Patents by Inventor William R. Roush

William R. Roush 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: 10723756
    Abstract: This disclosure features chemical entities (e.g., a compound that modulates (e.g., agonizes) Stimulator of Interferon Genes (STING), or a pharmaceutically acceptable salt, and/or hydrate, and/or coccrystal, and/or drug combination of the compound) that are useful, e.g., for treating a condition, disease or disorder in which a decrease or increase in STING activity (e.g., a decrease, e.g., a condition, disease or disorder associated with repressed or impaired STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: July 28, 2020
    Assignee: Innate Tumor Immunity Inc.
    Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
  • Publication number: 20200181095
    Abstract: We describe the use of comparative structural analysis and structure-guided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metalloproteinase 13 (MMP-13). We applied a three-step process, starting with a comparative analysis of the X-ray crystallographic structure of compound 5 in complex with MMP-13 with published structures of known MMP-13 inhibitor complexes followed by molecular design and synthesis of potent, but non-selective zinc-chelating MMP inhibitors (e.g., 10a and 10b). After demonstrating that the pharmacophores of the chelating inhibitors (S)-10a, (R)-10a, and 10b were binding within the MMP-13 active site, the Zn2+ chelating unit was replaced with non-chelating polar residues that bridged over the Zn2+ binding site and reach into a solvent accessible area.
    Type: Application
    Filed: June 6, 2018
    Publication date: June 11, 2020
    Applicants: Florida Atlantic University Board of Trustees, The Scripps Research Institute
    Inventors: Gregg B. FIELDS, William R. ROUSH, Jun Yong CHOI, Rita FUERST
  • Publication number: 20200172534
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
    Type: Application
    Filed: July 2, 2019
    Publication date: June 4, 2020
    Inventors: William R. Roush, Shankar Venkatraman, Gary Glick, Hans Martin Seidel
  • Publication number: 20200163972
    Abstract: The invention provides a method of inhibiting casein kinase 1? (CK1?), comprising contacting the CK1? with a compound of formula (I) as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1? can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1? and ?-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
    Type: Application
    Filed: November 25, 2019
    Publication date: May 28, 2020
    Inventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
  • Publication number: 20200165288
    Abstract: This disclosure features chemical entities (e.g., a compound that modulates (e.g., agonizes) Stimulator of Interferon Genes (STING), or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that are useful, e.g., for treating a condition, disease or disorder in which a decrease or increase in STING activity (e.g., a decrease, e.g., a condition, disease or disorder associated with repressed or impaired STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Application
    Filed: January 31, 2020
    Publication date: May 28, 2020
    Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
  • Publication number: 20200157097
    Abstract: This disclosure features compounds of Formula I, or a pharmaceutically acceptable salt thereof: in which R1, R2, R3, and R4 are as defined herein. These compounds are modulators of NLRP3, which are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 activity (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Application
    Filed: December 5, 2019
    Publication date: May 21, 2020
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
  • Publication number: 20200157096
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonizes or partially agonizes) NLRP3 that are useful, e.g., for treating a condition, disease or disorder in which an increase in NLRP3 signaling may correct a deficiency in innate immune activity (e.g., a condition, disease or disorder associated with an insufficient immune response) that contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Application
    Filed: November 25, 2019
    Publication date: May 21, 2020
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Daniel O'Malley
  • Patent number: 10604542
    Abstract: This disclosure features dinucleotide compounds that modulate Stimulator of Interferon Genes (STING) activity, for use for example in the treatment of cancer. This disclosure also features compositions as well as other methods of using and making the same (Formula (A)). A and B are each independently selected from the group consisting of Formulae (i), (ii), (iii), and (iv).
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: March 31, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
  • Patent number: 10603322
    Abstract: The invention provides a method of inhibiting casein kinase 1? (CK1?), comprising contacting the CK1? with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1? can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1? and ?-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: March 31, 2020
    Assignee: The Scripps Research Institute
    Inventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
  • Patent number: 10556903
    Abstract: This disclosure features compounds of Formula I, or a pharmaceutically acceptable salt thereof: in which R1, R2, R3, and R4 are as defined herein. These compounds are modulators of NLRP3, which are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 activity (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: February 11, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
  • Patent number: 10533005
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonizes or partially agonizes) NLRP3 that are useful, e.g., for treating a condition, disease or disorder in which an increase in NLRP3 signaling may correct a deficiency in innate immune activity (e.g., a condition, disease or disorder associated with an insufficient immune response) that contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: February 16, 2018
    Date of Patent: January 14, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Daniel O'Malley
  • Patent number: 10533007
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonize or partially agonize) NLRP3 and TLR7 and/or TLR8 that are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 and TLR7 and/or TLR8 activities (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 and TLR7 and/or TLR8 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: January 14, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush
  • Patent number: 10485804
    Abstract: The invention provides a method of inhibiting casein kinase 1? (CK1?), comprising contacting the CK1? with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1? can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1? and ?-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: November 26, 2019
    Assignee: The Scripps Research Institute
    Inventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
  • Publication number: 20190345191
    Abstract: This disclosure features chemical entities (e.g., a compound that modulates (e.g., agonizes or partially agonizes) Stimulator of Interferon Genes (STING), or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that are useful, e.g., for treating a condition, disease or disorder in which a decrease or increase in STING activity (e.g., a decrease, e.g., a condition, disease or disorder associated with repressed or impaired STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Application
    Filed: August 31, 2017
    Publication date: November 14, 2019
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Roger Jones
  • Publication number: 20190330228
    Abstract: The invention provides compounds that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.
    Type: Application
    Filed: June 13, 2019
    Publication date: October 31, 2019
    Inventors: Thomas D. Bannister, William R. Roush, Jun Yong Choi, Reji Nair, Andy S. Tsai, Jitendra K. Mishra, John L. Cleveland
  • Patent number: 10329303
    Abstract: The invention provides compounds that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: June 25, 2019
    Assignee: The Scripps Research Institute
    Inventors: Thomas D. Bannister, William R. Roush, Jun Yong Choi, Reji Nair, Andy S. Tsai, Jitendra K. Mishra, John L. Cleveland
  • Publication number: 20190127368
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonize or partially agonize) NLRP3 and TLR7 and/or TLR8 that are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 and TLR7 and/or TLR8 activities (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 and TLR7 and/or TLR8 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Application
    Filed: April 19, 2017
    Publication date: May 2, 2019
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush
  • Publication number: 20190127367
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonizes or partially agonizes) NLRP3 that are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 activity (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Application
    Filed: April 19, 2017
    Publication date: May 2, 2019
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James OIhava
  • Publication number: 20190119203
    Abstract: In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured: Formulae (I) and (II), wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.
    Type: Application
    Filed: April 18, 2017
    Publication date: April 25, 2019
    Inventors: Gary Glick, Shomir Ghosh, William R. Roush
  • Publication number: 20190119241
    Abstract: In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
    Type: Application
    Filed: April 18, 2017
    Publication date: April 25, 2019
    Inventors: Gary Glick, Shomir Ghosh, William R. Roush, Dong-Ming Shen