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KR920700206A - 테트라-아자 마크로싸이클 화합물과 이들의 금속착화합물 - Google Patents

테트라-아자 마크로싸이클 화합물과 이들의 금속착화합물

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Publication number
KR920700206A
KR920700206A KR1019890700624A KR890700624A KR920700206A KR 920700206 A KR920700206 A KR 920700206A KR 1019890700624 A KR1019890700624 A KR 1019890700624A KR 890700624 A KR890700624 A KR 890700624A KR 920700206 A KR920700206 A KR 920700206A
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compound
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formula
integer
compounds
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KR1019890700624A
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데이비드 파커
토마스 앤드류 밀리칸
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셀텍크 리미티드
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Publication of KR920700206A publication Critical patent/KR920700206A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6887—Antibody-chelate conjugates using chelates for therapeutic purposes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/0002—General or multifunctional contrast agents, e.g. chelated agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
    • B65G—TRANSPORT OR STORAGE DEVICES, e.g. CONVEYORS FOR LOADING OR TIPPING, SHOP CONVEYOR SYSTEMS OR PNEUMATIC TUBE CONVEYORS
    • B65G49/00—Conveying systems characterised by their application for specified purposes not otherwise provided for
    • B65G49/05—Conveying systems characterised by their application for specified purposes not otherwise provided for for fragile or damageable materials or articles
    • B65G49/06—Conveying systems characterised by their application for specified purposes not otherwise provided for for fragile or damageable materials or articles for fragile sheets, e.g. glass
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Cephalosporin Compounds (AREA)
  • External Artificial Organs (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
  • Saccharide Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

