Patents by Inventor Saul Jaime-Figueroa

Saul Jaime-Figueroa 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: 11986531
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: July 28, 2021
    Date of Patent: May 21, 2024
    Assignees: Arvinas Operations, Inc., Yale University
    Inventors: Andrew P. Crew, Keith R. Hornberger, Jing Wang, Saul Jaime-Figueroa, Hanqing Dong, Kurt Zimmermann, Craig M. Crews
  • Patent number: 11834460
    Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Grant
    Filed: December 17, 2021
    Date of Patent: December 5, 2023
    Assignee: YALE UNIVERSITY
    Inventors: Craig M. Crews, George Burslem, Philipp M. Cromm, Saul Jaime-Figueroa, Momar Toure
  • Publication number: 20230000994
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
    Type: Application
    Filed: July 28, 2021
    Publication date: January 5, 2023
    Inventors: Andrew P. Crew, Keith R. Hornberger, Jing Wang, Saul Jaime-Figueroa, Hanqing Dong, Lawrence B. Snyder
  • Publication number: 20220112211
    Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Application
    Filed: December 17, 2021
    Publication date: April 14, 2022
    Inventors: Craig M. CREWS, George BURSLEM, Philipp M. CROMM, Saul JAIME-FIGUEROA, Momar TOURE
  • Patent number: 11220515
    Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Grant
    Filed: January 26, 2019
    Date of Patent: January 11, 2022
    Assignee: Yale University
    Inventors: Craig M. Crews, George Burslem, Philipp M. Cromm, Saul Jaime-Figueroa, Momar Toure
  • Patent number: 11173211
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: September 7, 2019
    Date of Patent: November 16, 2021
    Assignees: ARVINAS OPERATIONS, INC., YALE UNIVERSITY
    Inventors: Andrew P. Crew, Keith R. Hornberger, Jing Wang, Saul Jaime-Figueroa, Hanqing Dong
  • Publication number: 20210284606
    Abstract: The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1 R5, R6 and R7 are as defined herein.
    Type: Application
    Filed: May 24, 2021
    Publication date: September 16, 2021
    Applicant: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Publication number: 20210220475
    Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.
    Type: Application
    Filed: March 4, 2021
    Publication date: July 22, 2021
    Inventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
  • Patent number: 11028088
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: June 8, 2021
    Assignee: Yale University
    Inventors: Craig M. Crews, Saul Jaime-Figueroa, Momar Toure
  • Patent number: 10994015
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: May 4, 2021
    Assignees: ARVINAS OPERATIONS, INC., YALE UNIVERSITY
    Inventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
  • Publication number: 20200325130
    Abstract: The present invention includes novel compounds and methods for preventing or treating diseases associated with and/or caused by overexpression and/or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: April 14, 2020
    Publication date: October 15, 2020
    Inventors: Craig CREWS, Momar TOURE, Eunhwa KO, Saul JAIME-FIGUEROA
  • Patent number: 10723717
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: July 28, 2020
    Assignees: ARVINAS OPERATIONS, INC., YALE UNIVERSITY
    Inventors: Andrew P. Crew, Keith R. Hornberger, Jing Wang, Hanqing Dong, Yimin Qian, Craig M. Crews, Saul Jaime-Figueroa
  • Publication number: 20200181154
    Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 12, 2020
    Publication date: June 11, 2020
    Applicant: Genentech, Inc.
    Inventors: Roland J. BILLEDEAU, James J. CRAWFORD, Saul JAIME-FIGUEROA, Wendy LEE, Francisco Javier LOPEZ-TAPIA, Sung-Sau SO
  • Publication number: 20200129627
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
    Type: Application
    Filed: September 7, 2019
    Publication date: April 30, 2020
    Inventors: ANDREW P. CREW, Keith R. Hornberger, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, Hanqing Dong, Yimin Qian, Kurt Zimmermann
  • Publication number: 20200121684
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
    Type: Application
    Filed: August 29, 2019
    Publication date: April 23, 2020
    Inventors: Craig M. Crews, Saul Jaime-Figueroa, Momar Toure
  • Publication number: 20200115333
    Abstract: The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1 R5, R6 and R7 are as defined herein.
    Type: Application
    Filed: December 5, 2019
    Publication date: April 16, 2020
    Applicant: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Publication number: 20190276459
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
    Type: Application
    Filed: March 8, 2019
    Publication date: September 12, 2019
    Inventors: Craig M. Crews, Saul Jaime-Figueroa, Momar Toure
  • Publication number: 20190233433
    Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Application
    Filed: January 26, 2019
    Publication date: August 1, 2019
    Inventors: Craig M. CREWS, George BURSLEM, Philipp M. CROMM, Saul JAIME-FIGUEROA, Momar TOURE
  • Publication number: 20190194209
    Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Applicant: Genentech, Inc.
    Inventors: Roland J. BILLEDEAU, James J. CRAWFORD, Saul JAIME-FIGUEROA, Wendy LEE, Francisco Javier LOPEZ-TAPIA, Sung-Sau SO
  • Publication number: 20180353501
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of c-Met and/or p38 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Application
    Filed: June 1, 2018
    Publication date: December 13, 2018
    Inventors: Andrew P. Crew, Hanqing Dong, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa