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公开(公告)号:US11572368B2
公开(公告)日:2023-02-07
申请号:US15234675
申请日:2016-08-11
申请人: The General Hospital Corporation , The Broad Institute, Inc. , Massachusetts Institute of Technology
发明人: Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Li-Huei Tsai , Stephen J. Haggarty , Yan-Ling Zhang
IPC分类号: C07D491/107 , C07D401/12 , C07D403/12 , C07D309/08 , C07D311/82 , C07D333/20 , C07D405/12 , C07D493/08 , C07D211/22 , C07D213/40 , C07C271/28 , C07C275/30 , C07C275/40 , C07C281/06 , C07C211/52 , C07C233/43 , C07C233/56 , C07C233/62 , C07C235/82 , C07D409/12 , C07C237/20 , C07D205/06 , C07D213/56 , C07D241/12 , C07D333/24 , C07C237/24 , C07D205/04 , C07D209/44 , C07D209/52 , C07D211/34 , C07D211/62 , C07D295/195 , C07D471/04 , A61K31/167 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/437 , A61K31/445 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/397 , A61K31/415 , A61K31/4178 , A61K31/439 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/519 , A61K31/5377 , C07C233/42 , C07D231/04 , C07D237/04 , C07D295/185 , C07D311/04 , C07D407/12 , C07D487/04 , C07D487/10 , C07D491/08
摘要: 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.
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公开(公告)号:US10662199B2
公开(公告)日:2020-05-26
申请号:US15786134
申请日:2017-10-17
申请人: The Broad Institute, Inc. , The General Hospital Corporation , Massachusetts Institute of Technology
发明人: Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Li-Huei Tsai , Stephen J. Haggarty , Yan-Ling Zhang
IPC分类号: C07D491/107 , C07D401/12 , C07D403/12 , C07D309/08 , C07D311/82 , C07D333/20 , C07D405/12 , C07D493/08 , C07D211/22 , C07D213/40 , C07C271/28 , C07C275/30 , C07C275/40 , C07C281/06 , C07C211/52 , C07C233/43 , C07C233/56 , C07C233/62 , C07C235/82 , C07D409/12 , C07C237/20 , C07D205/06 , C07D213/56 , C07D241/12 , C07D333/24 , C07C237/24 , C07D205/04 , C07D209/44 , C07D209/52 , C07D211/34 , C07D211/62 , C07D295/195 , C07D471/04 , A61K31/167 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/437 , A61K31/445 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/397 , A61K31/415 , A61K31/4178 , A61K31/439 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/519 , A61K31/5377 , C07C233/42 , C07D231/04 , C07D237/04 , C07D295/185 , C07D311/04 , C07D407/12 , C07D487/04 , C07D487/10 , C07D491/08
摘要: 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.
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公开(公告)号:US20180016282A9
公开(公告)日:2018-01-18
申请号:US15234675
申请日:2016-08-11
申请人: The General Hospital Corporation d/b/a Massachusetts General Hospital , The Broad Institute, Inc. , Massachusetts Institute of Technology
发明人: Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Li-Huei Tsai , Stephen J. Haggarty , Yan-Ling Zhang
IPC分类号: C07D491/107 , C07D401/12 , C07D493/08 , C07D491/08 , C07D487/10 , C07D487/04 , C07D471/04 , C07D409/12 , C07D407/12 , C07D405/12 , C07D403/12 , C07D333/24 , C07D333/20 , C07D311/82 , C07D311/04 , C07D309/08 , C07D295/195 , C07D295/185 , C07D241/12 , C07D237/04 , C07D231/04 , C07D213/56 , C07D213/40 , C07D211/62 , C07D211/34 , C07D211/22 , C07D209/52 , C07D209/44 , C07D205/06 , C07D205/04 , C07C281/06 , C07C275/40 , C07C275/30 , C07C271/28 , C07C237/24 , C07C237/20 , C07C235/82 , C07C233/62 , C07C233/56 , C07C233/43 , C07C233/42 , C07C211/52 , A61K31/5377 , A61K31/519 , A61K31/501 , A61K31/50 , A61K31/4965 , A61K31/496 , A61K31/4545 , A61K31/4535 , A61K31/445 , A61K31/4439 , A61K31/4433 , A61K31/4418 , A61K31/439 , A61K31/437 , A61K31/4178 , A61K31/415 , A61K31/4035 , A61K31/403 , A61K31/402 , A61K31/397 , A61K31/381 , A61K31/352 , A61K31/351 , A61K31/167
CPC分类号: C07D491/107 , A61K31/167 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/397 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4178 , A61K31/437 , A61K31/439 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/519 , A61K31/5377 , C07C211/52 , C07C233/42 , C07C233/43 , C07C233/56 , C07C233/62 , C07C235/82 , C07C237/20 , C07C237/24 , C07C271/28 , C07C275/30 , C07C275/40 , C07C281/06 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/50 , C07D205/04 , C07D205/06 , C07D209/44 , C07D209/52 , C07D211/22 , C07D211/34 , C07D211/62 , C07D213/40 , C07D213/56 , C07D231/04 , C07D237/04 , C07D241/12 , C07D295/185 , C07D295/195 , C07D309/08 , C07D311/04 , C07D311/82 , C07D333/20 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/08 , C07D493/08
摘要: 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.
