WO2016111523A3 - HNF4-α 길항제 및 이의 용도 - Google Patents

HNF4-α 길항제 및 이의 용도 Download PDF

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Publication number
WO2016111523A3
WO2016111523A3 PCT/KR2016/000055 KR2016000055W WO2016111523A3 WO 2016111523 A3 WO2016111523 A3 WO 2016111523A3 KR 2016000055 W KR2016000055 W KR 2016000055W WO 2016111523 A3 WO2016111523 A3 WO 2016111523A3
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hnf4
antagonist
present
inhibit
treating
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PCT/KR2016/000055
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English (en)
French (fr)
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WO2016111523A2 (ko
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김연희
남승윤
박희서
장혜령
정해림
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국립암센터
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Priority claimed from KR1020160000813A external-priority patent/KR101758208B1/ko
Publication of WO2016111523A2 publication Critical patent/WO2016111523A2/ko
Publication of WO2016111523A3 publication Critical patent/WO2016111523A3/ko

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37—Coumarins, e.g. psoralen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A61K31/515—Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Emergency Medicine (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)

Abstract

본 발명은 HNF4-α(Hepatocyte nuclear factor 4 alpha) 길항제 및 이의 용도에 관한 것으로, 본 발명의 HNF4-α(Hepatocyte nuclear factor 4 alpha) 길항제 및 이의 용도에 관한 것으로, 본 발명에서 선별한 HNF4-α 길항제는 HNF4-α의 리간드 바인딩 도메인에 특이적으로 결합하여 HNF4-α의 활성을 억제시키는 것을 확인하였으며, 본 발명의 HNF4-α 길항제는 기존에 알려진 HNF4-α 길항제에 비해 현저하게 Wnt5a의 발현을 특이적으로 감소시키고, 위암세포의 성장을 억제할 수 있으므로, 암 예방 및 치료용 약학적 조성물 또는 건강기능식품으로 활용될 수 있을 뿐만 아니라, HNF4-α 과발현으로 인해 발생하는 질환의 치료 또는 예방용 조성물로 응용할 수 있다.
PCT/KR2016/000055 2015-01-05 2016-01-05 HNF4-α 길항제 및 이의 용도 WO2016111523A2 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR10-2015-0000759 2015-01-05
KR20150000759 2015-01-05
KR10-2016-0000813 2016-01-05
KR1020160000813A KR101758208B1 (ko) 2015-01-05 2016-01-05 HNF4-α 길항제 및 이의 용도

Publications (2)

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WO2016111523A2 WO2016111523A2 (ko) 2016-07-14
WO2016111523A3 true WO2016111523A3 (ko) 2017-02-16

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US (2) US20160193238A1 (ko)
WO (1) WO2016111523A2 (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020206055A1 (en) * 2019-04-02 2020-10-08 Yale University Methods of treatment of diseases and disorders associated with increased tet level, increased h19 level, increased level of tgf signaling, or any combination thereof
WO2021072139A1 (en) * 2019-10-11 2021-04-15 Massachusetts Institute Of Technology Formulations for gastrointestinal delivery of oligonucleotides
CN112426420B (zh) * 2020-12-01 2021-12-28 浙江大学 香豆素-二硫代氨基甲酸酯衍生物在制备抗肿瘤药物中的应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US48638A (en) * 1865-07-11 Improved foot-rest
WO2010111713A2 (en) * 2009-03-27 2010-09-30 Zacharon Pharmaceuticals, Inc. N-linked glycan biosynthesis modulators
WO2010111711A2 (en) * 2009-03-27 2010-09-30 Zacharon Pharmaceuticals, Inc. Ganglioside biosynthesis modulators
WO2012030960A1 (en) * 2010-09-01 2012-03-08 Promega Corporation Oxidized glutathione assay
KR20120065311A (ko) * 2009-07-15 2012-06-20 씬산 강 저산소증 모방체인 화합물, 및 그의 조성물 및 용도

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001290241A1 (en) 2000-09-20 2002-04-02 Kyowa Hakko Kogyo Co. Ltd. Tumor cell proliferation inhibitors
JP5004331B2 (ja) 2006-11-29 2012-08-22 花王株式会社 ＨＮＦ−４α活性抑制剤
WO2010127264A2 (en) 2009-04-30 2010-11-04 Burnham Institute For Medical Research HNF4α ANTAGONISTS AND METHODS OF USE

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US48638A (en) * 1865-07-11 Improved foot-rest
WO2010111713A2 (en) * 2009-03-27 2010-09-30 Zacharon Pharmaceuticals, Inc. N-linked glycan biosynthesis modulators
WO2010111711A2 (en) * 2009-03-27 2010-09-30 Zacharon Pharmaceuticals, Inc. Ganglioside biosynthesis modulators
KR20120065311A (ko) * 2009-07-15 2012-06-20 씬산 강 저산소증 모방체인 화합물, 및 그의 조성물 및 용도
WO2012030960A1 (en) * 2010-09-01 2012-03-08 Promega Corporation Oxidized glutathione assay

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US20170189371A1 (en) 2017-07-06
US9795586B2 (en) 2017-10-24
US20160193238A1 (en) 2016-07-07
WO2016111523A2 (ko) 2016-07-14

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