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1. 发明申请

WO2011127406A3 ACRIDINES AS INHIBITORS OF HASPIN AND DYRK KINASES 审中-公开
公开(公告)号：WO2011127406A3
公开(公告)日：2011-10-13
申请号：PCT/US2011/031786
申请日：2011-04-08
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC. , PRESIDENT AND FELLOWS OF HARVARD COLLEGE , UNIVERSITY PAUL CEZANNE MARSEILLE III/AIX , HIGGINS, Jonathan , CUNY, Gregory D. , GLICKSMAN, Marcie , PATNAIK, Debasis , ROBIN, Maxime , STEIN, Ross L. , XIAN, Jun
发明人： HIGGINS, Jonathan , CUNY, Gregory D. , GLICKSMAN, Marcie , PATNAIK, Debasis , ROBIN, Maxime , STEIN, Ross L. , XIAN, Jun
IPC分类号： C07D219/04 , C07D219/02 , C07D219/10 , C07D219/06 , C07D401/12 , A61K31/473 , A61P35/00
摘要： The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.

2. 发明申请

WO2011127406A2 ACRIDINES AS INHIBITORS OF HASPIN AND DYRK KINASES 审中-公开
标题翻译：作为HASPIN和DYRK KINASES的抑制剂的ACRIDINES
公开(公告)号：WO2011127406A2
公开(公告)日：2011-10-13
申请号：PCT/US2011031786
申请日：2011-04-08
申请人： BRIGHAM & WOMENS HOSPITAL , HARVARD COLLEGE , UNIV PAUL CEZANNE MARSEILLE III AIX , HIGGINS JONATHAN , CUNY GREGORY D , GLICKSMAN MARCIE , PATNAIK DEBASIS , ROBIN MAXIME , STEIN ROSS L , XIAN JUN
发明人： HIGGINS JONATHAN , CUNY GREGORY D , GLICKSMAN MARCIE , PATNAIK DEBASIS , ROBIN MAXIME , STEIN ROSS L , XIAN JUN
IPC分类号： C07D219/04 , A61K31/473 , A61P35/00 , C07D219/02 , C07D219/06 , C07D219/10 , C07D401/12
CPC分类号： C07D401/12 , C07D219/04 , C07D219/06 , C07D219/12
摘要： The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
摘要翻译：本公开涉及式I化合物：其是Haspin激酶和DYRK激酶的抑制剂。本公开的化合物及其组合物可用于治疗与Haspin激酶和DYRK激酶表达和/或活性相关的疾病。

3. 发明申请

WO2013016193A3 ACTIVATORS OF CLASS I HISTONE DEACETLYASES (HDACS) AND USES THEREOF 审中-公开
标题翻译： I类HISTONE去乙酰化酶（HDACS）的活化剂及其用途
公开(公告)号：WO2013016193A3
公开(公告)日：2013-03-28
申请号：PCT/US2012047609
申请日：2012-07-20
申请人： MASSACHUSETTS INST TECHNOLOGY , GEN HOSPITAL CORP , TSAI LI-HUEI , PAN LING , HAGGARTY STEPHEN J , PATNAIK DEBASIS
发明人： TSAI LI-HUEI , PAN LING , HAGGARTY STEPHEN J , PATNAIK DEBASIS
IPC分类号： C07D307/40 , A61K31/55 , A61P25/28 , C07C217/54 , C07D405/12 , C07D411/12 , 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).
摘要翻译：本发明提供式（A），（B），（C）和（D）的化合物，其药学上可接受的盐，溶剂化物，水合物，多晶型物，共晶体，互变异构体，立体异构体，同位素标记的衍生物和前药，其药物组合物及其试剂盒。本发明进一步提供了使用所述化合物治疗或预防神经障碍的方法，所述神经障碍包括阿尔茨海默病，帕金森病，亨廷顿病，ALS（肌萎缩性侧索硬化症），创伤性脑损伤，缺血性脑损伤，中风，额颞叶痴呆，Pick' （例如克罗伊茨费尔特 - 雅各布病，Gerstmann-Straussler-Scheinker综合征，致命性家族性失眠和库鲁氏病），Nieman Pick C型，脊髓小脑性共济失调，脊髓性肌营养不良，共济失调毛细血管扩张症，海马硬化症，Cockayne综合征，Werner综合征，色素性干皮病和布鲁姆综合征。在一个方面，所述方法包括向需要治疗神经疾病的受试者施用治疗有效量的DAC-001，DAC-002，DAC-003，DAC-009或DAC-012或式（A），（B），（C）或（D）。

