KR950701231A - 카복스아미드 변성된 폴리아민 킬레이트제 및 방사성 착화합물 및 결합체(carboxamide modified polyamine chelators and radioactive complexes and conjugates) - Google Patents

카복스아미드 변성된 폴리아민 킬레이트제 및 방사성 착화합물 및 결합체(carboxamide modified polyamine chelators and radioactive complexes and conjugates)

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KR950701231A
KR950701231A KR1019940703764A KR19940703764A KR950701231A KR 950701231 A KR950701231 A KR 950701231A KR 1019940703764 A KR1019940703764 A KR 1019940703764A KR 19940703764 A KR19940703764 A KR 19940703764A KR 950701231 A KR950701231 A KR 950701231A
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independently hydrogen
alkyl
hydrogen
chr
carboxamidomethyl
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윌리암 제이. 쥬니어 크루퍼
윌리암 에이. 포다이스
에이. 딘 쉐리.
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스티븐 에스.그레이스
더 다우 케미칼 캄파니
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
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    • 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
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    • 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
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    • A61K51/04—Organic compounds
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    • A61K51/0482—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 chelates from cyclic ligands, e.g. DOTA
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Abstract

희토류 금속 이온과 착화합물을 형성하는 작용화된 폴리아미노카복스아미드 변성된 킬레이트 그룹이 개시된다. 항체 또는 항체 단편에 공유 결합된 착화합물은 치료 및/또는 진단 목적으로 사용될 수 있다.

