KR910007918A - 치환된5-[(테트라졸릴)알케닐]이미다졸 - Google Patents

치환된5-[(테트라졸릴)알케닐]이미다졸 Download PDF

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KR910007918A
KR910007918A KR1019900017301A KR900017301A KR910007918A KR 910007918 A KR910007918 A KR 910007918A KR 1019900017301 A KR1019900017301 A KR 1019900017301A KR 900017301 A KR900017301 A KR 900017301A KR 910007918 A KR910007918 A KR 910007918A
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tetrazol
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맥쿨로우치 키이난 리챠드
와인스톡 조셉
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스튜아트 알. 슈터
스미스클라인 비참 코포레이션
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Abstract

내용 없음

Description

치환된 5-[(테트라졸릴)알케닐]이미다졸
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 일반식 (Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염.
    상기식에서 R1은 아다만틸메틸, 또는 페닐, 비페닐 또는 나프틸이며, 여기서 각각의 아릴그룹은 비치환되거나, CI, Br, F, I, C1-6알킬, 니트로, CO2R7, C1-6알콕시, 하이드록시, SC1-6-C6알킬, SC1-6알킬, 테트라졸-5-일, SO2NHR7, SO3H, PO(OR7)2, CONR7R7, CN, NR7R7, NR7COH, NR7COC1-C6알킬, NR7CON(R7)2, NR7COW, SO2W, 및 W중에서 선택된 1내지 3개의 치환체에 의해 치환되고:R2는 비치환되거나, C1-6알킬, 니트로,CI, Br, F, I, 하이드록시, C1-6알콕시, NR7R7, CO2R7, CN, CONR7R7, W, NR7COH, NR7COC1-6알킬, N7COW, SO2W, SO2C1-6알킬 및 SC1-6알킬중에서 선택된 1내지 3개의 치환체에 의해 치환된 C2-10알킬, C3-10알케닐, (CH2)0-8-C3-6사이클로알킬 또는 (CH2)0-8페닐이며: X는 단일결합, S 또는 0이고: m은 0내지 4이며: R4는 수소, CI, Br, F, I, CHO, 하이드록시메틸, C1-6알킬, NR7R7, CONR7R7, NO2, CN, 페닐 또는 W이고:R3는 및 R5는 각각 독립적으로 수소, C1-8알킬, C3-6사이클로알킬, 테에닐-Y-, 퓨릴-Y-, 피라졸릴-Y-, 이미다졸릴-Y-, 티아졸릴-Y-, 피리딜-Y-, 테트라졸릴-Y-, 피롤릴-Y-, 트리아졸릴-Y-, 옥사졸리-Y-, 이속사졸릴-Y-, 또는 페닐-Y- 이며, 여기에서 아릴 또는 헤테로아릴 그룹은 비치환되거나 C1-C6알킬, C1-C6알콕시, CI, Br, F, I: NR7R7, CO2R7, CONR7R7, SO2NHR7, SO3H, OH, NO2, W, SO2C1-C6알킬, SO2W, SC1-C6알킬, NR7COW, NR7COH, 또는 N R7COC1-C6알킬이고: Y는 직쇄 또는 측쇄의 C1-C6알킬 또는 단일결합이며: R6는 Z-테트라졸-5-일 이고:Z는 단일결합: 비날: 또는 비치환되거나, C1-C4알킬, 1또는 2개의 벤질그룹, 티에닐메틸 또는 퓨밀메틸에 의해 치환된 메틸렌이며:W는 C2R20-1(여기에서 n은 1내지 4이다)이고: R7은 각각 독립적으로 수소 또는 C1-6알킬이다.
  2. 제1항에 있어서 R1이 비치환되거나 클로로 플루오로, 니트로, 메틸, 트리플루오로메틸, 메톡시, 하이드록시, 설폰아미도, 설파민, 시아노, 카복시, 카보 C1-6알콕시, 카바모일 및 테트라졸-5-일중에서 선택된 1내지 3개의 치환체에 의해 치환된 페닐이고: R2가 C2-8알킬이며: X가 단일결합 또는 S이고: m이 1 또는 2이며: R3가 수소, 클로로, 플루오로 또는 트리플루오로메틸이고:R4가 수소 또는 C1-6알킬이며: R5가 비치환되거나 메틸에 의해 치환된 티에닐메틸, 또는 비치환되거나 메톡시 또는 하이드록시에 의해 치환된 벤질이고: R6가 테트라졸-5-일인 화합물 또는 이의 약제학적으로 허용되는 염.
  3. 제1항 또는 제2항에 있어서, E이성체이고, 테트라졸 및 이미다졸그룹이 서로에 대하여 트랜스인 화합물.
  4. 제1항에 있어서 (E)-1-[2-n-부틸-1-{(4-카르복시페닐)메틸}-1H-이미다졸-5-일]-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜인 화합물 또는 이의 약제학적으로 허용되는 염.
  5. 제1항에 있어서 (E)-1-[2-n-부틸-1-{(2-클로로페닐)메틸}-1H-이미다졸-5-일]-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜:(E)-1-[2-n-부틸-1-{(2-니트로페닐)메틸}-1H-이미다졸-5-일)-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜:(E)-1-[2-n-부틸-1-{(4-트리플루오로메틸페닐)메틸}-1H-이미다졸-5-일]-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜: 염.(E)-1-((2-n-부틸-1-((2-클로로페닐)메틸)-H-이미다졸-5-일]-2-2(1H-테트라졸-5-일)-3-(2-티에닌)-1H-프로펜; (E)-1-[2-n-부틸-1-{(2-클로로페닐)메틸}-4-플루오로-1H-이미다졸-5-일)-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜:(E)-1-((2-n-부틸-1-((2-클로로페닐)메틸)-1H-이미다졸-5-일)-2-(1H-테트라졸-5-일)-3-(3-티에닐)-1H-프로펜: (E)-1-((2-n-부틸-1-((2-클로로페닐)메틸)-1H-이미다졸-5-일)-2-(1H-테트라졸-5-일)-3-(4-하이드록시페닐)-1H-프로펜:(E)-1-[2-(1-부테닐)-1-{(2-클로페닐)메틸}-1H-이미다졸-5-일]-2-(1-테트라졸-5-일)-3-(2-디에닐-H-프로펜; (E)-1-((2-n-부테닐-1-((2-클로로페닐)메틸)-1H-이미다졸-5-일)-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜: (E)-1-((2-n-부틸-1-((2-클로로페닐)메틸)-1H-이미다졸-5-일)-2-(1H-테트라졸-5-일)-3-(2-티에닐)-1H-프로펜:또는 (E)-1-((2-n-부틸-1-((4-테트라졸-5-일)-3-(2-티에닐)-1-프로펜인 화합물 또는 이의 약제학적으로 허용되는 염.
  6. 제1항 내지 제5항중 어느 한항에 따르는 화합물과 약제학적으로 허용되는 담체를 함유하는 약제학적 조성물.
  7. 하기의 일반식(Ⅱ)의 화합물을 아자이드와 반응시키고, 그후 필요한 경우 R1그룹이 C1-6알콕시에 의하여 치환된 일반식(I)화합물을 탈보호시켜 R1그룹이 하이드록시에 의하여 치환된 일반식(I)의 화합물로 전환시키거나, R1그룹이 CO2C1-6알킬에 의하여 치환된 일반식(I)화합물을 가수분해시켜 R1그룹이 카르복시에 의하여 치환된 일반식(I)의 화합물로 전환시키거나 R1그룹이 CN에 의하여 치환된 일반식(I)화합물을 아자이드와 반응시켜 R1그룹이 테트라졸-5-일에 의하여 치환된 일반식(I)의 화합물로 전환시키고, 그후 임의로 약제학적으로 선택되는 염을 형성시킴을 특징으로 하여, 제1항에서 정의한 바와 같은 일반식(I)의 화합물을 아자이드와 반응시켜 R1그룹이 테트라졸-5-일에 의하여 치환된 일반식(I)의 화합물로 전환시키고, 그 후 임의로 약제학적으로 선택되는 염을 형성시킴을 특징으로 하여, 제1항에서 정의된 바와 같은 일반식(I)의 화합물 또는 이의 약제학적으로 허용되는 염을 제조하는 방법.
    상기식에서 R2, R3, R4, R5, X 와 m은 제1항에서 정의한 바와 같고, R1는 제1항에서 정의한 바와같으며, 단 R1그룹에서 치환체는 테트라졸-5-일, OH 또는 CO2H를 포함해서는 안된다.
  8. 안지오텐신 Ⅱ수용체 길항작용이 인자된 질병의 치료를 위한 약제를 제조하는데 있어서 제1항에서 정의한 바와같은 일반식(I)의 화합물 또는 이의 약제학적으로 허용되는 염의 용도.
  9. 고혈압 치료를 위한 약제를 제조하는데 있어서 제1항에서 정의한 바와 같은 일반식(I)의 화합물 또는 이의약제학적으로 허용되는 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900017301A 1989-10-25 1990-10-25 치환된5-[(테트라졸릴)알케닐]이미다졸 KR910007918A (ko)

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CA (1) CA2027937A1 (ko)
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AU640417B2 (en) 1993-08-26
PT95684A (pt) 1991-09-13
ATE103604T1 (de) 1994-04-15
AU6470090A (en) 1991-05-02
EP0425211B1 (en) 1994-03-30
NZ235776A (en) 1991-09-25
DE69007740D1 (de) 1994-05-05
JPH03151379A (ja) 1991-06-27
EP0425211A1 (en) 1991-05-02
ZA908508B (en) 1992-01-29
DE69007740T2 (de) 1994-07-07
ES2062403T3 (es) 1994-12-16
CA2027937A1 (en) 1991-04-26
IE903822A1 (en) 1991-05-08

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