LTD.;HYUNDAI PHARM CO., LTD.;HYUNDAI PHARM CO.;현대약품 주식회사
发明人:
LEE, In Hee,이인희,KIM, Se Hoan,김세환,MOON, Soon Young,문순영,JANG, Jung In,장정인,KANG, Seung Tae,강승태,YOON, Hyun Ho,윤현호,LEE, Hyuck Ju,이혁주,RHEE, Jae Keol,이재걸
申请号：
KRKR2017/007853
公开号：
WO2018/021762A1
申请日:
2017.07.20
申请国别(地区):
KR
年份:
2018
代理人:
摘要：
The present invention relates to a novel compound inhibiting CDK5-mediated PPARγ phosphorylation, a preparation method therefor, and a pharmaceutical composition containing the same. The novel compound of the present invention binds to PPARγ with high affinity but does not induce transcriptional activity so as not to act as an agonist, does not cause side effects of a conventional anti-diabetic by blocking the phosphorylation activity of CDK5, and has improved pharmacological properties. Therefore, a pharmaceutical composition containing the compound of the present invention as an active ingredient can be usable in the treatment of metabolic diseases associated with PPARγ.La présente invention concerne un nouveau composé inhibant la phosphorylation de PPARγ médiée par CDK5, son procédé de préparation et une composition pharmaceutique le contenant. Le nouveau composé de la présente invention se lie à PPARγ avec une affinité élevée mais n'induit pas d'activité transcriptionnelle de manière à ne pas agir comme un agoniste, ne provoque pas d'effets secondaires d'un anti-diabétique classique en bloquant l'activité de phosphorylation de CDK5, et a des propriétés pharmacologiques améliorées. Par conséquent, une composition pharmaceutique contenant le composé de la présente invention en tant qu'ingrédient actif peut être utilisée dans le traitement de maladies métaboliques associées à PPARγ.본 발명은 CDK5에 의한 PPARγ 인산화를 억제하는 신규 화합물, 이의 제조방법 및 이를 포함하는 약학 조성물에 관한 것으로, 본 발명의 신규 화합물은 PPARγ에 고친화도로 결합하지만 유전자 전사(transcriptional activity)를 유도하지 않아 작용제(agonist)로 작용하지 않고, CDK5의 인산화 작용을 차단하여 종래의 당뇨병 치료제의 부작용이 발생하지 않을 뿐만 아니라, 약리물성이 우수하다. 따라서 본 발명의 화합물을 유효성분으로 포함하는 약학 조성물은 PPARγ 관련 대사성 질환을 치료하는데 유용하게 사용될 수 있다.
