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1. 发明申请

WO2010011836A2 TREATING VARIOUS DISORDERS WITH 7,8-DIHYDROXYFLAVONE AND DERIVATIVES THEREOF 审中-公开
标题翻译：用7,8-二羟基黄酮及其衍生物治疗各种疾病
公开(公告)号：WO2010011836A2
公开(公告)日：2010-01-28
申请号：PCT/US2009/051535
申请日：2009-07-23
申请人： EMORY UNIVERSITY , YE, Keqiang
发明人： YE, Keqiang
IPC分类号： A61K31/353 , A61P25/24 , A61P25/22 , A61P3/04 , A61P25/28
CPC分类号： A61K31/353
摘要： Novel compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of 7,8-dihydroxyflavone or derivative thereof. Specifically, methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof. A further method of promoting neuroprotection in a subject also is provided, which includes selecting a subject in need of neuroprotection, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof.
摘要翻译：提供了与TrkB受体活化有关的新化合物和方法。该方法包括体内或体外给予治疗有效量的7,8-二羟基黄酮或其衍生物。具体而言，提供了用于治疗包括神经病症，神经精神病症和代谢病症（例如肥胖症）的病症的方法和化合物。例如，提供了治疗或降低个体中抑郁症，焦虑症或肥胖症风险的第一种方法，其包括选择患有抑郁症，焦虑症或肥胖症或具有发展成抑郁症，焦虑症或肥胖症风险的个体，并且向个体施用治疗有效量的7,8-二羟基黄酮或其衍生物。还提供了在受试者中促进神经保护的另一种方法，其包括选择需要神经保护的受试者，并向受试者施用治疗有效量的7,8-二羟基黄酮或其衍生物。

2. 发明申请

WO2009036068A2 GAMBOGIC AMINE, A SELECTIVE TRKA AGONIST WITH NEUROPROTECTIVE ACTIVITY 审中-公开
标题翻译： GAMBOGIC胺，一种具有神经保护作用的选择性TRKA激动剂
公开(公告)号：WO2009036068A2
公开(公告)日：2009-03-19
申请号：PCT/US2008/075859
申请日：2008-09-10
申请人： EMORY UNIVERSITY , YE, Keqiang
发明人： YE, Keqiang
IPC分类号： C07D417/02 , A61K31/45 , A61K31/44
CPC分类号： C07D493/18
摘要： Small molecule agonists, partial agonists, and antagonists for the TrkA receptor are described. The compounds are gambogic amines, where the carboxylic acid group of gambogic acid (CO 2 H) has been replaced by an amine group (CH 2 NR 1 R 2 ). In some embodiments, the compounds selectively bind to TrkA but not TrkB or C, robustly induce its tyrosine phosphorylation and downstream signaling activation including Akt and MAP kinases. Further, they can strongly prevent glutamate-induced neuronal cell death and provoke prominent neurite outgrowth in PC12 cells. Gambogic amines specifically interact with the cytoplasmic juxtamembrane domain of TrkA receptor and trigger its dimerization. Administration of these compounds in can substantially diminishes Kainic acid-triggered neuronal cell death and decrease infarct volume in transient middle cerebral artery occlusion (MCAO) model of stroke. Thus, these compounds can provide effective treatments for debilitating neurodegenerative diseases and provide neuroprotection from patients suffering from stroke or other ischemic events.
摘要翻译：描述了TrkA受体的小分子激动剂，部分激动剂和拮抗剂。这些化合物是藤黄胺，其中藤黄酸的羧酸基团（CO 2 H）已经被胺基（CH 2 NR 1）子>ř<子> 2 ）。在一些实施方案中，化合物选择性结合TrkA但不结合TrkB或C，强烈诱导其酪氨酸磷酸化和下游信号传导活化，包括Akt和MAP激酶。此外，它们可以强烈预防谷氨酸诱导的神经元细胞死亡并在PC12细胞中引起突出的神经突生长。藤黄胺特异性与TrkA受体的细胞质近膜区域相互作用并触发其二聚化。这些化合物的给药可以实质上减少海人酸引发的神经元细胞死亡并减少中风的短暂大脑中动脉闭塞（MCAO）模型中的梗塞体积。因此，这些化合物可以为衰弱的神经退行性疾病提供有效的治疗，并为患有中风或其他缺血事件的患者提供神经保护。

3. 发明申请

WO2023288069A1 METHODS OF USING SUBSTITUTED FLAVONES FOR TREATING BONE DISORDERS 审中-公开
公开(公告)号：WO2023288069A1
公开(公告)日：2023-01-19
申请号：PCT/US2022/037301
申请日：2022-07-15
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang
IPC分类号： A61K31/352 , A61K31/35 , A61P19/10
摘要： Provided herein are methods of using 4-oxo-2-phenyl-4H-chromene-7,8-diyl bis(methylcarbamate) and derivatives thereof for treating or preventing a bone disorder. The methods include administering to the subject an effective amount of a compound of Formula I or a pharmaceutical composition as described herein. The bone disorder can include, for example, osteoporosis. Also provided herein are methods of inhibiting asparagine endopeptidase (AEP) activity in a cell and methods of promoting bone growth, increasing bone density, or increasing bone strength in a subject. Novel mechanisms of action in treating and preventing bone disorders are provided herein.

