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1.发明申请Compounds and methods for treatment of amyloid-beta-peptide related disorders 审中-公开用于治疗淀粉样蛋白-β-肽相关病症的化合物和方法公开(公告)号：US20090118282A1
公开(公告)日：2009-05-07
申请号：US11989024
申请日：2006-07-21
IPC分类号： A61K31/4709 , C07D401/12 , C07D413/12 , C07D215/36 , A61P25/28 , A61K31/47 , C07D471/04 , A61K31/5377
CPC分类号： C07D215/36 , C07D401/12
摘要： The present invention relates to compounds, preparation and uses thereof, particularly in the pharmaceutical industry. The present invention discloses novel compounds more particularly useful for the treatment of Alzheimer's disease and other similar diseases, and more specifically the inventive compounds modulate (in particular, inhibit) the level of amyloid-β peptide (Aβ) exhibited by cells or tissues; Aβ peptide is a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. This invention also relates the use of these inhibitors to prevent, treat or ameliorate the symptoms of Alzheimer's disease or any Amyloid-β-Peptide Related Disorder.
摘要翻译： 本发明涉及化合物，其制备和用途，特别是在制药工业中。 本发明公开了更特别可用于治疗阿尔茨海默病和其他类似疾病的新化合物，更具体地说，本发明化合物调节（特别是抑制）细胞或组织表现的淀粉样蛋白-β肽（Abeta）的水平; Abeta肽是阿尔茨海默氏症患者大脑中发现的淀粉样蛋白斑的主要成分。 本发明还涉及这些抑制剂用于预防，治疗或改善阿尔茨海默病或任何淀粉样蛋白-β-肽相关疾病症状的用途。
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2.发明申请Method involving pde4, compositions, and the screening thereof, for the treatment of degenerative ocular pathologies 失效涉及pde4，组合物及其筛选的方法，用于治疗退行性眼病公开(公告)号：US20060241062A1
公开(公告)日：2006-10-26
申请号：US10541503
申请日：2004-02-18
IPC分类号： A61K31/7056 , A61K31/4745
CPC分类号： A61K31/437 , A61K31/444 , A61K31/706
摘要： The invention relates to the field of biology, genetics and medicine. In particular, the invention relates to novel methods for the detection, characterization and/or treatment (or management) of neurodegenerative pathologies. The invention also relates to methods for the identification or screening of compounds active in the aforementioned pathologies. The invention further relates to the compounds, genes, cells, plasmids or compositions which are used to carry out said methods. In particular, the invention is based on the identification of the role of phosphodiesterase 4B, the peripheral benzodiazepine receptor (PBR) and GABA receptors of the type GABA(A) in neurodegenerative pathologies and describes the use of same as therapeutic, diagnostic or experimental markers or targets for said disorders.
摘要翻译： 本发明涉及生物学，遗传学和医学领域。 特别地，本发明涉及神经变性病理学的检测，表征和/或治疗（或治疗）的新方法。 本发明还涉及用于鉴定或筛选在上述病理学中有活性的化合物的方法。 本发明还涉及用于实施所述方法的化合物，基因，细胞，质粒或组合物。 特别地，本发明基于在神经变性病理学中鉴定磷酸二酯酶4B，外周苯并二氮杂受体（PBR）和GABA（A）类型的GABA受体的作用，并描述了其用于治疗，诊断或实验标记 或所述疾病的靶标。
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3.发明授权Methods involving PDE4, compositions, and the screening thereof, for the treatment of degenerative ocular pathologies 失效涉及PDE4，组合物及其筛选的方法用于治疗退行性眼病公开(公告)号：US07872015B2
公开(公告)日：2011-01-18
申请号：US10541503
申请日：2004-02-18
IPC分类号： A01N43/42 , A01N43/40 , A01N43/56 , A61K31/44 , A61K31/415
CPC分类号： A61K31/437 , A61K31/444 , A61K31/706
摘要： The invention relates to the field of biology, genetics and medicine. In particular, the invention relates to novel methods for the detection, characterization and/or treatment (or management) of neurodegenerative pathologies. The invention also relates to methods for the identification or screening of compounds active in the aforementioned pathologies. The invention further relates to the compounds, genes, cells, plasmids or compositions which are used to carry out said methods. In particular, the invention is based on the identification of the role of phosphodiesterase 4B, the peripheral benzodiazepine receptor (PBR) and GABA receptors of the type GABA(A) in neurodegenerative pathologies and describes the use of same as therapeutic, diagnostic or experimental markers or targets for said disorders.
