公开(公告)号：US09199944B2

公开(公告)日：2015-12-01

申请号：US14617079

申请日：2015-02-09

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Kwangho Lee ,  Hyoung Rae Kim ,  Chi Hoon Park ,  Chong Ock Lee ,  Jong Kook Lee ,  Hee Jung Jung ,  Sung Yun Cho ,  Chong Hak Chae ,  Sang Un Choi ,  Jae Du Ha

IPC: A61K31/506 ,  C07D239/48 ,  C07D403/12 ,  C07D403/14

CPC classification number: C07D239/48 ,  A61K31/506 ,  C07D403/12 ,  C07D403/14

Abstract: Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.

Abstract translation: 本文公开了一种新的N 2，N 4 - 双（4-（哌嗪-1-基）苯基）嘧啶-2,4-二胺衍生物或其药学上可接受的盐和用于预防或治疗含有其的癌症的药物组合物 作为活性成分。 本发明的化合物对于间变性淋巴瘤激酶（ALK）和活化的cdc42相关激酶（ACK1）的活性具有优异的抑制作用，因此可以改善对具有间变性淋巴瘤激酶融合蛋白的癌细胞的治疗效果，例如 EML4-ALK和NPM-ALK，并且还有效地预防癌症的复发因此可用作用于预防和治疗癌症的药物组合物。