KIM, SUNG WUK,김성욱,JUN, SUNG SOO,전성수,MIN, CHANG HEE,민창희,PARK, SE HWAN,박세환,KIM, YONG EUN,김용은,KIM, DUCK,김덕,LEE, JI SUN,이지선,OH, JU HOON,오주훈
申请号:
KR1020130064239
公开号:
KR1020130069704A
申请日:
2013.06.04
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
PURPOSE: A biguanide derivative is provided to have an excellent AMPKα activating effect and a cancer cell growth suppression effect with a small amount compared to a conventional drug. CONSTITUTION: A compound is represented by Formula 1 below, wherein R1 is a C4-12heteroaryl-substituted C1-4alkyl or an unsubstituted C7-10cycloalkyl, R2 is a hydrogen, R3 is 'a non-hydrogen-substituent that is selected from an unsubstituted C1-7alkyl; a phenyl or naphthyl-substituted C1-4alkyl; an unsubstituted C3-10cycloalkyl; and a phenyl', or R1 is 'a phenyl that is unsubstituted or substituted or with a halogen-substituted C1-4alkayl or a non-hydrogen substituent that is selected from halogens' R2 is a hydrogen, R3 is a phenyl-substituted C1-4 alkyl, or R1 is a phenyl-substituted C1-4alkyl, R2 is a hydrogen or a C1-4alkyl, and R3 is a phenyl or naphthyl-substituted C1-4alkyl.본 발명은 N4-N5-치환된 하기 화학식 1로 표시되는 바이구아나이드 유도체 또는 그의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 약학 조성물을 제공한다. 본 발명의 바이구아나이드 유도체는 기존 약물에 비해 적은 양으로도 우수한 AMPKα 활성화 효과 및 암세포 증식 억제 효과를 나타내어 당뇨, 비만, 고지혈증, 고콜레스테롤혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군, 대사성 증후군, 암 등의 치료를 위해 유용하게 이용될 수 있다.[화학식 1]