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KR960705843A - 펩티딜 화합물과 메탈로프로테인아제의 억제제로서 그들의 치료학적 용도(peptidyl compounds and their therapeutic use as inhibitors of metalloproteinases) - Google Patents

펩티딜 화합물과 메탈로프로테인아제의 억제제로서 그들의 치료학적 용도(peptidyl compounds and their therapeutic use as inhibitors of metalloproteinases)

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KR960705843A
KR960705843A KR1019960702437A KR19960702437A KR960705843A KR 960705843 A KR960705843 A KR 960705843A KR 1019960702437 A KR1019960702437 A KR 1019960702437A KR 19960702437 A KR19960702437 A KR 19960702437A KR 960705843 A KR960705843 A KR 960705843A
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alkyl
methylamide
phenylalanine
leusil
aryl
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존 몬타나
존나단 디킨즈
데이비드 알렌 오웬
앤드류 더글러스 박스터
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앤드류 리차드
키로사이언스 리미티드
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Publication of KR960705843A publication Critical patent/KR960705843A/ko

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Abstract

본 발명은 하기의 식(Ⅰ)의 화합물로서,
여기서 R1은 C1-6알킬, C2-6알케닐, 아릴, (C1-6알킬)아릴 또는 C1-6알킬-AR9이고, A는 O, NR9이고, 또는 S(O)m이고, m은 0 내지 2이고, R9은 H, C1-4알킬, 아릴 또는 (C1-4알킬)아릴; R2는 H 또는 C1-6알킬; R4는 H 또는 아미노(NH2), 아릴 아미노, 보호된 아미노, 아릴, 디(C1-6알킬)아미노, 모노(C1-6알킬)아미노, CO2H, 보호된 카르복실, 카르바모일, 모노(C1-6알킬)카르바모일 또는 디(C1-6알킬)카르바모일에 의해 선택적으로 치환된 C1-6알킬, 및 R5는 H 또는 C1-6알킬, 또는 NR4R5은 피롤리디노, 피페리디도 또는 모르포리노; R6는 선택적으로 치환된 C3-6시클로알킬, C3-6시클로알케닐, C1-6알킬, 벤질, (C1-6알콕시)벤질, 벤질옥시벤질 또는 3-인돌리메틸; Alk는 C1-6알킬 또는 C2-6알케닐 및 n=0 또는 1; R7은 H 또는 R10CO, 여기서 R10은 C1-4알킬, (C1-4알킬)아릴, C3-6시클로알킬, (C3-6시클로알킬) C1-4알킬, C2-6알케닐 또는 (C2-6알케닐)아릴; 및 R8은 H, C1-4알킬, (C1-4알킬)아릴 또는 아릴; 또는 그들의 염, 솔베이트 또는 수화물이다.
이런 화합물들은 메타로프로테인아제, TNF 및/또는 다른 활성도와 관련된 상태를 처리하는데 사용될 수 있다.