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公开(公告)号:US20160280693A1
公开(公告)日:2016-09-29
申请号:US14834587
申请日:2015-08-25
申请人: Massachusetts Institute of Technology , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人: Li-Huei Tsai , Ling Pan , Stephen J. Haggarty , Debasis Patnaik
IPC分类号: C07D405/12
CPC分类号: C07D405/12 , C07C217/58 , C07C219/28 , C07D307/40 , C07D307/52 , C07D409/12 , C07D411/12 , C07D487/04
摘要: 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. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
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公开(公告)号:US20160251351A1
公开(公告)日:2016-09-01
申请号:US15147201
申请日:2016-05-05
申请人: The Broad Institute, Inc. , The General Hospital Corporation d/b/a Massachusetts General Hospital , Massachusetts Institute of Technology
发明人: Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Li-Huei Tsai , Stephen J. Haggarty , Yan-Ling Zhang
IPC分类号: C07D471/04 , A61K31/167 , C07D211/62 , A61K31/445 , C07D295/195 , A61K31/437 , C07D211/34 , C07D209/44 , A61K31/4035 , C07D209/52 , A61K31/403 , C07C237/24 , A61K31/402
CPC分类号: C07D491/107 , A61K31/167 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/397 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4178 , A61K31/437 , A61K31/439 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/519 , A61K31/5377 , C07C211/52 , C07C233/42 , C07C233/43 , C07C233/56 , C07C233/62 , C07C235/82 , C07C237/20 , C07C237/24 , C07C271/28 , C07C275/30 , C07C275/40 , C07C281/06 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/50 , C07D205/04 , C07D205/06 , C07D209/44 , C07D209/52 , C07D211/22 , C07D211/34 , C07D211/62 , C07D213/40 , C07D213/56 , C07D231/04 , C07D237/04 , C07D241/12 , C07D295/185 , C07D295/195 , C07D309/08 , C07D311/04 , C07D311/82 , C07D333/20 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/08 , C07D493/08
摘要: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R1a, 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.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,水合物,溶剂合物或前药,其中U,J,V,X,R 1a,R 2b,R 2c,R 5和t如本文所述。 本发明一般涉及组蛋白脱乙酰酶的抑制剂及其制备和使用方法。 这些化合物可用于促进认知功能和增强学习和记忆形成。 此外,这些化合物可用于治疗,减轻和/或预防各种病症,包括例如神经障碍,记忆和认知功能障碍/损伤,灭绝学习障碍,真菌疾病和感染,炎性疾病,血液疾病和 人类和动物中的肿瘤性疾病。
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公开(公告)号:US11084803B2
公开(公告)日:2021-08-10
申请号:US16231324
申请日:2018-12-21
发明人: Li-Huei Tsai , Ling Pan , Stephen J. Haggarty , Debasis Patnaik
IPC分类号: C07D405/12 , C07D409/12 , C07C217/58 , C07D411/12 , C07D307/40 , C07C219/28 , C07D307/52 , C07D487/04
摘要: 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. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
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公开(公告)号:US11639325B2
公开(公告)日:2023-05-02
申请号:US17116427
申请日:2020-12-09
IPC分类号: C07C49/83 , A61K9/00 , A61K45/06 , A61K31/12 , C07C49/84 , C07C215/20 , C07C69/017 , A61P25/28 , C07C65/34
摘要: 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.
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公开(公告)号:US20190211000A1
公开(公告)日:2019-07-11
申请号:US16231324
申请日:2018-12-21
申请人: Massachusetts Institute of Technology , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人: Li-Huei Tsai , Ling Pan , Stephen J. Haggarty , Debasis Patnaik
IPC分类号: C07D405/12 , C07D307/40 , C07D411/12 , C07C217/58 , C07C219/28 , C07D409/12 , C07D307/52 , C07D487/04
CPC分类号: C07D405/12 , C07C217/58 , C07C219/28 , C07D307/40 , C07D307/52 , C07D409/12 , C07D411/12 , C07D487/04
摘要: 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. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
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公开(公告)号:US20170217955A9
公开(公告)日:2017-08-03
申请号:US15147201
申请日:2016-05-05
申请人: The Broad Institute, Inc. , The General Hospital Corporation d/b/a Massachusetts General Hospital , Massachusetts Institute of Technology
发明人: Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Li-Huei Tsai , Stephen J. Haggarty , Yan-Ling Zhang
IPC分类号: C07D471/04 , A61K31/167 , C07D211/62 , A61K31/445 , C07D295/195 , A61K31/437 , C07D211/34 , C07D209/44 , A61K31/4035 , C07D209/52 , A61K31/403 , C07C237/24 , A61K31/402
CPC分类号: C07D491/107 , A61K31/167 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/397 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4178 , A61K31/437 , A61K31/439 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/519 , A61K31/5377 , C07C211/52 , C07C233/42 , C07C233/43 , C07C233/56 , C07C233/62 , C07C235/82 , C07C237/20 , C07C237/24 , C07C271/28 , C07C275/30 , C07C275/40 , C07C281/06 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/50 , C07D205/04 , C07D205/06 , C07D209/44 , C07D209/52 , C07D211/22 , C07D211/34 , C07D211/62 , C07D213/40 , C07D213/56 , C07D231/04 , C07D237/04 , C07D241/12 , C07D295/185 , C07D295/195 , C07D309/08 , C07D311/04 , C07D311/82 , C07D333/20 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/08 , C07D493/08
摘要: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R1a, 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.
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公开(公告)号:US20220064151A1
公开(公告)日:2022-03-03
申请号:US17397752
申请日:2021-08-09
申请人: Massachusetts Institute of Technology , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人: Li-Huei Tsai , Ling Pan , Stephen J. Haggarty , Debasis Patnaik
IPC分类号: C07D405/12 , C07D307/52 , C07D411/12 , C07D307/40 , C07C217/58 , C07D487/04 , C07C219/28 , C07D409/12
摘要: 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. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
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