Abstract:
본 발명은 이소퀴놀리노 퀴나졸린계 비만 및 대사성질환 치료용 화합물에 관한 것으로서, 더욱 상세하게는 핵수용체인 PPAR gamma에 길항하는 이소퀴놀리노 퀴나졸린계 물질을 이용해 지방세포분화 및 PPARγ2에 의해 유도된 전사활성을 강력하게 억제하는 물질과 그 제조방법에 관한 것이다. 본 발명은 화학식 1로 표시되는 화합물을 제공하며, 화학식 중, R¹, R², R³은 수소, 메틸(methyl)기, 또는 메톡시(methoxy)기 중 하나이며, R⁴, R 5 는 수소, 염소 중 하나이며, Y는 카르보닐(carbonyl)기이며, X는 이민(immine)기이다. 상기와 같은 본 발명에 따른 화합물은 기존의 길항제들에 비해 독성이 적고, 최대 80%의 지방세포분화 억제효과를 보이는 바, 비만 및 대사성질환을 치료하는 데 효과가 있음을 확인하였다.
Abstract:
The present invention relates to a novel bis-amide derivative compound or a pharmaceutically acceptable salt thereof, a manufacturing method thereof, a pharmacological composition for the prevention or treatment of diseases induced by hepatitis C virus infection which includes the bis-amide derivative compound or pharmaceutically acceptable salt thereof as an effective ingredient and a health functional food for the prevention or treatment of diseases induced by hepatitis C virus infection. The novel bis-amide derivative compound of the present invention and, especially, WJCPA-126 are specifically combined to a catalyst position of CypA, effectively inhibits the activity of an isomerase and are able to extend inhibition effect duration by being combined to CypA with high combining force exhibiting low dissociation rate (K_off). Accordingly, WJCPA-126 has non-toxic and non-immunosuppressive properties and effectively inhibit HCV replication in vivo and in vitro model systems. The WJCPA-126 reactivates host interferon reactions through inhibiting interlukin-8 (IL-8) and increasing expression of an IFN stimulating gens (ISGs). Accordingly, the bis-amide derivatives including WJCPA-126 are able to be usefully used as novel CypA inhibitors exhibiting antivirus activity.