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1. 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。

2. 发明授权

US06740635B2 Antiviral linear polymers 失效
标题翻译：抗病毒线性聚合物
公开(公告)号：US06740635B2
公开(公告)日：2004-05-25
申请号：US09929014
申请日：2001-08-15
申请人： Barry Ross Matthews , George Holan
发明人： Barry Ross Matthews , George Holan
IPC分类号： A61K31795
CPC分类号： C08G69/10
摘要： An antiviral compound comprises a linear non-carbohydrate polymer having a plurality of side chain groups, wherein at least one of the side chain groups has an anionic- or cationic-containing moiety bonded or linked thereto.
摘要翻译：抗病毒化合物包含具有多个侧链基团的线性非碳水化合物聚合物，其中至少一个侧链基团具有与其结合或连接的阴离子或阳离子部分。

3. 发明授权

US06464971B1 Anionic or cationic dendrimer antimicrobial or autiprotozoan compositions 有权
标题翻译：阴离子或阳离子树枝状大分子抗微生物剂或自由基组合物
公开(公告)号：US06464971B1
公开(公告)日：2002-10-15
申请号：US09786913
申请日：2001-05-08
申请人： Barry Ross Matthews , George Holan
发明人： Barry Ross Matthews , George Holan
IPC分类号： A61K31785
CPC分类号： A61K31/00 , Y10S424/16
摘要： To inhibit, prophylactically or therapeutically, a bacterial, yeast, fungal, or parasitic agent in a patient, an effective amount of a dendrimer is administered to the patient, which dendrimer has a plurality of terminal groups, at least one of which has an anionic- or cationic-moiety covalently bonded or linked thereto. The anionic-containing moiety is not a disaccharide or oligosaccharide moiety, and, where the anionic-containing moiety is a neuraminic- or sialic acid-containing. moiety, it is modified in the 4-position by substitution with an amino, amido, cyano, azido or guanido group, or is unsaturated.
摘要翻译：为了在患者体内抑制或治疗细菌，酵母，真菌或寄生虫，向患者施用有效量的树枝状大分子，该树枝状聚合物具有多个端基，其中至少一个具有阴离子 - 或阳离子部分共价键合或连接。含阴离子的部分不是二糖或寡糖部分，并且其中含阴离子的部分是含神经氨酸或唾液酸的部分。部分，通过用氨基，酰胺基，氰基，叠氮基或胍基取代被4-位修饰，或是不饱和的。

4. 发明授权

US08158575B2 Agent for the prevention and treatment of sexually transmitted diseases-I 有权
标题翻译：预防和治疗性传播疾病的代理 - 我
公开(公告)号：US08158575B2
公开(公告)日：2012-04-17
申请号：US12498077
申请日：2009-07-06
申请人： Barry Ross Matthews , George Holan , Peter Karellas , Scott Andrew Henderson , David Francis O'Keefe
发明人： Barry Ross Matthews , George Holan , Peter Karellas , Scott Andrew Henderson , David Francis O'Keefe
IPC分类号： A01N61/00
CPC分类号： B82Y5/00 , A61K47/59 , A61K47/595 , A61K47/645 , A61K47/6949 , C08G69/10 , C08G83/003 , Y10S977/754
摘要： Use of a polylysine, polyamidoamine or polypropylenimine dendrimer having naphthyl disulphonate terminal groups as a topically applied agent in prophylaxis or treatment of sexually transmitted diseases.
摘要翻译：具有萘基二磺酸酯末端基团的聚赖氨酸，聚酰胺胺或聚丙烯亚胺树枝状大分子作为局部施用剂在预防或治疗性传播疾病中的应用。

5. 发明授权

US07572459B2 Anionic or cationic dendrimer antimicrobial or antiparasitic compositions 失效
标题翻译：阴离子或阳离子树枝状大分子抗微生物或抗寄生虫组合物
公开(公告)号：US07572459B2
公开(公告)日：2009-08-11
申请号：US10227538
申请日：2002-08-26
申请人： Barry Ross Matthews , George Holan
发明人： Barry Ross Matthews , George Holan
IPC分类号： A01N25/00 , A01N33/00 , A61K31/13 , A61K31/16
CPC分类号： A61K31/00 , Y02A50/411
摘要： To inhibit, prophylactically or therapeutically, a bacterial, yeast, fungal, or parasitic agent in a patient, an effective amount of a dendrimer is administered to the patient, which dendrimer has a plurality of terminal groups, at least one of which has an anionic- or cationic-moiety covalently bonded or linked thereto. The anionic-containing moiety is not a disaccharide or oligosaccharide moiety, and, where the anionic-containing moiety is a neuraminic- or sialic acid-containing moiety, it is modified in the 4-position by substitution with an amino, amido, cyano, azido or guanido group, or is unsaturated.
摘要翻译：为了在患者体内抑制或治疗细菌，酵母，真菌或寄生虫，向患者施用有效量的树枝状大分子，该树枝状聚合物具有多个端基，其中至少一个具有阴离子 - 或阳离子部分共价键合或连接。含阴离子的部分不是二糖或寡糖部分，并且其中含阴离子的部分是含有神经氨酸或唾液酸的部分，其通过用氨基，酰氨基，氰基，叠氮基或胍基，或不饱和的。

