KR920019722A - 신규의 아미노페놀 유도체 및 그의 약학 조성물 - Google Patents

신규의 아미노페놀 유도체 및 그의 약학 조성물 Download PDF

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KR920019722A
KR920019722A KR1019920005792A KR920005792A KR920019722A KR 920019722 A KR920019722 A KR 920019722A KR 1019920005792 A KR1019920005792 A KR 1019920005792A KR 920005792 A KR920005792 A KR 920005792A KR 920019722 A KR920019722 A KR 920019722A
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lower alkyl
hydrogen atom
propyl
amino
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나오끼 스기야마
후미히꼬 아까보시
하루꼬 야꾸마루
도모까즈 고또오
마사노리 스기우라
시게끼 구와하라
마사히꼬 가지이
요시꼬 다나까
다까오 곤도오
지까라 후까야
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스야마 다다까즈
가부시끼가이샤 미도리 쥬우지
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Abstract

내용 없음

Description

신규의 아미노페놀 유도체 및 그의 약학 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 하기 식(Ⅰ)의아미노페놀 유도체 또는 약학적으로 허용될 수 있는 그의 염.
    상기식에서, X는 수소 원자, 저급 알킬기, 또는 페놀성 하이드록시의 보호기이고, Y는 Y1~Y3이며, Z는 수소 원자, 저급 알킬기, 할로겐 원자 또는 트리플루오로메틸기이고, A는 A1~A5이며 B는 B1~B5인데, A가 A1일 때 B는 B1이고 Y는 Y1또는 Y2이며, A가 A2일 때 B는 B2이고 Y는 Y3이며, A가 A3일 때 B는 B3이고 Y는 Y3이며, A가 A4일 때 B는 B4이고 Y는 Y4이며, A가 A5일 때 B는 B5이고 Y는 Y3이며; 여기에서, A가 A1이고 B가 B1이며 Y가 Y1인 경우, A1및 B1은 서로 같거나 다르며 각각 수소 원자 저급 알킬기이거나, A1과 B1이 결합하여 탄소수 2~5의 알킬렌기를 형성할 수 있고, Y1은 다음
    [이 식에서, n은 1~4의 정수이고, R1은 R1A~R1E이고, R2는 R2A~R2E이며, R3는 R3A~R3E이고, R4는 R4A~R4E이며, R5는 R5A~R5E이며, R6은 R6A~R6E이며, R7는 R7A~R7E이고, D는 산소 원자, 질소 원자 또는 탄소 원자인데, D가 산소 원자일 때 R1~R7은 R1A~R7A이고, D가 질소 원자일 때 R1~R7은 R1BR7B또는 R1CR7C이고, D가 탄소 원자일 때 R1~R7은 R1D~R7D또는 R1E~R7E이고; 여기에서, D가 산소 원자인 경우, R1A는 페닐기 또는 피리딜기(이들 기는 치환체를 가지고 있을 수 있다)이고, R2A는 수소 원자 또는 저급 알킬기이며, R3A및 R4A는 없고, R5A~R7A는 서로 같거나 다르며 각각 수소 원자, 저급 알킬기이거나 R5A~R7A중에서 선택된 임의의 2개 기가 탄소수 2~5의 알킬렌기를 형성할 수 있고; D가 질소 원자인 경우, R1B는 페닐기 또는 피리딜기(이들 기는 치환체를 가지고 있을 수 있다)이고, R2B는 수소 원자 또는 저급 알킬기이며, R3B는 없고, R4B~R7B는 서로 같거나 다르며 각각 수소 원자, 저급 알킬기이거나 R4B~R7B중에서 선택된 임의의 2개 기가 탄소수 2~5의 알킬렌기를 형성할 수 있고, 또한 RC및 R2C는 서로 같거나 다르며 각각 수소 원자 또는 저급 알킬기이며, R3C는 없고, R4C는 페닐기 또는 피리딜기(이들 기는 치환체를 가지고 있을 수 있다)이며, R5C~R7C는 서로 같거나 다르며 각각 수소 원자, 저급 알킬기이거나 R5C~R7C중에서 선택된 임의의 2개 기가 탄소수 2~5의 알킬렌기를 형성할 수 있고; D가 탄소 원자인 경우, R1D는 페닐기 또는 피리딜기(이들 기는 치환체를 가지고 있을 수 있다)이고, R2D~R4D는 서로 같거나 다르며 각각 수소 원자 또는 저급 알킬기이며, R5D~R7D는 서로 같거나 다르며 각각 수소 원자, 저급 알킬기이거나 R5D~R7D중에서 선택된 임의의 2개 기가 탄소수 2~5의 알킬렌기를 형성할수 있고, 또한 R1E는 페닐기, 피리딜기, 벤질기또는 피리딜메틸기(이들 기는 치환체를 가지고 있을 수 있다)이며, R2E및 R3E는 단일 결합을 형성할 수 있고, R4E는 수소 원자 또는 저급 알킬기이며, R5E~R7E는 서로 같거나 다르며 각각 수소 원자 또는 저급 알킬기이거나 R5E~R7E중에서 선택된 임의의 2개 기가 탄소수 2~5의 알킬렌기를 형성할수 있다.]의 기이며; A가 A1이고 B가 B1이며 Y가 Y2인 경우, A1과 B1은 상술한 바와 같고, Y2는 다음 식
