Patents by Inventor Alex Waterson
Alex Waterson 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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Publication number: 20240174690Abstract: The present invention encompasses compounds of formula (I) wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.Type: ApplicationFiled: May 9, 2023Publication date: May 30, 2024Inventors: Joachim BROEKER, Jason ABBOTT, Jianwen CUI, Stephen W. FESIK, Julian FUCHS, Andreas GOLLNER, Lorenz HERDEIS, Tim HODGES, Andrew LITTLE, Andreas MANTOULIDIS, Jason PHAN, Juergen RAMHARTER, Dhruba SARKAR, Christian Alan Paul SMETHURST, Kevin SOKOL, Heinz STADTMUELLER, Qi SUN, Matthias TREU, Alex WATERSON, Birgit WILDING, Tobias WUNBERG
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Patent number: 11945812Abstract: The present invention encompasses compounds of formula (I) wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.Type: GrantFiled: June 1, 2021Date of Patent: April 2, 2024Assignees: Boehringer Ingelheim International GmbH, Vanderbilt UniversityInventors: Jason Abbott, Joachim Broeker, Jianwen Cui, Steve W. Fesik, Andreas Gollner, Tim Hodges, Jale Karolyi-Oezguer, Andrew Little, Andreas Mantoulidis, Jason Phan, Dhruba Sarkar, Christian Alan Paul Smethurst, Qi Sun, Matthias Treu, Alex Waterson
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TREATING PRIMARY OR IDIOPATHIC HYPEROXALURIA WITH SMALL MOLECULE INHIBITORS OF LACTATE DEHYDROGENASE
Publication number: 20230372308Abstract: The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amount of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.Type: ApplicationFiled: July 14, 2023Publication date: November 23, 2023Inventors: Matthew HALL, Daniel J. URBAN, John KNIGHT, Ross HOLMES, Kyle David WOOD, Alex WATERSON, Victor M. DARLEY-USMAR, Leonard M. NECKERS -
Treating primary or idiopathic hyperoxaluria with small molecule inhibitors of lactate dehydrogenase
Patent number: 11752138Abstract: The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amound of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.Type: GrantFiled: May 17, 2021Date of Patent: September 12, 2023Assignees: VANDERBILT UNIVERSITY, THE UAB RESEARCH FOUNDATION, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Matthew Hall, Daniel J. Urban, John Knight, Ross Holmes, Kyle David Wood, Alex Waterson, Victor M. Darley-Usmar, Leonard M. Neckers -
Publication number: 20230227470Abstract: The present invention encompasses compounds of formula (I) wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.Type: ApplicationFiled: November 30, 2022Publication date: July 20, 2023Inventors: Joachim BROEKER, Jason ABBOTT, Jianwen CUI, Stephen W. FESIK, Julian FUCHS, Andreas GOLLNER, Lorenz HERDEIS, Tim HODGES, Andrew LITTLE, Andreas MANTOULIDIS, Jason PHAN, Juergen RAMHARTER, Dhruba SARKAR, Christian Alan Paul SMETHURST, Kevin SOKOL, Heinz STADTMUELLER, Qi SUN, Matthias TREU, Alex WATERSON, Birgit WILDING, Tobias WUNBERG
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Publication number: 20230212164Abstract: The present invention encompasses compounds of formula (I), wherein R1a, R1b, R2a, R2b, Z, R3, R5, A, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.Type: ApplicationFiled: June 1, 2021Publication date: July 6, 2023Inventors: Jason ABBOTT, Joachim BROEKER, Jianwen CUI, Stephen W. FESIK, Andreas GOLLNER, Tim HODGES, Jale KAROLYI-OEZGUER, Andrew LITTLE, Andreas MANTOULIDIS, Jason PHAN, Dhruba SARKAR, Christian Alan Paul SMETHURST, Qi SUN, Matthias TREU, Alex WATERSON
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Publication number: 20230022304Abstract: Substituted N-heteroaryl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject such as cancer cell proliferation.Type: ApplicationFiled: November 18, 2020Publication date: January 26, 2023Inventors: Selena Chacon Simon, Alex Waterson, Jonathan D. MacDonald, Stephen Fesik, Shaun R. Stauffer, William P. Tansey
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Publication number: 20210380574Abstract: The present invention encompasses compounds of formula (I) wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.Type: ApplicationFiled: June 1, 2021Publication date: December 9, 2021Inventors: Jason ABBOTT, Joachim BROEKER, Jianwen CUI, Steve W. FESIK, Andreas GOLLNER, Tim HODGES, Jale KAROLYI-OEZGUER, Andrew LITTLE, Andreas MANTOULIDIS, Jason PHAN, Dhruba SARKAR, Christian Alan Paul SMETHURST, Qi SUN, Matthias TREU, Alex WATERSON
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TREATING PRIMARY OR IDIOPATHIC HYPEROXALURIA WITH SMALL MOLECULE INHIBITORS OF LACTATE DEHYDROGENASE
Publication number: 20210369683Abstract: The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amound of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.Type: ApplicationFiled: May 17, 2021Publication date: December 2, 2021Inventors: Matthew Hall, Daniel J. Urban, John Knight, Ross Holmes, Kyle David Wood, Alex Waterson, Victor M. Darley-Usmar, Leonard M. Neckers -
Patent number: 10501421Abstract: Benzimidazole compounds that increase the rate of SOS-mediated nucleotide exchange on Ras by binding to a functionally relevant, chemically tractable pocket on the SOS protein, as part of the Ras:SOS:Ras complex.Type: GrantFiled: January 27, 2017Date of Patent: December 10, 2019Assignee: Vanderbilt UniversityInventors: Steve Fesik, Alex Waterson, Michael Burns, Qi Sun, Jason Phan, James M. Salovich, Jason R. Abbott, Andrew Little
