KR970700698A - NEW POLYAMINOCARBOXYLATE CHELATORS - Google Patents

NEW POLYAMINOCARBOXYLATE CHELATORS Download PDF

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KR970700698A
KR970700698A KR1019960703633A KR19960703633A KR970700698A KR 970700698 A KR970700698 A KR 970700698A KR 1019960703633 A KR1019960703633 A KR 1019960703633A KR 19960703633 A KR19960703633 A KR 19960703633A KR 970700698 A KR970700698 A KR 970700698A
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formula
conjugated
complex
compound
bonded
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KR1019960703633A
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Korean (ko)
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서브라마니안 라미스워미
콜로니 제임스
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에프. 지. 엠. 헤르만스; 이. 에이취. 리링크
악조 노벨 엔. 브이.
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Application filed by 에프. 지. 엠. 헤르만스; 이. 에이취. 리링크, 악조 노벨 엔. 브이. filed Critical 에프. 지. 엠. 헤르만스; 이. 에이취. 리링크
Publication of KR970700698A publication Critical patent/KR970700698A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K17/00—Carrier-bound or immobilised peptides; Preparation thereof
    • C07K17/02—Peptides being immobilised on, or in, an organic carrier
    • 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
    • G01N33/531—Production of immunochemical test materials
    • G01N33/532—Production of labelled immunochemicals
    • G01N33/534—Production of labelled immunochemicals with radioactive label
    • 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
    • C07C245/00—Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
    • C07C245/20—Diazonium compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00—Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/16—Isothiocyanates
    • C07C331/28—Isothiocyanates having isothiocyanate groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D259/00—Heterocyclic compounds containing rings having more than four nitrogen atoms as the only ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Optics & Photonics (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Public Health (AREA)
  • Microbiology (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Food Science & Technology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Polyamides (AREA)

Abstract

본 발명은 폴리펩티드 분자에 금속 이온을 결합시키기에 적합한 일련의 신규한 폴리아미노카르복실레이트 킬레이트제에 관한 것이다. 상기 신규의 킬레이트제를 사용하여 제조된 폴리펩티드-폴리아미노카르복실레이트 공액 결합체는 금속이온과 함께 안정한 착체를 형성한다.The present invention relates to a series of novel polyaminocarboxylate chelating agents suitable for binding metal ions to polypeptide molecules. Polypeptide-polyaminocarboxylate conjugated conjugates prepared using these novel chelating agents form stable complexes with metal ions.

Description

폴리아미노카르복실레이트 킬레이트제(NEW POLYAMINOCARBOXYLATE CHELATORS)NEW POLYAMINOCARBOXYLATE CHELATORS

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

도1은 폴리아민 구조식이다, 도2는 LiLo2′의 구조식이다, 도3은 HETA 2의 구조식이다, 도4는 HETA2 및 LiLo2′를 제조하기 위하여 사용된 합성도식이다.1 is a polyamine structural formula, FIG. 2 is a structural formula of LiLo2 ', FIG. 3 is a structural formula of HETA 2, and FIG. 4 is a synthetic scheme used to prepare HETA2 and LiLo2'.

Claims (13)

