KR910000604A - 디에틸렌트리아민 펜타아세트산 유도체 - Google Patents

디에틸렌트리아민 펜타아세트산 유도체 Download PDF

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KR910000604A
KR910000604A KR1019890007823A KR890007823A KR910000604A KR 910000604 A KR910000604 A KR 910000604A KR 1019890007823 A KR1019890007823 A KR 1019890007823A KR 890007823 A KR890007823 A KR 890007823A KR 910000604 A KR910000604 A KR 910000604A
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radioactive metal
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스스무 곤도
미끼 구라미
마꼬또 아즈마
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도끼 가스유끼
니혼 메디피직꾸스 가부시끼가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • 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
    • 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
    • A61K51/0474—Organic 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
    • A61K51/0478—Organic 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
    • A61K51/048—DTPA (diethylenetriamine tetraacetic acid)
    • 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
    • A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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
    • C07C237/10—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C317/18—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

내용 없음

Description

디에틸렌트리아민 펜타아세트산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (24)

  1. 하기식(I)의 화합물 및 생리학적으로 허용 가능한 그의 염.
    [상기식에서, n은 2~10의 정수이고, 및 A는 교차 결합제의 2개의 반응기중 하나를 반응시켜 형성된 1가기이다.]
  2. 제1항에 있어서, n이 2~6의 정수인 화합물.
  3. 제1항에 있어서, A가 약 100 내지 약 1000의 분자량을 가지는 화합물.
  4. 제1항에 있어서, A가 적어도 하나의 생리학적으로 분해 가능한 연결기를 가지는 화합물.
  5. 제4항에 있어서, 전술한 생리학적으로 분해 가능한 연결기가 -O-, -COO-, -S-,-SS-, -SO- 및 -SO2-로 구성된 군에서 선택되는 화합물.
  6. 제5항에 있어서, A가 하기 :
    로 구성된 군에서 선택되는 화합물.
  7. 하기식(II)의 화합물 및 생리학적으로 허용 가능한 그의 염.
    [상기식에서 n은 2~10의 정수이고, 및 A′는 교차 결합제의 반응성기 둘다를 반응시켜 형성된 2가 연결기이고, 및 B는 폴리펩티드 화합물의 잔기이다]
  8. 제7항에 있어서, n이 2~6의 정수인 화합물.
  9. 제7항에 있어서, A′가 약 100 내지 약 1000의 분자량을 가지는 화합물.
  10. 제7항에 있어서, A′가 적어도 하나의 생리학적으로 분해 가능한 연결기를 가지는 화합물.
  11. 제10항에 있어서, 전술한 생리학적으로 분해 가능한 연결기가 -O-, -COO-, -S-, -SS-, -SO-, 및 -SO2-로 구성된 군에서 선택되는 화합물.
  12. 제11항에 있어서, A′가 하기 :
    -CO-CH2CH2-CO-O-CH2CH2-O-CO-CH2CH2-CO-
    -CO-CH2CH2-S-S-CH2CH2-CO-
    -CO-CHOH-CHOH-CO-, 및
    로 구성된 군에서 선택되는 화합물.
  13. 제7항에 있어서, B가 폴리펩티드, 단순단백질, 리포프로테인 및 글리코프로테인으로 구성된 군에서 선택되는 화합물.
  14. 제7항에 있어서, B가 생물학적 활성을 갖는 단백질인 화합물.
  15. 제7항에 있어서, B가 세럼 단백질, 펩티드 호르몬, 펩티드 항생물질, 항체 및 그의 단편물인 화합물.
  16. 제15항에 있어서, 전술한 세럼 단백질이 면역 글로불린인 화합물.
  17. 제7항에 따른 화합물을 적어도 1종 포함하는 방사성 등위원소용 담체.
  18. 방사성 금속원소로 표지된 제7항에 따른 화합물을 포함하는 방사성 진단 시약.
  19. 제18항에 있어서, 전술한 방사성 금속원소가 111In 99mTc, 67Ga68Ga62Cu및 62Zn으로 구성된 군에서 선택되는 시약.
  20. 방사성 금속원소로 표지된 제7항에 따른 화합물을 포함하는 방사성 치료제.
  21. 제20항에 있어서, 전술한 방사성 금속원소가 90Y, 186Re153Sm212Pb및 211Bi로 구성된 군에서 선택되는 치료제.
  22. 하기식(IIIa)의 화합물.
  23. 방사성 금속원소로 표지된 제7항에 따른 화합물을 포함하는 방사성 진단 시약.
  24. 제20항에 있어서, 진술한 방사성 금속원소가 90Y, 186Re153Sm212Pb및 211Bi로 구성된 군에서 선택되는 치료제.
    [상기식에서 n은 3~10의 정수이다.]
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890007823A 1988-06-07 1989-06-07 디에틸렌트리아민 펜타아세트산 유도체 KR0126238B1 (ko)

