KR880000470A - 펩티드 및 이의 제조방법 - Google Patents

펩티드 및 이의 제조방법 Download PDF

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KR880000470A
KR880000470A KR870005810A KR870005810A KR880000470A KR 880000470 A KR880000470 A KR 880000470A KR 870005810 A KR870005810 A KR 870005810A KR 870005810 A KR870005810 A KR 870005810A KR 880000470 A KR880000470 A KR 880000470A
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radical
formula
hydrogen
optionally
compound
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쾨니히 볼프강
브라이폴 게르하르트
가이거 롤프
크놀레 요헨
흐로포트 막스
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하인리히 벡커, 베른하르트 벡크
훽스트 아크티엔게젤샤프트
베른하르트 벡크
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Abstract

내용 없음

Description

펩티드 및 이의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 일반식(Ⅰ)의 화합물 및 이의 생리학적으로 허용되는 염.
    R4-L-N-B2-RC(Ⅰ)
    상기식에서 RN은 일반식(Ⅱ)의 라디칼이고;
    R2는 수소 또는 일반식 R-〔A〕-NH-의 라디칼이고 ; R3은 아미노, 구아니디노, -(R1-C3)-알킬아미노 또는 디(C1-C3)-알킬아미노이고 ; m은 1내지 6의 정수이고 : A는 일반식 -NH-CR4R5-CO-의 라디칼이고 : R은 수소, (C1-C6)-알카노일, (C7-C11)-아로일〔여기서, 방향족의 잔기는(C1-C4)-알킬, (C1-C4)-알콕시, (C1-C4)-알킬티오, 할로겐, 카바모일, (C1-C4)-알콕시카보닐 및 /또는 설파모일에 의해 임의로 일-또는 이-치환되거나, 메틸렌디옥시에 의해 일치환된다〕. (C5-C7)-시클로알킬-(C1-C|3)-알카노일 또는 (C6-C14)-아릴-(C1-C3)-알카노일이며, 여기에서 수소가 아닌 라디칼 R에서 -CH2-그룹은 -O- 또는 -S-에 의해 임의로 치환되고:
    n은 0 또는 1이고:
    R4및 R5는 동일하거나 상이하며 수소(C1-C6)-알킬 또는 (C7-C11)-아르알카노일이고:
    L은 ProㆍD-Pro 또는 일반식 -NH-CH(R6)-CO-라디칼이고:
    R6은 임의로 하이드록실, (C1-C6)-알콕시, (C1-C6)-알콕시카보닐, 카바모일 또는 R-NH(..., R은 상기 정의한 바와같으나 수소일수는 없다.)에 의해 일치환되는 (C1-C6)-알킬이거나, 방향족 환상에서 (C1-C6)-알콕시에 의해 임의로 일치환되는 (C7-C11)-아르알킬이거나, 3-인돌일메틸이고:
    N은 Pro D-Rro또는 일반식-NH-CH(R〃)-CO-의 라디칼이고:
    R7은 임의로 하이드록실, (C1-C6)-알콕시, (C1-C6)-알콕시카보닐, 카바모일 또는 R-NH(여기서, R은 상기 정의한 바와같으나 수소일수는 없다)에 의해 일치환되는 (C1-C6)-알킬이거나, 방향족 환상에서 (C1-C6)-알콕시에 의해 임의로 일치환되는 (C6-C11)-아르알킬이거나, 3-인돌일메틸이고:
    B2는 일반식(Ⅲ)의 라디칼이고
    (여기에서 R3및 m은 상기 정의한 바와 같다):
    Rc은 일반식-NR9-CH(R8)-(CO)p-R′의 라디칼이고:
    R8은 R7으로 정의된 바와 같으나, 단 -NH-에 대하여 β-위치에 존재하는 CH, CH2또는 CH3라디칼은 임의로 모노하이드록 실화되며,
    R9은 수소이거나:
    R8과 R9가 함께는 -〔CH2〕3-또는 -〔CH2〕4를 나타내고:
    p는 0 또는 1이고, R1은 p가 0인 경우에는 수소, 하이드록실 또는 (C1-C6)-알콕시이고,
    R1은 p가 1인 경우에는 OR10또는 NR10R11이며, R10및 R11은 동일하거나 상이하며 수소, (C1-C6)-알킬 또는 (C7-C11)-아르알킬이거나 NR10R11은 피롤리디노, 피페리디노 또는 모르폴리노이거나:
    p는 1이고, R 및 R1은 함께 결함을 나타내며, 나머지 라디칼은 상기 정의한 바와 같다.
  2. 제1항에 있어서, L이 이솔루신, 발린, 트레오닌, 세린, O-(C1-C9)-알킬트레오닌, O-(C1-C9)-알킬세린, 루신 또는 프롤린의 라디칼 또는 글루탐산 또는 아스파트산의 w-(C1-C6)-알킬에스테르, 바람직하게는 3급 부틸 에스테르의 라디칼이고:
    N은 발린, 이솔루신, 루신, 페닐알라닌, 트립토판, 임의로 O-(C1-C6)-알킬화된 티로신, 글루타민, 아스파라긴, γ-(C1-C6)-알킬글루타메이트 또는 β-(C1-C|6)-알킬 아스파테이트 또는 ε-아실-리신의 라디칼이며, B2는 Arg,D-Arg, Lys 또는 D-Lys인 일반식(Ⅰ)의 화합물 및 이의 생리학적으로 허용되는 염.
  3. 제1항 또는 2항에 있어서, p가 1이고, R 및 R1은 함께 결합을 나타내는 일반식(Ⅰ)의 화합물 및 이의 생리학적으로 허용되는 염.
  4. 제1항 또는 2항에 있어서, R 및 R1이 함께 결합을 나타내지 않는 일반식(Ⅰ)의 화합물 및 이의 생리학적으로 허용되는 염.
  5. 말단 카복실 그룹을 갖는 단편 또는 이의 반응성 유도체를 유리아미노 그룹을 갖는 적합한 단편과 커플링시키고, 경우에 따라 다른 작용성 그룹을 보호하기 위해 일시적으로 도입된 보호 그룹(들)을 제거하고, 경우에 따라 이렇게 수득된 화합물을 이의 생리학적으로 허용되는 염으로 전화시킴을 특징으로 하여 제1항 내지 4항중 어느하나에 청구된 일반식(Ⅰ)의 화합물을 제조하는 방법.
  6. 제1항 내지 4항중 어느 하나에 청구된 일반식(Ⅰ)화합물의 약제로서의 용도.
  7. 제1항 내지 4항중 어느하나에 청구된 일반식(Ⅰ)화합물의 이뇨 작용 및 나트륨뇨 배설 작용을 갖는 약제로서의 용도.
  8. 제1항 내지 4항중 어느 하나에 청구된 일반식(Ⅰ)의 화합물을 함유하는 약학적 제제.
  9. 제1항 내지 4하중 어느 하나에 청구된 일반식(Ⅰ)의 화합물을 부형제 및 경우에 따라 기타 첨가제 및 보조제와 함께 적합한 투여형태로 전환시킴을 특징으로 하여 제8항에 청구된 약학적 제제를 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870005810A 1986-06-11 1987-06-09 펩티드 및 이의 제조방법 KR880000470A (ko)

