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31. 发明授权

US08067549B2 Humanized antibodies and compositions for binding sphingosine-1-phosphate 有权
标题翻译：用于结合鞘氨醇-1-磷酸的人源化抗体和组合物
公开(公告)号：US08067549B2
公开(公告)日：2011-11-29
申请号：US12258337
申请日：2008-10-24
申请人： Roger A. Sabbadini , William A. Garland , Genevieve Hansen , Steven Tarran Jones , David Gareth Williams
发明人： Roger A. Sabbadini , William A. Garland , Genevieve Hansen , Steven Tarran Jones , David Gareth Williams
IPC分类号： C07K16/00 , C12P21/08 , A61K39/395 , A61K39/00
CPC分类号： C07K16/44 , A61K2039/505 , C07K2317/24 , C07K2317/56 , C07K2317/565
摘要： The present invention relates to anti-S1P agents, particularly humanized monoclonal antibodies (and antigen binding fragments thereof) specifically reactive with S1P, compositions containing such antibodies (or fragments), and the use of such antibodies (or fragments), for example, to treat diseases and conditions associated with aberrant levels of S1P.
摘要翻译：本发明涉及与S1P特异性反应的抗S1P试剂，特别是人源化单克隆抗体（及其抗原结合片段），含有此类抗体（或片段）的组合物，以及使用这种抗体（或片段），例如治疗与S1P异常水平相关的疾病和病症。

32. 发明申请

US20110143153A1 Biocide composition comprising pyrithione and pyrrole derivatives 有权
公开(公告)号：US20110143153A1
公开(公告)日：2011-06-16
申请号：US12930419
申请日：2011-01-06
申请人： Craig Waldron , Robert Martin , Gareth Williams , Tina Williams
发明人： Craig Waldron , Robert Martin , Gareth Williams , Tina Williams
IPC分类号： B32B15/08 , B32B21/04 , B32B9/02 , B32B15/04 , B32B27/00 , B32B21/08 , B32B27/30
CPC分类号： C09D5/1625 , A01N43/36 , C09D5/14 , Y10T428/31678 , Y10T428/31699 , Y10T428/31855 , Y10T428/31906 , Y10T428/31935 , Y10T428/31989 , A01N43/40 , A01N59/16 , A01N59/20 , A01N2300/00
摘要： The present invention is directed to a biocidal composition comprising a blend of one or more pyrithione compounds, and one or more pyrrole compounds of Formula I wherein said biocidal composition is copper free or low copper content.

33. 发明授权

US07956173B2 Nucleic acids coding for humanized antibodies for binding sphingosine-1-phosphate 有权
标题翻译：编码用于结合鞘氨醇-1-磷酸的人源化抗体的核酸
公开(公告)号：US07956173B2
公开(公告)日：2011-06-07
申请号：US12258353
申请日：2008-10-24
申请人： Roger A. Sabbadini , William A. Garland , Genevieve Hansen , Steven Tarran Jones , David Gareth Williams
发明人： Roger A. Sabbadini , William A. Garland , Genevieve Hansen , Steven Tarran Jones , David Gareth Williams
IPC分类号： C07H21/04 , C07K16/00 , C12P21/08 , A61K39/395 , A61K39/00
CPC分类号： C07K16/44 , A61K2039/505 , C07K2317/24 , C07K2317/56 , C07K2317/565
摘要： The present invention relates to anti-S1P agents, particularly humanized monoclonal antibodies (and antigen binding fragments thereof) specifically reactive with S1P, compositions containing such antibodies (or fragments), and the use of such antibodies (or fragments), for example, to treat diseases and conditions associated with aberrant levels of S1P.
摘要翻译：本发明涉及与S1P特异性反应的抗S1P试剂，特别是人源化单克隆抗体（及其抗原结合片段），含有此类抗体（或片段）的组合物，以及使用这种抗体（或片段），例如治疗与S1P异常水平相关的疾病和病症。