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JP63-139885 1988-06-07
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US (1) US5094950A (ko)
EP (1) EP0345723B1 (ko)
KR (1) KR0126238B1 (ko)
AT (1) ATE106075T1 (ko)
AU (1) AU617816B2 (ko)
CA (1) CA1331450C (ko)
DE (1) DE68915476T2 (ko)
DK (1) DK276789A (ko)
ES (1) ES2056150T3 (ko)

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US5686410A (en) * 1989-07-20 1997-11-11 Novartis Ag Polypeptide derivatives
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JP2901787B2 (ja) * 1991-07-15 1999-06-07 日本メジフィジックス株式会社 核磁気共鳴造影剤
US5562894A (en) * 1991-08-09 1996-10-08 Regents Of The University Of California Amino-acyl-type and catecholamine-type contrast agents for MRI
JP2894879B2 (ja) * 1991-10-04 1999-05-24 日本メジフィジックス株式会社 診断用造影剤
PT590766E (pt) * 1992-07-31 2000-07-31 Australian Nuclear Science Tec Complexos metalicos de hidroxiarilo contendo agentes quelantes de acido aminocarboxilico
AU5360994A (en) * 1992-10-13 1994-05-09 Mallinckrodt Medical, Inc. Novel compositions for magnetic resonance imaging
DE69421698T2 (de) * 1993-05-14 2000-03-09 Mallinckrodt, Inc. Die vorstufe eines liganden zum einbau in peptide
DE19505960A1 (de) * 1995-02-21 1996-08-22 Deutsches Krebsforsch Konjugat zur individuellen Dosierung von Arzneimitteln
AU2001234478A1 (en) * 2000-01-21 2001-07-31 Mallinckrodt, Inc. Chelating agents and method for their use as tandem metal chelators and hydrophilic spacers for medical diagnosis and therapy
WO2001052900A2 (en) * 2000-01-21 2001-07-26 Mallinckrodt Inc. Novel orthogonally protected amino acid chelators for biomedical applications
AU2001232845A1 (en) * 2000-01-21 2001-07-31 Mallinckrodt, Inc. Methods for incorporating metal chelators at carboxyl-terminal site of peptides
TW200505934A (en) * 2003-03-26 2005-02-16 Nihon Mediphysics Co Ltd Compound having affinity with calcified tissue
EP1771440A4 (en) * 2004-07-23 2009-09-02 Amgen Inc GENERIC PROBES FOR THE DETECTION OF PHOSPHORYLATED SEQUENCES
CN100382847C (zh) * 2005-02-05 2008-04-23 四川大学 用于影像诊断的配合体化合物及制备方法和影像诊断用化合物及其制备中间体
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DK276789D0 (da) 1989-06-06
DK276789A (da) 1989-12-08
ATE106075T1 (de) 1994-06-15
ES2056150T3 (es) 1994-10-01
CA1331450C (en) 1994-08-16
KR0126238B1 (ko) 1997-12-26
EP0345723A2 (en) 1989-12-13
US5094950A (en) 1992-03-10
AU3603989A (en) 1989-12-14
EP0345723B1 (en) 1994-05-25
DE68915476T2 (de) 1994-09-29
EP0345723A3 (en) 1991-01-09
DE68915476D1 (de) 1994-06-30
AU617816B2 (en) 1991-12-05

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