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1. 发明授权

US08389506B2 Compounds for therapy and diagnosis 有权
标题翻译：用于治疗和诊断的化合物
公开(公告)号：US08389506B2
公开(公告)日：2013-03-05
申请号：US12746382
申请日：2008-12-05
申请人： Kevin Jeffrey Barnham , Vijaya Kenche
发明人： Kevin Jeffrey Barnham , Vijaya Kenche
IPC分类号： A61K31/555 , C07F15/00
CPC分类号： C07D401/04 , A61K49/0017 , A61K51/0453 , A61K51/0478 , C07F15/0093
摘要： The present invention relates to a transition metal complex represented by Formula (I) or salts thereof, or to a ligand represented by Formula (H) or salts thereof, wherein X represents a transition metal, preferably Pt, and methods for their use and preparation. In particular, the invention relates to compounds which may possess useful therapeutic activity in treating amyloid diseases, and in particular, Alzheimer's disease. The invention also relates to the use of these compounds in methods of therapy, and diagnosis, and the manufacture of medicaments as well as compositions containing these compounds.
摘要翻译：本发明涉及由式（I）表示的过渡金属络合物或其盐，或由式（H）表示的配体或其盐，其中X表示过渡金属，优选Pt，及其用途及制备方法。特别地，本发明涉及在治疗淀粉样蛋白病，特别是阿尔茨海默病方面具有有用治疗活性的化合物。本发明还涉及这些化合物在治疗，诊断和制备药物以及含有这些化合物的组合物的方法中的用途。

2. 发明申请

US20110110850A1 COMPOUNDS FOR THERAPY AND DIAGNOSIS 有权
标题翻译：治疗和诊断的化合物
公开(公告)号：US20110110850A1
公开(公告)日：2011-05-12
申请号：US12746382
申请日：2008-12-05
申请人： Kevin Jeffrey Barnham , Vijaya Kenche
发明人： Kevin Jeffrey Barnham , Vijaya Kenche
IPC分类号： A61K51/00 , C07F15/00 , C07D401/10 , A61K31/555 , A61K49/00 , A61P43/00 , A61K49/06
CPC分类号： C07D401/04 , A61K49/0017 , A61K51/0453 , A61K51/0478 , C07F15/0093
摘要： The present invention relates to a transition metal complex represented by Formula (I) or salts thereof, or to a ligand represented by Formula (H) or salts thereof, wherein X represents a transition metal, preferably Pt, and methods for their use and preparation. In particular, the invention relates to compounds which may possess useful therapeutic activity in treating amyloid diseases, and in particular, Alzheimer's disease. The invention also relates to the use of these compounds in methods of therapy, and diagnosis, and the manufacture of medicaments as well as compositions containing these compounds.
摘要翻译：本发明涉及由式（I）表示的过渡金属络合物或其盐，或由式（H）表示的配体或其盐，其中X表示过渡金属，优选Pt，及其用途及制备方法。特别地，本发明涉及在治疗淀粉样蛋白病，特别是阿尔茨海默病方面具有有用治疗活性的化合物。本发明还涉及这些化合物在治疗，诊断和制备药物以及含有这些化合物的组合物的方法中的用途。

3. 发明申请

US20120270850A1 METAL DELIVERY AGENTS AND THERAPEUTIC USES OF THE SAME 审中-公开
标题翻译：金属递送剂及其相应的治疗用途
公开(公告)号：US20120270850A1
公开(公告)日：2012-10-25
申请号：US12515473
申请日：2007-11-20
申请人： Kevin Jeffrey Barnham , Paul Stephen Donnelly , Anthony Robert White
发明人： Kevin Jeffrey Barnham , Paul Stephen Donnelly , Anthony Robert White
IPC分类号： A61K31/555 , A61P25/00 , A61P35/00 , A61P25/28 , A61P9/10 , A61P27/12 , A61P25/08 , A61P27/06 , A61P25/14 , A61P1/00 , A61P27/02 , A61P33/06 , A61P25/16 , A61P25/18 , C12N5/07 , A61K31/315 , A61K31/30 , A61P9/00
CPC分类号： A61K31/555 , A61K31/145 , A61K31/28 , A61K31/30 , A61K31/315 , C07F1/08 , C07F3/06
摘要： The present invention relates to metal complexes, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment of conditions in which metal delivery can prevent, alleviate or ameliorate the condition. There are a number of clinical conditions which are caused by or associated with abnormal levels of metals (typically low metal levels). Conditions in of this type include cancer and conditions characterised by or associated with oxidative damage, more specifically neurodegenerative conditions such as Alzheimer's disease, Parkinson's disease or Huntington's disease. The invention also relates to ligands useful in the preparation of metal complexes of this type.
摘要翻译：本发明涉及金属络合物，其制备方法及其作为药物或兽用剂的用途，特别是用于治疗金属递送可以预防，减轻或改善病症的病症。有许多由金属异常水平引起或与异常水平相关的临床病症（通常为低金属水平）。这种类型的病症包括特征在于氧化损伤或与氧化损伤相关的癌症和病症，更具体地是神经变性疾病如阿尔茨海默病，帕金森病或亨廷顿病。本发明还涉及可用于制备这种金属络合物的配体。

