公开(公告)号：US20160355483A1

公开(公告)日：2016-12-08

申请号：US15244821

申请日：2016-08-23

Applicant: Hyundai Pharm Co., Ltd.

Inventor： In Hee LEE ,  Hee Il CHAE ,  Se hoan KIM ,  Soon Young MOON ,  Tae Young HA ,  Hyo sun CHOI ,  Young Seok KIM ,  Chun hwa KIM ,  Jae Keol RHEE

IPC: C07D215/48 ,  C07D401/12 ,  C07D405/12 ,  C07D265/36 ,  C07D413/12

CPC classification number: C07D215/48 ,  C07D265/36 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

Abstract: The present invention relates to a compound inhibiting CDK5-mediated PPARG phosphorylation and a pharmaceutical composition for treating PPARG-related diseases containing the same as an active ingredient. A compound represented by formula 1 or an optical isomer thereof according to the present invention that binds to PPARG at a high affinity level, but does not act as an agonist, thereby inducing no gene transcription; blocks CDK5, which is a cause of PPARG phosphorylation, thereby causing no side effects of existing anti-diabetic drugs; can be formulated into drugs due to improved pharmacological properties thereof; and can be favorably used as a pharmaceutical composition for treating PPARG-related diseases due to favorable treatment effects on PPARG-related diseases.

Abstract translation: 本发明涉及一种抑制CDK5介导的PPARG磷酸化合物的化合物和用于治疗含有其作为活性成分的PPARG相关疾病的药物组合物。 由式1表示的化合物或其根据本发明的光学异构体以高亲和力水平与PPARG结合但不作为激动剂，从而不诱导基因转录; 阻断CDK5，这是PPARG磷酸化的原因，从而不会引起现有抗糖尿病药物的副作用; 由于其药理学性质的改善，可以配制成药物; 并且由于对PPARG相关疾病的有利治疗作用，可以有利地用作治疗PPARG相关疾病的药物组合物。