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: 20240091213Abstract: 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: ApplicationFiled: May 23, 2023Publication date: March 21, 2024Applicants: DANA-FARBER CANCER INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION d/b/a MASSACHUSETTS GENERAL HOSPITALInventors: Nathanael S. Gray, Stephen J. Haggarty, Quan Cai, Tinghu Zhang, Maria Catarina Telo Baptista Lima da Silva, Fleur M. Ferguson
-
Publication number: 20230227852Abstract: 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: ApplicationFiled: June 11, 2021Publication date: July 20, 2023Applicants: President and Fellows of Harvard College, The General Hospital Corporation, Vesigen, Inc.Inventors: Quan Lu, Stephen J. Haggarty, Robert Millman
-
Publication number: 20230226195Abstract: 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: ApplicationFiled: June 16, 2021Publication date: July 20, 2023Applicants: DANA-FARBER CANCER INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATIONInventors: Fleur M. Ferguson, Nathanael S. Gray, Tinghu Zhang, Stephen J. Haggarty
-
Publication number: 20230133538Abstract: 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: ApplicationFiled: March 17, 2021Publication date: May 4, 2023Applicants: DANA-FARBER CANCER INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATIONInventors: Fleur M. Ferguson, Nathanael S. Gray, Stephen J. Haggarty, Maria Catarina Telo Baptista Lima Da Silva
-
Patent number: 11639325Abstract: 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: GrantFiled: December 9, 2020Date of Patent: May 2, 2023Assignees: Massachusetts Institute of Technology, The General Hospital CorporationInventors: Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
-
Patent number: 11572368Abstract: 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: GrantFiled: August 11, 2016Date of Patent: February 7, 2023Assignees: The General Hospital Corporation, The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
-
Patent number: 11377423Abstract: 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: GrantFiled: August 16, 2017Date of Patent: July 5, 2022Assignees: The Broad Institute, Inc., The General Hospital CorporationInventors: Edward Holson, Florence Fevrier Wagner, Stephen J. Haggarty, Yan-Ling Zhang, Morten Lundh, Bridget Wagner, Michael C. Lewis, Tracey Lynn Petryshen
-
Publication number: 20220160702Abstract: 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: ApplicationFiled: June 10, 2021Publication date: May 26, 2022Applicants: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: 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: 20220064151Abstract: 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: ApplicationFiled: August 9, 2021Publication date: March 3, 2022Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
-
Patent number: 11180438Abstract: 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: GrantFiled: June 15, 2018Date of Patent: November 23, 2021Assignees: Massachusetts Institute of Technology, The General Hospital CorporationInventors: Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
-
Patent number: 11084803Abstract: 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: GrantFiled: December 21, 2018Date of Patent: August 10, 2021Assignees: Massachusetts Institute of Technology, The General Hospital CorporationInventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
-
Patent number: 11052080Abstract: 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: GrantFiled: November 21, 2018Date of Patent: July 6, 2021Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital CorporationInventors: 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: 20210171429Abstract: 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: ApplicationFiled: December 9, 2020Publication date: June 10, 2021Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
-
Publication number: 20210154184Abstract: 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: ApplicationFiled: July 12, 2018Publication date: May 27, 2021Applicants: Dana-Farber Cancer Institute, Inc., The General Hospital Corporation D/B/A Massachusetts General HospitalInventors: Nathanael S. Gray, Stephen J. Haggarty, Quan Cai, Tinghu Zhang, Maria Catarina Telo Baptista Lima da Silva, Fleur M. Ferguson
-
Patent number: 10662199Abstract: 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: GrantFiled: October 17, 2017Date of Patent: May 26, 2020Assignees: The Broad Institute, Inc., The General Hospital Corporation, Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
-
Publication number: 20200087236Abstract: 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: ApplicationFiled: June 15, 2018Publication date: March 19, 2020Applicant: The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Li-Huei TSAI, Stephen J. HAGGARTY, Debasis PATNAIK, Ping-Chieh PAO
-
Publication number: 20200061050Abstract: 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: ApplicationFiled: November 21, 2018Publication date: February 27, 2020Inventors: 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: 20190211000Abstract: 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: ApplicationFiled: December 21, 2018Publication date: July 11, 2019Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
-
Publication number: 20190175584Abstract: 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: ApplicationFiled: November 21, 2018Publication date: June 13, 2019Inventors: 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: RE49240Abstract: 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: GrantFiled: March 11, 2020Date of Patent: October 11, 2022Assignee: The General Hospital CorporationInventors: Ralph Mazitschek, Teru Hideshima, Kenneth C. Anderson, Stephen J. Haggarty, Balaram Ghosh