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).
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Publication number: 20230218632Abstract: 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: ApplicationFiled: March 19, 2021Publication date: July 13, 2023Applicant: Amathus Therapeutics, Inc.Inventors: Edward Holson, Charles Blum
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Publication number: 20230174523Abstract: 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: ApplicationFiled: March 19, 2021Publication date: June 8, 2023Applicant: Amathus Therapeutics, Inc.Inventors: Edward Holson, Charles Blum
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Publication number: 20230159509Abstract: 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: ApplicationFiled: March 19, 2021Publication date: May 25, 2023Applicant: Amathus Therapeutics, Inc.Inventors: Edward Holson, Charles Blum
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Publication number: 20230143552Abstract: 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: ApplicationFiled: October 7, 2022Publication date: May 11, 2023Applicants: The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
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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
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Patent number: 11498896Abstract: 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: GrantFiled: March 20, 2020Date of Patent: November 15, 2022Assignees: The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
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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
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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
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Publication number: 20220112216Abstract: 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: ApplicationFiled: October 22, 2021Publication date: April 14, 2022Applicants: 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
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Patent number: 11203601Abstract: 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: GrantFiled: April 5, 2018Date of Patent: December 21, 2021Assignees: 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
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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
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Publication number: 20210177781Abstract: 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: ApplicationFiled: January 11, 2019Publication date: June 17, 2021Inventors: Edward Holson, Mariana Nacht
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Publication number: 20210147355Abstract: 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: ApplicationFiled: March 20, 2020Publication date: May 20, 2021Applicants: The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
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Patent number: 10793538Abstract: 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: GrantFiled: January 24, 2018Date of Patent: October 6, 2020Assignee: The Broad Institute, Inc.Inventors: Edward Holson, Fanny Lazzaro, David Olson, Florence Fevrier Wagner, Michel Weiwer
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Patent number: 10752588Abstract: 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: GrantFiled: December 18, 2015Date of Patent: August 25, 2020Assignees: The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier, Michel Weiwer, Edward Scolnick, Michelle Palmer, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
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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
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Patent number: 10633336Abstract: 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: GrantFiled: December 18, 2015Date of Patent: April 28, 2020Assignees: The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
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Patent number: 10626438Abstract: The invention relates to a compound of Formula I: F1—X1-L1-X2—P1—X3-G1??(Formula I).Type: GrantFiled: December 5, 2017Date of Patent: April 21, 2020Assignee: The Broad Institute, Inc.Inventors: Yan-Ling Zhang, Edward Holson, Florence F. Wagner
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Publication number: 20200109154Abstract: 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: ApplicationFiled: April 5, 2018Publication date: April 9, 2020Applicants: 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
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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