34. 发明申请

US20110039920A1 INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE 审中-公开
标题翻译： IKK-BETA丝氨酸蛋白激酶激酶的抑制剂
公开(公告)号：US20110039920A1
公开(公告)日：2011-02-17
申请号：US12989022
申请日：2008-04-23
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
IPC分类号： A61K31/381 , C07D333/38 , C12N9/99 , A61P35/00 , A61P37/06 , A61P29/00 , A61P19/02 , A61P3/10 , A61P11/06 , A61P1/04 , A61P25/28
CPC分类号： C07D333/38
摘要： Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
摘要翻译：（2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5（氨基甲酰基氨基）-2-噻吩基]苯基}戊-4-烯酸酯; 5- {3- [4-氨甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-降冰片烯环戊酯; （2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -5-甲基苯基}戊-4-烯酸酯; 环戊基（25,4E）-2-氨基-5- {5- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -2-甲基苯基}戊-4-烯酸酯; 环戊基O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; 环戊基O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸酯的环戊基酯; 和N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸叔丁酯通过细胞内羧酸酯酶水解成相应的羧酸，并且可用于抑制IKK和bgr; 活动。

35. 发明申请

US20090131327A1 NOGO RECEPTOR FUNCTIONAL MOTIFS AND PEPTIDE MIMETICS RELATED THERETO AND METHODS OF USING THE SAME 审中-公开
标题翻译：与其相关的NOGO受体功能运动和肽类物质及其使用方法
公开(公告)号：US20090131327A1
公开(公告)日：2009-05-21
申请号：US11913032
申请日：2006-04-28
申请人： Patrick Doherty , Gareth Williams
发明人： Patrick Doherty , Gareth Williams
IPC分类号： A61K38/08 , C07K7/00 , G01N33/566 , C07K16/18 , A61K38/07 , C12N5/06
CPC分类号： G01N33/6872 , A61K38/00 , C07K14/705 , G01N33/6896 , G01N2500/00 , G01N2800/28
摘要： The present invention provides novel isolated and purified polynucleotides and polypeptides related to functional motifs of the Nogo receptor 1 (NgR1) and use of peptides mimicking these functional motifs as antagonists to NgR1 ligands, e.g., myelin-associated glycoprotein, oligodendrocyte myelin glycoprotein, Nogo-A, Nogo-66, an antibody to Nogo receptor, an antibody to GT1b, an antibody to p75 neurotrophin receptor, and an antibody to Lingo-1, etc. The invention also provides antibodies to the mimetic peptide antagonists. The present invention is further directed to novel therapeutics and therapeutic targets and to methods of screening and assessing test compounds for treatments requiring axonal regeneration, i.e., reversal of the effects of NgR1 ligand binding to the NgR1 (i.e., producing inhibition of axonal growth). The present invention also is directed to novel methods for treating disorders arising from inhibition of axonal growth mediated by the binding of NgR1 ligands to the NgR1.
摘要翻译：本发明提供与Nogo受体1（NgR1）的功能基序相关的新型分离和纯化的多核苷酸和多肽，以及模仿这些功能基序的肽作为NgR1配体的拮抗剂的使用，例如髓磷脂相关糖蛋白，少突胶质细胞髓鞘糖蛋白，Nogo- A，Nogo-66，Nogo受体的抗体，GT1b的抗体，p75神经营养因子受体的抗体，以及Lingo-1的抗体等。本发明还提供了针对模拟肽拮抗剂的抗体。本发明还涉及新的治疗学和治疗靶标，以及筛选和评估需要轴突再生的治疗的试验化合物的方法，即逆转NgR1配体结合NgR1的作用（即产生轴突生长的抑制）。本发明还涉及用于治疗由NgR1配体与NgR1结合介导的轴突生长抑制引起的疾病的新方法。

