公开(公告)号：US09650389B2

公开(公告)日：2017-05-16

申请号：US15029075

申请日：2014-12-30

Applicant: Korea Research Institute of Chemical Technology ,  The Catholic University of Korea Industry-Academic Cooperation Foundation

Inventor： Heeyeong Cho ,  Hee-Jong Lim ,  Ge Hyeong Lee ,  Woo Kyu Park ,  Hyeon Young Kim ,  Dae Young Jeong ,  Wan Uk Kim ,  Chul Soo Cho ,  Su Jung Park ,  Eun Jin Han

IPC: C07D491/153 ,  A61K31/4745

CPC classification number: C07D491/153 ,  A61K31/4745

Abstract: The preset invention relates to a novel 8-oxoprotoberberine derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases associated with the activity of NFAT5 containing the same as an active ingredient. The novel 8-oxoproteoberberine derivative or the pharmaceutically acceptable salt thereof according to the present invention can be useful in a pharmaceutical composition for preventing or treating diseases associated with the activity of NFAT5, particularly rheumatoid arthritis or inflammatory diseases, since it is ascertained that the derivative or a pharmaceutically acceptable salt thereof has remarkably increased oral absorption compared with known protoberberine due to an improvement in the properties thereof, and inhibits the activity of NFAT5 and the secretion of inflammatory cytokines and reduces the expression of NAFT5 in mice with rheumatoid arthritis by directly inhibiting the transcription of NFT5.

公开(公告)号：US10526337B2

公开(公告)日：2020-01-07

申请号：US15567692

申请日：2016-06-01

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Ge Hyeong Lee ,  Hee-Jong Lim ,  Heeyeong Cho ,  Woo Kyu Park ,  Seong Hwan Kim ,  Jung Hwan Choi

IPC: C07D487/04 ,  A61K31/506 ,  C07D471/04

Abstract: The present invention relates to a heteroaryl derivative represented by Formula 1 wherein , A, R1, R2, R3, R4, and R5 are as defined herein, or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as cancers, autoimmune diseases, and respiratory diseases.

公开(公告)号：US20220009933A1

公开(公告)日：2022-01-13

申请号：US17294705

申请日：2019-11-20

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Heeyeong Cho ,  Hee-Jong Lim ,  Woo Kyu Park ,  Dae Young Jeong ,  Hyeon Young Kim ,  Sae-Bom Yoon ,  Chong Ock Lee ,  Heung Kyoung Lee ,  Victor Sukbong HONG ,  Ji Hye Choi

IPC: C07D487/04 ,  C07D519/00 ,  C07D487/14 ,  A23L33/10

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating autoimmune diseases or tumors, containing, as an active ingredient, a tricyclic compound represented by the following Chemical Formula 1 or a pharmaceutically acceptable salt thereof, and a health food composition for preventing or alleviating autoimmune diseases or tumors, containing the tricyclic compound as an active ingredient, wherein the tricyclic compound represented by Chemical Formula 1 has an excellent inhibitory activity against IRAK4, and thus can be usefully used for the prevention, treatment, or alleviation of autoimmune diseases or tumors.

公开(公告)号：US20180105527A1

公开(公告)日：2018-04-19

申请号：US15567692

申请日：2016-06-01

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Ge Hyeong Lee ,  Hee-Jong Lim ,  Heeyeong Cho ,  Woo Kyu Park ,  Seong Hwan Kim ,  Jung Hwan Choi

IPC: C07D487/04 ,  C07D471/04

Abstract: The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.