KR920002627A - α-케토 아미드 유도체 - Google Patents

α-케토 아미드 유도체 Download PDF

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KR920002627A
KR920002627A KR1019910012754A KR910012754A KR920002627A KR 920002627 A KR920002627 A KR 920002627A KR 1019910012754 A KR1019910012754 A KR 1019910012754A KR 910012754 A KR910012754 A KR 910012754A KR 920002627 A KR920002627 A KR 920002627A
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데쓰야 소메노
후미카 야마다
히데오 스기무라
야스히코 무라오카
마코토 쓰다
도미오 다케우치
다카아키 아오야기
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다케다 가주히코
닛뽄가야쿠 가부시키가이샤
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Abstract

내용 없음

Description

α-케토 아미드 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (26)

  1. 하기 일반식(1)의 신규한 α-케토 아미드 유도체 또는 이의 염:
  2. 상기식에서, X는 작용성 그룹이 보호될 수 있는 펩티드잔기 또는 아미노산 잔기이거나, 수소원자 또는 아미노-보호그룹이며; Y는 작용성 그룹이 보호될 수 있는 펩티드잔기 또는 아미노산 잔기이고; E는 알킬렌(CnH2n-1)상의 치환체를 나타내며, 할로겐, 저급알콕시 또는 수소이고; A는 카보닐그룹이거나, 일-또는 이-치환된 메틸렌이고, 이때 치환체 하이드록시, 저급알콕시, 페닐이미노 또는 벤질이미노이고; n은 2내지 6중의 한 정수이다.
  3. 제1항에 있어서, X가 저급알킬(C1-6)카보닐, 아미노그룹이 보호될 수 있는 α-아미노산 잔기, 또는 아미노 그룹이 보호될 수 있는 α-아미노산을 함유하는 디펩티드잔기이며; E는 수소이고, n은 3인 화합물.
  4. 제2항에 있어서, Y가 작용성 그룹이 보호될 수 있는 아미노산잔기 또는 작용성 그룹이 보호될 수 있는 디펩티드 잔기인 화합물.
  5. 제2항에 있어서, X가 측쇄 알킬(C3-6)카보닐, 아미노그룹이 보호되는 α-아미노알킬((C1-5)카보닐, N-보호된-2-피롤리디닐카보닐, 또는 아미노산그룹이 보호될 수 있는 α-아미노산(C2-10)을 함유하는 디펩티드잔기인 화합물.
  6. 제2항에 있어서, Y가 α-카복시그룹이 보호될 수 있는 α-카복시알킬(C1-6)아미노그룹인 화합물.
  7. 제4항에 있어서, X가 측쇄 알킬(C3-6)카보닐, Z-Phe-, Z-Pro-또는 Z-Val-Val이며; Y는 카복실그룹이 보호 또는 비보호될 수 있는 류신 또는 글리신잔기이거나, 카복실그룹이 보호되는 -Leu-Val인 화합물.
  8. 제4항에 있어서, A가 카보닐그룹인 화합물.
  9. 제5항에 있어서, Y가 카복실그룹이 비보되는 류신 또는 글리신잔기이거나, 카복실그룹이 보호되는 류신 또는 글리신 잔기이거나, 카복실그룹이 에스테르형 보호그룹 또는 아미드형 보호그룹에 의해 보호되는 -Leu-Val인 화합물.
  10. 제5항에 있어서, 카복실그룹이 알킬(C1-6)그룹 또는 알킬(C1-6)아미드그룹에 의해 보호되는 화합물.
  11. 제6항에 있어서, X가 (CH3)3CCH2CO- 또는 Z-Phe-인 화합물.
  12. 제10항에 있어서, Y가 -Leu-OH, -Leu-NH(t-Bu), -Leu-O(t-Bu), -Leu-OBzl, Gly-OH 또는 -Gly-O(t-Bu)인 화합물.
  13. 중에서 선택된 화합물 또는 이의 염.
  14. 내용없음
  15. 하기 일반식의 α-하이드록시아세트산 유도체:
  16. 상기식에서, X'는 작용성 그룹이 보호될 수 있는 펩티드잔기 또는 아미노산 잔기이거나, 아미노-보호그룹이며; Y'는 작용성 그룹이 보호되는 펩티드잔기 또는 아미노산 잔기이고; n은 2내지 6중의 한 정수이다.
  17. 하기 일반식(1")의 α-하이드록시아세트산 유도체를 산화시키고; 필요한 경우, 보호그룹을 제거함으로써 하기 일반식(1')의 신규한 α-케토 아미드유도체 또는 이의 염을 제조하는 방법;
  18. 상기식에서, X는 작용성 그룹이 보호될 수 있는 펩티드잔기 또느 아미노산 잔기이거나, 수소원자 또는 아미노-보호그룹이며; X'는 작용성 그룹이 보호되는 펩티드잔기 또는 아미노산 잔기이거나, 아미노-보호그룹이고; Y는 작용성 그룹이 보호될 수 있는 펩티드잔기 또는 아미노산 잔기이며; Y'는 작용성 그룹이 보호되는 펩티드잔기 또는 아미노산 잔기이고; E는 알킬렌(CnH2n-1)상의 치환체를 나타내며, 할로겐, 저급알콕시 또는 수소이며; A'는 카보닐그룹이거나, 일-또는 이-치환된 메틸렌이고, 이때 치환체는 저급알콕시, 페닐이미노 또는 벤질이미노이고; n은 2내지 6중의 한 정수이다.
  19. 제14항에 있어서, E가 수소이며, n은 정수 3인 신규한 α-케토 아미드유도체 또는 이의 염을 제조하는 방법.
  20. 제15항에 있어서, 하이드록실그룹을 산화제의 존재하에 산화시킴으로써 반응을 수행하여 신규한 α-케토아미드 유도체 또는 이의 염을 제조하는 방법.
  21. 제16항에 있어서, 불활성 유기 용매중에서 -10℃내지 용매의 비점에서 반응을 수행하여 신규한 α-케토아미드 유도체 또는 이의 염을 제조하는 방법.
  22. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910012754A 1990-03-01 1991-07-25 α-케토 아미드 유도체 KR920002627A (ko)

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JP91-57753 1990-03-01
JP90-197753 1990-07-27
JP19775390 1990-07-27
JP3057753A JPH04211648A (ja) 1990-07-27 1991-03-01 ケト酸アミド誘導体

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EP (1) EP0468339B1 (ko)
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KR (1) KR920002627A (ko)
DE (1) DE69125537T2 (ko)
ES (1) ES2102989T3 (ko)

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EP2545047B9 (en) 2010-03-10 2015-06-10 Probiodrug AG Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
JP6050264B2 (ja) 2011-03-16 2016-12-21 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej

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US4880827A (en) * 1986-03-18 1989-11-14 Sumitomo Pharmaceuticals Company, Ltd. Pyrrolidine derivatives having inhibitory action for proline specific endopepidase

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DE69125537T2 (de) 1997-07-17
DE69125537D1 (de) 1997-05-15
EP0468339A2 (en) 1992-01-29
JPH04211648A (ja) 1992-08-03
EP0468339B1 (en) 1997-04-09
ES2102989T3 (es) 1997-08-16
US5221752A (en) 1993-06-22

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