KR910018346A - 킬레이트화 화합물 및 그의 용도 - Google Patents

킬레이트화 화합물 및 그의 용도 Download PDF

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KR910018346A
KR910018346A KR1019910005737A KR910005737A KR910018346A KR 910018346 A KR910018346 A KR 910018346A KR 1019910005737 A KR1019910005737 A KR 1019910005737A KR 910005737 A KR910005737 A KR 910005737A KR 910018346 A KR910018346 A KR 910018346A
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시게미 세리
히로히꼬 야마우찌
마꼬또 아즈마
요지 아라따
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도끼 가쓰유끼
니혼메디피직스 가부시끼가이샤
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    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0474Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0478Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
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    • A61K51/0478Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • A61K51/048DTPA (diethylenetriamine tetraacetic acid)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
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    • A61K51/04Organic compounds
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/10Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00Preparations for testing in vivo

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Abstract

내용 없음

Description

킬레이트화 화합물 및 그의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 In-111-B-DNS-etn-DAPA를 투여한 지 70시간 후의 간암조직 이식된 쥐의 신티그램(scintigram)을 나타낸다.

Claims (14)

  1. 하기 일반식(Ⅰ)의 킬레이트화 화합물 또는 그의 염 :
    (R-NHOC-CH2)n-A-(CH2COOH)m(Ⅰ)
    〔식중, R은 방향족 고리-함유 유기기이고, A는 아세트산기(-CH2COOH)가 배제된 아미노폴리아세트산 잔기이며, m은 2이상의 정수이고, n은 1 또는 2는 정수이다〕.
  2. 제1항에 있어서, 방향족 고리-함유 유기기가, 아릴부분이 저급알킬, 저급 알킬아미노 또는 디 (저급) 알킬아미노에 의해 임의로 치환된 페닐 또는 나프틸인 아릴, 아르 (저급) 알킬, 아릴술포닐, 아르 (저급) 알킬술포닐, 아릴아미노 (저급)알킬, 아르 (저급) 알킬, 아미노 (저급) 알킬 아실술포닐아미노 (저급) 알킬 또는 아르 (저급) 알킬술포닐아미노 (저급) 알킬인 화합물 또는 그의 염.
  3. 제1항에 있어서, 방향족 고리-함유 유기기가, 단실인 화합물 또는 그의 염.
  4. 제1항에 있어서, 방향족 고리-함유 유기기가, 단실아미노 (저급) 알킬인 화합물 또는 그의 염.
  5. 제1항에 있어서, 아미노폴리아세트산이 직쇄, 측쇄 또는 고리형의 탄화수소 사슬, 탄화수소 사슬내 및/또는 말단 위치에 존재하는 2이상의 아미노기 및 상기 아미노기내 질소 원자에 각각 결합된 3이상의 아세트산기(-CH2COOH)를 함유하는 화합물 또는 그의 염.
  6. 제1항에 있어서, 아미노폴리아세트산인 에틸렌디아민-테트라아세트산 (EDTA), 디에틸렌트리아민-펜타아세트산(DAPA), 트랜스-1,2-시클로헥사디아민-테트라아세트산(CyDTA) 또는 1,4,7,10-테트라아자시클로도데칸-테트라아세트산(DOTA)인 화합물 또는 그의 염.
  7. 제1항 내지 제6항중 어느 한 항에 따른 화합물 및 킬레이트 결합을 통해 결합된 금속 원소를 함유하는 킬레이트 화합물.
  8. 제7항에 있어서, 금속원자가 방사능 원소인 킬레이트 화합물.
  9. 제8항에 있어서, 방사능 원소가 테크네튬-99m, 인듐-111, 레늄-186, 레늄-188 또는 이트륨-90인 킬레이트 화합물.
  10. 제7항에 있어서, 금속 원소가 상자성 원소인 킬레이트 화합물.
  11. 제10항에 있어서, 상자성 원소가 가돌리늄인 킬레이트 화합물.
  12. 제1항에 내지 제6항중 어느 한 항에 따른 킬레이트화 화합물을 함유하며 킬레이트 형성능 및 간담즙성 기관 또는 조직에 대해 특이성을 갖는, 금속원소에 대한 담체.
  13. 제7항에 내지 제11항중 어느 한 항에 따른 킬레이트 화합물을 함유하는, 간담즙성 기관 또는 조직에 대한 진단제.
  14. 제7항에 내지 제11항중 어느 한 항에 따른 킬레이트 화합물을 함유하는, 간담즙성 기관 또는 조직에 대한 치료제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910005737A 1990-04-10 1991-04-10 킬레이트화 화합물 및 그의 용도 KR100189388B1 (ko)

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JP94353/1990 1990-04-10
JP094353/1990 1990-04-10
JP2094353A JP2776953B2 (ja) 1990-04-10 1990-04-10 多官能性金属キレート化合物とその用途

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US (2) US5196576A (ko)
EP (1) EP0451824B1 (ko)
JP (1) JP2776953B2 (ko)
KR (1) KR100189388B1 (ko)
AT (1) ATE134190T1 (ko)
AU (1) AU634645B2 (ko)
CA (1) CA2040204C (ko)
DE (1) DE69117084T2 (ko)
DK (1) DK0451824T3 (ko)
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US5138039A (en) 1992-08-11
JPH03291260A (ja) 1991-12-20
DE69117084T2 (de) 1996-10-02
JP2776953B2 (ja) 1998-07-16
CA2040204C (en) 2002-07-02
ATE134190T1 (de) 1996-02-15
EP0451824B1 (en) 1996-02-14
US5196576A (en) 1993-03-23
DK0451824T3 (da) 1996-03-11
ES2085924T3 (es) 1996-06-16
KR100189388B1 (ko) 1999-06-01
AU634645B2 (en) 1993-02-25
EP0451824A3 (en) 1992-09-02
AU7428191A (en) 1991-10-17
DE69117084D1 (de) 1996-03-28
EP0451824A2 (en) 1991-10-16
CA2040204A1 (en) 1991-10-11

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