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DE19863619633 DE3619633A1 (de) 1986-06-11 1986-06-11 Peptide mit einfluss auf die diurese und natriurese, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung
DEP3619633.9 1986-06-11

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US4935492A (en) * 1987-12-24 1990-06-19 California Biotechnology Inc. Cyclic analogs of atrial natriuretic peptides
WO1989005654A1 (en) * 1987-12-24 1989-06-29 California Biotechnology Inc. Linear analogs of atrial natriuretic peptides
US5047397A (en) * 1988-08-26 1991-09-10 California Biotechnology Inc. Linear analogs of atrial natriuretic peptides
DK15888D0 (da) * 1988-01-14 1988-01-14 Carlsberg Biotechnology Ltd Enzymatisk fremgangsmaade til fremstilling af immunmodulerende pentapeptider samt mellemprodukter til brug ved fremgangsmaaden
US6602856B1 (en) * 1995-01-17 2003-08-05 J. Mark Quillan Antagonists of alpha-melanocyte stimulating hormone and methods based thereon
MY148144A (en) 2006-11-10 2013-03-15 Cara Therapeutics Inc Synthetic peptide amides
US8236766B2 (en) 2006-11-10 2012-08-07 Cara Therapeutics, Inc. Uses of synthetic peptide amides
US7713937B2 (en) 2006-11-10 2010-05-11 Cara Therapeutics, Inc. Synthetic peptide amides and dimeric forms thereof
US7842662B2 (en) 2006-11-10 2010-11-30 Cara Therapeutics, Inc. Synthetic peptide amide dimers
US8906859B2 (en) 2006-11-10 2014-12-09 Cera Therapeutics, Inc. Uses of kappa opioid synthetic peptide amides
WO2010122423A2 (en) * 2009-04-22 2010-10-28 Dsm Ip Assets B.V. Novel composition
CN105693817B (zh) 2014-11-27 2020-06-05 西北大学 一类三肽化合物及其制备方法与应用
US11918624B2 (en) 2020-06-10 2024-03-05 Kelsius Laboratories LLC Therapeutic composition for use in the treatment of COVID-19 and other cytokine storm associated disorders

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US4389342A (en) * 1980-04-02 1983-06-21 Perignon Investments, Ltd. Synthetic hormone-like peptides and method for their synthesis
JPS59130254A (ja) * 1982-10-18 1984-07-26 Mitsubishi Chem Ind Ltd ポリペプチド
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US4692511A (en) * 1984-07-03 1987-09-08 Immunetech Pharmaceuticals Peptide antagonists for the C5a anaphylatoxin

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FI88401C (fi) 1993-05-10
AU7408887A (en) 1987-12-17
DE3619633A1 (de) 1987-12-17
DE3783657D1 (de) 1993-03-04
EP0249169B1 (de) 1993-01-20
GR3007609T3 (ko) 1993-08-31
FI872576A0 (fi) 1987-06-09
DK296487D0 (da) 1987-06-10
AU601436B2 (en) 1990-09-13
FI88401B (fi) 1993-01-29
DK296487A (da) 1987-12-12
ATE84795T1 (de) 1993-02-15
ZA874163B (en) 1987-12-14
US5011825A (en) 1991-04-30
PT85053B (pt) 1990-03-08
IL82813A0 (en) 1987-12-20
CA1317068C (en) 1993-04-27
IL82813A (en) 1991-01-31
JPS62292798A (ja) 1987-12-19
EP0249169A2 (de) 1987-12-16
PT85053A (de) 1987-07-01
EP0249169A3 (en) 1990-01-31
FI872576A (fi) 1987-12-12

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