4. 发明申请

WO2014018741A1 HETEROCYCLIC FLAVONE DERIVATIVES, COMPOSITIONS, AND METHODS RELATED THERETO 审中-公开
标题翻译：杂环衍生物衍生物，组合物及其相关方法
公开(公告)号：WO2014018741A1
公开(公告)日：2014-01-30
申请号：PCT/US2013/052030
申请日：2013-07-25
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang
IPC分类号： C07D311/30 , C07D311/28 , A61K31/353 , A61P25/00
CPC分类号： A61K31/352 , A61K31/353 , A61K31/407 , A61K31/4188 , A61K31/5377 , A61K45/06 , C07D311/30 , C07D491/052 , C07D491/06 , A61K2300/00
摘要： In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of 5 treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein to a subject in need thereof.
摘要翻译：在某些实施方案中，本公开涉及杂环黄酮衍生物，例如由本文提供的式所述的那些，药物组合物及其相关方法。在某些实施方案中，本公开涉及通过施用有效量的包含本文公开的化合物的药物组合物来治疗或预防与BDNF和TrkB活性相关的疾病或病症，例如抑郁症，中风，Rett综合征，帕金森病和阿尔茨海默氏病的方法涉及有需要的受试者。

5. 发明申请

WO2012047628A2 METHODS OF MANAGING BLOOD SUGAR LEVELS AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：管理血糖水平的方法和与之相关的组合物
公开(公告)号：WO2012047628A2
公开(公告)日：2012-04-12
申请号：PCT/US2011/053396
申请日：2011-09-27
申请人： EMORY UNIVERSITY , YE, Keqiang
发明人： YE, Keqiang
IPC分类号： C07D277/84 , C07D307/92 , C07D417/12 , A61K31/428 , A61K31/343 , A61P3/10
CPC分类号： A61K31/122 , A61K31/428 , A61K31/4439 , C07C69/65 , C07C225/30 , C07C321/22 , C07D277/84 , C07D307/92 , C07D417/12
摘要： The disclosure relates to methods of managing blood sugar levels and compositions related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diabetes, insulin resistance, or hyperglycemia comprising administering to a subject diagnosed with, at risk of, or exhibiting symptoms of diabetes, insulin resistance, or hyperglycemia a pharmaceutical composition comprising a compound comprising formula I.
摘要翻译：本公开涉及管理血糖水平的方法和与之相关的组合物。在某些实施方案中，本公开涉及治疗或预防糖尿病，胰岛素抵抗或高血糖症的方法，其包括向被诊断患有糖尿病，胰岛素抵抗或高血糖症状的患者诊断患有或表现出糖尿病，胰岛素抵抗或高血糖症的对象的药物组合物，所述药物组合物包含公式一

6. 发明申请

WO2020033960A1 Substituted Dihydroxyflavone Derivatives, Compositions, and Methods Related Thereto 审中-公开
公开(公告)号：WO2020033960A1
公开(公告)日：2020-02-13
申请号：PCT/US2019/046194
申请日：2019-08-12
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang
IPC分类号： A61K31/35 , A61P25/22 , A61P25/24
摘要： In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein to a subject in need thereof.

7. 发明申请

WO2015157376A1 ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS FOR MANAGING CANCER AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：用于管理癌症和组合物的阿伐他汀内肽（AEP）抑制剂
公开(公告)号：WO2015157376A1
公开(公告)日：2015-10-15
申请号：PCT/US2015/024850
申请日：2015-04-08
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang , FU, Haian , DU, Yuhong
IPC分类号： C07D473/04 , C07D473/06 , A61K31/52 , A61P35/00
CPC分类号： C07D473/06 , A61K31/4015 , A61K31/4168 , A61K31/433 , A61K31/47 , A61K31/496 , A61K31/519 , A61K31/522 , A61K31/5355 , A61K45/06 , C07D207/452 , C07D215/06 , C07D257/04 , C07D273/02 , C07D277/54 , C07D285/135 , C07D471/04
摘要： This disclosure relates to asparagine endopeptidase inhibitors for managing cancer and compositions related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are substituted 3,7-dihydropurine-2,6-dione derivatives useful for treating or preventing metastasis, tumor growth, and/or cancer. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating a cancer comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.
摘要翻译：本公开涉及用于管理癌症的天冬酰胺内肽酶抑制剂及其相关的组合物。在某些实施方案中，天冬酰胺内肽酶抑制剂是用于治疗或预防转移，肿瘤生长和/或癌症的取代的3,7-二氢嘌呤-2,6-二酮衍生物。在某些实施方案中，本公开涉及包含天冬酰胺内肽酶抑制剂和药学上可接受的赋形剂的药物组合物。在某些实施方案中，本公开涉及治疗癌症的方法，包括向有需要的受试者施用有效量的本文公开的天冬酰胺内肽酶抑制剂的药物组合物。

