Patents by Inventor Stephen J. Haggarty

Stephen J. Haggarty 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: 20240091213
    Abstract: Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
    Type: Application
    Filed: May 23, 2023
    Publication date: March 21, 2024
    Applicants: DANA-FARBER CANCER INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION d/b/a MASSACHUSETTS GENERAL HOSPITAL
    Inventors: Nathanael S. Gray, Stephen J. Haggarty, Quan Cai, Tinghu Zhang, Maria Catarina Telo Baptista Lima da Silva, Fleur M. Ferguson
  • Publication number: 20230227852
    Abstract: Methods, systems, compositions and strategies for the use of ARMM-mediated delivery of molecules (e.g., biological molecules, small molecules, proteins, and nucleic acids (e.g., DNA, RNA), DNA plasmids shRNA, mRNA) to cells of the nervous system (e.g., central nervous system and peripheral nervous system).
    Type: Application
    Filed: June 11, 2021
    Publication date: July 20, 2023
    Applicants: President and Fellows of Harvard College, The General Hospital Corporation, Vesigen, Inc.
    Inventors: Quan Lu, Stephen J. Haggarty, Robert Millman
  • Publication number: 20230226195
    Abstract: Disclosed are bispecific compounds (degraders) that target ?-synuclein protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative diseases.
    Type: Application
    Filed: June 16, 2021
    Publication date: July 20, 2023
    Applicants: DANA-FARBER CANCER INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION
    Inventors: Fleur M. Ferguson, Nathanael S. Gray, Tinghu Zhang, Stephen J. Haggarty
  • Publication number: 20230133538
    Abstract: Disclosed are bispecific compounds (degraders) that target tau protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative and neuropsychiatric diseases associated with aberrant tau.
    Type: Application
    Filed: March 17, 2021
    Publication date: May 4, 2023
    Applicants: DANA-FARBER CANCER INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION
    Inventors: Fleur M. Ferguson, Nathanael S. Gray, Stephen J. Haggarty, Maria Catarina Telo Baptista Lima Da Silva
  • Patent number: 11639325
    Abstract: The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
    Type: Grant
    Filed: December 9, 2020
    Date of Patent: May 2, 2023
    Assignees: Massachusetts Institute of Technology, The General Hospital Corporation
    Inventors: Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
  • 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: 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: 20220064151
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick's disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt-Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome.
    Type: Application
    Filed: August 9, 2021
    Publication date: March 3, 2022
    Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • Patent number: 11180438
    Abstract: The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
    Type: Grant
    Filed: June 15, 2018
    Date of Patent: November 23, 2021
    Assignees: Massachusetts Institute of Technology, The General Hospital Corporation
    Inventors: Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
  • Patent number: 11084803
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick's disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt-Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: August 10, 2021
    Assignees: Massachusetts Institute of Technology, The General Hospital Corporation
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • 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: 20210171429
    Abstract: The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
    Type: Application
    Filed: December 9, 2020
    Publication date: June 10, 2021
    Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
  • Publication number: 20210154184
    Abstract: Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
    Type: Application
    Filed: July 12, 2018
    Publication date: May 27, 2021
    Applicants: Dana-Farber Cancer Institute, Inc., The General Hospital Corporation D/B/A Massachusetts General Hospital
    Inventors: Nathanael S. Gray, Stephen J. Haggarty, Quan Cai, Tinghu Zhang, Maria Catarina Telo Baptista Lima da Silva, Fleur M. Ferguson
  • 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
  • Publication number: 20200087236
    Abstract: The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
    Type: Application
    Filed: June 15, 2018
    Publication date: March 19, 2020
    Applicant: The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Li-Huei TSAI, Stephen J. HAGGARTY, Debasis PATNAIK, Ping-Chieh PAO
  • 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
  • Publication number: 20190211000
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick's disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt-Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome.
    Type: Application
    Filed: December 21, 2018
    Publication date: July 11, 2019
    Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • Publication number: 20190175584
    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: June 13, 2019
    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
  • Patent number: RE49240
    Abstract: The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 11, 2020
    Date of Patent: October 11, 2022
    Assignee: The General Hospital Corporation
    Inventors: Ralph Mazitschek, Teru Hideshima, Kenneth C. Anderson, Stephen J. Haggarty, Balaram Ghosh