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1. 发明授权

US08846696B2 Purine derivatives 有权
标题翻译：嘌呤衍生物
公开(公告)号：US08846696B2
公开(公告)日：2014-09-30
申请号：US12489663
申请日：2009-06-23
申请人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , C07D473/16
CPC分类号： C07D473/16 , A61K31/52 , Y02A50/411
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病中的用途。

2. 发明授权

US07544689B2 Purine derivatives 有权
标题翻译：嘌呤衍生物
公开(公告)号：US07544689B2
公开(公告)日：2009-06-09
申请号：US11238533
申请日：2005-09-28
申请人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , A61P3/10 , A61P31/20 , A61P31/14 , A61P17/06 , A61P35/02 , A61P25/28
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or un branched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, CNS disorders, diabetes, stroke, alopecia or neurodegenerative disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中枢神经系统疾病，糖尿病，中风，脱发或神经变性疾病中的用途。

3. 发明授权

US07582642B2 Purine derivatives 有权
标题翻译：嘌呤衍生物
公开(公告)号：US07582642B2
公开(公告)日：2009-09-01
申请号：US11033692
申请日：2005-01-11
申请人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , A61P31/14 , A61P31/20 , C07D473/40
CPC分类号： C07D473/16 , A61K31/52 , Y02A50/411
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病中的用途。

4. 发明申请

US20050256142A1 New purine derivatives 有权
标题翻译：新嘌呤衍生物
公开(公告)号：US20050256142A1
公开(公告)日：2005-11-17
申请号：US11033692
申请日：2005-01-11
申请人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , A61P3/10 , A61P9/00 , A61P17/06 , A61P17/14 , A61P25/28 , A61P31/12 , A61P35/00 , C07D473/16 , C07D473/12
CPC分类号： C07D473/16 , A61K31/52 , Y02A50/411
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, CNS disorders, diabetes, stroke, alopecia or neurodegenerative disorders.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链C 1 -C 6烷基或芳基并且其中R 3和R 4中的至少一个不是H; R 5是支链或非支链C 1 -C 5烷基或C 1 -C 3亚烷基其中每一个可以任选地被一个或多个OH基团取代; R 6，R 7，R 8和R 9各自独立地为H，卤素，NO 3， 2，OH，OMe，CN，NH 2，COOH，CONH 2或SO 2 NH 2， / SUB>。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中枢神经系统疾病，糖尿病，中风，脱发或神经变性疾病中的用途。

5. 发明申请

US20060183760A1 New purine derivatives 有权
标题翻译：新嘌呤衍生物
公开(公告)号：US20060183760A1
公开(公告)日：2006-08-17
申请号：US11238533
申请日：2005-09-28
申请人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , C07D473/12
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or un branched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, CNS disorders, diabetes, stroke, alopecia or neurodegenerative disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R 1和R 2中的一个为甲基，乙基或异丙基，另一个为H; R 3和R 4各自独立地为H，支链或非支链C 1 -C 6烷基，或芳基，并且其中R 3和R 4中的至少一个不是H; R 5是支链或非支链C 1 -C 5烷基或C 1 -C 3亚烷基其中每一个可以任选地被一个或多个OH基团取代; R 6，R 7，R 8和R 9各自独立地为H，卤素，NO 3， 2，OH，OMe，CN，NH 2，COOH，CONH 2或SO 2 NH 2， / SUB>。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中枢神经系统疾病，糖尿病，中风，脱发或神经变性疾病中的用途。