4. 发明申请

WO2013016193A2 ACTIVATORS OF CLASS I HISTONE DEACETLYASES (HDACS) AND USES THEREOF 审中-公开
标题翻译：一类HISTONE DEACETLYASES（HDACS）的激活剂及其用途
公开(公告)号：WO2013016193A2
公开(公告)日：2013-01-31
申请号：PCT/US2012/047609
申请日：2012-07-20
申请人： MASSACHUSETTS ISTITUTE OF TECHNOLOGY , THE GENERAL HOSPITAL CORPORATION D/B/A MASSACHUSETTS GENERAL HOSPITAL , TSAI, Li-Huei , PAN, Ling , HAGGARTY, Stephen, J. , PATNAIK, Debasis
发明人： TSAI, Li-Huei , PAN, Ling , HAGGARTY, Stephen, J. , PATNAIK, Debasis
IPC分类号： C07D307/40 , C07D405/12 , C07D411/12 , C07D487/04 , C07C217/54 , A61K31/55 , A61P25/28
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).
摘要翻译：本发明提供式（A），（B），（C）和（D）的药学上可接受的盐，溶剂合物，水合物，多晶型物，共晶体，互变异构体，立体异构体，同位素标记的衍生物和前药的化合物，其药物组合物及其试剂盒。本发明还提供了使用该化合物治疗或预防神经障碍的方法，包括阿尔茨海默病，帕金森病，亨廷顿病，ALS（肌萎缩性侧索硬化），创伤性脑损伤，缺血性脑损伤，中风，额颞痴呆，（例如，克雅氏综合征，杰斯特曼 - 斯特劳斯勒 - 舍金综合征，致命性失眠症和库鲁），尼曼皮克C型，脊髓小脑共济失调，脊髓性肌营养不良症，共济失调毛细血管扩张症，海马硬化症，科克尼综合征，维纳综合征，色素性皮肤病和布卢姆综合征。在一个方面，所述方法包括向需要治疗神经障碍的受试者施用治疗有效量的DAC-001，DAC-002，DAC-003，DAC-009或DAC-012或式（A），（B），（C）或（D）。

5. 发明申请

WO2011133795A3 BETA-CARBOLINES AS INHIBITORS OF HASPIN AND DYRK KINASES 审中-公开
标题翻译：作为HASPIN和DYRK KINASES的抑制剂的BETA-CARBOLINES
公开(公告)号：WO2011133795A3
公开(公告)日：2012-05-03
申请号：PCT/US2011033466
申请日：2011-04-21
申请人： BRIGHAM & WOMENS HOSPITAL , HIGGINS JONATHAN , PATNAIK DEBASIS , ULYANOVA NATALIA , STEIN ROSS L , XIAN JUN , GLICKSMAN MARCIE , CUNY GREGORY D
发明人： HIGGINS JONATHAN , PATNAIK DEBASIS , ULYANOVA NATALIA , STEIN ROSS L , XIAN JUN , GLICKSMAN MARCIE , CUNY GREGORY D
IPC分类号： C07D471/04 , A61K31/403 , A61K31/437 , A61P3/10 , A61P35/00 , C07D209/88 , C07D491/147
CPC分类号： C07D471/04 , C07D209/56 , C07D209/88 , C07D491/14
摘要： The present disclosure is directed to compounds of Formula ( I ) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
摘要翻译：本公开涉及作为Haspin激酶和DYRK激酶抑制剂的式（I）化合物。本公开的化合物及其组合物可用于治疗与Haspin激酶和DYRK激酶表达和/或活性相关的疾病。

6. 发明申请

WO2011133795A2 BETA-CARBOLINES AS INHIBITORS OF HASPIN AND DYRK KINASES 审中-公开
标题翻译：作为HASPIN和DYRK KINASES的抑制剂的BETA-CARBOLINES
公开(公告)号：WO2011133795A2
公开(公告)日：2011-10-27
申请号：PCT/US2011/033466
申请日：2011-04-21
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC. , HIGGINS, Jonathan , PATNAIK, Debasis , ULYANOVA, Natalia , STEIN, Ross L. , XIAN, Jun , GLICKSMAN, Marcie , CUNY, Gregory D.
发明人： HIGGINS, Jonathan , PATNAIK, Debasis , ULYANOVA, Natalia , STEIN, Ross L. , XIAN, Jun , GLICKSMAN, Marcie , CUNY, Gregory D.
IPC分类号： C07D471/04 , C07D209/88 , C07D491/147 , A61K31/437 , A61K31/403 , A61P35/00 , A61P3/10
CPC分类号： C07D471/04 , C07D209/56 , C07D209/88 , C07D491/14
摘要： The present disclosure is directed to compounds of Formula ( I ) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
摘要翻译：本公开涉及作为Haspin激酶和DYRK激酶抑制剂的式（I）化合物。本公开的化合物及其组合物可用于治疗与Haspin激酶和DYRK激酶表达和/或活性相关的疾病。

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