Patents by Inventor Edward Holson

Edward Holson 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).

  • Publication number: 20230218632
    Abstract: The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as ?-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g.
    Type: Application
    Filed: March 19, 2021
    Publication date: July 13, 2023
    Applicant: Amathus Therapeutics, Inc.
    Inventors: Edward Holson, Charles Blum
  • Publication number: 20230174523
    Abstract: The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as ?-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g.
    Type: Application
    Filed: March 19, 2021
    Publication date: June 8, 2023
    Applicant: Amathus Therapeutics, Inc.
    Inventors: Edward Holson, Charles Blum
  • Publication number: 20230159509
    Abstract: The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as a-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g.
    Type: Application
    Filed: March 19, 2021
    Publication date: May 25, 2023
    Applicant: Amathus Therapeutics, Inc.
    Inventors: Edward Holson, Charles Blum
  • Publication number: 20230143552
    Abstract: The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
    Type: Application
    Filed: October 7, 2022
    Publication date: May 11, 2023
    Applicants: The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
  • Patent number: 11572368
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: February 7, 2023
    Assignees: The General Hospital Corporation, The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
  • Patent number: 11498896
    Abstract: The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
    Type: Grant
    Filed: March 20, 2020
    Date of Patent: November 15, 2022
    Assignees: The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
  • Patent number: 11377423
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein X1, X2, X3, X4, X5, W1, W2, W3, and W4 are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. In one aspect, the invention relates to selective HDAC3 inhibitors useful for protecting ?-cells and improving insulin resistance. The selective HDAC3 inhibitors are also useful for promoting cognitive function and enhancing learning and memory formation.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: July 5, 2022
    Assignees: The Broad Institute, Inc., The General Hospital Corporation
    Inventors: Edward Holson, Florence Fevrier Wagner, Stephen J. Haggarty, Yan-Ling Zhang, Morten Lundh, Bridget Wagner, Michael C. Lewis, Tracey Lynn Petryshen
  • Publication number: 20220160702
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Application
    Filed: June 10, 2021
    Publication date: May 26, 2022
    Applicants: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji
  • Publication number: 20220112216
    Abstract: The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).
    Type: Application
    Filed: October 22, 2021
    Publication date: April 14, 2022
    Applicants: The Broad Institute, Inc., Biogen MA Inc.
    Inventors: Florence Fevrier Wagner, Michel Weiwer, Arthur J. Campbell, Joshua R. Sacher, Edward Holson, Brian Stuart Lucas, TeYu Chen
  • Patent number: 11203601
    Abstract: The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).
    Type: Grant
    Filed: April 5, 2018
    Date of Patent: December 21, 2021
    Assignees: The Broad Institute, Inc., Biogen MA Inc.
    Inventors: Florence Fevrier Wagner, Michel Weiwer, Arthur J. Campbell, Joshua R. Sacher, Edward Holson, Brian Stuart Lucas, TeYu Chen
  • Patent number: 11052080
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: July 6, 2021
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji
  • Publication number: 20210177781
    Abstract: Aspects of the disclosure relate to compositions, kits, and methods for the treatment of cancer that utilize a selective histonc deacetylase 3 (HDAC3) inhibitor. In some aspects, the compositions, kits, and methods relate to use of a selective HDAC3 inhibitor in combination with an immunotherapy agent (e.g., an immune checkpoint inhibitor).
    Type: Application
    Filed: January 11, 2019
    Publication date: June 17, 2021
    Inventors: Edward Holson, Mariana Nacht
  • Publication number: 20210147355
    Abstract: The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
    Type: Application
    Filed: March 20, 2020
    Publication date: May 20, 2021
    Applicants: The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
  • Patent number: 10793538
    Abstract: The present invention provides compounds of formula (I): or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: October 6, 2020
    Assignee: The Broad Institute, Inc.
    Inventors: Edward Holson, Fanny Lazzaro, David Olson, Florence Fevrier Wagner, Michel Weiwer
  • Patent number: 10752588
    Abstract: The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: August 25, 2020
    Assignees: The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier, Michel Weiwer, Edward Scolnick, Michelle Palmer, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
  • Patent number: 10662199
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: May 26, 2020
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
  • Patent number: 10633336
    Abstract: The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and/or on the cAMP pathway.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: April 28, 2020
    Assignees: The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
  • Patent number: 10626438
    Abstract: The invention relates to a compound of Formula I: F1—X1-L1-X2—P1—X3-G1??(Formula I).
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: April 21, 2020
    Assignee: The Broad Institute, Inc.
    Inventors: Yan-Ling Zhang, Edward Holson, Florence F. Wagner
  • Publication number: 20200109154
    Abstract: The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).
    Type: Application
    Filed: April 5, 2018
    Publication date: April 9, 2020
    Applicants: The Broad Institute, Inc., Biogen MA Inc.
    Inventors: Florence Fevrier Wagner, Michel Weiwer, Arthur J. Campbell, Joshua R. Sacher, Edward Holson, Brian Stuart Lucas, TeYu Chen
  • Publication number: 20200061050
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.
    Type: Application
    Filed: November 21, 2018
    Publication date: February 27, 2020
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji