公开(公告)号：US20250009742A1

公开(公告)日：2025-01-09

申请号：US18699156

申请日：2022-10-12

Applicant: AM SCIENCES INC ,  KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Nakcheol JEONG ,  Misun LEE ,  Heewoo SIM ,  Myungjin KIM ,  Jung-Hee KIM ,  Soo Bong HAN ,  Young Sik JUNG ,  Hye jin KIM ,  Chang Soo YUN ,  Heeyeong CHO ,  Mee Hyein KIM ,  Joo Youn LEE

IPC: A61K31/501 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/422 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61P31/20 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D491/052 ,  C07D491/056 ,  C07D495/04

Abstract: The present invention relates to a series of novel pyrazolylmethylurea derivatives, and the use thereof for the inhibition of capsid assembly and the prevention or treatment of viral diseases through the inhibition.

公开(公告)号：US20160251368A1

公开(公告)日：2016-09-01

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.

Abstract translation: 本发明涉及一种新颖的8-氧八环素衍生物或其药学上可接受的盐，其制备方法和用于预防或治疗与含有其作为活性成分的NFAT5的活性相关的疾病的药物组合物。 根据本发明的新型8-氧代青霉素衍生物或其药学上可接受的盐可用于预防或治疗与NFAT5的活性相关的疾病，特别是类风湿性关节炎或炎性疾病的药物组合物，因为确定该衍生物 或其药学上可接受的盐由于其性质的改善而与已知的青蒿素相比具有显着增加的口服吸收，并且抑制NFAT5的活性和炎性细胞因子的分泌，并通过直接抑制类风湿性关节炎的小鼠中降低NAFT5的表达 NFT5的转录。

公开(公告)号：US20150141439A1

公开(公告)日：2015-05-21

申请号：US14594448

申请日：2015-01-12

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY ,  SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

Inventor： Heeyeong CHO ,  Gildon CHOI ,  Woo Kyu PARK ,  Dae Young JEONG ,  Hyeon Young KIM ,  Sunkyung LEE ,  Do Hyun NAM ,  Ho Jun SEOL

IPC: A61K31/52 ,  A61K31/495

CPC classification number: A61K31/52 ,  A61K31/495

Abstract: The present invention relates to a pharmaceutical composition for the prevention or treatment of cancer or Temodal resistant glioblastoma multiform comprising azathioprine as an active ingredient. The azathioprine of the present invention is not only effective in inhibiting the growth of glioblastoma multiform, a kind of brain tumor, but also excellent in treating glioblastoma multiform that displays resistance against Temodal (temozolomide), the conventional therapeutic agent for glioblastoma multiform, so that it can be effectively used as an active ingredient of a pharmaceutical composition for the prevention or treatment of such cancer as brain tumor (particularly, glioblastoma multiform) and particularly Temodal resistant glioblastoma multiform.

Abstract translation: 本发明涉及用于预防或治疗包含硫唑嘌呤作为活性成分的多形态的癌症或耐炎性胶质母细胞瘤的药物组合物。 本发明的硫唑嘌呤不仅能有效抑制多形性成胶质细胞瘤的形成，而且是一种脑肿瘤，也是治疗多形性胶质母细胞瘤的优良表现，对于多形性胶质母细胞瘤的常规治疗药物Temodal（替莫唑胺）具有抗性， 它可以有效地用作药物组合物的活性成分，用于预防或治疗诸如脑肿瘤（特别是多形性胶质母细胞瘤）的癌症，特别是多形性的耐纹形胶质母细胞瘤。