基本信息:
- 专利标题: 인간 EZH2의 억제제 및 이의 사용 방법
- 专利标题(英):Inhibitors of human ezh2, and methods of use thereof
- 专利标题(中):人EZH2的抑制剂及其使用方法
- 申请号:KR1020147028560 申请日:2013-03-12
- 公开(公告)号:KR1020140147836A 公开(公告)日:2014-12-30
- 发明人: 쿤츠케빈웨인 , 넛슨사라캐슬린 , 위글티모시제임스넬슨
- 申请人: 에피자임, 인코포레이티드
- 申请人地址: *** Technology Square, *th Floor, Cambridge, MA *****, U.S.A.
- 专利权人: 에피자임, 인코포레이티드
- 当前专利权人: 에피자임, 인코포레이티드
- 当前专利权人地址: *** Technology Square, *th Floor, Cambridge, MA *****, U.S.A.
- 代理人: 김진회
- 优先权: US13/418,242 2012-03-12
- 国际申请: PCT/US2013/030565 2013-03-12
- 国际公布: WO2013138361 2013-09-19
- 主分类号: A61K31/52
- IPC分类号: A61K31/52 ; A61K31/519 ; A61K31/7076 ; C12Q1/68 ; G01N33/50 ; A61P35/00
The present invention relates to a catalytic subunit of inhibition of wild type and a specific mutant form of human histone methyl transferase EZH2 of PRC2 complexes catalyzed mono-methylated to trimethyl Chemistry of lysine 27 (H3-K27) on the histone H3 . In one embodiment, the inhibition is selective for a mutant form of EZH2, thereby, Chemistry of trimethyl H3-K27 are associated with a particular cancer is suppressed. You may use this method to treat cancers, including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). It also provides a method of measuring the reactivity of the EZH2 inhibitors in a method to determine the small molecule selective inhibitor of the mutant form of EZH2, and a subject.
信息查询:
EspacenetIPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品(专门适用于将药品制成特殊的物理或服用形式的装置或方法A61J3/00;空气除臭,消毒或灭菌,或者绷带、敷料、吸收垫或外科用品的化学方面,或材料的使用入A61L;肥皂组合物入C11D) |
------A61K31/00 | 含有机有效成分的医药配制品 |
--------A61K31/33 | .杂环化合物 |
----------A61K31/395 | ..有氮作为环杂原子的,例如胍乙啶、利福霉素 |
------------A61K31/495 | ...有仅以两个氮原子作为环杂原子的六元环,例如哌嗪(A61K31/48优先) |
--------------A61K31/505 | ....嘧啶;氢化嘧啶,例如甲氧苄啶 |
----------------A61K31/519 | .....与杂环系统邻位或迫位稠合的 |
------------------A61K31/52 | ......嘌呤,例如腺嘌呤 |