8. 发明申请

WO2008148008A1 HIGH THROUGHPUT BIOASSAY FOR IDENTIFYING SELECTIVE TRKA RECEPTOR AGONISTS, AND GAMBOGIC AMIDE, A SELECTIVE TRKA AGONIST WITH NEUROPROTECTIVE ACTIVITY 审中-公开
标题翻译：用于识别选择性TRKA受体激动剂的高通量生物传感器和游离氨基酸，具有神经保护活性的选择性TRKA激动剂
公开(公告)号：WO2008148008A1
公开(公告)日：2008-12-04
申请号：PCT/US2008/064723
申请日：2008-05-23
申请人： EMORY UNIVERSITY , YE, Keqiang
发明人： YE, Keqiang
IPC分类号： A61K31/352 , A61K31/45 , A61K31/497 , C07D313/06 , C07D311/78
CPC分类号： C07D493/10
摘要： A high-throughput screening assay for identifying small molecule agonists for the TrkA receptor is described. One such agonist, gambogic amide, selectively binds to TrkA but not TrkB or C, robustly induces its tyrosine phosphorylation and downstream signaling activation including Akt and MAP kinases. Further, it strongly prevents glutamate-induced neuronal cell death and provokes prominent neurite outgrowth in PC 12 cells. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of TrkA receptor and triggers its dimerization. Administration of this molecule in mice substantially diminishes Kainic acid-triggered neuronal cell death and decreases infarct volume in transient middle cerebral artery occlusion (MCAO) model of stroke. Thus, gambogic amide and other selective TrkA agonists can provide effective treatments for debilitating neurodegenerative diseases and provide neuroprotection from patients suffering from stroke or other ischemic events.
摘要翻译：描述了用于鉴定TrkA受体的小分子激动剂的高通量筛选试验。一种这样的激动剂，吡喃酰胺选择性结合TrkA而不是TrkB或C，可以强烈诱导其酪氨酸磷酸化和下游信号激活，包括Akt和MAP激酶。此外，它强烈地防止谷氨酸诱导的神经元细胞死亡并且引起PC12细胞中突出的神经突生长。甘草酰胺特异性地与TrkA受体的细胞质结膜结构域相互作用并引发其二聚化。该分子在小鼠中的施用基本上减少了Kainic酸触发的神经元细胞死亡，并减少了中风大脑中动脉闭塞（MCAO）模型中的梗死体积。因此，弓形酰胺和其他选择性TrkA激动剂可以为衰老性神经变性疾病提供有效的治疗，并从患有卒中或其他缺血事件的患者提供神经保护。

9. 发明申请

WO2023004044A2 COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES BY INHIBITING FSH 审中-公开
公开(公告)号：WO2023004044A2
公开(公告)日：2023-01-26
申请号：PCT/US2022/037882
申请日：2022-07-21
申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI , EMORY UNIVERSITY
发明人： ZAIDI, Mone , YE, Keqiang
IPC分类号： A61K39/395 , A61P5/06 , A61P5/08 , A61P25/28 , C07K16/26 , A61K41/00
摘要： The present disclosure provides compositions and methods for treating neurodegenerative diseases, in particular, Alzheimer's Disease, by inhibiting FSH in a subject in need thereof. A method comprising of treating Alzheimer's Disease (AD), preventing the onset of AD, or reducing cognitive or functional decline in AD, in a subject in need or at risk thereof.

10. 发明申请

WO2020242933A1 ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS, COMPOSITIONS, AND USES RELATED THERETO 审中-公开
公开(公告)号：WO2020242933A1
公开(公告)日：2020-12-03
申请号：PCT/US2020/034193
申请日：2020-05-22
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang
IPC分类号： A61K31/4245 , C07D271/12 , C07D285/14 , C07D417/14
摘要： This disclosure relates to asparagine endopeptidase inhibitors and compositions and uses related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are useful for improving memory, treating or preventing cancer, neurodegenerative diseases, and cognitive disorders. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient.

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