Patents by Inventor Stephen W. Fesik

Stephen W. Fesik 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: 12144816
    Abstract: The present disclosure provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present disclosure also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Grant
    Filed: December 9, 2022
    Date of Patent: November 19, 2024
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, James C. Tarr, KyuOk Jeon, James M. Salovich, Subrata Shaw, Nagarathanam Veerasamy, Kwangho Kim, Plamen P. Christov, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik, Zhiguo Bian
  • Patent number: 12060367
    Abstract: 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: Grant
    Filed: May 9, 2023
    Date of Patent: August 13, 2024
    Assignees: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, VANDERBILT UNIVERSITY
    Inventors: 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
  • Publication number: 20240262822
    Abstract: Isoquinolinone compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
    Type: Application
    Filed: May 6, 2022
    Publication date: August 8, 2024
    Inventors: Taekyu Lee, Kevin B. Teuscher, Somenath Chowdhury, Jianhua Tian, Kenneth M. Meyers, Stephen W. Fesik
  • Patent number: 11999716
    Abstract: Isoquinolinone compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
    Type: Grant
    Filed: October 24, 2019
    Date of Patent: June 4, 2024
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, Joseph R. Alvarado, Jianhua Tian, Kenneth M. Meyers, Changho Han, Jonathan J. Mills, Kevin B. Teuscher, Shaun R. Stauffer, Stephen W. Fesik, Rocco D. Gogliotti
  • Publication number: 20240174690
    Abstract: 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: Application
    Filed: May 9, 2023
    Publication date: May 30, 2024
    Inventors: 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
  • Publication number: 20230330099
    Abstract: The present disclosure provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present disclosure also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Application
    Filed: December 9, 2022
    Publication date: October 19, 2023
    Inventors: Taekyu Lee, James C. Tarr, KyuOk Jeon, James M. Salovich, Subrata Shaw, Nagarathanam Veerasamy, Kwangho Kim, Plamen P. Christov, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik, Zhiguo Bian
  • Publication number: 20230227470
    Abstract: 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: Application
    Filed: November 30, 2022
    Publication date: July 20, 2023
    Inventors: 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
  • Publication number: 20230212164
    Abstract: 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: Application
    Filed: June 1, 2021
    Publication date: July 6, 2023
    Inventors: 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
  • Patent number: 11596639
    Abstract: The present disclosure provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present disclosure also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: March 7, 2023
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, James C. Tarr, KyuOk Jeon, James M. Salovich, Subrata Shaw, Nagarathanam Veerasamy, Kwangho Kim, Plamen P. Christov, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik, Zhiguo Bian
  • Publication number: 20230039309
    Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Application
    Filed: November 4, 2021
    Publication date: February 9, 2023
    Inventors: Taekyu Lee, Zhiguo Bian, Johannes Belmar, Plamen P. Christov, Nicholas F. Pelz, Subrata Shaw, Kwangho Kim, James C. Tarr, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik
  • Publication number: 20230026466
    Abstract: Isoquinolmone compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
    Type: Application
    Filed: November 8, 2020
    Publication date: January 26, 2023
    Inventors: Taekyu Lee, Kevin B. Teuscher, Jianhua Tian, Kenneth M. Meyers, Somenath Chowdhury, Stephen W. Fesik
  • Publication number: 20230012362
    Abstract: Isoquinolinone compounds and derivatives inhibit WDRS and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
    Type: Application
    Filed: October 24, 2019
    Publication date: January 12, 2023
    Inventors: Taekyu Lee, Joseph R. Alvarado, Jianhua Tian, Kenneth M. Meyers, Changho Han, Jonathan J. Mills, Kevin B. Teuscher, Shaun R. Stauffer, Stephen W. Fesik
  • Publication number: 20220289673
    Abstract: Substituted N-phenyl 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: Application
    Filed: July 29, 2020
    Publication date: September 15, 2022
    Inventors: William P. Tansey, Stephen W. Fesik, Shaun R. Stauffer, Alex G. Waterson, Changho Han, Joseph R. Alvarado, Jonathan D. MacDonald, Selena Chacon Simon, Sameer S. Nikhar, Alexey Kuznetsov
  • Publication number: 20220242849
    Abstract: Quinazolin-4(3H)-one, 2,3-dihydroquinazolin-4(1H)-one, 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one, and 3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
    Type: Application
    Filed: June 4, 2020
    Publication date: August 4, 2022
    Inventors: Taekyu Lee, Changho Han, Jonathan J. Mills, Kevin B. Teuscher, Jianhua Tian, Kenneth M. Meyers, Somenath Chowdhury, Stephen W. Fesik
  • Patent number: 11318137
    Abstract: The present invention relates to quinazoline compounds and compositions that modulate Ras signaling. Compounds and compositions of the present invention are useful in the treatment of cancers and other disease states associated with Ras dysfunction (e.g., Ras-associated autoimmune leukoproliferative disorder, or certain types of mitochondrial dysfunction) in a subject, for example a mammal or a human.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: May 3, 2022
    Assignee: Vanderbilt University
    Inventors: Alex G. Waterson, Jason R. Abbott, J. Phillip Kennedy, Stephen W. Fesik, Qi Sun, Jason Phan, Michael C. Burns, Pratiq Patel
  • Patent number: 11208415
    Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Grant
    Filed: November 19, 2019
    Date of Patent: December 28, 2021
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, Zhiguo Bian, Johannes Belmar, Plamen P. Christov, Nicholas F. Pelz, Subrata Shaw, Kwangho Kim, James C. Tarr, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik
  • Publication number: 20210283138
    Abstract: The present disclosure provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present disclosure also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Application
    Filed: March 3, 2017
    Publication date: September 16, 2021
    Inventors: Taekyu Lee, James C. Tarr, KyuOk Jeon, James M. Salovich, Subrata Shaw, Nagarathanam Veerasamy, Kwangho Kim, Plamen P. Christov, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik, Zhiguo Bian
  • Patent number: 10954193
    Abstract: The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.
    Type: Grant
    Filed: May 10, 2018
    Date of Patent: March 23, 2021
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, Kwangho Kim, Plamen P. Christov, Johannes Belmar, Jason P. Burke, Edward T. Olejniczak, Stephen W. Fesik
  • Patent number: 10844044
    Abstract: Described are imino-azacycle-benzamide compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: November 24, 2020
    Assignee: Vanderbilt University
    Inventors: Joseph R. Alvarado, Shaun R. Stauffer, Rocco D. Gogliotti, Changho Han, Kenneth M. Meyers, Jianhua Tian, Jonathan D. Macdonald, Stephen W. Fesik, Taekyu Lee
  • Patent number: 10844032
    Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: November 24, 2020
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, Nicholas F. Pelz, Johannes Belmar, Zhiguo Bian, Edward T. Olejniczak, Stephen W. Fesik, Brian A. Chauder