4. 发明授权

US07704987B1 β-amyloid peptide inhibitors 有权
标题翻译：淀粉样蛋白肽抑制剂
公开(公告)号：US07704987B1
公开(公告)日：2010-04-27
申请号：US10031478
申请日：2000-07-21
申请人： Kevin Jeffrey Barnham , Thomas David McCarthy , Susanne Pallich , Barry Ross Matthews , Robert Alan Cherny
发明人： Kevin Jeffrey Barnham , Thomas David McCarthy , Susanne Pallich , Barry Ross Matthews , Robert Alan Cherny
IPC分类号： A61K31/555 , A61K31/4745 , C07D471/14
CPC分类号： C07K14/4711 , A61K38/00 , A61K47/54 , A61K47/547
摘要： The present invention relates to compounds which inhibit the binding of metal ions to a region in the N-terminal loop of the β-amyloid peptide which includes a cluster of histidine residues. In addition, the invention relates to pharmaceutical compositions including these compounds as the active agent, and to methods of treatment involving the administration of these compounds. The compounds of the invention are useful in the treatment of Alzheimer's Disease and other amyloid-related conditions. In a first aspect the present invention provides a compound which interacts with the β-amyloid peptide in such a way that the N-terminal loop of the peptide (amino acid residues 1-15) is blocked or destabilised, thereby inhibiting the binding of one or more metal ions to at least one histidine residue within the N-terminal loop. Preferably the compound inhibits binding of Cu2+, Zn2+ and Fe3+ ions, but not Mg2+ or Ca2+ ions.
摘要翻译：本发明涉及抑制金属离子与包含一组组氨酸残基的β-淀粉状蛋白肽的N-末端环区域的结合的化合物。此外，本发明涉及包含这些化合物作为活性剂的药物组合物以及涉及施用这些化合物的治疗方法。本发明的化合物可用于治疗阿尔茨海默病和其他淀粉样蛋白相关病症。在第一方面，本发明提供了一种与β-淀粉样蛋白肽相互作用的化合物，使得肽（氨基酸残基1-15）的N-末端环被阻断或不稳定，从而抑制一个或多个金属离子至N末端环内的至少一个组氨酸残基。优选地，化合物抑制Cu 2+，Zn 2+和Fe 3+离子而不是Mg 2+或Ca 2+离子的结合。

5. 发明授权

US07692011B2 8-hydroxy and 8-mercapto quinazolinones 有权
标题翻译： 8-羟基和8-巯基喹唑啉酮
公开(公告)号：US07692011B2
公开(公告)日：2010-04-06
申请号：US10530137
申请日：2003-10-03
申请人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
发明人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
IPC分类号： C07D239/70
CPC分类号： A61K31/4375 , A61K31/435 , A61K31/436 , A61K31/47 , A61K31/473 , A61K31/4745 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/5025 , A61K31/517 , A61K31/519 , C07C233/54 , C07D239/88 , C07D241/42 , C07D471/04
摘要： The present invention relates to neurologically active 8-hydroxy- or 8-mercapto-quinazolinones. Also disclosed are processes for the preparation of these compounds and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions, such as Alzheimer's disease.
摘要翻译：本发明涉及神经活性8-羟基或8-巯基喹唑啉酮。还公开了用于制备这些化合物的方法及其作为药物或兽药的用途，特别是用于治疗神经病症，更具体地说是神经变性病症如阿尔茨海默氏病。

