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1.发明授权Acyclic amine inhibitors of 5-methytioadenosine phosphorylase and nucleosidase 有权5-甲基硫代腺苷磷酸化酶和核苷酶的非环胺抑制剂公开(公告)号：US08383636B2
公开(公告)日：2013-02-26
申请号：US12310597
申请日：2007-09-07
申请人： Keith Clinch , Gary Brian Evans , Richard Frohlich , Richard Hubert Furneaux , Peter Michael Kelly , Jennifer Mary Mason , Vern L. Schramm , Peter Charles Tyler , Shivall Ashwah Ashwin Gulab
发明人： Keith Clinch , Gary Brian Evans , Richard Frohlich , Richard Hubert Furneaux , Peter Michael Kelly , Jennifer Mary Mason , Vern L. Schramm , Peter Charles Tyler , Shivall Ashwah Ashwin Gulab
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.
摘要翻译： 本发明涉及作为5'-甲硫基腺苷磷酸化酶或5'-甲硫基腺苷核苷酸酶抑制剂的通式（I）化合物。 本发明还涉及这些化合物在治疗期望抑制5'-甲硫基腺苷磷酸化酶或包括癌症的5'-甲基硫代腺苷核苷酸酶的疾病或病症的用途，以及含有该化合物的药物组合物。
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2.发明申请ACYCLIC AMINE INHIBITORS OF 5-METHYTIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE 有权5-甲基腺苷磷酸酶和核苷酸酶的聚合胺抑制剂公开(公告)号：US20110046167A1
公开(公告)日：2011-02-24
申请号：US12310597
申请日：2007-09-07
申请人： Keith Clinch , Gary Brian Evans , Richard Frohlich , Richard Hubert Furneaux , Peter Michael Kelly , Jennifer Mary Mason , Vern L. Schramm , Peter Charles Tyler , Shivall Ashwin Gulab
发明人： Keith Clinch , Gary Brian Evans , Richard Frohlich , Richard Hubert Furneaux , Peter Michael Kelly , Jennifer Mary Mason , Vern L. Schramm , Peter Charles Tyler , Shivall Ashwin Gulab
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.
摘要翻译： 本发明涉及作为5'-甲硫基腺苷磷酸化酶或5'-甲硫基腺苷核苷酸酶抑制剂的通式（I）化合物。 本发明还涉及这些化合物在治疗期望抑制5'-甲硫基腺苷磷酸化酶或包括癌症的5'-甲基硫代腺苷核苷酸酶的疾病或病症的用途，以及含有该化合物的药物组合物。
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公开(公告)号：US20110130412A1
公开(公告)日：2011-06-02
申请号：US12310708
申请日：2007-09-07
申请人： Keith Clinch , Gary Brian Evans , Richard Hubert Furneaux , Shivali Ashwin Gulab , Peter Michael Kelly , Vern L. Schramm , Peter Charles Tyler , Anthony David Woolhouse
发明人： Keith Clinch , Gary Brian Evans , Richard Hubert Furneaux , Shivali Ashwin Gulab , Peter Michael Kelly , Vern L. Schramm , Peter Charles Tyler , Anthony David Woolhouse
IPC分类号： A61K31/519 , C07D487/04 , A61P33/02 , A61P35/00 , A61P31/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.
摘要翻译： 本发明涉及作为嘌呤核苷磷酸化酶（PNP）和/或核苷水解酶（NH））的抑制剂的通式（I）的化合物。 本发明还涉及这些化合物在治疗包括癌症，细菌感染，原生动物感染和T细胞介导的疾病的疾病和感染中的用途以及含有该化合物的药物组合物。
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公开(公告)号：US08853224B2
公开(公告)日：2014-10-07
申请号：US12310708
申请日：2007-09-07
申请人： Keith Clinch , Gary Brian Evans , Richard Hubert Furneaux , Shivali Ashwin Gulab , Peter Michael Kelly , Vern L. Schramm , Peter Charles Tyler , Anthony David Woolhouse
发明人： Keith Clinch , Gary Brian Evans , Richard Hubert Furneaux , Shivali Ashwin Gulab , Peter Michael Kelly , Vern L. Schramm , Peter Charles Tyler , Anthony David Woolhouse
IPC分类号： C07D487/00 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.