36. 发明申请

US20080069938A1 COHESIVE NON-FREE FLOWING SWEETENER COMPOSITIONS INCLUDING LOW-CALORIE INGREDIENTS 审中-公开
标题翻译：包含低卡路里成分的非自由流动感觉器组合
公开(公告)号：US20080069938A1
公开(公告)日：2008-03-20
申请号：US11532885
申请日：2006-09-18
申请人： Renny Ison , Melanie Loades , Gareth Williams
发明人： Renny Ison , Melanie Loades , Gareth Williams
IPC分类号： A23L1/236
CPC分类号： A23L27/37 , A23L27/32 , A23L27/33 , A23L27/34 , A23L29/35
摘要： Cohesive non-free flowing sweetener compositions, e.g., sweetener cubes, useful for adding sweetness to liquid foodstuffs, for example, beverages, having a reduced caloric burden as compared to conventional sucrose cubes, are provided. More particularly, a cohesive non-free flowing sweetener composition containing a high intensity sweetener and a low-calorie bulking agent, wherein a sweetener cube formed from the cohesive non-free flowing sweetener composition has a lower caloric burden than that of a conventional sucrose cube of about the same dimensions and an equivalent sweetness. Also provided are sweetener cubes containing sucralose, polydextrose, trehalose, erythritol, tagatose, and/or lactose, wherein the sweetener cubes have a caloric burden of about 0.2, about 1, about 2, about 3, or about 4 kilocalories per cube and a sweetness equivalent to about one teaspoon of sucrose. Methods of making such cohesive non-free flowing sweetener compositions are also provided.
摘要翻译：提供了与常规蔗糖立方体相比具有降低热量负担的液体食品例如饮料中的甜味剂的粘性非自由流动甜味剂组合物，例如增甜剂立方体。更具体地，包含高强度甜味剂和低热量填充剂的粘性非自由流动甜味剂组合物，其中由粘性非自由流动甜味剂组合物形成的甜味剂立方体具有比常规蔗糖立方体低的热量负担大约相同的尺寸和相当的甜度。还提供了含有三氯蔗糖，聚右旋糖，海藻糖，赤藓糖醇，塔格糖和/或乳糖的甜味剂立方体，其中甜味剂立方体具有每立方体约0.2，约1，约2，约3或约4千卡的热量负担，相当于约一茶匙蔗糖的甜度。还提供制备这种内聚非自由流动甜味剂组合物的方法。

37. 发明申请

US20080069937A1 BALANCING HEAT OF SOLUTION IN NON-FREE FLOWING SWEETENER COMPOSITIONS 审中-公开
标题翻译：解决方案的平衡热量在非自由流动的SWEETENER组合物中
公开(公告)号：US20080069937A1
公开(公告)日：2008-03-20
申请号：US11532880
申请日：2006-09-18
申请人： Renny Ison , Melanie Loades , Gareth Williams
发明人： Renny Ison , Melanie Loades , Gareth Williams
IPC分类号： A23L1/236
CPC分类号： A23L27/33 , A23L27/30
摘要： Cohesive non-free flowing sweetener composition for adding sweetness to liquid foodstuffs, for example, beverages, having a reduced caloric burden as compared to a conventional sucrose cubes of the same dimensions, are provided. More particularly, a cohesive non-free flowing sweetener composition containing a high intensity sweetener and a bulking agent with a negative heat of solution in an amount sufficient to produce a total heat of solution in the cohesive non-free flowing sweetener composition of from about 5 kilocalories to about −20 kilocalories, and a lower caloric burden and an equivalent sweetness compared to that of a conventional sucrose cube of the same dimensions. Also provided is a sweetener cube comprising a high intensity sweetener, a bulking agent, and a compound with a positive heat of solution in an amount sufficient to produce a total heat of solution in the sweetener cube between about 5 kilocalories and about —20 kilocalories, wherein the cohesive non-free flowing sweetener composition has a lower caloric burden and an equivalent sweetness compared to that of a conventional sucrose cube of the same dimensions. Methods of making such sweetener cubes are also provided.
摘要翻译：提供了与相同尺寸的常规蔗糖立方体相比，具有降低热量负担的液体食品例如饮料的甜味的粘性非自由流动甜味剂组合物。更具体地说，一种含有高强度甜味剂和填充剂的内聚非自由流动的甜味剂组合物，其具有足够的量的足够的热量以产生粘性非自由流动的甜味剂组合物中的溶液的总热量为约5 千卡达到约-20千卡，并且与相同尺寸的常规蔗糖立方体相比，具有较低的热量负担和相当的甜度。还提供了一种甜味剂立方体，其包含高强度甜味剂，填充剂和具有足以在甜味剂立方体中产生约5千卡和约-20千卡之间的溶液总热量的正溶解热的化合物，其中与相同尺寸的常规蔗糖立方体相比，内聚非自由流动甜味剂组合物具有较低的热量负担和相当的甜度。还提供了制备这种甜味剂立方体的方法。

