Publication date: May 9, 2019
    Inventors: Paul J. HERGENROTHER, Michelle Richter, Andrew Riley, Bryon Drown, Martin Chavez, Sarah Tasker, Alfredo Garcia
  • Patent number: 10272099
    Abstract: The therapies described herein can be selectively lethal toward a variety of different cancer cell types and cancer conditions in a subject. The combination therapies described herein can be useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy, particularly where the disease is accompanied by elevated levels of NQO1.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: April 30, 2019
    Assignees: The Board of Regents of the University of Texas System, The Board of Trustees of the University of Illinois.
    Inventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Lifen Cao, Jinming Gao, Xiumei Huang, Xiuquan Luo, Xinpeng Ma, Zachary R. Moore, Elizabeth I. Parkinson
  • Publication number: 20190099419
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Application
    Filed: October 1, 2018
    Publication date: April 4, 2019
    Applicants: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc., The Johns Hopkins University
    Inventors: Paul J. HERGENROTHER, Rachel C. BOTHAM, Timothy M. FAN, Mark J. GILBERT, Michael K. HANDLEY, Avadhut JOSHI, Gregory J. RIGGINS, Theodore M. TARASOW
  • Publication number: 20190099418
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Application
    Filed: October 1, 2018
    Publication date: April 4, 2019
    Applicants: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc.
    Inventors: Paul J. HERGENROTHER, Rachel C. BOTHAM, Timothy M. FAN, Mark J. GILBERT, Michael K. HANDLEY, Howard S. ROTH, Theodore M. TARASOW
  • Patent number: 10220099
    Abstract: The synthesis of various pyrazino[1?,2?:1,5]pyrrolo[2,3-b]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-c: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R4-R8, R3?, R6?, and n are as defined herein, are provided. These biologically active derivatives have been further used to prepare cell-specific drug conjugates effective in treating various diseases including cancer.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: March 5, 2019
    Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of Illinois
    Inventors: Mohammad Movassaghi, Justin Kim, Paul J. Hergenrother, Karen Morrison, Nicolas Boyer