KR950704256A - 2―히드라지노피리딘 유도체를 사용하는 분자표시방법(molecule labelling using 2―hydrazinopyridine derivatives) - Google Patents

2―히드라지노피리딘 유도체를 사용하는 분자표시방법(molecule labelling using 2―hydrazinopyridine derivatives) Download PDF

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KR950704256A
KR950704256A KR1019950701810A KR19950701810A KR950704256A KR 950704256 A KR950704256 A KR 950704256A KR 1019950701810 A KR1019950701810 A KR 1019950701810A KR 19950701810 A KR19950701810 A KR 19950701810A KR 950704256 A KR950704256 A KR 950704256A
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acid addition
addition salts
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제프리 아브람스 마이클
제임스 브리저 가리
아론 슈바르츠 데이비드
파드마나반 스리니바산
에버트 율테 마이클
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아이엔 카미첼 위샤르트
존슨 맛쎄이 퍼블릭 리미티드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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Abstract

일반식(I)
(상기식에서 E는 알케닐 또는 H2이며, J는 ―CONH―, ―COO―COS― 또는 ―NHCO―이고, T는 알킬렌이거나 또는 만일 J가―CONH―이면 T는 아미노산 부분의 잔기이고, Q는 친수성 또는 절단가능부분이며, Z는 아민― 및/또는 티올―반응성 부분이다)의 신규한 2관능성 히드라진 유도체는 MAB´ 또는 MAB의 단편들과 같은 고분자에99mTc같은 금속이온을 부착하기 위한 유용한 링커분자이다.

Description

2―히드라지노피리딘 유도체를 사용하는 분자표시방법(MOECULE LABELLING USING 2―HYDRAZINOPYRIDINE DERIVATIVES)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도 내지 제3도는 본 발명 화합물의 합성에 사용될 수 있는 반응 개요도들을 나타낸다.

Claims (26)

  1. 일반식 I의 화합물
    상기식에서 E는 알케닐이거나 또는 H2를 나타내는데 이경우에는 화합물이 산부가염의 형태이며, J가 ―CO―NH―, ―CP―O―, ―CO―S―및 ―NH―CO―로부터 선택되며, T는 알킬렌 사슬이거나, 또는 만일 J가 ―CO―NH―이면, T는 아미노산부분의 잔기이며, Q는 친수성 또는 절단가능부분이며, Z는 아민― 및/또는 티올―반응성 부분이다.
  2. 제1항에 있어서, E가 알케닐기일 때, 그것은 직쇄 또는 분지쇄저급 알케닐인 것을 특징으로 하는 일반식 I의 화합물.
  3. 제1항 또는 제2항에 있어서, ―Y―Z가 활성에스테르, α―브로모아세틸, α―브로모아세타미딜 또는 혼합된 치환 또는 비치환 피리딜 이황화인 것을 특징으로 하는 일반식 I의 화합물.
  4. 일반식 Ia의 화합물
    상기식에서 E는 제1항에 정의된 것과 같으며, R은 H 또는 CH3이고 R´는 H 또는 NO2이다.
  5. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  6. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  7. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  8. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  9. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  10. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  11. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  12. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  13. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  14. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  15. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  16. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  17. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  18. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  19. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  20. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  21. 제1항에 있어서,
    및 그것의 산부가염인 것을 특징으로 하는 화합물.
  22. 전술한 어느 한 항에 따르는 화합물과 고분자의 반응에 의해 형성된 콘주게이트.
  23. 제20항에 있어서, 고분자는 면역글로불린 또는 그것의 단편인 것을 특징으로 하는 콘주게이트.
  24. 제20항 또는 제21항에 따르는 콘주게이트에 결합된 금속원자로 이루어지는 표지된 고분자.
  25. 제22항에 있어서, 금속은 Tc 및 Re의 방사성 동위원소로 부터 선택되는 것을 특징으로 하는 표지된 고분자.
  26. 일반식 II의 화합물.
    상기식에서 E는 제1항에 정의된 것과 같다.
    ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
KR1019950701810A 1992-11-05 1993-11-03 2-히드라지노피리딘유도체를사용하는분자표지방법 KR100295545B1 (ko)

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GB9223168.7 1992-11-05
GB929223168A GB9223168D0 (en) 1992-11-05 1992-11-05 Improvements in molecule labelling
PCT/GB1993/002259 WO1994010149A1 (en) 1992-11-05 1993-11-03 Molecule labelling using 2-hydraninopyridine derivatives

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JP2004529922A (ja) 2001-04-03 2004-09-30 ザ ボード オブ トラスティーズ オブ ザ リーランド スタンフォード ジュニア ユニバーシティ 生体内における細胞死の画像化の方法
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EP1807092B1 (en) 2004-11-05 2016-09-07 The Children's Hospital of Philadelphia Biodegradable linkers for molecular therapies
EP2942351B1 (en) * 2011-01-31 2016-10-12 ETH Zurich Trifunctional crosslinking reagents
CA2838158C (en) 2011-06-03 2019-07-16 3M Innovative Properties Company Heterobifunctional linkers with polyethylene glycol segments and immune response modifier conjugates made therefrom
EP3153180A1 (en) 2011-06-03 2017-04-12 3M Innovative Properties Company Heterobifunctional linkers with polyethylene glycol segments and immune response modifier conjugates made therefrom

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US4861869A (en) * 1986-05-29 1989-08-29 Mallinckrodt, Inc. Coupling agents for joining radionuclide metal ions with biologically useful proteins
IL93432A (en) * 1989-02-24 1994-02-27 Johnson Mathey Inc Hydrazines and hydrazides, their conjugates with macromolecules, and such conjugates labeled with metallic ions
US5112953A (en) * 1989-12-29 1992-05-12 Neorx Corporation Radiolabeled proteins for diagnostic or therapeutic use

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FI952141A0 (fi) 1995-05-04
HU226459B1 (en) 2008-12-29
WO1994010149A1 (en) 1994-05-11
DE69329293T2 (de) 2000-12-28
HUT72332A (en) 1996-04-29
AU676863B2 (en) 1997-03-27
CA2148595C (en) 2002-05-21
NO951751L (no) 1995-06-12
EP0667859B1 (en) 2000-08-23
JP3542597B2 (ja) 2004-07-14
EP0667859A1 (en) 1995-08-23
JPH08502744A (ja) 1996-03-26
ATE195730T1 (de) 2000-09-15
NO305364B1 (no) 1999-05-18
HK1013420A1 (en) 1999-08-27
AU5375594A (en) 1994-05-24
PT667859E (pt) 2001-02-28
KR100295545B1 (ko) 2001-09-17
DE69329293D1 (de) 2000-09-28
DK0667859T3 (da) 2000-10-16
CA2148595A1 (en) 1994-05-11
US5679778A (en) 1997-10-21
FI952141A (fi) 1995-05-04
GR3034883T3 (en) 2001-02-28
NO951751D0 (no) 1995-05-04
FI113044B (fi) 2004-02-27
GB9223168D0 (en) 1992-12-16
NZ257376A (en) 1996-02-27
ES2150950T3 (es) 2000-12-16

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