하기 화학식(1)의 킬레이트제에 결합된 폴리펩티드, 올리고뉴클레오티드, 폴리뉴클레오티드 또는 합성 중합체를 포함하는 공액결합체;Conjugates including polypeptides, oligonucleotides, polynucleotides or synthetic polymers bound to chelating agents of formula (1); 화학식 1Formula 1 상기식에서, n은 0 내지 12이고; m은 2내지 12이며; o는 1내지 4이고; p는 1내지 4이며; R′는 -CS-NH, -CH2-CO-NH-, 또는 결합이며, 단 o+p≥2인 경우에는 폐환 구조를 형성할 수 있다.In which n is 0 to 12; m is 2 to 12; o is 1 to 4; p is 1 to 4; R ′ is —CS—NH, —CH 2 —CO—NH—, or a bond, provided that o + p ≧ 2 may form a ring closure structure. 하기 화학식 (2)의 화합물:A compound of formula (2) 화학식 2Formula 2 상기식에서, n은 0 내지 12이고;m은 2내지 12이며; o는 1내지 4이고; p는 1내지 4이며; R는 아미노산 서열에 공유적으로 결합되는 반응성부이며, 단 o+p≥2인 경우에는 폐환 구조를 형성할 수 있다.Wherein n is 0 to 12; m is 2 to 12; o is 1 to 4; p is 1 to 4; R is a reactive moiety covalently linked to the amino acid sequence, provided that o + p ≧ 2 can form a ring-closure structure. 하기 화학식(3)의 화합물 : 화학식 3A compound of formula (3): 상기식에서, R3은 NO2이고: R4는 H, 또는 -CO-CH2-NH(CH2-CH2-NH)yH이며: R5은 H, -CO-CH2-NH(CH2-CH2-NH)zH이거나; 또는 R4및 R5는 함께를 나타내며; 이때, n은 0 내지 12이고, m은 2내지 12이며, y는 0내지 3이고, z는 0내지 3이다.Wherein R 3 is NO 2: R 4 is H, or —CO—CH 2 —NH (CH 2 —CH 2 —NH) y H: R 5 is H, —CO—CH 2 —NH (CH 2 —CH 2 —NH) z H; Or R 4 and R 5 together Represents; In this case, n is 0 to 12, m is 2 to 12, y is 0 to 3, and z is 0 to 3. 제1항에 있어서, 킬레이트제가 하기 화학식(4)의 LiLO2′인 공액 결합체:The conjugate of claim 1 wherein the chelating agent is LiLO 2 ′ of formula (4): 화학식 4Formula 4 제2항에 있어서, 하기 화학식(4)를 갖는 화합물: 화학식 4The compound of claim 2 having the formula (4): 화학식 4Formula 4 제1항에 있어서, 킬레이트제가 하기 화학식(5)의 HETA2인 공액 결합체:The conjugate of claim 1 wherein the chelating agent is HETA2 of formula (5): 화학식 5Formula 5 제2항에 있어서, 하기 화학식(5)를 갖는 화합물: 화학식 5A compound according to claim 2 having the formula (5): 화학식 5Formula 5 금속에 결합된 제2항의 화합물을 포함하는 공액 결합 착제.A conjugated conjugated complex comprising the compound of claim 2 bonded to a metal. 금속에 결합된 제5항의 화합물을 포함하는 공액 결합 착제.A conjugated conjugate complex comprising the compound of claim 5 bonded to a metal. 금속에 결합된 제7항의 화합물을 포함하는 공액 결합 착제.A conjugated conjugate complex comprising the compound of claim 7 bonded to a metal. 금속에 결합된 제1항의 착체를 포함하는 공액 결합 착제.A conjugated conjugate complex comprising the complex of claim 1 bonded to a metal. 금속에 결합된 제4항의 착체를 포함하는 공액 결합 착제.A conjugated conjugated complex comprising the complex of claim 4 bonded to a metal. 금속에 결합된 제6항의 착체를 포함하는 공액 결합 착제.A conjugated conjugated complex comprising the complex of claim 6 bonded to a metal. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019960703633A 1994-01-07 1995-01-05 NEW POLYAMINOCARBOXYLATE CHELATORS KR970700698A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17867594A 1994-01-07 1994-01-07
US08/178675 1994-01-07
PCT/US1995/000068 WO1995018832A1 (en) 1994-01-07 1995-01-05 New polyaminocarboxylate chelators

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KR970700698A true KR970700698A (en) 1997-02-12

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EP (1) EP0738283A4 (en)
JP (1) JPH09507488A (en)
KR (1) KR970700698A (en)
AU (1) AU692224B2 (en)
CA (1) CA2180662A1 (en)
FI (1) FI962772A (en)
WO (1) WO1995018832A1 (en)

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US6207858B1 (en) * 1999-03-03 2001-03-27 Idec Pharmaceuticals Corporation Regioselective synthesis of DTPA derivatives

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SE8301395L (en) * 1983-03-15 1984-09-16 Wallac Oy KELATIZING COMPOUNDS WITH FUNCTIONAL GROUPS WHICH ALLOW COVALENT COUPLING TO BIO-ORGANIC MOLECULES
DE353450T1 (en) * 1988-06-24 1990-09-06 The Dow Chemical Co., Midland, Mich. MACROCYCLIC BIFUNCTIONAL CHELATORS, COMPLEXES OF THEM AND THEIR CONJUGATED ANTIBODIES.
US5101041A (en) * 1989-04-26 1992-03-31 The Curators Of The University Of Missouri Triamines and their derivatives as bifunctional chelating agents
US5292868A (en) * 1989-05-26 1994-03-08 Akzo N.V. Chelating agents for attaching metal ions to proteins
EP0429644B1 (en) * 1989-05-26 1995-09-20 Akzo Nobel N.V. Chelating agents for attaching metal ions to proteins

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WO1995018832A1 (en) 1995-07-13
EP0738283A1 (en) 1996-10-23
AU1597595A (en) 1995-08-01
CA2180662A1 (en) 1995-07-13
JPH09507488A (en) 1997-07-29
FI962772A0 (en) 1996-07-05
FI962772A (en) 1996-07-05
AU692224B2 (en) 1998-06-04
EP0738283A4 (en) 1999-03-24

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