摘要翻译： 本发明涉及作为嘌呤核苷磷酸化酶（PNP）和/或核苷水解酶（NH））的抑制剂的通式（I）的化合物。 本发明还涉及这些化合物在治疗包括癌症，细菌感染，原生动物感染和T细胞介导的疾病的疾病和感染中的用途以及含有该化合物的药物组合物。
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公开(公告)号：US20150210701A1
公开(公告)日：2015-07-30
申请号：US14419669
申请日：2013-08-07
申请人： Vern L. Schramm , Shanzhi Wang , Antti Marko Haapalainen , Gary Brian Evans , Richard Hubert Furneaux , Keith Clinch , Peter Charles Tyler , Shivali Ashwin Gulab
发明人： Vern L. Schramm , Shanzhi Wang , Antti Marko Haapalainen , Gary Brian Evans , Richard Hubert Furneaux , Keith Clinch , Peter Charles Tyler , Shivali Ashwin Gulab
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/519 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： Methods of treating infections due to Helicobacter pylori (H. pylori), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors of H. pylori MTAN (5′-methylthioadenosine nucleosidase) to the subject.
摘要翻译： 公开了治疗由于幽门螺杆菌（幽门螺杆菌）感染的方法，特别是在具有消化性溃疡的受试者中的方法，其中所述方法包括向受试者施用幽门螺旋杆菌MTAN（5'-甲基硫代腺苷核苷酸酶）的抑制剂。
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公开(公告)号：US20090325986A1
公开(公告)日：2009-12-31
申请号：US12086134
申请日：2006-12-15
申请人： Richard Hubert Furneaux , Peter Charles Tyler , Gary Brian Evans , Vern L. Schramm , Keith Clinch
发明人： Richard Hubert Furneaux , Peter Charles Tyler , Gary Brian Evans , Vern L. Schramm , Keith Clinch
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P33/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
摘要翻译： 本发明涉及式（I）化合物，其为核苷类似物的L-对映体形式，以及含有该化合物的药物组合物，治疗某些疾病的方法，包括癌症，细菌感染，寄生虫感染和T细胞介导 使用化合物的疾病，制备化合物的方法和可用于制备化合物的中间体。
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7.发明授权Methods, assays and compounds for treating bacterial infections by inhibiting methylthioinosine phosphorylase 有权通过抑制甲硫噻糖磷酸化酶治疗细菌感染的方法，测定和化合物公开(公告)号：US09290501B2
公开(公告)日：2016-03-22
申请号：US13884298
申请日：2011-11-28
申请人： Vern L. Schramm , Keith Clinch , Peter Charles Tyler , Gary Brian Evans , Richard Hubert Furneaux
发明人： Vern L. Schramm , Keith Clinch , Peter Charles Tyler , Gary Brian Evans , Richard Hubert Furneaux
IPC分类号： A01N43/04 , A61K31/70 , C07D487/04 , A61K31/7076 , A61K31/7064 , A61K31/7042 , A61K31/7052 , A61K31/708 , A61K31/706 , A61K31/00 , A61K31/519 , A61K31/7068 , A61K45/06 , C12Q1/48
CPC分类号： C07D487/04 , A61K31/00 , A61K31/519 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61K31/708 , A61K45/06 , C12Q1/48
摘要： The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.