38. 发明授权

US07196061B2 Compounds that modulate neuronal growth and their uses 失效
标题翻译：调节神经元生长及其用途的化合物
公开(公告)号：US07196061B2
公开(公告)日：2007-03-27
申请号：US10938409
申请日：2004-09-09
申请人： Patrick Doherty , Gareth Williams
发明人： Patrick Doherty , Gareth Williams
IPC分类号： A61K38/12
CPC分类号： A61K38/08 , A61K38/10 , C07K7/06 , C07K7/08
摘要： Cyclic peptides and peptidomimetics are provided that bind to and/or modulate activities associated with Trk receptors, including processes associated with the growth and repair of the central nervous system (e.g., neuronal growth and survival, axonal growth, neurite outgrowth and synaptic plasticity). Cyclic peptides and peptidomimetics are also provided that block or reduce the effect of other factors that inhibit growth and/or repair of the central nervous system. Pharmaceutical compositions and other formulations comprising these compounds are provided. In addition, the invention provides methods for using the cyclic peptides and peptidomimetics to modulate Trk mediated activities, including processes such as neuronal growth, survival and recover, axonal growth, neurite outgrowth, and synaptic plasticity. Further, the invention provides methods for promoting central nervous system (CNS) neuron growth by administering a p75 receptor binding agent.
摘要翻译：提供了结合和/或调节与Trk受体相关活性（包括与中枢神经系统的生长和修复相关的过程）（例如，神经元生长和存活，轴突生长，神经突生长和突触可塑性）的循环肽和肽模拟物。还提供了循环肽和肽模拟物，其阻断或减少抑制中枢神经系统生长和/或修复的其他因子的作用。提供了包含这些化合物的药物组合物和其它制剂。此外，本发明提供了使用环肽和肽模拟物调节Trk介导的活性的方法，包括神经元生长，存活和恢复，轴突生长，神经突生长和突触可塑性等过程。此外，本发明提供了通过施用p75受体结合剂促进中枢神经系统（CNS）神经元生长的方法。

