申请人:Wiestner Adrian
公开号:US20120316198A1
公开(公告)日:2012-12-13
Disclosed herein are novel hydrazone and diacyl hydrazine derivatives that are inhibitors of the endoplasmic reticulum-associated protein degradation (ERAD) pathway. Also disclosed are hydrazone and diacyl hydrazine derivatives as potent and selective inhibitors of the p97 ATPase. These agents provide useful tools for the study of protein degradation and other processes involving p97. Methods of treating diseases or disorders for which p97 inhibition and/or ER stress induction is an effective treatment with certain hydrazone and diacyl hydrazine derivatives are also disclosed.
本文披露了一种新型的腙和二酰基肼衍生物,它们是内质网相关蛋白降解(ERAD)途径的抑制剂。还披露了腙和二酰基肼衍生物作为p97 ATP酶的有效和选择性抑制剂。这些药剂为研究蛋白降解和其他涉及p97的过程提供了有用的工具。还披露了使用某些腙和二酰基肼衍生物治疗p97抑制和/或ER应激诱导是有效治疗某些疾病或疾病的方法。