JUNG, KYUNG YUN,정경윤,CHUNG, JAE UK,정재욱,JEONG, MIN WOOK,정민욱,JUNG, HEE KYUNG,정희경,LA, HYUN JU,라현주,MA, SANG HO,마상호,LEE, YONG SIL,이용실
申请号：
KR1020117026683
公开号：
KR1020120028877A
申请日:
2010.04.14
申请国别(地区):
KR
年份:
2012
代理人:
摘要：
PURPOSE: A pharmaceutical composition containing reverse-turn mimetic with pyrazino-triazinone as a basic structure is provided to effectively suppress proliferation of acute myeloid leukemia cells. CONSTITUTION: A novel compound of reverse-turn mimetics is denoted by chemical formula I. A pharmaceutical composition contains the compound of chemical formula I and pharmaceutically acceptable excipient. A method for treating acute myelocytic leukemia(AML) comprises a step of administering effective amount of the pharmaceutical composition to a patient with AML. A method for preparing the compound of chemical formula I comprises: a step of introducing an acyl group to indole-7-carbaldehyde by Friedel-Crafts acylation to prepare 3-acyl-indole-7-carbaldehyde； a step of introducing alkyl groups and amino acetal groups to 3-acyl-indole-7-carbaldehyde to prepare a 1-alkyl-3-acyl-indole derivative； a step of performing amidation to prepare reaction intermediates； a step of cyclizing to prepare a cyclic intermediate； and a step of phosphating the cyclic intermediate.본 발명은 피라지노트리아지논(Pyrazino-triazinone)을 기본 구조로 갖는, 리버스-턴 유사체의 신규한 화합물 및 항암효과 등의 질병치료, 특히 급성 골수성 백혈병의 치료 용도에 관한 것이다. 또한 본 발명의 리버스-턴 유사체를 경제적으로 대량생산할 수 있는 제조방법을 제공한다.
