公开(公告)号：US12050224B2

公开(公告)日：2024-07-30

申请号：US17021438

申请日：2020-09-15

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Ghil Soo Nam ,  Hyun Ah Choo ,  Ahmed A. Elbatrawy ,  Gyo Chang Keum ,  Yun Kyung Kim ,  Sung Su Lim ,  Jae Kyun Lee ,  Eun Kyoung Bang

IPC: G01N33/68 ,  C07D215/20 ,  C07D215/48 ,  C07D401/06 ,  G01N33/58

CPC classification number: G01N33/6896 ,  C07D215/20 ,  C07D215/48 ,  C07D401/06 ,  G01N33/582 ,  G01N2800/2814 ,  G01N2800/2821 ,  G01N2800/2835

Abstract: Disclosed are a compound with near-infrared fluorescence that selectively binds to tau aggregates, a method for preparing the same, a tau-targeting near-infrared fluorescent probe including the compound, a composition for detecting a tau fiber protein containing the near-infrared fluorescent probe as an active ingredient, and the use of the composition for the diagnosis of tauopathy. In particular, the compound does not bind to an amyloid beta protein and has high selectivity to a tau aggregate, specifically reported as an etiology of the initial state of tauopathy, thus being useful as a near-infrared fluorescent detector for detecting a tau fiber protein for early diagnosis of a tauopathy including Alzheimer's disease.

公开(公告)号：US09663464B2

公开(公告)日：2017-05-30

申请号：US14629821

申请日：2015-02-24

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Hyunah Choo ,  Gyo Chang Keum ,  Youngjae Kim ,  Mi Young Yeom

IPC: C07D403/06 ,  A61K31/496 ,  C07D209/86 ,  C07D401/06 ,  C07D413/06

CPC classification number: C07D209/86 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06

Abstract: The present invention provides a carbazole derivative represented by Formula 1: wherein X is CH2 or C(O), Y is selected from NR1R2, piperidinyl groups in which two of the carbon atoms are substituted with R3 and R4, piperazinyl groups in which the nitrogen atom is substituted with R5, and morpholinyl groups, n is an integer from 2 to 5, R1 and R2, which may be identical or different, are each independently selected from C1-C6 alkyl, phenyl, and benzyl, with the proviso that R1 and R2 may be bonded together to form a ring, R3 and R4, which may be identical or different, are each independently selected from hydrogen, C1-C6 alkyl, phenyl, and benzyl, and R5 is selected from C1-C6 alkyl, C1-C4 alkylcarbonyl, phenyl substituted with C1-C4 alkyloxy, hydroxyphenyl, benzyl, and benzoisoxazol-3-yl; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US10421779B2

公开(公告)日：2019-09-24

申请号：US15687203

申请日：2017-08-25

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  POSTECH ACADEMY-INDUSTRY FOUNDATION

Inventor： Gyo Chang Keum ,  Eunice Eun Kyeong Kim ,  Sung Key Jang ,  Hee Sun Kim ,  Ae Nim Pae ,  Hua Li ,  Jin Hyeong Park ,  Jin Sook Kwak

IPC: C07D209/88 ,  C07K5/065 ,  C07K5/062 ,  A61K38/00

Abstract: The present invention relates to a carbazole compound having anti-virus activity, and more particularly, to a novel compound selected from the group of consisting of a carbazole compound which shows excellent anti-proliferative efficacy against hepatitis C virus (HCV), a pharmaceutically acceptable salt thereof, a hydrate thereof, and an isomer thereof; an anti-virus pharmaceutical composition including the novel compound as an active ingredient; a pharmaceutical composition for preventing or treating liver diseases caused by hepatitis C virus; and a method of preparing the novel compound.

公开(公告)号：US10190120B2

公开(公告)日：2019-01-29

申请号：US15671901

申请日：2017-08-08

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Gyo Chang Keum ,  Eun Kyoung Bang ,  Jin Bum Kim

IPC: C07F3/06 ,  C07D401/12 ,  A61K48/00 ,  C12N15/113 ,  C07D213/38 ,  C07D495/04 ,  C12N15/11

Abstract: Provided herein are a novel Zn-DPA complex compound and an siRNA delivery system including the same as a transporter, the Zn-DPA complex compound including: a phosphate-directing functional part of zinc (II)-dipicolylamine (“Zn-DPA”); a cell membrane-directing functional part; and a linker part that links the phosphate-directing functional part and the cell membrane-directing functional part. The Zn-DPA complex compound has low toxicity and efficiently delivers siRNA to cells, thereby useful in various ways for various studies and diagnosis and treatment of diseases, which use siRNA.

公开(公告)号：US11407745B2

公开(公告)日：2022-08-09

申请号：US16897987

申请日：2020-06-10

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Gyo Chang Keum ,  Ashraf Kareem El-Damasy ,  Hee Won Jin ,  Taek Kang ,  Eun Kyoung Bang

IPC: C07D413/12 ,  C07D403/12 ,  C07D231/56 ,  A61P35/02

Abstract: Disclosed are a compound selected from novel indazole derivatives, pharmaceutically acceptable salts thereof, hydrates thereof and stereoisomers thereof, a method for preparing the compound, and a pharmaceutical composition for preventing, alleviating or treating cancer containing the compound as an active ingredient. The novel indazole derivatives exhibit excellent ABL/DDR1 inhibitory efficacy and anti-proliferative efficacy against cancer cells, specifically blood cancer cells, and inhibitory activity against ABL T315I point mutations, thus being useful for the prevention, alleviation or treatment of cancer, specifically blood cancer, especially chronic myelogenous leukemia.

公开(公告)号：US08895602B1

公开(公告)日：2014-11-25

申请号：US14013487

申请日：2013-08-29

Applicant: Korea Institute of Science and Technology

Inventor： Ghil Soo Nam ,  Kyung Il Choi ,  Ae Nim Pae ,  Seon Hee Seo ,  Hyun Ah Choo ,  Gyo Chang Keum ,  Jung Hyun Kim

IPC: A61K31/4155 ,  C07D403/12

CPC classification number: C07D403/12 ,  A61K31/4155

Abstract: The present invention relates to a 6-pyrazolylamido-3-substituted azabicyclo[3.1.0]hexane derivatives useful as calcium channel blockers, pharmaceutically acceptable salts thereof and medical use of the calcium channel inhibiting effect of the compounds for treatment of diseases.

Abstract translation: 本发明涉及可用作钙通道阻滞剂的6-吡唑基氨基-3-取代的氮杂双环[3.1.0]己烷衍生物，其药学上可接受的盐，以及该化合物治疗疾病的钙通道抑制作用的医学应用。