39. 发明申请

US20050164920A1 Compounds that modulate neuronal growth and their uses 失效
标题翻译：调节神经元生长及其用途的化合物
公开(公告)号：US20050164920A1
公开(公告)日：2005-07-28
申请号：US10938409
申请日：2004-09-09
申请人： Patrick Doherty , Gareth Williams
发明人： Patrick Doherty , Gareth Williams
IPC分类号： A61K20060101 , A61K38/00 , A61K38/12 , C07K7/64
CPC分类号： A61K38/08 , A61K38/10 , C07K7/06 , C07K7/08
摘要： Cyclic peptides and peptidomimetics are provided that bind to and/or modulate activities associated with Trk receptors, including processes associated with the growth and repair of the central nervous system (e.g., neuronal growth and survival, axonal growth, neurite outgrowth and synaptic plasticity). Cyclic peptides and peptidomimetics are also provided that block or reduce the effect of other factors that inhibit growth and/or repair of the central nervous system. Pharmaceutical compositions and other formulations comprising these compounds are provided. In addition, the invention provides methods for using the cyclic peptides and peptidomimetics to modulate Trk mediated activities, including processes such as neuronal growth, survival and recover, axonal growth, neurite outgrowth, and synaptic plasticity. Further, the invention provides methods for promoting central nervous system (CNS) neuron growth by administering a p75 receptor binding agent.
摘要翻译：提供了结合和/或调节与Trk受体相关活性（包括与中枢神经系统的生长和修复相关的过程）（例如，神经元生长和存活，轴突生长，神经突生长和突触可塑性）的循环肽和肽模拟物。还提供了循环肽和肽模拟物，其阻断或减少抑制中枢神经系统生长和/或修复的其他因子的作用。提供了包含这些化合物的药物组合物和其它制剂。此外，本发明提供了使用环肽和肽模拟物调节Trk介导的活性的方法，包括神经元生长，存活和恢复，轴突生长，神经突生长和突触可塑性等过程。此外，本发明提供了通过施用p75受体结合剂促进中枢神经系统（CNS）神经元生长的方法。

40. 发明授权

US06297395B1 Calixarenes and their use for sequestration of metals 失效
标题翻译：杯芳烃及其用于金属螯合的用途
公开(公告)号：US06297395B1
公开(公告)日：2001-10-02
申请号：US09460237
申请日：1999-12-13
申请人： Graeme P. Nicholson , Mark J. Kan , Gareth Williams , Michael G. Drew , Paul D. Beer
发明人： Graeme P. Nicholson , Mark J. Kan , Gareth Williams , Michael G. Drew , Paul D. Beer
IPC分类号： C07C22900
CPC分类号： C07C235/20 , C07C235/24 , C07C327/42 , C07C2603/92 , C07D273/00 , C22B3/002 , G01N27/3335 , Y02P10/234
摘要： Disclosed are “acid-amide” calixarenes of formula (I) wherein: L is [—CH2—] or [—O—CH2—O—] and may be the same or different between each aryl group; R5 is H, halogen, or C1-C10 aliphatic hydrocarbyl group, C6-C20 aryl group, C6-C10 hydrocarbyaryl group, any of which may optionally be substituted by one or more halo or oxo groups or interrupted by one or more oxo groups, and R5 may be the same or different on each aryl group; R1 comprises an optionally protected carboxy group; two groups out of R2, R3, and R4 are H; the one group out of R2, R3, and R4 not being H comprises an amide group. The amide group may be linked to a second calixarene to form a dimer. Also disclosed are methods of use of such calixarenes for the purposes of metal sequestration, especially of lanthanides and actinides. Also disclosed are calixarene dimer derivatives of the calixarenes of the invention. Also disclosed are processes for preparing the calixarenes and dimers.
摘要翻译：公开了式（I）的“酸酰胺”杯芳烃，其中：L是[-CH 2 - ]或[-O-CH 2 -O-]，并且在每个芳基之间可以相同或不同; R5是H，卤素或C1-C10脂族烃基，C6-C20芳基，C6-C10烃氧基，其中任何一个可以任选地被一个或多个卤代或氧代基取代或被一个或多个氧代基中断，并且R 5可以在每个芳基上相同或不同; R1包含任选保护的羧基; R2，R3和R4中的两个基团是H; R2，R3和R4不为H的一个基团包含酰胺基。酰胺基团可以与第二杯咖啡连接以形成二聚体。还公开了使用这种杯芳烃用于金属螯合的方法，特别是镧系元素和锕系元素的方法。还公开了本发明的杯芳烃的杯芳烃二聚体衍生物。还公开了制备杯芳烃和二聚体的方法。

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