公开(公告)号：US09029344B2

公开(公告)日：2015-05-12

申请号：US13704857

申请日：2011-06-01

申请人： Genbin Shi ,  Gary X. Shaw ,  Xinhua Ji

发明人： Genbin Shi ,  Gary X. Shaw ,  Xinhua Ji

IPC分类号： A61K31/70 ,  A61K31/50 ,  C07H19/16 ,  C07D475/00 ,  C07H19/167 ,  C07D475/04 ,  G06F19/16

CPC分类号： C07H19/16 ,  C07D475/04 ,  C07H19/167 ,  G06F19/16

摘要： The disclosure provides linked purine pterin compounds and analogs thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.

摘要翻译： 本公开提供了连接的嘌呤蝶呤化合物及其类似物，其是新型HPPK抑制剂。 本文所述的HPPK抑制剂是通式I的化合物及其药学上可接受的盐。 A1〜A3，R1〜R4，L1，L2，B1，B2。 式I的化合物和盐以高亲和力和特异性结合HPPK。 还提供了含有式I的HPPK抑制剂和通过向患者提供一种或多种式I的HPPK抑制剂来治疗患者细菌感染的方法的药物组合物。 还提供了可用于制备式I化合物的方法和中间体。 还提供了使用所公开的化合物指导另外的新型抗菌剂的开发的方法。

公开(公告)号：US20130172285A1

公开(公告)日：2013-07-04

申请号：US13704857

申请日：2011-06-01

申请人： Genbin Shi ,  Gary X. Shaw ,  Xinhua Ji

发明人： Genbin Shi ,  Gary X. Shaw ,  Xinhua Ji

IPC分类号： C07H19/167 ,  G06F19/16 ,  C07D475/04

CPC分类号： C07H19/16 ,  C07D475/04 ,  C07H19/167 ,  G06F19/16

摘要： The disclosure provides linked purine pterin compounds and analogues thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.