6. 发明授权

US07612079B2 2,6,9-substituted purine derivatives and their use in the treatment of proliferative disorders 失效
标题翻译： 2,6,9-取代的嘌呤衍生物及其在治疗增殖性疾病中的用途
公开(公告)号：US07612079B2
公开(公告)日：2009-11-03
申请号：US10742237
申请日：2003-12-18
申请人： Peter Martin Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , C07C215/08 , A61P17/06 , A61P35/02
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein R3 is hydrogen or methyl and R4 is methyl, ethyl or isopropyl; R6 is 3-nitrophenylamino, 3,4-dimethoxybenzylamino, 3-iodobenzyl-amino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino; R9 is isopropyl or cyclopentanyl. In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R2是2-羟甲基吡咯烷-1-基或NHCH（R4）CH（R3）OH，其中R3是氢或甲基，R4是甲基，乙基或异丙基 R6是3-硝基苯基氨基，3,4-二甲氧基苄基氨基，3-碘苄基 - 氨基，吡啶-2-基 - 甲基氨基，吡啶-4-基 - 甲基氨基或茚满-5-氨基; R9是异丙基或环戊基。在另一方面，本发明涉及包含所述化合物的药物组合物及其在治疗抗增生性疾病和/或病毒性疾病中的用途。

7. 发明申请

US20050009846A1 2,6,9-Substituted purine derivatives and their use in the treatment of proliferative disorders 失效
标题翻译： 2,6,9-取代的嘌呤衍生物及其在治疗增殖性疾病中的应用
公开(公告)号：US20050009846A1
公开(公告)日：2005-01-13
申请号：US10742237
申请日：2003-12-18
申请人： Peter Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , A61P17/06 , A61P25/28 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D473/16 , C07D473/14
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein R3 is hydrogen or methyl and R4 is methyl, ethyl or isopropyl; R6 is 3-nitrophenylamino, 3,4-dimethoxybenzylamino, 3-iodobenzyl-amino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino; R9 is isopropyl or cyclopentanyl. In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R2是2-羟甲基吡咯烷-1-基或NHCH（R4）CH（R3）OH，其中R3是氢或甲基，R4是甲基，乙基或异丙基 R6是3-硝基苯基氨基，3,4-二甲氧基苄基氨基，3-碘苄基 - 氨基，吡啶-2-基 - 甲基氨基，吡啶-4-基 - 甲基氨基或茚满-5-氨基; R9是异丙基或环戊基。在另一方面，本发明涉及包含所述化合物的药物组合物及其在治疗抗增生性疾病和/或病毒性疾病中的用途。

8. 发明申请

US20120107865A1 DETECTION OF BACTERIA AND FUNGI 有权
标题翻译：检测细菌和真菌
公开(公告)号：US20120107865A1
公开(公告)日：2012-05-03
申请号：US13264177
申请日：2010-04-19
申请人： Stuart Wilson , William Mullen
发明人： Stuart Wilson , William Mullen
IPC分类号： C12Q1/25
CPC分类号： C12Q1/04 , C12Q1/68 , C12Q1/689 , C12Q1/6895 , C12Q2521/501 , C12Q2527/119 , C12Q2533/10 , C12Q2537/149 , G01N2333/9015
摘要： A method of detecting a ligase expressing micro-organism in a sample comprises steps of treating the sample under conditions that inhibit the activity of ATP-dependent ligase from mammalian cells but which do not inhibit the activity of the microbial ligases, contacting the sample or a portion of the sample with a nucleic acid molecule which acts as a substrate for ligase activity in the sample, incubating the thus contacted sample under conditions suitable for ligase activity; and specifically determining the presence and/or the amount of a ligated nucleic acid molecule resulting from the action of the ligase on the substrate nucleic acid molecule to indicate the presence of the ligase expressing micro-organism. The micro-organism may be a fungus or a bacterium or both. High pH conditions may be employed to inactivate mammalian ligases. Related kits are described.
摘要翻译：检测样品中连接酶表达微生物的方法包括以下步骤：在抑制ATP依赖性连接酶从哺乳动物细胞的活性但不抑制微生物连接酶的活性，接触样品或样品的一部分与核酸分子起作用，作为样品中连接酶活性的底物，在适合连接酶活性的条件下孵育由此接触的样品; 并且具体地确定由连接酶对底物核酸分子的作用产生的连接的核酸分子的存在和/或量，以指示表达微生物的连接酶的存在。微生物可以是真菌或细菌或两者。可以使用高pH条件来灭活哺乳动物连接酶。描述相关工具包。