    [이 식에서, t는 1~5의 정수이고, 1 및 m은 각각 2~4의 정수이며, E 및 W는 서로 같거나 다르며 각각 질소 원자 또는 CH이고, F는 직접 결합 또는 산소 원자이며, P 및 Q는 서로 같거나 다르며 각각 수소 원자, 할로겐 원자, 저급 알킬기 또는 저급 알콕시기이고, R8은 수소 원자, 하이드록시기 또는 하이드록시-보호기이다.]의 기이고; A가 A2이고 B가 B2이며 Y가 Y3인 경우, Y3는 수소 원자 또는 저급 알킬기이고, A2는 페닐기, 피리딜기, 벤질기 또는 피리딜메틸기(이들 기는 치환체를 가지고 있을 수 있다)이며, B2는 다음 식
    [이 식에서, G는 1~3의 정수이고, R9~R11은 서로 같거나 다르며 각각 수소 원자, 저급 알킬기이거나 R9~R11중에서 선택된 임의의 2개 기가 탄소수 2~5의 알킬렌기를 형성할 수 있다.]의 기이며; A가 A3이고 B가 B3이며 Y가 Y3인 경우, Y3는 상술한 바와 같고, A3는 수소 원자 또는 저급 알킬기이거나, A3및 R12는 탄소수 2~5의 알킬렌기를 형성할 수 있고, B3는 다음 식
    [이 식에서, k는 1~3의 정수이고, h는 0 또는 1이며, R12는 수소 원자 또는 저급 알킬기이거나, R12및 A3는 탄소수 2~5의 알킬렌기를 형성할 수 있고, R13및 R14는 서로 같거나 다르면 각각 페닐기 또는 피리딜기(이들기는 치환체를 가지고 있을 수 있다)이다.]의 기이고; A가 A4이고 B가 B4이며 Y가 Y3인 경우, Y3는 상술한 바와 같고, A4는 수소 원자 또는 저급 알킬기이거나, A4및 V가 인접 질소 원자와 함께 4~6-원 고리를 형성할 수 있고, B4는 다음 식
    [이 식에서, V는 알킬렌기이거나 V 및 A4가 인접 질소 원자와 함께 4~6-원 고리를 형성할 수 있고, W는 질소 원자 또는 CH이다.]의 기이며; A가 A5이고 B가 B5이며 Y가 Y3인 경우, Y3는 상술한 바와 같고, A5는 수소 원자 또는 저급 알킬기이며, B5는 다음 식
    [이 식에서 각 기호는 상술한 바와 같다]의 기이다.
  2. 제1항에 있어서,는 화합물(Ⅰ)의 OX에 대하여 오르토-위치에 결합되고, Y는 파라-위치에 결합되어 있는 것을 특징으로 하는 아미노페놀 유도체 또는 약학적으로 허용될 수 있는 그의 염.
  3. 제1항에 있어서, 다음 식으로 나타내는 아미노페놀 유도체 또는 약학적으로 허용될 수 있는 그의 염.
    [상기식에서, X는 수소 원자, 저급 알킬기, 또는 페놀성 하이드록시의 보호기이고, Y3는 수소 원자 또는 저급 알킬기이며, Z는 수소 원자, 저급 알킬기, 할로겐 원자 또는 트리플루오로메틸기이고, A5는 수소 원자 또는 저급 알킬기이며, t는 1~5의 정수이고, 1 및 m은 각각 2~4의 정수이며, E 및 W는 서로 같거나 다르며 각각 질소 원자 또는 CH이고, F는 직접 결합 또는 산소 원자이며, P 및 Q는 서로 같거나 다르며 각각 수소 원자, 할로겐 원자, 저급 알킬기 또는 저급 알콕시기이고, R8은 수소 원자, 하이드록시기 또는 하이드록시-보호기이다.
  4. 제3항에 있어서, N은 OX에 대하여 오르토-위치에 결합되고, Y3는 파라-위치에 결합되어 있는 것을 특징으로 하는 아미노페놀 유도체 또는 약학적으로 허용될 수 있는 그의 염.
  5. 제1항에 있어서, 2-[1-(4-클로로페닐)-1-(3-디메틸아미노-4-하이드록시페닐)메톡시]-N, N-디메틸에틸아민, 2-[(3-디메틸아미노-4-하이드록시페닐)-2-피리딜메톡시]-N, N-디메틸에틸아민, 4-(4-클로로페닐-4-메틸피페라지노)메틸-2-디메틸아미노페놀, 2-디메틸아미노-4-(N-2-디메틸아미노에틸-N-페닐)아미노메틸페놀, 1-(4-클로로페닐)-3-디메틸아미노-1-(3-디메틸아미노-4-하이드록시페닐)-1-프로펜, 4-[1-(4-클로로페닐)3-디메틸아미노프로필]-2-디메틸아미노페놀, 