6. 发明授权

US07619091B2 8-hydroxy quinoline derivatives 有权
标题翻译： 8-羟基喹啉衍生物
公开(公告)号：US07619091B2
公开(公告)日：2009-11-17
申请号：US10521902
申请日：2003-07-16
申请人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Guy Krippner
发明人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Guy Krippner
IPC分类号： C07D215/38
CPC分类号： C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要： The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.
摘要翻译：本发明涉及一种治疗，改善和/或预防神经系统疾病，特别是神经变性疾病的方法，其包括向有需要的受试者施用有效量的式（I）化合物。本发明还涉及式（II）的化合物及其制备方法。

7. 发明申请

US20100160346A1 NEUROLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：神经活性化合物
公开(公告)号：US20100160346A1
公开(公告)日：2010-06-24
申请号：US12717631
申请日：2010-03-04
申请人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
发明人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： A61K31/4375 , A61K31/435 , A61K31/436 , A61K31/47 , A61K31/473 , A61K31/4745 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/5025 , A61K31/517 , A61K31/519 , C07C233/54 , C07D239/88 , C07D241/42 , C07D471/04
摘要： The present invention relates to neurologically-active compounds, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions such as Alzheimer's disease.
摘要翻译：本发明涉及神经活性化合物，其制备方法及其作为药物或兽药的用途，特别是用于治疗神经病症，更具体地说是神经变性疾病如阿尔茨海默病。

8. 发明申请

US20110263450A1 ALZHEIMER'S DISEASE BIOMARKERS 审中-公开
标题翻译：阿尔茨海默病的生物标志物
公开(公告)号：US20110263450A1
公开(公告)日：2011-10-27
申请号：US13121119
申请日：2009-09-25
申请人： Kevin Jeffrey Barnham , Victor Luis Villemagne , Kayla Azorena Perez Camacaro
发明人： Kevin Jeffrey Barnham , Victor Luis Villemagne , Kayla Azorena Perez Camacaro
IPC分类号： C40B30/04 , C07K2/00 , C07K14/435 , C40B40/10 , G01N33/53
CPC分类号： G01N33/6896 , G01N33/6848 , G01N2333/4709 , G01N2800/2821
摘要： The invention provides a biomarker for qualifying Alzheimer's disease status, the biomarker being detectable in a biological sample containing blood cellular elements and being derived from amyloid precursor protein or amyloid β peptide. Particularly the biomarker includes an Aβ 1-42 or Aβ 1-43 species (monomer) and, or an Aβ 1-42 dimer. An alternative or additional biomarker includes an APP cathepsin D cleavage product or includes a biomarker identifiable by a peak of molecular weight of about 9962 or 9980 Daltons when identified by SELDI-TOF MS utilising antibody WO2.
摘要翻译：本发明提供了用于鉴定阿尔茨海默氏病状态的生物标志物，该生物标志物可在含有血液细胞元件的生物样品中检测并且衍生自淀粉样蛋白前体蛋白或淀粉样蛋白; 肽。特别是生物标志物包括A＆bgr; 1-42或A＆bgr; 1-43种（单体），或A＆bgr; 1-42二聚体。替代或额外的生物标志物包括APP组织蛋白酶D切割产物，或者包括当通过SELDI-TOF MS利用抗体WO2鉴定时，通过分子量为约9962或9980道尔顿的峰可鉴定的生物标志物。

9. 发明申请

US20080161353A1 8-Hydroxy quinoline derivatives 有权
标题翻译： 8-羟基喹啉衍生物
公开(公告)号：US20080161353A1
公开(公告)日：2008-07-03
申请号：US11901941
申请日：2007-09-19
申请人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Guy Krippner
发明人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Guy Krippner
IPC分类号： A61K31/4725 , A61P25/00 , A61K31/47
CPC分类号： C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要： The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
摘要翻译：本发明描述了治疗受试者神经学病症的方法，其包括向有需要的受试者施用治疗有效量的下式化合物或其药学上可接受的盐，水合物或溶剂化物。

10. 发明授权

US08975278B2 8-hydroxy quinoline derivatives 有权
公开(公告)号：US08975278B2
公开(公告)日：2015-03-10
申请号：US11901941
申请日：2007-09-19
申请人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Guy Krippner
发明人： Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Guy Krippner
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00 , C07D215/38 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/26 , C07D215/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14
CPC分类号： C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要： The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.

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