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1.发明专利Single use of pkc activator, or use of combination of pkc inhibitor therewith for enhancing long-term memory 审中-公开PKC激活剂的单次使用或PKC抑制剂组合使用以增强长期记忆
公开(公告)号：JP2013189439A
公开(公告)日：2013-09-26
申请号：JP2013095921
申请日：2013-04-30
发明人： ALKON DANIEL L
IPC分类号： A61K45/00 , A61K31/265 , A61K31/355 , A61K31/365 , A61K31/4015 , A61P25/28 , A61P43/00
CPC分类号： A61K31/366 , A61K31/365 , A61K31/40 , A61K31/4015 , A61K31/407 , A61K31/437
摘要： PROBLEM TO BE SOLVED: To provide a method of enhancing memory by up-regulating and down-regulating proteinkinase C for loss of memory most frequently associated with Alzheimer's disease.SOLUTION: Provided is a method of contacting proteinkinase C (PKC) with a PKC activation factor such as a large ring lactone typified by bryostatin so as to stimulate protein synthesis sufficient to fix or enhance a long-term memory.
摘要翻译： 要解决的问题：提供通过上调和下调蛋白激酶C以减少与阿尔茨海默病最相关的记忆丧失来增强记忆的方法。解决方案：提供一种使蛋白蛋白酶C（PKC）与PKC激活接触的方法 因子，例如由苔藓抑素代表的大环内酯，以刺激足以固定或增强长期记忆的蛋白质合成。
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2.发明专利Diagnosis of alzheimer's disease based on mitogen-activated protein kinase phosphorylation 有权基于激活蛋白激酶的磷酸化酶对阿尔茨海默病的诊断
公开(公告)号：JP2009148247A
公开(公告)日：2009-07-09
申请号：JP2008286869
申请日：2008-11-07
发明人： ALKON DANIEL L , ZHAO WEI-QIN
IPC分类号： C12Q1/48 , G01N33/50 , A61K45/00 , A61P25/28 , A61P43/00 , C12N5/10 , C12N9/99 , C12Q1/02 , G01N33/15 , G01N33/53 , G01N33/68
CPC分类号： G01N33/6896 , A61K31/404 , A61K31/519 , A61K31/5377 , A61K31/69 , G01N2333/4709 , G01N2333/91205 , G01N2500/00 , G01N2500/10 , G01N2800/2821
摘要： PROBLEM TO BE SOLVED: To provide a method of diagnosing Alzheimer's disease of a patient. SOLUTION: The method includes the step of determining whether a phosphorylation level of an indicator protein in a patient's cell has abnormally rises from a basic phosphorylation level after stimulated by an activator compound, wherein the indicator protein is Erk1/2 for example and the activator compound is bradykinin for example. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译： 要解决的问题：提供诊断患者的阿尔茨海默氏病的方法。 解决方案：该方法包括确定患者细胞中的指示蛋白的磷酸化水平是否在由活化剂化合物刺激后的碱性磷酸化水平异常升高，其中指示蛋白例如为Erk1 / 2， 活化剂化合物例如是缓激肽。 版权所有（C）2009，JPO＆INPIT
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3.发明专利Therapeutic effects of bryostatins, bryologs, and other related substances on head trauma-induced memory impairment and brain injury 有权BRYOSTATINS，BRYOSS和其他相关物质对头部TRAUMA诱导的记忆损伤和脑损伤的治疗效果
公开(公告)号：JP2014088406A
公开(公告)日：2014-05-15
申请号：JP2013261788
申请日：2013-12-18
发明人： ZOHAR OPHIR , ALKON DANIEL L
IPC分类号： A61K45/00 , A61K31/192 , A61K31/365 , A61K31/40 , A61K38/00 , A61P9/00 , A61P9/10 , A61P17/02 , A61P19/00 , A61P25/00
CPC分类号： A61K38/1825 , A61K31/00 , A61K31/05 , A61K31/335 , A61K31/35 , A61K31/365 , A61K31/395 , A61K31/4015 , A61K38/00
摘要： PROBLEM TO BE SOLVED: To provide use of protein kinase activators or boosters of nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF) or other neurotrophic factors to treat head trauma.SOLUTION: A method of treating head trauma comprises the steps of: identifying a subject having suffered a head trauma; and administering to said subject an amount of a pharmaceutical composition comprising a protein kinase C (PKC) activator or 4-methylcatechol acetic acid (MCBA) and a pharmaceutically acceptable carrier effective to treat at least one symptom of head trauma.
