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公开(公告)号：US09095587B2
公开(公告)日：2015-08-04
申请号：US13522228
申请日：2011-01-19
IPC分类号： A61K31/472 , A61K31/437 , A61K31/4375 , A61K31/522
CPC分类号： A61K31/472 , A61K31/437 , A61K31/4375 , A61K31/522
摘要： The present invention provides methods and compositions for the effective treatment of impaired nerve signal conduction. Compositions including selective AT2 receptor antagonists as active agents and methods of use in relation to improving nerve signal conduction or reversing impaired nerve signal conduction are described.
摘要翻译： 本发明提供用于有效治疗受损的神经信号传导的方法和组合物。 描述了包括选择性AT2受体拮抗剂作为活性剂的组合物和用于改善神经信号传导或逆转受损神经信号传导的方法。
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公开(公告)号：US20130131103A1
公开(公告)日：2013-05-23
申请号：US13522228
申请日：2011-01-19
IPC分类号： A61K31/472 , A61K31/437
CPC分类号： A61K31/472 , A61K31/437 , A61K31/4375 , A61K31/522
摘要： The present invention provides methods and compositions for the effective treatment of impaired nerve signal conduction. Compositions including selective AT2 receptor antagonists as active agents and methods of use in relation to improving nerve signal conduction or reversing impaired nerve signal conduction are described.
摘要翻译： 本发明提供用于有效治疗受损的神经信号传导的方法和组合物。 描述了包括选择性AT2受体拮抗剂作为活性剂的组合物和用于改善神经信号传导或逆转受损神经信号传导的方法。
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公开(公告)号：US20120022101A1
公开(公告)日：2012-01-26
申请号：US13187882
申请日：2011-07-21
申请人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
发明人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
IPC分类号： A61K31/47 , A61P25/00 , C07D217/04
CPC分类号： C07D217/26 , A61K31/47
摘要： (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
摘要翻译： 与其钠盐和溶剂化物一起描述基本上纯的形式的（S）-2-（二苯基乙酰基）-1,2,3,4-四氢-6-甲氧基-5-（苯基甲氧基）-3-异喹啉羧酸。 还描述了制备化合物，其钠盐及其溶剂合物的方法和包含它们的药物组合物。
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公开(公告)号：US20150218180A1
公开(公告)日：2015-08-06
申请号：US14373357
申请日：2013-01-25
发明人： Thomas David McCarthy , Alan Naylor
IPC分类号： C07D491/056 , C07D211/60 , C07D401/04 , C07D471/04
CPC分类号： C07D491/056 , C07D211/60 , C07D401/04 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
摘要翻译： 本发明涉及可用于拮抗血管紧张素II型2型（AT2）受体的杂环化合物。 更具体地，本发明涉及哌啶化合物，含有它们的组合物及其在治疗或预防与AT2受体功能相关的病症或疾病的方法中的用途，包括神经性疼痛，炎性疼痛，与神经元超敏反应相关的病症，神经传导速度受损，细胞增殖紊乱 ，与骨吸收和骨形成之间的不平衡相关的疾病以及与异常神经再生相关的疾病。
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公开(公告)号：US08193248B2
公开(公告)日：2012-06-05
申请号：US12294024
申请日：2007-03-21
CPC分类号： A61K31/785 , Y10S977/754
摘要： The present invention relates to a contraceptive composition including an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor. The contraceptive composition may also exhibit antimicrobial activity. The invention also relates to a method of selectively reducing or preventing conception in a female animal, including a human, which method includes administering to the animal an effective amount of a contraceptive composition which composition includes an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor.