Description

펩티딜 화합물과 메탈로프로테인아제의 억제제로서 그들의 치료학적 용도(PEPTIDYL COMPOUNDS AND THEIR THERAPEUTIC USE AS INHIBITORS OF METALLOPROTEINASES)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 하기 일반식(Ⅰ)의 화합물, 또는 그들의 염, 솔베이트 또는 수화물.
    여기서 R1은 C1-6알킬, C2-6알케닐, 아릴, (C1-6알킬)아릴 또는 C1-6알킬-AR9이고, A는 O, NR9이고, 또는 S(O)m이고, m은 0 내지 2이고, R9은 H, C1-4알킬, 아릴 또는 (C1-4알킬)아릴; R2는 H 또는 C1-6알킬; R4는 H 또는 아미노(NH2), 아릴 아미노, 보호된 아미노, 아릴, 디(C1-6알킬)아미노, 모노(C1-6알킬)아미노, CO2H, 보호된 카르복실, 카르바모일, 모노(C1-6알킬)카르바모일 또는 디(C1-6알킬)카르바모일에 의해 선택적으로 치환된 C1-6알킬, 및 R5는 H 또는 C1-6알킬, 또는 NR4R5은 피롤리디노, 피페리디노 또는 모르포리노; R6는 선택적으로 치환된 C3-6시클로알킬, C3-6시클로알케닐, C1-6알킬, 벤질, (C1-6알콕시)벤질, 벤질옥시벤질 또는 3-인돌리메틸, Alk는 C1-6알킬 또는 C2-6알케닐 및 n=0 또는 1; R7은 H 또는 R10CO, 여기서 R10은 C1-4알킬, (C1-4알킬)아릴, C3-6시클로알킬, (C3-6시클로알킬)C1-4알킬, C2-6알케닐 또는 (C2-6알케닐)아릴; 및 R8은 H, C1-4알킬, (C1-4알킬)아릴 또는 아릴이다; 또는 그들의 염, 솔베이트 또는 수화물.
  2. 제1항에 있어서, R1은 알킬, 알케닐, 아릴, 알킬아릴이고, R7및 R8은 각각 H인 화합물.
  3. 제1항에 있어서, 화합물은 N-〔N-(메르캅토아세틸)-L-레우실〕-L-페닐알라닌 메틸아미드, N-〔(아세토메르캅토아실)-L-레우실〕-L-페닐알라닌 메틸아미드, (RS)
    -2-(아세틸티오)펜타노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-(아세틸티오)프로파노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-(아세틸티오)-3-메틸부타노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-(아세틸티오)-2-페닐아세틸
    -L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-(아세틸티오)-3-페닐프로파노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-(아세틸티오)-4-페닐부타노일-L-레우실
    -L-페닐알라닌 N-메틸아미드, N-(아세틸메르캅토아실)-L-트레오닐-L-페닐알라닌 메틸아미드, N-(아세틸메르캅토아실)-L-트레오닐-L-레우실-L-트립토판 메틸아미드, (RS)-2-메르캅토펜타노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-메르캅토프로파노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-메르캅토-3-메틸부타노일-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-메르캅토-2-페닐아세틸-L-레우실-L-페닐알라닌 N-메틸아미드, (RS)-2-메르캅토-3-페닐프로파노일-L-레우실-L-페닐알라닌 N-메틸아미드, N-〔N-(메르캅토아세틸)-L-트레오닐〕-L-페닐알라닌 메틸아미드 및 N-〔N-(메르캅토아세틸)-L-레우실〕-L-트립토판 메틸아미드로부터 선택된 화합물.
  4. 제1항 내지 제3항 중 어느 하나의 항의 화합물과 생리학적으로 허용가능한 희석액 또는 담체로 이루어지는 치료에 사용하기 위한 제약학적 조성물.
  5. 매트릭스 메탈로프로테인아제 또는 TNF 활성과 관련된 상태의 억제 또는 치료를 위한 약제의 제조를 위한 제1항 내지 제3항 중 어느 하나의 항의 화합물의 용도.
  6. 제5항에 있어서, 상기 상태는 염증, 발열, 심장맥관의 효과, 출혈, 응고 및 급성상태 반응, 악태증 및 식욕결핍, 급성 간염, 쇼크 상태, 조직이식 대 숙주 반응, 자가면역 질병, 말라리아, 리퍼퓨션(reperfusion)질병, 수막염, 건선, 류마토이드 관절염, 다중 경화증 및 종양들로부터 선택되는 화합물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960702437A 1993-11-10 1994-11-10 펩티딜 화합물과 메탈로프로테인아제의 억제제로서 그들의 치료학적 용도(peptidyl compounds and their therapeutic use as inhibitors of metalloproteinases) KR960705843A (ko)

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GB939323165A GB9323165D0 (en) 1993-11-10 1993-11-10 Compounds
GB9323165.2 1993-11-10
PCT/GB1994/002471 WO1995013289A1 (en) 1993-11-10 1994-11-10 Peptidyl compounds and their therapeutic use as inhibitors of metalloproteinases

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Publication number Publication date
CN1134705A (zh) 1996-10-30
HK1015139A1 (en) 1999-10-08
CZ134996A3 (en) 1996-10-16
BR9408025A (pt) 1996-12-17
DE69422726T2 (de) 2000-06-08
GB9323165D0 (en) 1994-01-05
JPH09505041A (ja) 1997-05-20
CA2173470A1 (en) 1995-05-18
US5853623A (en) 1998-12-29
ATE188969T1 (de) 2000-02-15
NO961888L (no) 1996-05-09
DK0728144T3 (da) 2000-07-03
ES2143611T3 (es) 2000-05-16
FI961976A0 (fi) 1996-05-09
PL180403B1 (pl) 2001-01-31
HUT73799A (en) 1996-09-30
FI961976A (fi) 1996-05-09
PL314300A1 (en) 1996-09-02
NO961888D0 (no) 1996-05-09
DE69422726D1 (de) 2000-02-24
HU217344B1 (hu) 2002-02-28
PT728144E (pt) 2000-07-31
WO1995013289A1 (en) 1995-05-18
EP0728144B1 (en) 2000-01-19
HU9601244D0 (en) 1996-07-29
EP0728144A1 (en) 1996-08-28
GR3033103T3 (en) 2000-08-31
CZ287780B6 (en) 2001-02-14
AU679286B2 (en) 1997-06-26
AU8113394A (en) 1995-05-29

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