摘要翻译： 要解决的问题：提供使用蛋白激酶激活剂或神经生长因子（NGF）的促进剂，脑源性神经营养因子（BDNF）或其他神经营养因子来治疗头部创伤。解决方案：一种治疗头部创伤的方法包括步骤 ：识别遭受头部创伤的受试者; 以及向所述受试者施用一定量的包含蛋白激酶C（PKC）激活剂或4-甲基儿茶酚乙酸（MCBA）的药物组合物和有效治疗头部创伤的至少一种症状的药学上可接受的载体。
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4.发明专利Therapeutic effects of bryostatins, bryologs, and other related substances on ischemia/stroke-induced memory impairment and brain injury 有权BRYOSTATINS，BRYOSS，和其他相关物质对异位/诱导性记忆损伤和脑损伤的治疗效果
公开(公告)号：JP2014074037A
公开(公告)日：2014-04-24
申请号：JP2013243368
申请日：2013-11-25
发明人： MIAO-KUN SUN , ALKON DANIEL L
IPC分类号： A61K45/00 , A61K31/11 , A61K31/18 , A61K31/19 , A61K31/192 , A61K31/201 , A61K31/231 , A61K31/235 , A61K31/357 , A61K31/407 , A61K31/5025 , A61K31/517 , A61K31/519 , A61K31/63 , A61P9/10 , A61P25/28 , A61P43/00
CPC分类号： A61K31/05 , A61K31/00 , A61K31/335 , A61K31/35 , A61K31/365 , A61K31/395 , A61K31/4015 , A61K38/00 , A61K38/1825
摘要： PROBLEM TO BE SOLVED: To identify a subject having suffered a stroke and provide a pharmaceutical composition effective to treat at least one symptom of a subject having suffered a stroke.SOLUTION: The present invention provides methods of treating stroke comprising the steps of identifying a subject having suffered a stroke and administering to the subject an amount of a pharmaceutical composition comprising a protein kinase C (PKC) activator or 4-methylcatechol acetic acid (MCBA) and a pharmaceutically acceptable carrier effective to treat at least one symptom of a stroke.
摘要翻译： 要解决的问题：鉴定遭受卒中的受试者，并提供有效治疗遭受中风的受试者的至少一种症状的药物组合物。解决方案：本发明提供了治疗中风的方法，其包括以下步骤：鉴定受试者 已经遭受中风并且给予受试者一定量的包含蛋白激酶C（PKC）激活剂或4-甲基儿茶酚乙酸（MCBA）的药物组合物和有效治疗至少一种中风症状的药学上可接受的载体。
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5.发明专利Treatment of alzheimer's disease and method for increasing cognitive ability 审中-公开阿尔茨海默病的治疗和提高认知能力的方法
公开(公告)号：JP2013100308A
公开(公告)日：2013-05-23
申请号：JP2012286466
申请日：2012-12-28
发明人： ALKON DANIEL L
IPC分类号： A61K45/00 , A61K45/06 , A61K31/00 , A61K31/355 , A61K31/365 , A61K31/4015 , A61K31/7048 , A61P3/02 , A61P3/08 , A61P23/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P35/00 , A61P39/02 , A61P43/00
CPC分类号： A61K31/355 , A61K31/00 , A61K31/365 , A61K31/366 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a medical treatment of Alzheimer's disease and a method for increasing cognitive ability.SOLUTION: Provided is a composition containing a combination of PKC activator and PKC inhibitor. Also, provided are a method for adjusting α-secretase activity, improving or increasing cognitive ability, and/or alleviating nerve degeneration in an individual having a cognitive ability decreased disease, especially Akzheimer's disease, and a method for increasing the production of non-amyloid productive soluble APP (sAPP), including activation of protein kinase C in the brain and inhibition of PKC in peripheral tissue. Incidentally, macrocyclic lactone (or bryostatin class and neristatin class) is a desirable PKC activator, and vitamin E is a desirable PKC inhibitor.