摘要翻译： 本发明涉及生物学，遗传学和医学领域。 特别地，本发明涉及神经变性病理学的检测，表征和/或治疗（或治疗）的新方法。 本发明还涉及用于鉴定或筛选在上述病症中活性的化合物的方法。 本发明还涉及用于实施所述方法的化合物，基因，细胞，质粒或组合物。 特别地，本发明基于在神经变性病理学中鉴定磷酸二酯酶4B，外周苯并二氮杂受体（PBR）和GABA（A）类型的GABA受体的作用，并描述了其用于治疗，诊断或实验标记 或所述疾病的靶标。
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公开(公告)号：US20070027146A1
公开(公告)日：2007-02-01
申请号：US11190070
申请日：2005-07-27
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4709
CPC分类号： A61K31/5375 , A61K31/4709 , A61K31/496 , A61K31/541
摘要： The invention relates to compositions and methods for treating nervous disorders. More particularly, the invention relates to methods of treating amyloïd beta peptide-related disorders, particularly Alzheimer's disease, using Rac1 inhibitors. The invention may be used in mammalian subjects, particularly human subjects, at various stages of the disease, including disease onset. The invention also provides methods of producing, identifying, selecting or optimising compounds for use in the treatment of amyloïd beta peptide-related disorders, based on a determination of the ability of a test compound to inhibit Rac1.
摘要翻译： 本发明涉及用于治疗神经障碍的组合物和方法。 更具体地，本发明涉及使用Rac1抑制剂治疗淀粉样肽相关病症，特别是阿尔茨海默氏病的方法。 本发明可用于哺乳动物受试者，特别是人类受试者，在疾病的各个阶段，包括发病。 本发明还提供了基于测定化合物抑制Rac1的能力的测定来制备，鉴定，选择或优化化合物用于治疗淀粉样肽相关病症的方法。
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公开(公告)号：US20090285820A1
公开(公告)日：2009-11-19
申请号：US12223520
申请日：2007-01-30
CPC分类号： C07K14/47 , A61K31/7088 , A61K38/00 , C07K14/4706
摘要： The invention relates to compositions and methods for treating degenerative disorders. More particularly, the invention relates to methods of treating amyloïd beta peptide-related disorders, particularly Alzheimer's disease, using Rac1b inhibitors. The invention may be used in mammalian subjects, particularly human subjects, at various stages of the disease, including disease onset. The invention also provides methods of producing, identifying, selecting or optimising compounds for use in the treatment of amyloïd beta peptide-related disorders, based on a determination of the ability of a test compound to inhibit Rac1b.
摘要翻译： 本发明涉及用于治疗退行性疾病的组合物和方法。 更具体地，本发明涉及使用Rac1b抑制剂治疗淀粉样肽相关病症，特别是阿尔茨海默氏病的方法。 本发明可用于哺乳动物受试者，特别是人类受试者，在疾病的各个阶段，包括发病。 本发明还提供了基于测定化合物抑制Rac1b的能力的测定来制备，鉴定，选择或优化用于治疗淀粉样肽相关病症的化合物的方法。
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公开(公告)号：US20090093471A1
公开(公告)日：2009-04-09
申请号：US11989396
申请日：2006-07-26
申请人： Laurent Desire , Bertrand Leblond , Eric Beausoleil , Thierry Taverne , Fabien Schweighoffer , Virginie Picard
发明人： Laurent Desire , Bertrand Leblond , Eric Beausoleil , Thierry Taverne , Fabien Schweighoffer , Virginie Picard
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4709 , G01N33/566 , A61P25/28
CPC分类号： A61K31/5375 , A61K31/4709 , A61K31/496 , A61K31/541
摘要： The invention relates to compositions and methods for treating nervous disorders. More particularly, the invention relates to methods of treating amyloÊd beta peptide-related disorders, particularly Alzheimer's disease, using Rac1 inhibitors. The invention may be used in mammalian subjects, particularly human subjects, at various stages of the disease, including disease onset. The invention also provides methods of producing, identifying, selecting or optimising compounds for use in the treatment of amyloÊd beta peptide-related disorders, based on a determination of the ability of a test compound to inhibit Rac 1.
摘要翻译： 本发明涉及用于治疗神经障碍的组合物和方法。 更具体地说，本发明涉及使用Rac1抑制剂治疗β淀粉样肽相关疾病，特别是阿尔茨海默氏病的方法。 本发明可用于哺乳动物受试者，特别是人类受试者，在疾病的各个阶段，包括发病。 本发明还提供了基于测试化合物抑制Rac 1的能力的测定来制备，鉴定，选择或优化用于治疗淀粉样肽相关病症的化合物的方法。
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公开(公告)号：US20060142326A1
公开(公告)日：2006-06-29
申请号：US10560774
申请日：2004-06-25
IPC分类号： A61K31/4745
CPC分类号： A61K31/437
摘要： The invention relates to methods which are used to improve, increase or facilitate the cognition of individuals with neurodegenerative pathologies. More specifically, the invention relates to the use of compounds from the family of pyrazolopyridines in order to improve the cognitive faculties of individuals with neurodegenerative diseases. The invention can be used to improve the condition of individuals with different neurodegenerative diseases and, in particular, Alzheimer's disease and vascular dementia.
