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1. 发明申请

US20140235649A1 USE OF PHOSPHATASE INHIBITORS OR HISTONE DEACETYLASE INHIBITORS TO TREAT DISEASES CHARACTERIZED BY LOSS OF PROTEIN FUNCTION 审中-公开
标题翻译：使用磷酸酯酶抑制剂或组蛋白脱乙酰酶抑制剂治疗由蛋白质功能丧失所引起的疾病
公开(公告)号：US20140235649A1
公开(公告)日：2014-08-21
申请号：US14119849
申请日：2012-05-24
申请人： John S. Kovach , Zhengping Zhuang , Jie Lu , Chunzhang Yang , Russell Lonser
发明人： John S. Kovach , Zhengping Zhuang , Jie Lu , Chunzhang Yang , Russell Lonser
IPC分类号： A61K31/34 , A61K31/4406 , A61K31/4178 , A61K31/167 , A61K31/496 , A61K31/4525
CPC分类号： A61K31/34 , A61K31/167 , A61K31/343 , A61K31/4178 , A61K31/4406 , A61K31/4468 , A61K31/4525 , A61K31/496 , A61K45/06 , A61K2300/00
摘要： A method of treating a mammalian subject afflicted with a disease characterized by a loss of protein function caused by a genetic abnormality associated with the disease comprising administering to the subject a therapeutically effective amount of a protein phosphatase 2A inhibitor or a histone deacetylase inhibitor.
摘要翻译：一种治疗以疾病为特征的哺乳动物受试者的方法，其特征在于由与该疾病相关的遗传异常引起的蛋白质功能丧失，其包括向受试者施用治疗有效量的蛋白质磷酸酶2A抑制剂或组蛋白脱乙酰酶抑制剂。

2. 发明申请

US20100029683A1 Methods for regulating cell mitosis by inhibiting serine/threonine phosphateses 审中-公开
标题翻译：通过抑制丝氨酸/苏氨酸磷酸盐调节细胞有丝分裂的方法
公开(公告)号：US20100029683A1
公开(公告)日：2010-02-04
申请号：US12460407
申请日：2009-07-17
申请人： John S. Kovach , Zhengping Zhuang , Jie Lu
发明人： John S. Kovach , Zhengping Zhuang , Jie Lu
IPC分类号： A61K31/496 , A61K31/4525 , A61K31/34 , C12Q1/02 , C12N5/06 , A61P35/00
CPC分类号： G01N33/5011 , A61K31/34 , A61K31/4525 , A61K31/496 , G01N2510/00 , G01N2800/52
摘要： Disclosed herein are methods of inhibiting proliferation of a cancer cell or inducing apoptosis of a cancer cell, which does not overexpress N—CoR. Also disclosed herein are methods of inhibiting proliferation or inducing apoptosis of a cancer cell that overexpresses TCTP and methods for determining whether a compound is effective in inducing cell death.
摘要翻译：本文公开了抑制癌细胞增殖或诱导不过度表达N-CoR的癌细胞凋亡的方法。本文还公开了抑制过表达TCTP的癌细胞的增殖或诱导凋亡的方法以及用于确定化合物是否有效诱导细胞死亡的方法。

3. 发明申请

US20090018142A9 Use of phosphatases to treat tumors overexpressing N-CoR 审中-公开
标题翻译：使用磷酸酶治疗过度表达N-CoR的肿瘤
公开(公告)号：US20090018142A9
公开(公告)日：2009-01-15
申请号：US11703401
申请日：2007-02-06
申请人： Zhengping Zhuang , Edward H. Oldfield , Deric M. Park , Irina Lubensky , Jie Li , John S. Kovach
发明人： Zhengping Zhuang , Edward H. Oldfield , Deric M. Park , Irina Lubensky , Jie Li , John S. Kovach
IPC分类号： A61K31/496 , C12Q1/02 , G01N33/50 , A61P35/00
CPC分类号： A61K31/496 , G01N33/5011 , G01N33/57407 , G01N33/57484
摘要： This invention provides a method of treating a patient suffering from a tumor overexpressing N—CoR comprising administering to the patient a phosphatase ligand, alone or in combination with a retinoid receptor ligand, a histone deacetylase ligand, or both, in amounts effective to treat the patient. This invention also provides a method of inhibiting tumor growth in a patient suffering from a tumor overexpressing N—CoR. This invention further provides a method of identifying a compound or a mixture of compounds capable of inducing differentiation of cells of a tumor overexpressing N—CoR. This invention still further provides a method of determining the likelihood of successfully treating a subject suffering from a tumor overexpressing N—CoR. This invention also provides a method of assessing the likelihood that a patient is suffering from a tumor overexpressing N—CoR. This invention yet also provides a method of assessing the likelihood that a patient previously suffering from and treated for a tumor overexpressing N—CoR has suffered a recurrence of a tumor overexpressing N—CoR. Finally, this invention provides analogous methods for use on glioblastoma multiforme.
摘要翻译：本发明提供一种治疗患有过表达N-CoR的肿瘤患者的方法，其包括向患者施用有效治疗以下成分的量的单独或与类视色素受体配体，组蛋白脱乙酰酶配体或两者结合的磷酸酶配体患者。本发明还提供了抑制患有过量表达N-CoR的肿瘤患者的肿瘤生长的方法。本发明还提供鉴定能够诱导过表达N-CoR的肿瘤细胞分化的化合物或化合物的混合物的方法。本发明还提供了确定成功治疗患有过量表达N-CoR的肿瘤患者的可能性的方法。本发明还提供了评估患者患有过度表达N-CoR的肿瘤的可能性的方法。本发明还提供了一种评估先前患有和治疗过度表达N-CoR的肿瘤的患者遭受过度表达N-CoR的肿瘤复发的可能性的方法。最后，本发明提供了用于多形性成胶质细胞瘤的类似方法。