4-[4-(4-클로로벤즈하이드릴)피페라지노]메틸-2-디메틸아미노페놀, N, N-디메틸-N′-(2-하이드록시-5-메틸페닐)-N′-페닐에틸렌디아민, N-벤질-N′, N′-디메틸-N-(2-하이드록시-5-메틸에틸)에틸렌디아민, 2-(N-2-벤즈하이드릴옥시에틸-N-메틸)아미노-4-메틸페놀, 3-(4-클로로페닐)-N-(2-메톡시-4-메틸페닐)-N-n-옥틸-3-(2-피리딜)프로필아민, 2-[1-메틸-2-(페노티아진-10-일)에틸]아미노-4-메틸페놀, 2-[N-메틸-N-[1-메틸-2-(페노티아진-10-일)에틸]아미노-4-메틸페놀, 2-[3-(4-벤즈하이드릴피페라지노)프로필]아미노-4-메틸페놀, 2-[3-[4-(4-클로로벤즈하이드릴)피페라지노]프로필]아미노-4-메틸페놀, 2-[N-[3-(4-벤즈하이드릴피페라지노)프로필]-N-메틸]아미노-4-메틸페놀, 2-[3-[4-(4-클로로벤즈하이드릴)호모피페라지노]프로필]아미노-4-메틸페놀, 2-[3-(4-하이드록시디페닐메틸-1-피페리디닐)프로필]아미노-4-메틸페놀, 2-[3-(4-벤즈하이드릴옥시-1-피폐리디닐)프로필]아미노-4-메틸페놀, 2-t-부틸-6-[3-[4-(4-클로로벤즈하이드릴)피페라지노]프로필]아미노-4-메틸페놀, 2-[N-[3-(4-(4-클로로벤즈하이드릴)피페라니조)프로필]-N-이소프로필]아미노-4-메틸페놀, 6-t-부틸-2-[N-[3-[4-(4-클로로벤즈하이드릴)피페라지노]프로필]-N-이소프로필]아미노-4-메틸페놀, 2-[N-[3-(4-하이드록시디페닐메틸-1-피페리디닐)프로필]-N-이소프로필]아미노-4-메틸페놀, 4-t-부틸-2-[3-[4-(4-클로로벤즈하이드릴)피페라지노]프로필]아미노페놀, 4-t-부틸-2-[N-[3-[4-(4-클로로벤즈하이드릴)피페라지노]프로필]-N-이소프로필]아미노페놀, 2-[3-[4-[(4-클로로페닐)하이드록시페닐메틸]-1-피페리디닐]프로필]아미노-4-메틸페놀, 2-[N-[3-[4-(4-클로로페닐)하이드록시페닐메틸]-1-피페리디닐]프로필]-N-이소프로필]아미노-4-메틸페놀, 2-[3-[4-(4-클로로벤즈하이드릴옥시)-1-피페리디닐]프로필]아미노-4-메틸페놀, 2-[3-[4-(4,4′-디클로로벤즈하이드릴)피페라지노]프로필]아미노-4-메틸페놀, 2-[N-[3-[4-(4,4′-디클로로벤즈하이드릴)피페라지노]프로필]-N-이소프로필]아미노-4-메틸페놀, 2-[N-[3-(4-벤즈하이드릴피페라지노)프로필]-N-이소프로필]아미노-4-메틸페놀, 2-[3-[4-(4,4′-디플루오로벤즈하이드릴)피페라지노]프로필]아미노-4-메틸페놀, 및 2-[N-[3-[4-(4,4′-디플루오로벤즈하이드릴)피페라지노]프로필]-N-이소프로필]아미노-4-메틸페놀로 이루어진 군으로부터 선택된 것을 특징으로 하는 아미노페놀 유도체.
  6. 제1항에 따른 아미노페놀 유도체 또는 약학적으로 허용될 수 있는 그의 염을 활성 성분으로서 함유하는 것을 특징으로 하는 약학 조성물.
  7. 제6항에 있어서, 활성 산소 생성 억제제 또는 활성 산소 포착제인 것을 특징으로 하는 약학 조성물.
  8. 제6항에 있어서, 항감염제인 것을 특징으로 하는 약학 조성물.
  9. 제6항에 있어서, 항알레르기제인 것을 특징으로 하는 약학 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920005792A 1991-04-08 1992-04-08 신규의 아미노페놀 유도체 및 그의 약학 조성물 KR920019722A (ko)

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US20030045722A1 (en) * 1994-05-18 2003-03-06 Henton Daniel R. Processes for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives, polymorphs and pseudomorphs thereof
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WO1996031479A1 (en) * 1995-04-07 1996-10-10 Novo Nordisk A/S Novel heterocyclic compounds
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DE3000441A1 (de) * 1980-01-08 1981-07-09 Merck Patent Gmbh, 6100 Darmstadt Anilinderivate,,diese enthaltende pharmazeutische zubereitungen und verfahren zu ihrer herstellung
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