摘要翻译： 要解决的问题：提供阿尔茨海默病的治疗和提高认知能力的方法。 提供了含有PKC活化剂和PKC抑制剂的组合的组合物。 此外，提供了一种用于调节α-分泌酶活性，提高或增加认知能力和/或减轻具有认知能力降低的疾病，特别是阿兹海默氏症的个体的神经变性的方法，以及用于增加非淀粉样蛋白生产的方法 生产性可溶性APP（sAPP），包括脑中蛋白激酶C的活化和外周组织中PKC的抑制。 顺便提及，大环内酯（或苔藓抑制素类和神经抑制素类）是理想的PKC激活剂，维生素E是理想的PKC抑制剂。 版权所有（C）2013，JPO＆INPIT
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6.发明专利Alzheimer's disease diagnosis based on mitogen-activated protein kinase phosphorylation 审中-公开基于激活蛋白激酶的磷酸化酶的ALZHEIMER病毒诊断
公开(公告)号：JP2013078330A
公开(公告)日：2013-05-02
申请号：JP2012268633
申请日：2012-12-07
发明人： ALKON DANIEL L , ZHAO WEI-QIN
IPC分类号： C12N5/077 , G01N33/50 , A61K45/00 , A61P25/28 , A61P43/00 , C12N5/10 , C12Q1/02 , C12Q1/04 , C12Q1/48 , G01N33/15 , G01N33/53 , G01N33/68
CPC分类号： G01N33/6896 , A61K31/404 , A61K31/519 , A61K31/5377 , A61K31/69 , G01N2333/4709 , G01N2333/91205 , G01N2500/00 , G01N2500/10 , G01N2800/2821
摘要： PROBLEM TO BE SOLVED: To provide a method for reducing, in vitro, proteolysis of amyloid precursor protein, secretion of amyloid protein β, and/or phosphorylation of tau protein in a human skin fibroblast cell.SOLUTION: The method for reducing, in vitro, proteolysis of amyloid precursor protein, secretion of amyloid protein β, and/or phosphorylation of tau protein in the human skin fibroblast cell includes: bringing the cell into contact with an inhibitor of phosphorylation of MAPK effective to reduce phosphorylation to the level in the control cell, wherein the inhibitor is bisindolylmaleimide-1 (BiSM-1), protein phosphatase 1 (PP1), or 2-aminoethoxydiphenyl borate (2ABP).
摘要翻译： 待解决的问题：提供在人皮肤成纤维细胞中减少体外淀粉样蛋白前体蛋白的蛋白水解，淀粉样蛋白β的分泌和/或tau蛋白的磷酸化的方法。 解决方案：人体皮肤成纤维细胞中淀粉样前体蛋白的体外降解，淀粉样蛋白β的分泌和/或tau蛋白的磷酸化的方法包括：使细胞与磷酸化抑制剂接触 的MAPK有效地将磷酸化降低至对照细胞中的水平，其中抑制剂是双吲哚基马来酰亚胺-1（BiSM-1），蛋白磷酸酶1（PP1）或2-氨基乙氧基二苯基硼酸盐（2ABP）。 版权所有（C）2013，JPO＆INPIT
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公开(公告)号：JP2012112968A
公开(公告)日：2012-06-14
申请号：JP2012000206
申请日：2012-01-04
发明人： DANIEL L ALCON , MIAO-KUN SUN
IPC分类号： G01N33/50 , A61K31/045 , A61K31/05 , A61K31/192 , A61K31/196 , A61K31/365 , A61K31/4164 , A61K31/4172 , A61P25/24 , G01N33/15
CPC分类号： A61K38/1825 , A61K31/045 , A61K31/05 , A61K31/192 , A61K31/196 , A61K31/365 , A61K31/366 , A61K31/4164 , A61K31/4172
摘要： PROBLEM TO BE SOLVED: To provide methods for screening an agent for antidepressant activity.SOLUTION: The present invention provides methods for screening an agent for antidepressant activity, comprising the steps of: a) administering an agent in a pharmaceutically acceptable carrier to a test subject and administering the pharmaceutically acceptable carrier to a control subject; b) placing each of the test subjects and the control subjects into a pool of water and measuring the distance and/or duration of swimming during a testing period; and c) comparing the distances or durations of swimming of the test subjects and the control subjects, where increased distances or durations of swimming of the test subjects compared to the control subjects are indicative of antidepressant activity.
摘要翻译： 要解决的问题：提供筛选抗抑郁药活性剂的方法。 解决方案：本发明提供了筛选抗抑郁药活性试剂的方法，包括以下步骤：a）将药物在药学上可接受的载体中施用于受检对象，并向对照受试者施用药学上可接受的载体; b）将每个测试对象和对照受试者放入水池中并测量测试期间游泳的距离和/或持续时间; 和c）比较测试对象和对照受试者的游泳距离或持续时间，其中与对照受试者相比，测试受试者的游泳距离或持续时间增加表明抗抑郁活性。 版权所有（C）2012，JPO＆INPIT
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8.发明专利
公开(公告)号：JP2013079254A
公开(公告)日：2013-05-02
申请号：JP2012266541
申请日：2012-12-05
发明人： ALKON DANIEL L , HONGPAISAN JARIN
IPC分类号： A61K31/335 , A61K31/395 , A61K31/4015 , A61P25/28 , A61P43/00
CPC分类号： A61K31/366 , A61K31/365 , A61K31/407 , A61K45/06 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss, to provide methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling, and to also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory, and to also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.SOLUTION: A pharmaceutical composition includes the PKC activity factor selected from macrocyclic lactone, benzolactam, and pyrrolidinone.