4. 发明申请

US20170136008A1 OXABICYCLOHEPTANES AND OXABICYCLOHEPTENES FOR THE TREATMENT OF OVARIAN CANCER 审中-公开
公开(公告)号：US20170136008A1
公开(公告)日：2017-05-18
申请号：US15320153
申请日：2015-06-19
申请人： John S. Kovach , Zhengping Zhuang , Ki-eun Chang , Matthew Hall , Michael M. Gottesman
发明人： John S. Kovach , Zhengping Zhuang , Ki-eun Chang , Matthew Hall , Michael M. Gottesman
IPC分类号： A61K31/496 , A61K31/704 , A61K33/24
CPC分类号： A61K31/496 , A61K31/343 , A61K31/555 , A61K31/704 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： A method of treating ovarian cancer in a subject afflicted therewith comprising administering to the subject an effective amount of an anti-cancer agent and an effective amount of a compound having the structure:

5. 发明申请

US20090035292A1 Use of phosphatases to treat neuroblastomas and medulloblastomas 审中-公开
标题翻译：使用磷酸酶治疗神经母细胞瘤和成神经管细胞瘤
公开(公告)号：US20090035292A1
公开(公告)日：2009-02-05
申请号：US12221360
申请日：2008-08-01
申请人： John S. Kovach , Zhengping Zhuang
发明人： John S. Kovach , Zhengping Zhuang
IPC分类号： A61K38/46 , A61K31/496 , A61K31/34 , A61K38/02 , A61K38/12 , A61P35/00 , A61K31/07 , A61K38/15 , A61K31/44 , A61K33/16
CPC分类号： A61K31/07 , A61K31/34 , A61K31/44 , A61K31/496 , A61K33/16 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are methods of treating neuroblastomas and medulloblastomas in a subject comprising administering to the subject a phosphatase ligand in an amount effective to treat the subject. Also disclosed herein are method of treating neuroblastomas and medulloblastomas in a subject comprising administering to the subject a histone deacteylase ligand in an amount effective to treat the subject.
摘要翻译：本文公开了治疗受试者中神经母细胞瘤和成神经管细胞瘤的方法，包括以有效治疗受试者的量向受试者施用磷酸酶配体。本文还公开了治疗受试者中神经母细胞瘤和成神经管细胞瘤的方法，包括以有效治疗受试者的量向受试者施用组蛋白失活酶配体。

6. 发明申请

US20080214569A1 Use of phosphatases to treat tumors overexpressing N-CoR 审中-公开
标题翻译：使用磷酸酶治疗过度表达N-CoR的肿瘤
公开(公告)号：US20080214569A1
公开(公告)日：2008-09-04
申请号：US11703401
申请日：2007-02-08
申请人： Zhengping Zhuang , Edward H. Oldfield , Deric M. Park , Irina Lubensky , Jie Li , John S. Kovach
发明人： Zhengping Zhuang , Edward H. Oldfield , Deric M. Park , Irina Lubensky , Jie Li , John S. Kovach
IPC分类号： A61K31/496 , C12Q1/02 , G01N33/50 , A61P35/00
CPC分类号： A61K31/496 , G01N33/5011 , G01N33/57407 , G01N33/57484
摘要： This invention provides a method of treating a patient suffering from a tumor overexpressing N—CoR comprising administering to the patient a phosphatase ligand, alone or in combination with a retinoid receptor ligand, a histone deacetylase ligand, or both, in amounts effective to treat the patient. This invention also provides a method of inhibiting tumor growth in a patient suffering from a tumor overexpressing N—CoR. This invention further provides a method of identifying a compound or a mixture of compounds capable of inducing differentiation of cells of a tumor overexpressing N—CoR. This invention still further provides a method of determining the likelihood of successfully treating a subject suffering from a tumor overexpressing N—CoR. This invention also provides a method of assessing the likelihood that a patient is suffering from a tumor overexpressing N—CoR. This invention yet also provides a method of assessing the likelihood that a patient previously suffering from and treated for a tumor overexpressing N—CoR has suffered a recurrence of a tumor overexpressing N—CoR. Finally, this invention provides analogous methods for use on glioblastoma multiforme.
摘要翻译：本发明提供一种治疗患有过表达N-CoR的肿瘤患者的方法，其包括向患者施用有效治疗以下成分的量的单独或与类视色素受体配体，组蛋白脱乙酰酶配体或两者结合的磷酸酶配体患者。本发明还提供了抑制患有过量表达N-CoR的肿瘤患者的肿瘤生长的方法。本发明还提供鉴定能够诱导过表达N-CoR的肿瘤细胞分化的化合物或化合物的混合物的方法。本发明还提供了确定成功治疗患有过量表达N-CoR的肿瘤患者的可能性的方法。本发明还提供了评估患者患有过度表达N-CoR的肿瘤的可能性的方法。本发明还提供了一种评估先前患有和治疗过度表达N-CoR的肿瘤的患者遭受过度表达N-CoR的肿瘤复发的可能性的方法。最后，本发明提供了用于多形性成胶质细胞瘤的类似方法。

