基本信息:
- 专利标题： NAPHTHAQUINONE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
- 专利标题（中）：维生素DAVON的萘普生 - 甲基泼尼松
- 申请号：EP15788940.3 申请日：2015-05-08
- 公开(公告)号：EP3140274A1 公开(公告)日：2017-03-15
- 发明人： LUO, Minkui , SANCHEZ, Glorymar, Ibanez , BLUM, Gil, Joseph , YANG, Li , PITTELLA SILVA, Fabio
- 申请人： Sloan-kettering Institute For Cancer Research
- 申请人地址： 1275 York Avenue New York, NY 10065 US
- 专利权人： Sloan-kettering Institute For Cancer Research
- 当前专利权人： Sloan-kettering Institute For Cancer Research
- 当前专利权人地址： 1275 York Avenue New York, NY 10065 US
- 代理机构： Crooks, Elizabeth Caroline
- 优先权： US201461990905P 20140509; US201462033938P 20140806
- 国际公布： WO2015172076 20151112
- 主分类号： C07C50/10
- IPC分类号： C07C50/10 ; C07C50/12
摘要：
Provided herein are compounds of (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, and prodrugs thereof. Also provided are pharmaceutical compositions and methods involving the inventive compounds for the treatment of proliferative diseases (e.g., cancer (e.g., leukemia, breast cancer, melanoma, metastatic cancer) and diseases associated with inappropriate SET8 activity. Also provided are methods for inhibiting SET8 and methods for labelling SET8.
摘要（中）：
本文提供了（I）化合物及其药学上可接受的盐，溶剂化物，水合物，多晶型物，共晶体，互变异构体，立体异构体和前药。 还提供了涉及用于治疗增殖性疾病（例如癌症（例如，白血病，乳腺癌，黑素瘤，转移性癌症）和与不适当的SET8活性相关的疾病的本发明化合物的药物组合物和方法。还提供了抑制SET8和 SET8标签的方法。