JEONG, Hyeon Gun,정현근,SHIN, Young June,신영준,KWAK, Ho Young,곽호영,HAN, Dong-Oh,한동오,HAN, Cheol Kyu,한철규,AUH, Jin,HAN, Chang Kyun,한창균,YOON, Jeong Hyeok,윤정혁,KIM, Nam Doo,김남두,KIM, Tae Jeong,김태정,LEE, Youn Ho,이윤호
申请号：
KRKR2011/003656
公开号：
WO2011/149213A3
申请日:
2011.05.17
申请国别(地区):
WO
年份:
2012
代理人:
摘要：
The present invention relates to a novel derivative having inhibitory activity against 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient. The compound according to the present invention selectively inhibits 11β-HSD1, and thus can be used as a therapeutic agent for treating diseases caused by over-activation of 11β-HSD1, for example, non-insulin dependent diabetes mellitus (type II diabetes), insulin resistance, obesity, lipid disorders, metabolic syndrome, and diseases and state mediated by the action of excessive glucocorticoid.Linvention concerne un nouveau dérivé ayant une activité inhibitrice contre 11β-hydroxystéroide déhydrogénase de type 1 (11β-HSD1), son procédé de préparation, et une composition pharmaceutique le contenant comme principe actif. Le composé selon linvention, qui inhibe de manière sélective 11β-HSD1, peut donc servir comme agent thérapeutique pour traiter des maladies causées par une hyperactivité de 11β-HSD1, par exemple, diabètes sucrés non insulinodépendants (diabètes type II), résistance à linsuline, obésité, troubles lipidiques, syndrome métabolique, et maladies et état médiés par laction glucocorticoïde excessive.본 발명은 11-베타-HSD1 효소의 억제활성을 갖는 신규 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물에 관한 것으로, 본 발명에 따른 화합물은 11-베타-하이드록시스테로이드 데하이드로게나아제 타입 1(11β-HSD1)을 선택적으로 억제함으로 상기 11β-HSD1의 과활성에 의해 유발되는 질환, 예를 들면 인슐린 비의존성 타입 2 당뇨병, 인슐린 내성, 비만, 지질 장애, 대사 증후군, 및 과도한 글루코코르티코이드 작용에 의해 매개되는 질환 및 상태를 치료하기 위한 치료제로서 유용하게 사용할 수 있다.
