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。