摘要翻译： 本发明公开了一种用于治疗受试者细菌感染的方法，其包括对受试者施用次生长抑制量的5'-甲硫基肌苷磷酸化酶（MTIP）抑制剂以及用于鉴定此类抑制剂的测定法，以及包含 抑制剂。
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8.发明申请METHODS, ASSAYS AND COMPOUNDS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING METHYLTHIOINOSINE PHOSPHORYLASE 有权通过抑制甲硫氨酸磷酸酶处理细菌感染的方法，测定和化合物公开(公告)号：US20130274220A1
公开(公告)日：2013-10-17
申请号：US13884298
申请日：2011-11-28
申请人： Vern L. Schramm , Keith Clinch , Peter Charles Tyler , Gary Brian Evans , Richard Hubert Furneaux
发明人： Vern L. Schramm , Keith Clinch , Peter Charles Tyler , Gary Brian Evans , Richard Hubert Furneaux
IPC分类号： C07D487/04 , A61K45/06 , A61K31/519 , C12Q1/48
CPC分类号： C07D487/04 , A61K31/00 , A61K31/519 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61K31/708 , A61K45/06 , C12Q1/48
摘要： The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.
摘要翻译： 本发明公开了一种用于治疗受试者细菌感染的方法，其包括对受试者施用次生长抑制量的5'-甲硫基肌苷磷酸化酶（MTIP）抑制剂以及用于鉴定此类抑制剂的测定法，以及包含 抑制剂。
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公开(公告)号：US06379911B2
公开(公告)日：2002-04-30
申请号：US09125808
申请日：1999-02-22
IPC分类号： C12Q134
CPC分类号： C07H21/00 , C12Q1/34 , Y10S435/975
摘要： The invention relates to a method of detecting and/or assaying nucleoside hydrolases or nucleoside phosphorylases using a chromogenic substrate. Preferred chromogenic substrates have formula (I) where X is OH, or H, and Y is the residue of Y—OH where Y—OH is a chromophore or a compound readily converted to a chromophore and the substrates are hydrolyzed by the nucleoside hydrolase to yield ribose or 2-deoxyribose plus Y—OH. Alternatively, those substrates may be phosphorylysed by nucleoside phosphorylase to yield ribose-1-phosphate plus Y—OH. The methods may be used to detect and/or assay parasites in biological samples.
摘要翻译： 本发明涉及使用显色底物检测和/或测定核苷水解酶或核苷磷酸酶的方法。 优选的显色底物具有式（I），其中X是OH或H，Y是Y-OH的残基，其中Y-OH是发色团或易于转化为发色团的化合物，并且底物被核苷水解酶水解成 产生核糖或2-脱氧核糖加Y-OH。 或者，这些底物可以被核苷磷酸化酶磷酸化以产生核糖-1-磷酸加上Y-OH。 该方法可用于检测和/或测定生物样品中的寄生虫。
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10.发明授权Nucleoside hydrolase and nucleoside phosphorylase detection kits, dipsticks and substrates 失效核苷水解酶和核苷磷酸化酶检测试剂盒，浸渍和底物公开(公告)号：US06764829B2
公开(公告)日：2004-07-20
申请号：US10101074
申请日：2002-03-18
IPC分类号： C12Q134
CPC分类号： C07H21/00 , C12Q1/34 , Y10S435/975
摘要： The invention relates to a method of detecting and/or assaying nucleoside hydrolases or nucleoside phosphorylases using a chromogenic substrate. Preferred chromogenic substrates have formula (I) where X is OH, or H, and Y is the residue of Y—OH where Y—OH is a chromophore or a compound readily converted to a chromophore and the substrates are hydrolyzed by the nucleoside hydrolase to yield ribose or 2-deoxyribose plus Y—OH. Alternatively, those substrates may be phosphorylysed by nucleoside phosphorylase to yield ribose-1-phosphate plus Y—OH. The methods may be used to detect and/or assay parasites in biological samples.
摘要翻译： 本发明涉及使用显色底物检测和/或测定核苷水解酶或核苷磷酸酶的方法。 优选的显色底物具有式（I），其中X是OH或H，Y是Y-OH的残基，其中Y-OH是发色团或易于转化为发色团的化合物，并且底物被核苷水解酶水解成 产生核糖或2-脱氧核糖加Y-OH。 或者，这些底物可以被核苷磷酸化酶磷酸化以产生核糖-1-磷酸加上Y-OH。 该方法可用于检测和/或测定生物样品中的寄生虫。
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