公开(公告)号：EP3212196A1

公开(公告)日：2017-09-06

申请号：EP15854524.4

申请日：2015-10-29

申请人： Wisconsin Alumni Research Foundation

发明人： RAINES, Ronald T. ,  WINDSOR, Ian ,  PALTE, Michael ,  LUKESH, John

IPC分类号： A61K31/69 ,  A61P31/18 ,  C07C311/15

CPC分类号： C07F5/025 ,  A61K31/00 ,  A61K31/34 ,  A61K31/341 ,  A61K31/366 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/69 ,  A61K33/22 ,  A61K2300/00

摘要： Protease inhibitors, particularly aspartyl protease inhibitors, and more particularly HIV protease inhibitors which are boronated to enhance activity or to enhance entry into cells. Compounds, prodrugs and salts thereof of this invention contain phenylboronate groups, in particular p -B(OH)2-phenyl groups, benzoxaborole groups or borono-pyridyl groups or analogous groups in which the boronate group is protected. Methods for treating AIDS and ARC as well as providing a method for treating or preventing HIV infection.

摘要翻译： 蛋白酶抑制剂，特别是天冬氨酰蛋白酶抑制剂，更特别是硼化以增强活性或增强进入细胞的HIV蛋白酶抑制剂。 本发明的化合物，前药和盐包含苯基硼酸酯基团，特别是p-B（OH）2 - 苯基基团，苯并氧杂硼杂环戊二烯基团或硼代吡啶基团或其中硼酸酯基团被保护的类似基团。 治疗艾滋病和ARC的方法以及提供治疗或预防HIV感染的方法。