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Patent number: 10045966Abstract: Embodiments of the presently-disclosed subject matter include activators of HssRS that induce endogenous heme biosynthesis by perturbing central metabolism. These molecules are toxic to fermenting S. aureus, including clinically relevant small colony variants (SCVs). The utility of targeting fermenting bacteria is exemplified by the fact that this compound prevents the emergence of antibiotic resistance, enhances phagocyte killing, and reduces S. aureus pathogenesis. This small molecule is a powerful tool not only for studying bacterial heme biosynthesis and central metabolism, but also establishes targeting of fermentation as a viable antibacterial strategy.Type: GrantFiled: April 21, 2017Date of Patent: August 14, 2018Assignee: Vanderbilt UniversityInventors: Eric P. Skaar, Laura Anzaldi Mike, Gary Sulikowski, Alex Waterson, Paul Reid
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Patent number: 9867879Abstract: A method for treating a microbial infection involves administering an effective amount of a compound of the formula: wherein R1 is H, alkyl, aryl, heteroaryl, R2 is H, halogen, alkyl, aryl, heteroaryl, R3 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R4 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R5 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R6 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R7 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R8 is —CR3, O, S, wherein R5 and R6, R7 and R6, R5 and R4, R4 and R3 can cyclize forming a 3-10 member ring comprising C, O, S, and/or N optionally substituted with one or more R3; and administering light therapy, such as a photodynamic therapy (PDT) light source.Type: GrantFiled: January 22, 2016Date of Patent: January 16, 2018Assignee: Vanderbilt UniversityInventors: Eric P. Skaar, Matthew Surdel, Gary A. Sulikowski, Brendan Dutter, Paul Reid, Alex Waterson
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Publication number: 20170246149Abstract: Embodiments of the presently-disclosed subject matter include activators of HssRS that induce endogenous heme biosynthesis by perturbing central metabolism. These molecules are toxic to fermenting S. aureus, including clinically relevant small colony variants (SCVs). The utility of targeting fermenting bacteria is exemplified by the fact that this compound prevents the emergence of antibiotic resistance, enhances phagocyte killing, and reduces S. aureus pathogenesis. This small molecule is a powerful tool not only for studying bacterial heme biosynthesis and central metabolism, but also establishes targeting of fermentation as a viable antibacterial strategy.Type: ApplicationFiled: April 21, 2017Publication date: August 31, 2017Inventors: Eric P. Skaar, Laura Anzaldi Mike, Gary Sulikowski, Alex Waterson, Paul Reid
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Publication number: 20160213780Abstract: A method for treating a microbial infection involves administering an effective amount of a compound of the formula: wherein R1 is H, alkyl, aryl, heteroaryl, R2 is H, halogen, alkyl, aryl, heteroaryl, R3 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R4 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R5 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R6 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R7 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R8 is —CR3, O, S, wherein R5 and R6, R7 and R6, R5 and R4, R4 and R3 can cyclize forming a 3-10 member ring comprising C, O, S, and/or N optionally substituted with one or more R3; and administering light therapy, such as a photodynamic therapy (PDT) light source.Type: ApplicationFiled: January 22, 2016Publication date: July 28, 2016Inventors: Eric P. Skaar, Matthew Surdel, Gary A. Sulikowski, Brendan Dutter, Paul Reid, Alex Waterson
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Publication number: 20150174130Abstract: Embodiments of the presently-disclosed subject matter include activators of HssRS that induce endogenous heme biosynthesis by perturbing central metabolism. These molecules are toxic to fermenting S. aureus, including clinically relevant small colony variants (SCVs). The utility of targeting fermenting bacteria is exemplified by the fact that this compound prevents the emergence of antibiotic resistance, enhances phagocyte killing, and reduces S. aureus pathogenesis. This small molecule is a powerful tool not only for studying bacterial heme biosynthesis and central metabolism, but also establishes targeting of fermentation as a viable antibacterial strategy.Type: ApplicationFiled: July 26, 2013Publication date: June 25, 2015Inventors: Eric P. Skaar, Laura Anzaldi, Gary Sulikowski, Alex Waterson, Paul Reid
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Publication number: 20080051395Abstract: The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.Type: ApplicationFiled: December 6, 2005Publication date: February 28, 2008Inventors: David Uehling, Kirk Stevens, Scott Dickerson, Alex Waterson, Philip Harris, Douglas Sammond, Robert Hubbard, Holly Emerson, Joseph Wilson
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Publication number: 20060205740Abstract: The present invention discloses pyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such pyrimidine derivatives are useful in the treatment of diseases associated with inappropriate ErbB family kinase.Type: ApplicationFiled: August 11, 2004Publication date: September 14, 2006Inventors: Michael Reno, Kirk Stevens, Alex Waterson, Yuemei Zhang