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KR950032081A - 신규한 벤질아미노에톡시벤젠 유도체 - Google Patents

신규한 벤질아미노에톡시벤젠 유도체 Download PDF

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KR950032081A
KR950032081A KR1019950002690A KR19950002690A KR950032081A KR 950032081 A KR950032081 A KR 950032081A KR 1019950002690 A KR1019950002690 A KR 1019950002690A KR 19950002690 A KR19950002690 A KR 19950002690A KR 950032081 A KR950032081 A KR 950032081A
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마사카즈 반
세이다카 시노다
미다쓰 다카하시
슈헤이 데구치
히토오 다구치
다케오 가츠시마
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시바타 미노루
도요 보세키 가부시키가이샤
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Abstract

본 발명은 아드레날린 α1수용체 차단제로서 유용한 신규한 벤질아미노에톡시벤젠 유도체를 제공하고자 한다. 또한, 하기 일반식(Ⅰ)로 표시되는 신규한 벤질아미노에톡시벤젠 유도체, 이의 염 및 이의 용매화물에 관한 것이다 :
상기 식에서, R1은 수소 원자, 저급 알킬기, 저급 히드록시 알킬시, 저급 알콕시 알킬기, 알릴기 또는 벤질기; R2는 수소 원자, 저급 알킬기, 저급 아실기, 알릴또는 벤질기; R3는 수소 원자, 저급 알킬기, 저급 알콕시 알킬기, 저급 디알킬 아미노 알킬기 또는 저급 아실기; R4는 수소 원자, 할로겐 원자, 저급 알콕시기, 아미노기, 저급 아실 아미노기, 히드록시기, 저급 아실옥시기, 저급 아실기, 카르복실기 또는 저급 알콕시 카르보닐기를 나타낸다.
이는 강한 아드레날린 α1수용체 차단 작용을 갖는 동시에, 기립성 저혈압등의 부작용이 적은 아드레날린 α1수용체 차단체를 얻을 수 있다.