Description

카복스아미드 변성된 폴리아민 킬레이트제 및 방사성 착화합물 및 결합체(CARBOXAMIDE MODIFIED POLYAMINE CHELATORS AND RADIOACTIVE COMPLEXES AND CONJUGATES)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Y 또는 Sc 중에서 선택된 금속 이온과 착화된 하기 일반식(Ⅰ)의화합물 또는 그의 약학적으로 허용 가능한 염을 포함하는 착화합물;
    상기식에서, Q는 각각 독립적으로 수소, (CHR5)pCO2R, 또는(CHR5)pC(O)N(R6)2이고, 단 적어도 하나의 Q는(CHR5)pC(O)N(R6)2이고, R은 각각 독립적으로 수소, 벤질 또는 C1-C4알킬이고; R5는 각각 독립적으로 수소, C1-C4알킬 또는 -(C1-C2알킬)페닐이고; R6은 각각 독립적으로 수소, C1-C9알킬 또는 -(C1-C2알킬)페닐이고; X 및 Y는 각각 독립적으로 수소이거나 또는 인접 X 및 Y와 결합하여 부가적인 탄소-탄소 결합을 형성하여 알텐 또는 알킨을 생성하고; n은 0 또는 1이고; m은 0 내지 10의 정수이고; P는 1또는 2이고; r은 0 또는 1이고; w는 0 또는 1이고; 단, X 및/또는 Y가 부가적인 탄소-탄소 결합을 형성할 경우 n은 오직 1이고, r과 w의합은 0 또는 1이고; R2및 R4는 독립적으로 수소, 아미노, 이소티오시아네이토, 세미카브아지도, 티오세미타브아지도, 말레이미도, 브로모아세트아미도 또는 카복실이고; R3는 C1-C4알콕시, -OCH2CO2H, 하이드록시 또는 수소이고; 단, R2및 R4는 둘다 수소일 수 없으나 R2및 R4중의 하나는 수소이어야 한다.
  2. 제1항에 있어서, 금속이온이153Sm,166Ho,99Y,149Pm.159Gd,140La,177Lu,175Yb,47Sc 또는142Pr인 착화합물.
  3. 제1항에 있어서, 일반식(Ⅰ)의 X 및 Y 가 수소이고, r이 0이고, m이 5의정수인 착화합물.
  4. 제2항 또는 제3항에 있어서, 상기 화합물이 1, 4, 7, 10-테트라아자-1-N-(1-카복시-3-(4-니트로페닐)프로필)-비스-4,7-N,N-(카복시메틸)-10-N-(카복스아미도메틸)사이클로도데칸; 1, 4, 7, 10-테트라아자-1-N-(1-카복시-3-(4-아미노페닐)프로필)-비스-4,7-N,N-(카복시메틸)-10-N-(카복스아미도메틸)사이클로도데칸; 1, 4, 7, 10-테트라-1-N-(1-카복시-3-(4-아미노페닐)프로필)-7-N-(1-카복시메틸)-비스-4,10-N,N-(카복스아미도메틸)사이클로도데칸; 또는 1, 4, 7, 10-테트라아자-1-N-(1-카복시-3-(4-니트로페닐)프로필)-7--N-(1-카복시메틸)-비스-4,10-N,N-(카복스아미도메틸)사이클로도데칸인 착화합물.
  5. 제4항에 있어서, 금속이온이153Sm,166Ho,99Y, 또는177Lu,인 착화합물.
  6. 항체 또는 항체 단편에 공규 결합된 제1항 내지 제5항중의 어느 한 항의 착화합물을 포함하는 결합체.
  7. 제6항에 있어서, 항체 또는 항체 단편이 단일클론 항체 또는 그의 단편인 결합체.
  8. 제6항 또는 제7항의 결합체와 약학적으로 허용가능한 담체를 포함하는 약제.
  9. 효과량의 제8항의 약제를 포유동물에 투여함을 포함하는, 포유 동물의 질환을 진단하는 방법.
  10. 효과량의 제8항의 약제를 포유 동물에 투여함을 포함하는, 포유동물의 질환을 치료하는 방법.
  11. 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염;
    상기식에서, Q는 각각 독립적으로 수소, (CHR5)pCO2R, 또는(CHR5)pC(O)N(R6)2이고, 단 적어도 하나의 Q는(CHR5)pC(O)N(R6)2이고, R은 각각 독립적으로 수소, 벤질 또는 C1-C4알킬이고; R5는 각각 독립적으로 수소,C1-C4알킬 또는 -(C1-C2알킬)페닐이고; R6은 각각 독립적으로 수소, C1-C9알킬 또는 -(C1-C2알킬)페닐이고; X 및 Y는 각각 독립적으로 수소이거나 또는 인접 X 및 Y와 결합하여 부가적인 탄소-탄소 결합을 형성하여 알텐 또는 알킨을 생성하고; n은 0 또는 1이고; m은 0 내지 10의 정수이고; P는 1또는 2이고; r은 0 또는 1이고; w는 0 또는 1이고; 단, X 및/또는 Y가 부가적인 탄소-탄소 결합을 형성할 경우 n은 오직 1이고, r과 w의합은 0 또는 1이고; R2및 R4는 독립적으로 수소, 아미노, 이소티오시아네이토, 세미카브아지도, 티오세미카브아지도, 말레이미도, 브로모아세트아미도 또는 카복실이고; R3는 C1-C4알콕시, -OCH2CO2H, 하이드록시 또는 수소이고; 단, R2및 R4는 둘다 수소일 수 없으나 R2및 R4중의 하나는 수소이어야 한다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940703764A 1992-04-24 1993-04-23 카복스아미드 변성된 폴리아민 킬레이트제 및 방사성 착화합물 및 결합체 KR100245941B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US7/874,244 1992-04-24
US07/874,244 US5310535A (en) 1992-04-24 1992-04-24 Carboxamide modified polyamine chelators and radioactive complexes thereof for conjugation to antibodies
US7/874244 1992-04-24
PCT/US1993/003844 WO1993021963A2 (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes and conjugation

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KR100245941B1 KR100245941B1 (ko) 2000-04-01

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DE69317771D1 (de) 1998-05-07
WO1993021963A2 (en) 1993-11-11
DK0637253T3 (da) 1999-02-01
EP0637253A1 (en) 1995-02-08
NO304552B1 (no) 1999-01-11
FI944973A0 (fi) 1994-10-21
CA2134092A1 (en) 1993-11-11
NO944019L (no) 1994-12-12
US5310535A (en) 1994-05-10
DE69317771T2 (de) 1998-07-30
JP3850870B2 (ja) 2006-11-29
CA2134092C (en) 2003-07-29
EP0637253B1 (en) 1998-04-01
NO944019D0 (no) 1994-10-21
WO1993021963A3 (en) 1993-12-09
ES2114051T3 (es) 1998-05-16
AU674853B2 (en) 1997-01-16
HUT70429A (en) 1995-10-30
HK1006632A1 (en) 1999-03-05
HU222761B1 (hu) 2003-10-28
US5739323A (en) 1998-04-14
JPH07506365A (ja) 1995-07-13
ATE164522T1 (de) 1998-04-15
SG49756A1 (en) 1998-06-15
FI944973A (fi) 1994-12-02
AU4292693A (en) 1993-11-29
GR3026533T3 (en) 1998-07-31
NZ252867A (en) 1997-03-24

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