摘要翻译： 本发明涉及用于改善，增加或促进具有神经变性病理学的个体认知的方法。 更具体地，本发明涉及使用吡唑并吡啶酮类化合物，以改善具有神经变性疾病的个体的认知能力。 本发明可用于改善具有不同神经变性疾病，特别是阿尔茨海默病和血管性痴呆的个体的状况。
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公开(公告)号：US20090317842A1
公开(公告)日：2009-12-24
申请号：US12309492
申请日：2007-07-20
IPC分类号： G01N33/53 , C07D471/04 , C07D243/14
CPC分类号： G01N33/6896 , G01N33/5306 , G01N33/9426 , G01N2800/2821 , G01N2800/52
摘要： The present invention concerns compositions and methods for the treatment of neurodegenerative diseases in which the cognitive functions are altered, such as observed in Alzheimer's disease. More particularly, the invention presents a strategy for human clinical monitoring of the activity and/or effectiveness of neuroprotective treatments, based on biochemical assay of certain platelet parameters, and thus can be done by blood sampling. The invention also concerns methods, tools, constructions and compositions suitable for implementing these strategies.
摘要翻译： 本发明涉及用于治疗其中认知功能改变的神经变性疾病的组合物和方法，例如在阿尔茨海默病中观察到的。 更具体地说，本发明基于某些血小板参数的生物化学测定，提出了人类临床监测神经保护治疗的活性和/或有效性的策略，因此可以通过血液取样进行。 本发明还涉及适于实施这些策略的方法，工具，构造和组合。
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9.发明申请Compounds Which Inhibits Protein Prenylation E.G. Geranylgeransferse or Farnesyltransferase Inhibitors for Treating Parkinson's Disease 审中-公开抑制蛋白质磷酸化的化合物E.G. Geranylgeransferse或法呢基转移酶抑制剂治疗帕金森病公开(公告)号：US20080153758A1
公开(公告)日：2008-06-26
申请号：US11719342
申请日：2005-11-14
IPC分类号： A61K38/06 , A61K31/47 , A61K31/4545 , A61K31/5513 , A61K31/4427 , A61K31/496 , A61P25/16 , A61K31/426 , A61K31/4164 , A61K31/19 , A61K31/215
CPC分类号： A61K31/00 , A61K31/216
摘要： The invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention more specifically relates to new uses of compounds that inhibit the prenylation of proteins, in particular the geranylgeranyl and/or farnesyl modifications of proteins, for treating neurodegeneration involving oxidative stress and, more particularly, Parkinson's disease. The invention also relates to corresponding methods of treatment, and can be used in human subjects for preventive or curative treatment, either alone is or in combination with other active agents or treatments.
摘要翻译： 本发明涉及化合物及其用途，特别是在制药工业中。 本发明更具体地涉及抑制蛋白质异戊烯化的化合物的新用途，特别是蛋白质的香叶基香叶基和/或法呢基修饰物，用于治疗涉及氧化应激的神经变性，更具体地涉及帕金森病。 本发明还涉及相应的治疗方法，并且可以在人类受试者中用于预防或治疗性治疗，单独或与其它活性剂或治疗组合。
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10.发明授权Antibody to BACE455, an alternative splice variant of the human beta-secretase 失效BACE455的抗体，人β-分泌酶的替代剪接变体公开(公告)号：US07790864B2
公开(公告)日：2010-09-07
申请号：US10578493
申请日：2004-11-05
申请人： Laurent Desire
发明人： Laurent Desire
IPC分类号： C07K16/00 , C12P21/08 , A61K39/395
CPC分类号： C12N9/6421 , A61K38/00
摘要： The present invention relates generally to the fields of genetics, biochemistry, medicinal chemistry and medicine. The present invention more particularly discloses the identification of a human gene variant involved in neuropathological conditions, and methods for the diagnosis, prevention and treatment of such diseases and related disorders, as well as for the screening of therapeutically active drugs. The present invention relates to catalytically active beta-secretase (Memapsin2, BACE) variants, and nucleic acids encoding them. The invention is useful in the identification of agents that inhibit the activity of a particular BACE isoform and thus agents and therapies affecting the genesis, development or progression of neuropathological conditions, including Alzheimer's disease and dementia.
摘要翻译： 本发明一般涉及遗传学，生物化学，药物化学和医学领域。 本发明更具体地公开了鉴定涉及神经病理学病症的人基因变体，以及用于诊断，预防和治疗这些疾病和相关疾病以及用于筛选治疗活性药物的方法。 本发明涉及催化活性β-分泌酶（Memapsin2，BACE）变体和编码它们的核酸。 本发明可用于鉴定抑制特定BACE同种型的活性的药剂，因此可用于影响神经病理学病症（包括阿尔茨海默病和痴呆）的发生，发展或进展的药剂和疗法。
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