摘要翻译： 本发明涉及一种避孕组合物，其包含有效量的包含一个或多个萘基二磺酸表面基团的树枝状大分子化合物，或其树枝状大分子化合物的药学上可接受的盐或溶剂合物; 和其药学上可接受的载体，赋形剂和/或稀释剂。 避孕组合物还可以表现出抗微生物活性。 本发明还涉及在女性动物（包括人）中选择性地减少或预防受孕的方法，该方法包括向动物施用有效量的避孕组合物，该组合物包含有效量的包括一种或多种的树突状化合物 萘基二磺酸表面基团，或其树枝状大分子化合物的药学上可接受的盐或溶剂合物; 和其药学上可接受的载体，赋形剂和/或稀释剂。
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公开(公告)号：US20100252050A1
公开(公告)日：2010-10-07
申请号：US12090580
申请日：2006-02-01
CPC分类号： A61K9/0034 , A01N41/04
摘要： A microbicidal delivery system including: a microbicidal composition including a microbicidal compound including a dendrimer including one or more surface groups of formula (IV); a microbicidally active derivative thereof, or pharmaceutically acceptable salt or solvate thereof; and a carrier, excipient or diluent therefor; and a prophylactic device; the microbicidal composition being carried on a surface of the prophylactic device and being compatible therewith.
摘要翻译： 一种杀菌剂输送系统，包括：杀菌组合物，其包含包含一种或多种式（IV）表面基团的树枝状大分子的杀菌化合物; 其杀微生物活性衍生物或其药学上可接受的盐或溶剂合物; 及其载体，赋形剂或稀释剂; 和预防装置; 所述杀微生物组合物携带在所述预防装置的表面上并与之相容。
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公开(公告)号：US08568753B2
公开(公告)日：2013-10-29
申请号：US12090580
申请日：2006-02-01
IPC分类号： A01N25/10 , A01N41/04 , A61F6/04 , A61F6/06 , A61K31/785
CPC分类号： A61K9/0034 , A01N41/04
摘要： A microbicidal delivery system including: a microbicidal composition including a microbicidal compound including a dendrimer including one or more surface groups of formula (IV); a microbicidally active derivative thereof, or pharmaceutically acceptable salt or solvate thereof; and a carrier, excipient or diluent therefor; and a prophylactic device; the microbicidal composition being carried on a surface of the prophylactic device and being compatible therewith.
摘要翻译： 一种杀菌剂输送系统，包括：杀菌组合物，其包含包含一种或多种式（IV）表面基团的树枝状大分子的杀菌化合物; 其杀微生物活性衍生物或其药学上可接受的盐或溶剂合物; 及其载体，赋形剂或稀释剂; 和预防装置; 所述杀微生物组合物携带在所述预防装置的表面上并与之相容。
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公开(公告)号：US08614227B2
公开(公告)日：2013-12-24
申请号：US13187882
申请日：2011-07-21
申请人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
发明人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
IPC分类号： C07D217/06 , A61K31/47
CPC分类号： C07D217/26 , A61K31/47
摘要： (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
摘要翻译： 与其钠盐和溶剂化物一起描述基本上纯的形式的（S）-2-（二苯基乙酰基）-1,2,3,4-四氢-6-甲氧基-5-（苯基甲氧基）-3-异喹啉羧酸。 还描述了制备化合物，其钠盐及其溶剂合物的方法和包含它们的药物组合物。
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公开(公告)号：US20090275507A1
公开(公告)日：2009-11-05
申请号：US12294024
申请日：2007-03-21
CPC分类号： A61K31/785 , Y10S977/754
摘要： The present invention relates to a contraceptive composition including an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor. The contraceptive composition may also exhibit antimicrobial activity. The invention also relates to a method of selectively reducing or preventing conception in a female animal, including a human, which method includes administering to the animal an effective amount of a contraceptive composition which composition includes an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor.
摘要翻译： 本发明涉及一种避孕组合物，其包含有效量的包含一个或多个萘基二磺酸表面基团的树枝状大分子化合物，或其树枝状大分子化合物的药学上可接受的盐或溶剂合物; 和其药学上可接受的载体，赋形剂和/或稀释剂。 避孕组合物还可以表现出抗微生物活性。 本发明还涉及一种在女性动物（包括人）中选择性地减少或预防受孕的方法，该方法包括向动物施用有效量的避孕组合物，该组合物包含有效量的包括一种或多种的树突状化合物 萘基二磺酸表面基团，或其树枝状大分子化合物的药学上可接受的盐或溶剂合物; 和其药学上可接受的载体，赋形剂和/或稀释剂。
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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。
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