Description

신규한 벤질아미노에톡시벤젠 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 일반식(Ⅰ)으로 표시되는 신규한 벤질아미노산에톡시벤젠 유도체, 이의 염 및 이의 용매화물 :
    상기 식에서, R1은 수소원자, 저급 알킬기, 저급 히드록시 알킬시, 저급 알콕시 알킬기, 알릴기 또는 벤질기; R2는수소 원자, 저급 알킬기, 저급 아실기, 알릴 또는 벤질기; R3는 수소원자, 저급 알킬기, 저급 알콕시 알킬기, 저급 디알킬 아미노 알킬기 또는 저급 아실기; R4는 수소 원자, 할로겐 원자, 저급 알콕시기, 아미노기, 저급 아실 아미노기, 히드록시기, 저급 아실옥시기, 저급 아실기, 카르복실기 또는 저급 알콕시 카르보닐기를 나타낸다.
  2. 하기 일반식(I)로 표시되는 신규한 벤질아미노에톡시벤젠 유도체, 이의 염 및 이의 용매화물 :
    상기 식에서, R1은 수소 원자, 저급 알킬기, 저급 히드록시 알킬기 또는 저급 알콕시 알킬기; R2는 수소원자 또는 저급 아실기; R3는 수소 원자, 저급 알킬기 또는 저급 알콕시 알킬기; R4는 히드록시기 또는 저급 아실옥시기를 나타낸다.
  3. 하기 일반식(I)으로 표시되는 신규한 벤질아미노에톡시벤젠 유도체, 이의 염 및 이의 용매화물을 함유하는 의약 조성물 :
    상기 식에서, R1은 수소 원자, 저급 알킬기, 저급 히드록시 알킬시, 저급 알콕시 알킬기, 알릴기 또는 벤질기; R2는 수소 원자, 저급 알킬기, 저급 아실기, 알기릴 또는 벤질기; R3는수소원자, 저급 알킬기, 저급 알콕시 알킬기, 저급 디알킬 아미노 알킬기 또는 저급 아실기; R4는 수소 원자, 할로겐 원자, 저급 알콕시기, 아미노기, 저급 아실 아미노기, 히드록시기, 저급 아실옥시기, 저급 아실기, 카르복실기 또는 저급 알콕시 카르보닐기를 나타낸다.
  4. 하기 일반식(I)으로 표시되는 신규한 벤질아미노에톡시벤젠 유도체, 이의 염 및 이의 용매화물을 함유하는 의약 조성물 :
    상기 식에서, R1은 수소 원자, 저급 알킬기, 저급 히드록시 알킬기 또는 저급 알콕시 알킬기; R2는 수소원자 또는 저급 아실기; R3는 수소 원자, 저급 알킬기 또는 저급 알콕시 알킬기; R4는 히드록시기 또는 지급 아실옥시기를 나타낸다.
  5. N-(3-히드록시-6-메톡시-2,4,5-트리메틸벤질)-N-메틸-2-(4-히드록시-2-이소프로필-5-메틸페녹시)에틸아민, 이의 염 및 이의 용매화물.
  6. N-(3-히드록시-6-메톡시-2,4,5-트리메틸벤질)-2-(4-히드록시-2-이소프로필-5-메틸페녹시)에틸아민, 이의 의약적으로 허용가능한 염 및 이의 용매화물.
  7. N-(2-에톡시-5-히드록시-3,4,6-트리메틸벤질)-2-(4-히드록시-2-이소프로필-5-메틸페녹시)에틸아민, 이의 염 및 이의 용매화물.
  8. N-(3-히드록시-6-메톡시-2,4,5-트리메틸벤질)-N-메틸-2-(4-히드록시-2-이소프로필-5-메틸페녹시)에틸아민, 이의 염 및 이의 용매화물을 함유하는 의약 조성물.
  9. N-(3-히드록시-6-메톡시-2,4,5-트리메틸벤질)-2-(4-히드록시-2-이소프로필-5-메틸페녹시)에틸아민, 이의 염 및 이의 용매화물을 함유하는 의약 조성물.
  10. N-(2-에톡시-5-히드록시-3.4,6-트리메틸벤질)-2-(4-히드록시-2-이소프로필-5-메틸페녹시)에틸아민, 이의 염 및 이의 용매화물을 함유하는 의약 조성물.
  11. 제1항에 기재한 일반식(I)으로 표시되는 신규한 벤질아미노에톡시벤젠 유도체의 제조방법으로서, 하기 일반식(Ⅱ)로 표시되는 벤젠 유도체를, 염기의 존재하 또는 부재하, 통상의 용매중 또는 무용매로 하기 일반식(Ⅲ)로 표시되는 아민 또는 이의 산부가염과 냉각하 내지 가열화(환류화) 축합함으로써, 목적하는 일반식(I)으로 표시되는 벤질아미노에톡시벤젠 유도체를 제조하고, 필요에 따라, 벤질아미노에톡시벤젠 유도체의 유리염기 형태를 적당한 유기 또는 무기 산 또는 염기를 첨하여 이의 의약적으로 허용가능한 염 및 용매화물을 형성시키는 방법 :
    상기 식에서, R1은 수소원자. 저급 알킬기, 저급 히드록시 알킬기, 저급 알콕시 알킬기, 알릴기 또는 벤질기: R2는 수소 원자, 저급 알킬기, 저급 아실기 또는 알릴기, R3는 수소 원자, 저급 알킬기, 저급 알콕시 알킬기, 저급 디알킬 아미노 알킬기 또는 저급 아실기; R4는 수소 원자, 할로겐 원자, 저급 알콕시기, 아미노기, 저급 아실아미노기, 히드록시기. 저급 아실옥시기, 저급 아실기, 카르복실기 또는 저급 알콕시 카르보닐기; X는 할로겐 원자, C1-C4알킬 설포닐옥시기 또는 C6-C|10아릴 설포닐옥시기를 나타낸다.
  12. 제1항에 기재한 일반식(I)으로 표시되는 신규한 벤질아미노에톡시벤젠 유도체의 제조방법으로서 하기 일반식(Ⅳ)로 표시하는 벤즈알데히드 유도체를 산 또는 염기 촉매의 존재하 또는 부재하, 통상의 용매중 또는 무용매로, 하기 일반식(Ⅴ)로 표시되는 아민과 탈수제의 존재하 또는 부재하에 냉각하 내지 가열화(환류하), 탈수 축합함으로써 하기 일반식(Ⅵ)로 표시되는 벤질리덴 알킬 아민 유도체를 합성 중간체로서 제조한 후, 이것을 통상의 용매중 또는 무용매로 환원제를 사용하여, 냉각하 내지 가열하(환류하) 환원함으로써 목적하는 일반식(I)으로 표시되는 벤질아미노에톡시벤젠 유도체를 제조하고, 필요에 따라 벤질아미노에톡시벤젠 유도체를 유리 염기 형태를, 적당한 유기 또는 무기산 또는 염기를 첨가하여 이의 약학적으로 허용가능한 염 및 용매화물을 형성시키는 방법 :
    상기 식에서, R1은 수소 원자, 저급 알킬기, 저급 히드록시 알킬기, 저급 알콕시 알킬기, 알릴기 또는 벤질기; R2는 수소 원자, 저급 알킬기, 저급 아실기 또는 알릴기, R4은 수소 원자, 할로겐 원자, 저급 알콕시기, 아미노기, 저급 아실아미노기, 히드록시기, 저급 아실옥시기, 저급 아실기, 카르복실기 또는 저급 알콕시 카르보닐기를 나타낸다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950002690A 1994-02-10 1995-02-10 신규한 벤질아미노에톡시벤젠 유도체 Expired - Fee Related KR100220283B1 (ko)

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US6730691B1 (en) 2000-02-10 2004-05-04 Miles A. Galin Uses of alpha adrenergic blocking agents
US20040229781A1 (en) * 2000-05-10 2004-11-18 Marks Andrew Robert Compounds and methods for treating and preventing exercise-induced cardiac arrhythmias
US20040048780A1 (en) * 2000-05-10 2004-03-11 The Trustees Of Columbia University In The City Of New York Method for treating and preventing cardiac arrhythmia
US7393652B2 (en) * 2000-05-10 2008-07-01 The Trustees Of Columbia University In The City Of New York Methods for identifying a chemical compound that directly enhances binding of FKBP12.6 to PKA-phosphorylated type 2 ryanodine receptor (RyR2)
US8022058B2 (en) 2000-05-10 2011-09-20 The Trustees Of Columbia University In The City Of New York Agents for preventing and treating disorders involving modulation of the RyR receptors
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US6489125B1 (en) * 2000-05-10 2002-12-03 The Trustees Of Columbia University In The City Of New York Methods for identifying chemical compounds that inhibit dissociation of FKBP12.6 binding protein from type 2 ryanodine receptor
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