6. 发明授权

US06426067B1 Angiogenic inhibitory compounds 失效
标题翻译：血管生成抑制性化合物
公开(公告)号：US06426067B1
公开(公告)日：2002-07-30
申请号：US09230188
申请日：1999-03-22
申请人： Barry Ross Matthews , George Holan
发明人： Barry Ross Matthews , George Holan
IPC分类号： A61K3174
CPC分类号： C08G83/003 , A61K31/795 , C08G69/10 , Y10S424/16
摘要： For proposes of prophylactic or treatment of diseases related to inappropriate angiogenesis, a compound can be administered that is (i) a linear, non-carbohydrate polymer having a plurality of side chain groups or (ii) a dendrimer having a plurality of terminal groups. At least one of the side chain groups of the linear, non-carbohydrate polymer has an anionic- or cationic-containing moiety bonded or linked thereto. The plurality of terminal groups of the dendrimer has at least one anionic- or cationic-containing moiety bonded or linked thereto.
摘要翻译：对于与不适当血管发生相关的疾病的预防或治疗的建议，可以给予化合物，其为（i）具有多个侧链基团的线性，非碳水化合物聚合物或（ii）具有多个末端基团的树枝状聚合物。线性非碳水化合物聚合物的至少一个侧链基团具有与其结合或连接的含阴离子或阳离子的部分。树枝状聚合物的多个端基具有至少一个与阴离子或阳离子结合或连接的部分。

7. 发明授权

US07589056B2 Agent for the prevention and treatment of sexually transmitted diseases-I 有权
标题翻译：预防和治疗性传播疾病的代理 - 我
公开(公告)号：US07589056B2
公开(公告)日：2009-09-15
申请号：US10472439
申请日：2002-03-28
申请人： Barry Ross Matthews , George Holan , Peter Karellas , Scott Andrew Henderson , David Francis O'Keefe
发明人： Barry Ross Matthews , George Holan , Peter Karellas , Scott Andrew Henderson , David Francis O'Keefe
IPC分类号： A01N61/00
CPC分类号： B82Y5/00 , A61K47/59 , A61K47/595 , A61K47/645 , A61K47/6949 , C08G69/10 , C08G83/003 , Y10S977/754
摘要： Use of a polylysine, polyamidoamine or polypropylenimine dendrimer having naphthyl disulphonate terminal groups as a topically applied agent in prophylaxis or treatment of sexually transmitted diseases.
摘要翻译：具有萘基二磺酸酯末端基团的聚赖氨酸，聚酰胺胺或聚丙烯亚胺树枝状大分子作为局部施用的药物用于预防或治疗性传播疾病。

8. 发明授权

US06190650B1 Antiviral dendrimers 失效
标题翻译：抗病毒树枝状大分子
公开(公告)号：US06190650B1
公开(公告)日：2001-02-20
申请号：US08765528
申请日：1997-04-28
申请人： Barry Ross Matthews , George Holan
发明人： Barry Ross Matthews , George Holan
IPC分类号： A61K3178
CPC分类号： B82Y5/00 , A61K31/785 , A61K31/787 , A61K31/795 , A61K47/595 , A61K47/645 , A61K47/6949 , C08G69/10 , C08G69/48 , C08G83/003 , Y10S424/16
摘要： An antiviral compound comprises a dendrimer such as a polyamidoamine or polyly sine dendrimer having a plurality of terminal groups, wherein at least one of the terminal groups has an anionic- or cationic-containing moiety bonded thereto, particularly a sulfonic acid-containing, carboxylic acid-containing or trimethylammonium-containing moiety or the like.
摘要翻译：抗病毒化合物包括具有多个端基的树状聚合物如聚酰胺胺或聚正辛醛树枝状聚合物，其中至少一个端基具有与其结合的含阴离子或阳离子的部分，特别是含磺酸的羧酸或含三甲基铵的部分等。

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