내용 없음

Description

테트라－아자 마크로싸이클 화합물과 이들의 금속착화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. 구조식(1)의 화합물과 이의 금속착화합물 및 염.
    여기에서, m과 n은 0이거나 1, 2또는 3인 정수로 각각은 서로 같거나 상이할 수 있으며; b는 0 또는 1, 2또는 3인 정수;R, R1, R2와 R3는 수소원자 또는 알킬, 알콕시알킬, －CO2H, －SO3H, －PO2H2나 아릴기로 각각은 서로 같거나 상이할수 있으며; L은 공유결합 또는 연결기이고, Z는 수소원자 또는 반응성 관능기로, L이 공유결합이면 Z는 반응성 관능기이다.
  2. 제1항에 있어서, q는 1 내지 6인 정수이고,R, R1, R2와 R3가 －CO2H기인 화합물.
  3. 제2항에 있어서, q는 1인 화합물.
  4. 전술한 어느 한 항에 있어서, L은 임의로 치환된 지방족 하이드로카르빌 사슬과, －O－또는 －S－로부터 선택된 하나 또는 그 이상의 이종 원자에 의하여 임의로 차단되거나 또는 하나 또는 그 이상의 －N(R5)－(여기에서 R5는 수소원자나 C1-6알킬기), －CON(R5)－, N(R5)CO－, 시클로지방족, 방향족 혹은 헤테로 방향족기들에 의하여 임의로 차단된 것인 화합물.
  5. 전술한 어느 한 항에 있어서, Z가 티올, 아미노, 카르복실, 하이드록실, 알데히드, 방향족 또는 헤테로방향족기와 반응할 수 있는 것인 화합물.
  6. 제5항에 있어서, Z는 할로겐 원자 또는 －SH, －NH2, 하이드라진 또는 그 유도체, －NCO, －NCS, －COR10(여기에서 R10은 할로겐원자 또는 N3, C1-6알콕시, C6-12아릴옥시, 이미딜옥시 혹은 이미다 조일옥시기이다.), 이미드, －Het1－C(Het2)=CH2(여기에서 Het1과 Het2는 같거나 상이할 수도 있는 질소함유 헤테로시클릭기 이거나, Het1은 질소 함유 헤테로시클릭기이고 Het2는 수소원자 이다.) 또는 구조식(여기에서 R11은 C1-4알킬기이다)으로 구성된 군으로부터 선택된 것인 화합물.
  7. 금속의 이온가가 +2가 또는 +3가이고 배위수가 6 또는 그 이상의 금속이 착화된 전술한 항에서 언급한 구조식(1)화합물의 금속착화합물.
  8. 제7항에 있어서, 금속이 구리, 납, 비스무스, 이트륨, 테르븀, 가돌리늄 또는 스탄듐인 화합물.
  9. 특허청구의 범위 제1항 내지 제7항에서 언급한 구조식(1)화합물의 이트륨착화합물.
  10. 전술한 어느 한항에 있어서, d가 1인 화합물.
  11. 구조식 (1a)화합물과 이의 금속착화합물 및 염.
    여기에서 R1, R2와 R3는 수소원자 또는 알킬, 알콕시알킬, －CO2H, －SO3H, －PO2H2혹은 아릴기로 서로 같거나 다를수 있으며; L은 공유결합 또는 연결기; Z는 수소원자 또는 반응성관능기로서 L이 공유결합이면 Z는 반응성 관능기이다.
  12. 제11항에 있어서, R1, R2와 R3는 각각이 －CO2H기인 화합물.
  13. 구조식(1)화합물이나 금속착화합물 및 이들의 염이 단백질, 펩타이드 혹은 탄수화물과 결합된 공액화합물(conjugated compound).
    여기에서, m과 n은 0 또는 1, 2 또는 3인 정수로 서로 같거나 다를수 있으며; d는 0 또는 1, 2 또는 3인 정수; q는 0 또는 1 내지 6인 정수; R, R1, R2와 R3는 수소원자 또는 알킬, 알콕시알킬, －CO2H, －SO3H, －PO2H2또는 아릴기로 서로 같거나 다를수 있으며; L은 공유결합 또는 연결기; Z는 수소원자 또는 반응성 관능기로, L이 공유결합이면 Z는 반응성 관능기이다.
  14. 구조식(2)의 공액화합물(conjugated compound)과 이의 금속착화합물 및 이들의 염.
    여기에서, m과 n은 0 또는 1, 2 또는 3인 정수로 서로 같거나 다를수 있으며, d는 0 또는 1, 2 또는 3인 정수; q는 0 또는 1내지 6인 정수이며, R, R1, R2와 R3는 수소원자 또는 알킬, 알콕시 알킬, －CO3H, －SO3H, －PO2H2또는 아릴기로 서로 같거나 다를수 있으며; L은 공유결합 또는 연결기; Z1는 반응성관능기의 잔기; W는 0또는 1인 정수; z는 그이상의 정수; Ab는 항체이다.
  15. 특허청구의 범위 1항기재의 구조식(1)화합물이나 이들의 금속착화합물 또는 이들의 염과 하나또는 그 이상의 약학적으로 유용한 담체들로 구성된 조성물.
  16. 특허청구의 범위 제14항 기재의 구조식(2)화합물이나 이들의 금속착화합물 또는 이들의 염과 하나 이상의 약학적으로 유용한 담체들로 구성된 조성물.
  17. 구조식(3)화합물(여기에서 m, n, d, L과 Z는 구조식(1)의 화합물의 기재와 같다)이나 이들의 금속 착화합물을 R1(CH2)qD(여기에서 D는 치환기이고 R1과 q는 구조식(1)화합물의 기재와 같다.)인 시약과 반응시킴을 특징으로 하는 특허청구의 번위 제1항기재의 구조식(1)화합물 이들의 금속착화합물의 제조방법.
  18. 특허청구의 범위 제1항기재의 구조식(1)의 화합물을 항체 Ab와 반응시킴을 특징으로 하는 특허청구의 범위 제14항 기재의 구조식(2)의 공액화합물(conjugated compound)의 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890700624A 1987-08-12 1988-08-12 테트라-아자 마크로싸이클 화합물과 이들의 금속착화합물 KR920700206A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB8719042 1987-08-12
GB878719042A GB8719042D0 (en) 1987-08-12 1987-08-12 Conjugate compounds
PCT/GB1988/000671 WO1989001476A1 (en) 1987-08-12 1988-08-12 Tetra-aza macrocycles and metal complexes thereof

Publications (1)

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KR920700206A true KR920700206A (ko) 1992-02-19

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Country Status (11)

Country Link
US (1) US6774228B1 (ko)
EP (1) EP0328589B1 (ko)
JP (1) JPH02501141A (ko)
KR (1) KR920700206A (ko)
AT (1) ATE136302T1 (ko)
AU (1) AU629515B2 (ko)
CA (1) CA1341102C (ko)
DE (1) DE3855177T2 (ko)
DK (1) DK172789A (ko)
GB (1) GB8719042D0 (ko)
WO (1) WO1989001476A1 (ko)

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