KR890011827A - 화학적 화합물 - Google Patents

화학적 화합물 Download PDF

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KR890011827A
KR890011827A KR1019890000660A KR890000660A KR890011827A KR 890011827 A KR890011827 A KR 890011827A KR 1019890000660 A KR1019890000660 A KR 1019890000660A KR 890000660 A KR890000660 A KR 890000660A KR 890011827 A KR890011827 A KR 890011827A
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compound
hydroxy
alkyl
optionally substituted
formula
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윌리암 로드니 카울케트 피터
죤 쿠퍼 미첼
알란 에아킨 무르도크
죤스 케라인트
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원본미기재
임페리얼 케미칼 인더스트리스 피엘씨
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Abstract

내용 없음

Description

화학적 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 하기식 (Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 염.
    상기식에서, R1은 수소, 플루오로 또는 클로로; R2는 수소, C1-6알킬 또는 C3-6알케닐 인데 이들 각각은 히드록시, C1-4알콕시, 페녹시, 카르바모일, C1-6알킬카르바모일, 디-C1-6알킬카르바모일, 피리딜, 페닐 또는 클로로페닐로 임의로 치환되거나 또는 R2는 C3-6알키닐, C3-5시클로알킬이거나 또는 할로, C1-4알킬, C1-4알콕시, 트리플루오로 메틸, 시아노 또는 니트로로 임의로 치환된 페닐; R3은 수소, C1-6알킬 또는 -OR4로서 R4는 수소이거나, 또는 히드록시 또는 C1-4알콕시로 임의로 치환된 C1-6알킬이거나 또는 히드록시 또는 C1-4알콕시로 임의로 치환된 C3-6알케닐 또는 R4는 C3-5알키닐 페닐, 나프틸, 페닐 C1-4알킬 또는 나프틸 C1-4알킬; 또는 R2와 R3는 함께 C4-7메틸렌 사슬을 형성 (하나의 메틸렌 단위는 임의로 -NR2R3의 질소 원자로부터 멀리 있는 적어도 2개의 탄소원자에 위치한 산소 또는 황에 의하여 임의로 치환됨)하는데 두개의 이웃된 메틸렌 단위는 상기 C4-7메틸렌 사슬에 연결된 벤젠환의 2개의 탄소원자에 의하여 임의로 치환되며 상기 벤젠환은 할로, C1-4알킬, C1-4알콕시, 트리플루오로메틸, 시아노 또는 니트로에 의하여 임의로 치환되거나 또는 R2와 R4는 함께 C3-4메틸렌 사슬을 형성한다.
  2. 제1항에 있어서, R1이 수소인 화합물.
  3. 제1항 또는 제2항에 있어서, 페녹시 프로필아미노에틸기와 -OCH2CONR2R3치환체가 파라관계에 있는 화합물
  4. 제1항 내지 제3항중 어느 한 항에 있어서, R2가 C1-6알킬 또는 C3-6알케닐이고 이들중 하나는 선택적으로 히드록시, C1-4알콕시 또는 페닐로 치환된 화합물.
  5. 제1항 내지 제4항 중 어느 한 항에 있어서, R3이 수소 또는 C1-6알킬인 화합물.
  6. 제1항 내지 제4항 중 어느 한 항에 있어서, R3이 히드록시 또는 C1-6알킬인 화합물.
  7. 제1항에 있어서, N-2-메톡시에틸-4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세트아미드, N-3-메톡시프로필 4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세트아미드, N-3-메톡시프로필 4-[2-(2S-히드록시-3-페녹시프로필아미노)에틸]페녹시아세트아미드, N-2-에톡시프로필 4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세토아미드인 화합물 또는 그들의 약학적으로 허용 가능한 염.
  8. 제1항에 있어서, N,N-디에틸 4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세트아미드, N-에틸-N-메틸 4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세트아미드, N-(4-[2-(2-히드록시-3-페녹시프로필아미노)에틸])모르폴린, N-(4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세틸)피페리딘, 4-[2-(2-히드록시-3-페녹시프로필아미노)에틸]페녹시아세토히드록사민산 또는 약학적으로 허용가능한 그들의 염.
  9. 하기식 (Ⅱ)의 화합물 또는 약학적으로 허용가능한 그의 염.
    상기식에서 R1은 수소, 클로로 또는 플루오로이다.
  10. 제1 내지 9항중 어느 한 항에 있어서, 좌선성 광학활성형인 화합물.
  11. 제1 내지 10항중 어느 한 항의 화합물 또는 약학적으로 허용가능한 그의 염 및 약학적으로 허용가능한 담체로 구성된 약학적 조성물.
  12. 제11항에 있어서, 서방성 방출형태인 약학적 조성물.
  13. ⒜ 하기식 (Ⅲ)의 화합물과 하기식(Ⅳ)의 화합물을 반응시키거나; 또는 ⒝ 하기식 (Ⅴ)의 화합물과 하기식(Ⅵ)의 화합물을 반응시키거나; 또는 ⒞ 하기식(Ⅶ)의 화합물과 하기식(Ⅷ)의 화합물을 반응시키거나; 또는 ⒟ 하기식 (Ⅸ)의 화합물을 탈보호하거나; 또는 ⒠ 하기식(Ⅹ)의 알맞게 보호된 화합물 또는 그의 활성화된 유도체를 상기 정의된 식(Ⅳ)의 화합물과 반응시키고; 그뒤 필요하다면 약학적으로 허용가능한 염을 형성하는 것으로 구성된 제1항에서 정의된 하기식 (Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 염의 제조방법.
    상기식에서, R1은 수소, 플루오로 또는 클로로; R2는 수소, C1-6알킬 또는 C3-6알케닐인데 이들 각각은 히드록시, C1-4알콕시, 페녹시, 카르바모일, C1-6알킬카르바모일, 디-C1-6알킬카르바모일 피리딜, 페닐 또는 콜로로페닐로 임의로 치환되거나 또는 R2는 C3-6알키닐, C3-5시클로알킬이거나 또는 할로, C1-4알킬, C1-4알콕시, 트리플루오로 메틸, 시아노 또는 니트로로 임의로 치환된 페닐; R3은 수소, C1-6알킬 또는 -OR4로서 R4는 수소이거나, 또는 히드록시 또는 C1-4알콕시로 임의로 치환된 C1-6알킬이거나 또는 히드록시 또는 C1-4알콕시로 임의로 치환된 C3-6알케닐 또는 R4는 C3-6알키닐 페닐, 나프틸, 페닐 C1-4알킬 또는 나프틸 C1-4알킬 ; 또는 R2와 R3는 함께 C4-7메틸렌 사슬을 형성 (하나의 메틸렌 단위는 임의로 -NR2R3의 질소원자로부터 멀리 있는 적어도 2개의 탄소원자에 위치한 산소 또는 황에 의하여 임의로 치환됨)하는데 두개의 이웃된 메틸렌 단위는 상기 C4-7메틸렌 사슬에 연결된 벤젠환의 2개의 탄소원자에 의하여 임의로 치환되며 상기 벤젠환은 할로, C1-4알킬, C1-4알콕시, 트리플루오로메틸, 시아노 또는 니트로에 의하여 임의로 치환되거나 또는 R2와 R4는 함께 C3-4메틸렌 사슬을 형성한다. R5는 치환 가능한 기, Y는 이탈기, Q는 보호기.
  14. 제13항에서 정의된 식(Ⅸ)의 화합물.
  15. 하기식의 화합물
    상기식에서 R2와 R3은 제1항에서 정의된 것과 같으며 R0은 수소 또는 보호기이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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