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).
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Patent number: 10807944Abstract: The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.Type: GrantFiled: March 30, 2015Date of Patent: October 20, 2020Assignees: University of Florida Research Foundation, Inc., The Scripps Research InstituteInventors: Daiqing Liao, William R. Roush, Ryan L. Stowe
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Patent number: 10723756Abstract: 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: GrantFiled: January 11, 2017Date of Patent: July 28, 2020Assignee: Innate Tumor Immunity Inc.Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
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Publication number: 20200181095Abstract: 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: ApplicationFiled: June 6, 2018Publication date: June 11, 2020Applicants: Florida Atlantic University Board of Trustees, The Scripps Research InstituteInventors: Gregg B. FIELDS, William R. ROUSH, Jun Yong CHOI, Rita FUERST
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Publication number: 20200172534Abstract: 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: ApplicationFiled: July 2, 2019Publication date: June 4, 2020Inventors: William R. Roush, Shankar Venkatraman, Gary Glick, Hans Martin Seidel
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Publication number: 20200163972Abstract: 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: ApplicationFiled: November 25, 2019Publication date: May 28, 2020Inventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
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Publication number: 20200165288Abstract: 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: ApplicationFiled: January 31, 2020Publication date: May 28, 2020Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
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Publication number: 20200157096Abstract: 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: ApplicationFiled: November 25, 2019Publication date: May 21, 2020Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Daniel O'Malley
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Publication number: 20200157097Abstract: 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: ApplicationFiled: December 5, 2019Publication date: May 21, 2020Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
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Publication number: 20200129500Abstract: The present invention provides compounds of Formula (I): (I) wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).Type: ApplicationFiled: July 12, 2018Publication date: April 30, 2020Inventors: Daniel O'Malley, Ashvinikumar V. Gavai, Patrice Gill, Christine M. Tarby, Scott Hunter Watterson, Hua Gong, David K. Williams, Shomir Ghosh, William R. Roush
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Patent number: 10603322Abstract: 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: GrantFiled: October 5, 2016Date of Patent: March 31, 2020Assignee: The Scripps Research InstituteInventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
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Patent number: 10604542Abstract: 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: GrantFiled: January 11, 2017Date of Patent: March 31, 2020Assignee: Innate Tumor Immunity, Inc.Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
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Patent number: 10556903Abstract: 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: GrantFiled: April 19, 2017Date of Patent: February 11, 2020Assignee: Innate Tumor Immunity, Inc.Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
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Patent number: 10533005Abstract: 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: GrantFiled: February 16, 2018Date of Patent: January 14, 2020Assignee: Innate Tumor Immunity, Inc.Inventors: Gary Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Daniel O'Malley
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Patent number: 10533007Abstract: 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: GrantFiled: April 19, 2017Date of Patent: January 14, 2020Assignee: Innate Tumor Immunity, Inc.Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush
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Patent number: 10485804Abstract: 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: GrantFiled: October 5, 2016Date of Patent: November 26, 2019Assignee: The Scripps Research InstituteInventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
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Publication number: 20190345191Abstract: 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: ApplicationFiled: August 31, 2017Publication date: November 14, 2019Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava, Roger Jones
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Publication number: 20190330228Abstract: 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: ApplicationFiled: June 13, 2019Publication date: October 31, 2019Inventors: Thomas D. Bannister, William R. Roush, Jun Yong Choi, Reji Nair, Andy S. Tsai, Jitendra K. Mishra, John L. Cleveland
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Patent number: 10329303Abstract: 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: GrantFiled: January 22, 2016Date of Patent: June 25, 2019Assignee: The Scripps Research InstituteInventors: Thomas D. Bannister, William R. Roush, Jun Yong Choi, Reji Nair, Andy S. Tsai, Jitendra K. Mishra, John L. Cleveland
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Publication number: 20190127368Abstract: 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: ApplicationFiled: April 19, 2017Publication date: May 2, 2019Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush
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Publication number: 20190127367Abstract: 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: ApplicationFiled: April 19, 2017Publication date: May 2, 2019Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James OIhava