摘要翻译： 要解决的问题：提供减缓或逆转记忆丧失和学习丧失的方法，包括以下步骤：将有效量的PKC激活剂与蛋白激酶C（PKC）接触，所述受试者被识别为记忆丧失减缓的受试者或 逆转记忆损失，提供刺激细胞生长，神经元生长，树突生长，树突棘形成，树突棘密度和ELAV向近端树突的易位和突触重塑的方法，并且还提供使蛋白激酶C （PKC）激活剂与PKC激活剂以足以刺激足以巩固长期记忆的蛋白质的合成的方式，并且还提供使蛋白激酶C（PKC）激活剂与PKC激活剂接触的方法，其方式足以 下调PKC。 解决方案：药物组合物包括选自大环内酯，苯并内酰胺和吡咯烷酮的PKC活性因子。 版权所有（C）2013，JPO＆INPIT
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9.发明专利
公开(公告)号：JP2012131799A
公开(公告)日：2012-07-12
申请号：JP2012021053
申请日：2012-02-02
IPC分类号： A61K47/42 , A61K9/10 , A61K9/127 , A61K31/197 , A61K31/65 , A61K31/704 , A61K38/00 , A61K45/00 , A61K47/24 , A61K47/28 , A61K47/48 , A61P5/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P43/00
CPC分类号： A61K9/127 , A61K9/1275 , A61K31/704 , Y10S977/906
摘要： PROBLEM TO BE SOLVED: To provide a highly efficient artificial low-density lipoprotein (LDL) carrier system for the targeted delivery of therapeutic agents across the blood-brain barrier (BBB).SOLUTION: This invention relates to artificial LDL particles comprised of three lipid elements e.g. phosphatidyl choline, fatty-acyl-cholesterol esters, and at least one apolipoprotein. The present invention further relates to compositions, methods and kits comprising artificial LDL particles for targeting drugs to and across the BBB for the prevention and treatment of brain diseases.
摘要翻译： 要解决的问题：提供一种用于跨血脑屏障（BBB）靶向递送治疗剂的高效人造低密度脂蛋白（LDL）载体系统。 解决方案：本发明涉及由三种脂质元素组成的人造LDL颗粒，例如 磷脂酰胆碱，脂肪酰基胆固醇酯和至少一种载脂蛋白。 本发明进一步涉及包含人造LDL颗粒的组合物，方法和试剂盒，用于将药物靶向和穿过BBB以预防和治疗脑部疾病。 版权所有（C）2012，JPO＆INPIT
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10.发明专利PKC ACTIVATION AS MEANS FOR ENHANCING sAPPα SECRETION AND IMPROVING COGNITION USING BRYOSTATIN TYPE COMPOUND 审中-公开PKC激活作为增强sAPPα分泌和改善使用BRYOSTATIN型化合物的认知的手段
公开(公告)号：JP2012041348A
公开(公告)日：2012-03-01
申请号：JP2011201952
申请日：2011-09-15
IPC分类号： A61K45/00 , A61K31/00 , A61K31/335 , A61K31/35 , A61K31/365 , A61K31/7048 , A61P25/00 , A61P25/16 , A61P25/28 , A61P35/00 , A61P43/00
CPC分类号： A61K31/00 , A61K31/365 , A61K31/7048
摘要： PROBLEM TO BE SOLVED: To provide a composition and a method to modulate α-secretase and/or to improve cognitive ability.SOLUTION: The method includes administering PKC activator, specifically a factor for selectively activating PKCα, PKCδ and PKCε. Specifically, macrocyclic lactone, benzolactam and pyrrolidinone or a combination thereof is preferred for use with the composition.
摘要翻译： 要解决的问题：提供调节α-分泌酶和/或提高认知能力的组合物和方法。 解决方案：该方法包括施用PKC活化剂，特别是选择性激活PKCα，PKCδ和PKCε的因子。 具体地，大环内酯，苯并内酰胺和吡咯烷酮或其组合优选与组合物一起使用。 版权所有（C）2012，JPO＆INPIT
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