公开(公告)号：US20130210904A1

公开(公告)日：2013-08-15

申请号：US13586687

申请日：2012-08-15

申请人： Jeremy E. Wulff ,  Michael G. Brant ,  Jeremy W. Mason ,  Caleb M. Bromba ,  Martin J. Boulanger

发明人： Jeremy E. Wulff ,  Michael G. Brant ,  Jeremy W. Mason ,  Caleb M. Bromba ,  Martin J. Boulanger

IPC分类号： C07C279/16 ,  C07C215/44 ,  C07C211/41 ,  C07D333/78 ,  C07C35/31

CPC分类号： C07C279/16 ,  C07C29/56 ,  C07C35/31 ,  C07C67/08 ,  C07C67/29 ,  C07C211/41 ,  C07C215/44 ,  C07C233/52 ,  C07C279/22 ,  C07C2602/22 ,  C07D333/78 ,  C07C69/145 ,  C07C69/16

摘要： Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.

摘要翻译： 公开的实施方案涉及用于治疗新出现的流感病毒株并最小化对这些菌株的抗性的治疗化合物的合成和用途。 制备所公开的化合物的方法涉及使用碱介导的加成/环化顺序，随后进行官能团操作以开发可靶向神经氨酸酶的官能化化合物，这使其成为治疗流感的理想候选物。 还描述了包含治疗化合物和生物学上可接受的材料的药物组合物。 还描述了怀疑含有神经氨酸酶的受试者中抑制神经氨酸酶的方法。 所公开化合物的代谢物的使用也可用于所公开化合物的治疗剂量的诊断测定。

公开(公告)号：US08883846B2

公开(公告)日：2014-11-11

申请号：US13586687

申请日：2012-08-15

申请人： Jeremy E. Wulff ,  Michael G. Brant ,  Jeremy W. Mason ,  Caleb M. Bromba ,  Martin J. Boulanger

发明人： Jeremy E. Wulff ,  Michael G. Brant ,  Jeremy W. Mason ,  Caleb M. Bromba ,  Martin J. Boulanger

IPC分类号： A61K31/381 ,  C07D333/78 ,  C07C279/16 ,  C07C279/22 ,  C07C67/08 ,  C07C215/44 ,  C07C35/31 ,  C07C211/41 ,  C07C67/29 ,  C07C29/56 ,  C07C233/52

CPC分类号： C07C279/16 ,  C07C29/56 ,  C07C35/31 ,  C07C67/08 ,  C07C67/29 ,  C07C211/41 ,  C07C215/44 ,  C07C233/52 ,  C07C279/22 ,  C07C2602/22 ,  C07D333/78 ,  C07C69/145 ,  C07C69/16

摘要： Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.

摘要翻译： 公开的实施方案涉及用于治疗新出现的流感病毒株并最小化对这些菌株的抗性的治疗化合物的合成和用途。 制备所公开的化合物的方法涉及使用碱介导的加成/环化顺序，随后进行官能团操作以开发可靶向神经氨酸酶的官能化化合物，这使其成为治疗流感的理想候选物。 还描述了包含治疗化合物和生物学上可接受的材料的药物组合物。 还描述了怀疑含有神经氨酸酶的受试者中抑制神经氨酸酶的方法。 所公开化合物的代谢物的使用也可用于所公开化合物的治疗剂量的诊断测定。

公开(公告)号：US20140186861A1

公开(公告)日：2014-07-03

申请号：US14127568

申请日：2012-07-10

申请人： Caroline E. Cameron ,  Martin J. Boulanger ,  Brenden C. Smith

发明人： Caroline E. Cameron ,  Martin J. Boulanger ,  Brenden C. Smith

IPC分类号： C07K14/20 ,  G01N33/569

CPC分类号： G01N33/571 ,  C07K14/20 ,  G01N33/56911 ,  G01N2333/20 ,  G01N2469/20

摘要： The present application provides methods of producing soluble Treponema pallidum protein Tp0453 (such as the fragment shown in SEQ ID NO: 3). For example, the protein can be expressed from the pET28a vector in a cell and the resulting soluble Tp0453 protein isolated from the cell. Also provided are the isolated soluble Tp0453 protein, as well as Tp0453-Tp0326 chimeric proteins (e.g., SEQ ID NO: 11), and methods of using the proteins to detect antibodies specific for T. pallidum subsp. pallidum, for example to diagnose syphilis. Devices and kits that incorporate Tp0453 protein and Tp0453-Tp0326 chimeric proteins, such as lateral flow devices, are also disclosed. Kits that include the soluble Tp0453 protein and kits that include solid substrates containing the soluble Tp0453 protein are also provided.

摘要翻译： 本申请提供了生产可溶性梅毒螺旋体蛋白Tp0453（例如SEQ ID NO：3所示的片段）的方法。 例如，蛋白质可以从细胞中的pET28a载体表达，并从细胞中分离得到的可溶性Tp0453蛋白质。 还提供了分离的可溶性Tp0453蛋白以及Tp0453-Tp0326嵌合蛋白（例如SEQ ID NO：11），以及使用该蛋白质检测对苍白假单胞菌亚种特异性的抗体的方法。 苍白球，例如诊断梅毒。 还公开了包含Tp0453蛋白和Tp0453-Tp0326嵌合蛋白（例如侧流装置）的装置和试剂盒。 还提供了包含可溶性Tp0453蛋白的试剂盒和包含含有可溶性Tp0453蛋白质的固体底物的试剂盒。