7. 发明授权

US08227473B2 Oxabicycloheptanes and oxabicycloheptenes, their preparation and use 有权
标题翻译：氧杂双环庚烷和氧杂双环庚烯，其制备和用途
公开(公告)号：US08227473B2
公开(公告)日：2012-07-24
申请号：US12460404
申请日：2009-07-17
申请人： John S. Kovach , Francis Johnson
发明人： John S. Kovach , Francis Johnson
IPC分类号： A61K31/496 , C07D493/08 , A61K31/4178 , A61K31/34
CPC分类号： C07D307/00 , A61K31/4178 , A61K31/496 , C07D405/12
摘要： This invention provides compounds having the structure which may be used for the treatment of tumors.
摘要翻译：本发明提供具有可用于治疗肿瘤的结构的化合物。

8. 发明授权

US08058268B2 Neuroprotective agents for the prevention and treatment of neurodegenerative diseases 有权
标题翻译：用于预防和治疗神经退行性疾病的神经保护剂
公开(公告)号：US08058268B2
公开(公告)日：2011-11-15
申请号：US12462182
申请日：2009-07-29
申请人： John S. Kovach
发明人： John S. Kovach
IPC分类号： A61K31/54 , A61K31/44
CPC分类号： A61K31/34 , A61K31/167 , A61K31/4406 , A61K31/445 , A61K31/4525 , A61K31/496 , A61K31/5377
摘要： Disclosed herein are methods of treating neurodegenerative diseases comprising administering to the subject a compound having the structure: wherein α and R1-R8 are described herein, or a compound having the structure: wherein Y, Z, and R21, R24, R25, and R31-R33 are described herein.
摘要翻译：本文公开了治疗神经变性疾病的方法，包括向受试者施用具有以下结构的化合物：其中α和R 1 -R 8在本文中描述，或具有以下结构的化合物：其中Y，Z和R21，R24，R25和R31 -R33在本文中描述。

9. 发明申请

US20100029484A1 Oxabicycloheptanes and oxabicycloheptenes, their preparation and use 有权
标题翻译：氧杂双环庚烷和氧杂双环庚烯，其制备和用途
公开(公告)号：US20100029484A1
公开(公告)日：2010-02-04
申请号：US12460404
申请日：2009-07-17
申请人： John S. Kovach , Francis Johnson
发明人： John S. Kovach , Francis Johnson
IPC分类号： A01N43/60 , C07D493/08 , A61K31/496 , A61K31/4178 , A01N43/50 , A61P31/10 , A61P35/00 , A61P25/00 , C12N5/00
CPC分类号： C07D307/00 , A61K31/4178 , A61K31/496 , C07D405/12
摘要： This invention provides compounds having the structure which may be used for the treatment of tumors.
摘要翻译：本发明提供具有可用于治疗肿瘤的结构的化合物。

10. 发明授权

US08455688B2 HDAC inhibitors 有权
标题翻译： HDAC抑制剂
公开(公告)号：US08455688B2
公开(公告)日：2013-06-04
申请号：US13426417
申请日：2012-03-21
申请人： John S. Kovach , Francis Johnson
发明人： John S. Kovach , Francis Johnson
IPC分类号： C07C233/65 , A61K31/16
CPC分类号： C07D213/82
摘要： This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N, wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.
摘要翻译：本发明提供具有n为1-10的结构的化合物; X是C-R11或N，其中R11是H，OH，SH，F，Cl，SO2R7，NO2，三氟甲基，甲氧基或CO-R7，其中R7是烷基，烯基，炔基，C3-C8环烷基或芳基 ; Z是R 2是H或NR 3 R 4，其中R 3和R 4各自独立地是H，C 1 -C 6烷基或C 3 -C 8环烷基; R5是OH或SH; 并且R 6，R 12，R 13和R 14各自独立地为H，OH，SH，F，Cl，SO 2 R 15，NO 2，三氟甲基，甲氧基或CO-R 15，其中R 15是烷基，烯基，炔基，C 3 -C 8环烷基或芳基或该化合物的盐，其可用于治疗肿瘤。

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