WO2011149250A3 - 트리카르보닐 테크네슘-99ｍ 또는 레늄-188 표지 고리 알지디 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신생혈관 관련 질환의 진단 또는 치료용 약학적 조성물 - Google Patents

트리카르보닐 테크네슘-99ｍ 또는 레늄-188 표지 고리 알지디 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신생혈관 관련 질환의 진단 또는 치료용 약학적 조성물 Download PDF

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WO2011149250A3
WO2011149250A3 PCT/KR2011/003801 KR2011003801W WO2011149250A3 WO 2011149250 A3 WO2011149250 A3 WO 2011149250A3 KR 2011003801 W KR2011003801 W KR 2011003801W WO 2011149250 A3 WO2011149250 A3 WO 2011149250A3
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Prior art keywords
derivative
rhenium
label
angiogenesis
diagnosis
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PCT/KR2011/003801
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English (en)
French (fr)
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WO2011149250A2 (ko
Inventor
이병철
김상은
김지선
문병석
정재호
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서울대학교 산학협력단
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Priority to CN201180031236.6A priority Critical patent/CN102985413B/zh
Priority to JP2013512534A priority patent/JP5774687B2/ja
Priority to US13/699,511 priority patent/US9439986B2/en
Priority to EP11786882.8A priority patent/EP2583966B1/en
Publication of WO2011149250A2 publication Critical patent/WO2011149250A2/ko
Publication of WO2011149250A3 publication Critical patent/WO2011149250A3/ko

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/082—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the peptide being a RGD-containing peptide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
    • C07D273/06—Seven-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G01N33/60—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances involving radioactive labelled substances

Abstract

본 발명은 트리카르보닐 테크네슘-99m 또는 레늄-188 표지 고리 알지디 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신생혈관 관련 질환의 진단 또는 치료용 약학적 조성물에 관한 것으로, 본 발명의 트리카르보닐 테크네슘-99m 또는 레늄-188 표지 고리 알지디 유도체는 종양에 의해 유도되는 신생혈관작용에서 활성화된 비트로넥틴(Vitronectin) 수용체라고도 불리는 αvβ3 인테그린에 서브나노몰(subnanomolar) 단위의 높은 친화도를 가지고, 암세포가 이식된 동물에서 트리카르보닐 테크네슘-99m 표지 고리 알지디 유도체 초기 섭취 후 높은 종양 영상을 반영하고 간과 장에서의 섭취율이 기존의 알려진 방사성동위원소 표지 고리 알지디 유도체에 비해 현저하게 낮아 선택적으로 αvβ3 인테그린이 활성화된 암세포에만 작용함을 알 수 있으며, 이와 같은 결과를 바탕으로 테크네슘-99m 표지에 사용된 동일 전구체를 사용한 치료 핵종인 레늄-188 표지 유도체의 경우 생리식염수만 주입한 종양 동물모델과는 달리 꼬리 정맥 주입 시 효과적인 종양의 성장 저해와 치료 효능을 나타내기 때문에 신생혈관 관련 질환의 진단 또는 치료용 의약품으로 유용하게 이용될 수 있다.
PCT/KR2011/003801 2010-05-24 2011-05-24 트리카르보닐 테크네슘-99ｍ 또는 레늄-188 표지 고리 알지디 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신생혈관 관련 질환의 진단 또는 치료용 약학적 조성물 WO2011149250A2 (ko)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CN201180031236.6A CN102985413B (zh) 2010-05-24 2011-05-24 三羰基锝-99m或铼-188标记的环RGD衍生物、其制备方法和包含所述衍生物作为活性成分用于诊断或治疗血管发生相关疾病的药物组合物
JP2013512534A JP5774687B2 (ja) 2010-05-24 2011-05-24 トリカルボニルテクネシウム−９９ｍまたはレニウム−１８８標識サイクリックＲＧＤ誘導体、その製造方法及びそれを有効成分として含む新生血管関連疾患の診断または治療用薬学的組成物
US13/699,511 US9439986B2 (en) 2010-05-24 2011-05-24 Tricarbonyl technetium-99m, rhenium-185/187, or rhenium-188 labeled cyclic RGD derivatives and uses thereof
EP11786882.8A EP2583966B1 (en) 2010-05-24 2011-05-24 Tricarbonyl technetium-99m or rhenium-188 label ring rgd derivative, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment of angiogenesis-related diseases

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR20100048289 2010-05-24
KR10-2010-0048289 2010-05-24
KR1020110043544A KR101383655B1 (ko) 2010-05-24 2011-05-09 트리카르보닐 테크네슘-99ｍ 또는 레늄-188 표지 고리 알지디 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신생혈관 관련 질환의 진단 또는 치료용 약학적 조성물
KR10-2011-0043544 2011-05-09

Publications (2)

Publication Number Publication Date
WO2011149250A2 WO2011149250A2 (ko) 2011-12-01
WO2011149250A3 true WO2011149250A3 (ko) 2012-03-22

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US (1) US9439986B2 (ko)
EP (1) EP2583966B1 (ko)
JP (1) JP5774687B2 (ko)
KR (1) KR101383655B1 (ko)
CN (1) CN102985413B (ko)
WO (1) WO2011149250A2 (ko)

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HUE063437T2 (hu) 2013-09-24 2024-01-28 Fujifilm Corp Nitrogént tartalmazó vegyületet vagy sóját vagy fémkomplexét tartalmazó gyógyászati készítmény
WO2016153054A1 (ja) 2015-03-25 2016-09-29 富士フイルム株式会社 新規な含窒素化合物またはその塩の製造方法およびそれらの製造中間体
CN106474495B (zh) * 2016-11-21 2019-07-09 中国医学科学院阜外医院 含亚氨基二乙酸的99mTc标记的RGD多肽肿瘤诊断药物及其制备方法
KR102250737B1 (ko) * 2020-06-01 2021-05-11 주식회사 비아이케이테라퓨틱스 약물 전달과 내재화 효율이 강화된 약물복합체

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Also Published As

Publication number Publication date
CN102985413B (zh) 2016-04-20
US9439986B2 (en) 2016-09-13
EP2583966A2 (en) 2013-04-24
JP5774687B2 (ja) 2015-09-09
KR20110128732A (ko) 2011-11-30
US20130064766A1 (en) 2013-03-14
EP2583966B1 (en) 2016-08-10
WO2011149250A2 (ko) 2011-12-01
CN102985413A (zh) 2013-03-20
JP2013533852A (ja) 2013-08-29
EP2583966A4 (en) 2013-11-13
KR101383655B1 (ko) 2014-04-10

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