9. 发明申请

US20100291564A1 Methods for Detection of Micro-Organisms 审中-公开
标题翻译：微生物检测方法
公开(公告)号：US20100291564A1
公开(公告)日：2010-11-18
申请号：US12667818
申请日：2008-07-09
申请人： Christopher John Stanley , Stuart Wilson
发明人： Christopher John Stanley , Stuart Wilson
IPC分类号： C12Q1/68 , C12N9/48
CPC分类号： C12Q1/04 , C12N9/93 , C12Q1/02 , C12Q1/18 , C12Q1/25 , C12Q1/689 , G01N2333/9015 , C12Q2565/301 , C12Q2521/501
摘要： NAD-dependent ligase is identified as an indicator of micro-organisms in a sample. A method of detecting the presence of an NAD-dependent ligase expressing micro-organism in a sample comprises the steps of: (a) contacting the sample with a nucleic acid molecule which acts as a substrate for NAD-dependent ligase activity in the sample, (b) incubating the thus contacted sample under conditions suitable for NAD-dependent ligase activity; and (c) specifically determining the presence of a ligated nucleic acid molecule resulting from the action of the NAD-dependent ligase on the substrate nucleic acid molecule to indicate the presence of the NAD-dependent ligase expressing micro-organism. The method has a number of applications and kits for carrying out the methods are also provided. Lysostaphin preparations substantially free from nuclease and/or ligase contaminants are produced by heating a lysostaphin preparation which contains nuclease and/or ligase contaminants under conditions whereby nuclease and/or ligase activity is reduced whereas endopeptidase activity of the lysostaphin is substantially unaffected.
摘要翻译： NAD依赖性连接酶被鉴定为样品中微生物的指标。检测样品中NAD依赖性连接酶表达微生物的存在的方法包括以下步骤：（a）使样品与作为样品中NAD依赖性连接酶活性的底物的核酸分子接触，（b）在适合于NAD依赖性连接酶活性的条件下孵育由此接触的样品; 和（c）特异性地确定由NAD依赖性连接酶在底物核酸分子上的作用产生的连接的核酸分子的存在，以指示表达微生物的NAD依赖性连接酶的存在。该方法还提供了许多用于执行方法的应用和套件。通过在其中核酸酶和/或连接酶活性降低的条件下加热含有核酸酶和/或连接酶污染物的溶葡萄球菌素制剂而产生基本上不含核酸酶和/或连接酶污染物的溶葡萄球菌素制剂，而溶葡萄球菌素的内肽酶活性基本上不受影响。

10. 发明申请

US20050221404A1 Binding of pathological forms of prion proteins 有权
标题翻译：结合朊病毒蛋白的病理形式
公开(公告)号：US20050221404A1
公开(公告)日：2005-10-06
申请号：US10506131
申请日：2003-02-28
申请人： Amin Lane , Christopher Stanley , Stuart Wilson
发明人： Amin Lane , Christopher Stanley , Stuart Wilson
IPC分类号： G01N33/68 , C07K1/22 , C07K14/47 , G01N33/53 , G01N33/537 , G01N33/543
CPC分类号： G01N33/6803 , G01N33/54326 , G01N33/68 , G01N33/6896 , G01N2333/968 , G01N2800/2828
摘要： Infective aggregating forms of proteins such as PrP, amyloid, and tau are bound selectively in the presence of the normal form protein using a polyionic binding agent such as dextran sulphate or pentosan (anionic), or polyamine compounds such as pDADMAC (cationic) under selective binding conditions including the use of n-lauroylsarcosine at mildly alkaline pH, and may then be assayed.
摘要翻译：蛋白质如PrP，淀粉样蛋白和tau的感染性聚集形式在正常形式的蛋白质存在下使用聚离子结合剂如硫酸葡聚糖或戊聚糖（阴离子）或多胺化合物如pDADMAC（阳离子）在选择性包括在弱碱性pH下使用正月桂酰肌氨酸的结合条件，然后可以进行测定。

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