KR930019648A - 테트라아자시클로도덴칸 유도체 및 그의 용도 - Google Patents

테트라아자시클로도덴칸 유도체 및 그의 용도 Download PDF

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KR930019648A
KR930019648A KR1019930004755A KR930004755A KR930019648A KR 930019648 A KR930019648 A KR 930019648A KR 1019930004755 A KR1019930004755 A KR 1019930004755A KR 930004755 A KR930004755 A KR 930004755A KR 930019648 A KR930019648 A KR 930019648A
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physiologically acceptable
hydrogen
compound
reactor
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KR1019930004755A
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칸 쿠보무라
시게미 세리
쿠미코 이와이
마코토 아즈마
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도키 가츠유키
니혼 메디피직스 가부시키가이샤
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Publication of KR930019648A publication Critical patent/KR930019648A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/085—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier conjugated systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • A61K49/101—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
    • A61K49/106—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals the complex-forming compound being cyclic, e.g. DOTA

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

본 발명은 의학적 화상진단이나 치료에 유용한 금속복합체를 형성하여 얻은 이 관성 착화제를 제공한다. 다음 구조식(Ⅰ)로 표시되는 이관능성 테트라아자시클로도데칸 유도체 및 이관능성 테트라아자시클로도데칸 유도체-기능성 물질과 금속이온을 착화시킨 금속착체 복합체이다.

Description

테트라아자시클로도데칸 유도체 및 그의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 화합물 투여전의 간자을 포함하는 복부관상 단층을 나타내는 생물의 형태 사진.
제2도는 DNS-DO3MA-Gd 용액투어 약 55분후의 간장을 포함하는 복부관상 단층을 나타내는 생물의 형태사진이다.

Claims (10)

  1. 다음 구조식(Ⅰ)로 표시되는 생리학적으로 허용가능한 화합물 및 그의 염.
    윗식에서, n은 1 내지 6의 정수를 나타내고,는 같거나 다를 수 있고, 수소원자 또는내지의 알킬기를 나타내고 A는 수소원자 또는 말단위치에 반응기를 함유하고, 카르보닐기로서 개재시킴으로써 포화 또는 불포화된 직쇄 또는 분지쇄의내지의 알킬렌기로 이루어진 반응성 관능기를 나타낸다.
  2. 제1항에 있어서, 말단위치의 반응기는 할로겐 원자, 티올기, 히드라진기 및 그의 유도체, -, -COO(는내지의 알킬기), 알데히드기, -COX(X는 염소 또는 브롬등의 할로겐 원자) 또는 N-히드록시숙신이미드에스테르기인 화합물.
  3. 제1항 내지 제3항중의 어느 하나의 항에 있어서,은 메틸,는 수소 n은 1 내지 3인 화합물.
  4. 제1항 내지 제3항중의 어느 하나의 항에 있어서,은 메틸기, n은 1 내지 3인 화합물.
  5. 제1항에 있어서, A는 수소인 화합물.
  6. 제1항에 있어서, A는 할로아세틸기인 화합물.
  7. 다음 구조식(Ⅱ)로 표시되는 생리학적으로 허용가능한 복합체 화합물 및 그의 염.
    윗식에서, n은 1 내지 6의 정수를 나타내고,는 같거나 다를 수 있고, 수소원자 또는내지의 알킬기를 나타내고 A′는 말단위치에 반응기를 함유하고, 카르보닐기로서 개재시킴으로써 포화 또는 불포화된 직쇄 또는 분지쇄의내지의 알킬렌으로 이루어진 반응성 관능기 잔기를 나타내고, Z는 기능성 물질에서 선택된 화합물을 나타낸다.
  8. 제7항에 기재된 생리학적으로 허용가능한 복합체화합물 및 그의 염과 원자번호 31,39,43,44,49 또는 57내지 71,76,77,79,81,83의 군에서 선택되어진 적어도 1종류의 금속이온이 착화되어진 생리학적으로 허용가능한 금속착체 복합체 화합물.
  9. 제8항에 있어서, 금속이온이 Gd, Dy, Ho, Bi, Os, In, Ga, Tc, Y, Sm인 금속착체 복합체 화합물.
  10. 제8항 및 제9항에 기재된 생리학적을 허용가능한 금속착체 복합체 화합물을 적어도 1종류 함유하는 것을 특징으로 하는 핵자기공명, X선 또는 방사선 진단용 약재 및 방사선 치료용 약재.
    ※ 참고사항 : 최초출원 내용에 있어서 공개하는 것임.
KR1019930004755A 1992-03-27 1993-03-26 테트라아자시클로도덴칸 유도체 및 그의 용도 KR930019648A (ko)

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JP10203392 1992-03-27
JP102033/199 1992-03-27

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EP (1) EP0565930A1 (ko)
KR (1) KR930019648A (ko)
AU (1) AU663572B2 (ko)
CA (1) CA2092596A1 (ko)

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JP3878208B2 (ja) * 1994-04-08 2007-02-07 ブラッコ インターナショナル ベスローテン フェンノートシャップ 芳香族アミド化合物およびそれらのキレート
US6693190B1 (en) 1994-05-11 2004-02-17 Bracco International B.V. Enhanced relaxivity monomeric and multimeric compounds
TR28540A (tr) * 1995-03-16 1996-09-30 Guerbet Sa Poliamine edilmis baglayicilar ve bunlarin metal kompleksleri.
US6106866A (en) * 1995-07-31 2000-08-22 Access Pharmaceuticals, Inc. In vivo agents comprising cationic drugs, peptides and metal chelators with acidic saccharides and glycosaminoglycans, giving improved site-selective localization, uptake mechanism, sensitivity and kinetic-spatial profiles, including tumor sites
WO1997014443A1 (en) * 1995-10-19 1997-04-24 Bracco International B.V. Magnetically labeled chemoattractants as targeted contrast agents in the nmr imaging of living tissues
US6565828B2 (en) 2000-04-07 2003-05-20 Bristol-Myers Squibb Company Macrocyclic chelants for metallopharmaceuticals
US6517814B2 (en) 2001-01-09 2003-02-11 Bristol-Myers Squibb Pharma Company Macrocyclic chelants useful for metallopharmaceuticals
JP2004530654A (ja) 2001-02-23 2004-10-07 ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー アテローム硬化症および脆弱性プラークを画像診断するための標識マクロファージスカベンジャー受容体拮抗薬
DE10135355C1 (de) * 2001-07-20 2003-04-17 Schering Ag Konjugate makrocyclischer Metallkomplexe mit Biomolekülen und deren Verwendung zur Herstellung von Mitteln für die NMR- und Radiodiagnostik sowie die Radiotherapie
DE10135356C1 (de) 2001-07-20 2003-04-17 Schering Ag Makrocyclische Metallkomplexe und deren Verwendung zur Herstellung von Konjugaten mit Biomolekülen
FR2857967B1 (fr) * 2003-07-25 2015-04-24 Centre Nat Rech Scient Complexes de lanthanide, leur preparation et leurs utilisations
DE102004062258B3 (de) * 2004-12-23 2006-01-05 Schering Ag Hydroxypyridinon-Derivate, deren Metallkomplexe und deren Verwendung zur Herstellung von Konjugaten mit Biomolekülen
DE102007002726A1 (de) 2007-01-18 2008-07-31 Bayer Schering Pharma Aktiengesellschaft Neue Kaskaden-Polymer-Komplexe, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Mittel

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AU3551993A (en) 1993-09-30
EP0565930A1 (en) 1993-10-20
CA2092596A1 (en) 1993-09-28

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