EULJI UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
发明人:
KIM, JI YEONKR,김지연,SON, YOU HWAKR,손유화
申请号：
KR1020140134137
公开号：
KR1020160040795A
申请日:
2014.10.06
申请国别(地区):
KR
年份:
2016
代理人:
摘要：
The present invention relates to a pharmaceutical composition for preventing or treating osteoporosis. The pharmaceutical composition includes, as an active ingredient, 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinoline-2-one or a pharmaceutically acceptable salt thereof. It is shown that the pharmaceutical composition (1) has an activity of stimulating differentiation and growth of osteoblasts as determined by the test for determining an effect upon the differentiation of human bone morphogenic protein (BMP)-derived osteoblasts (2) stimulates the activity of BMP-2-derived alkaline phosphatase (ALP) as determined by the test for determining an activity of stimulating production of ALP as a marker for differentiation of osteoblasts, and (3) stimulates phosphorylation of ERK1/2 and p38 and phosphorylation of smad1/5/8 and transfer thereof toward the nuclei as determined by the test for determining an effect upon the phosphorylation of ERK1/2, p38 MAPK and smad1/5/8 as a mechanism for related signal transfer. Therefore, the pharmaceutical composition is useful for treating and preventing bone-related diseases, such as osteoporosis.COPYRIGHT KIPO 2016본 발명은 4-아미노-5-플루오로-3-[6-(4-메틸피페라진-1-일)-1H-벤즈이미다졸-2-일]-1H-퀴놀린-2-온 또는 그의 제약상 허용가능 염을 유효성분으로 포함하는 골다공증 질환의 예방 또는 치료용 약학 조성물에 관한 것이다. 본 발명에 따른 (1) 사람 재조합 Bone morphogenic protein (BMP)-유도 조골세포(osteoblast)의 분화에 대한 영향실험을 통하여 조골세포(osteoblast)의 분화 및 성장 촉진활성을 확인하고 (2) 조골세포분화의 표지자로서 ALP 생성촉진 활성실험을 통하여 BMP-2-유도 ALP(alkaline phosphatase)의 활성을 촉진하였으며, (3) 관련 신호전달 기전인 ERK1/2, p38 MAPK 와 smad1/5/8 의 인산화에 대한 영향실험을 통하여 ERK1/2 및 p38 의 인산화를 촉진하고 smad1/5/8 의 인산화 및 핵으로의 이동도 증가시킴을 확인하여, 골다공증과 같은 골 관련 질환 치료 및 예방에 유용하다.
