KR870006027A - 치환 피페라진-1,4-나프탈렌디온과 그 산부가염 및 그들의 제조방법 - Google Patents

치환 피페라진-1,4-나프탈렌디온과 그 산부가염 및 그들의 제조방법 Download PDF

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KR870006027A
KR870006027A KR860010896A KR860010896A KR870006027A KR 870006027 A KR870006027 A KR 870006027A KR 860010896 A KR860010896 A KR 860010896A KR 860010896 A KR860010896 A KR 860010896A KR 870006027 A KR870006027 A KR 870006027A
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piperazinyl
halogen
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브라이언 메드워드 제프리
웨인 토오리 로오런스
스티븐 톰커후시크 앤드루
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존 제이 헤이간
아메리칸 사이아나밋드 캄파니
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Abstract

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Description

치환 피페라진-1,4-나프탈렌디온과 그 산부가염 및 그들의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기의 일반식을 화합물들과 약리학적으로 허용되는 2 산부가염.
    여기에서 R1은 할로겐, 히드록시, 알킬(C1-C4), 알콕시(C1-C3), -NHCOCH3혹은 -N(COCH3)2; R2는 수소 혹은 알킬(C1-C4); R3및 R4는 개별적으로 알킬(C1-C3), 또는 함께 결합하여 -(CH2)n- (여기서, n은 2 또는 3의 정수); R5은 수소, 포밀, 아세틸, -COO 알킬(C1-C4), -COOCH2C(할로겐)3, -CO(CH2)7CH=CH(CH2)7CH3, -CON[알킬(C1-C3)]2, 페닐, 벤질, 2-, 3- 또는 4-피리디닐, 2-피리디미닐, 2-,3- 혹은 4-할로벤조일, 2-,3- 혹은 4-알킬-(C1-C6)벤조일. 일치환 페닐(여기서 치환체는 오토, 메타 혹은 파라가 될 것이며, 할로겐 및 트리플루오로메틸로 부터 선택될 것이다),
    일치환 페닐 카르복스아미드(여기서 치환체는 메타 혹은 파라의 위치이고, 할로겐과 트리플루오로메틸로부터 선택될 것이다),
  2. 제1항에 있어서, 화합물이 2-클로로-3-[4-(페닐메틸)-1-피페라지닐]-1, 4-나프탈렌디온, 2-클로로-3-[4-(2-퀴놀리닐)-1-피페라지닐]-1,4-나프탈렌디온, 히드로클로라이드 4-(3-클로로-1,4-디히드로-1,4-디옥소-2-나프탈레닐)-N-[3-(트리플루오로메틸)페닐]-1-피페라진 카르콕스아미드, N-[3-[3-[4-(2-벤조티아존일)-1-피페라지닐]-1,4-디히드로-1,4-디옥소-2-나프탈레닐]아세트 아미드 혹은 2-클로로-3-[4-(2-피리디닐)-1-피페라지닐]-1,4-프탈렌디온, 히드로클로라이드인 화합물.
  3. 제1항에 있어서, 화합물이 2-[[2-(2-벤조티아존일 메틸아미노) 에틸] 메틸아미노]-3-클로로-1,4-타프탈렌디온, 4-(1,4-디히드로-3-메틸-1,4-디옥소-2-나프탈레닐)-1-피페라진-카르복실산, 에틸 에스테르, 2-메틸-3-[4-(페닐 메틸)-1-피페라지닐]-1,4-나프탈렌디온, 2-메틸-3-[4-[3-(트리플루오로메틸)페닐]-1-피페라지닐]-1,4-나프탈렌디온 혹은 2-메틸-3-[4-(2-피리디닐)-1-피페라지닐]-1,4-나프탈렌디온인 화합물.
  4. 하기의 일반식의 화합물로 부터 선택되는 화합물 약 5mg-1500mg으로 구성되는 단위 용량 형태의 조성물,
    여기서 R1,R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
  5. 2,3-디클로로나프로퀴논을 다음 일반식(2)의 아민과 용매내에서 몇시간 환류시키면서 반응시키는 것으로 구성되는 하기 일반식(1)의 화합물들의 제조 방법.
    여기서 R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
    여기서 R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
  6. 2-아세틸아미노-3-클로로-1,4-나프로퀴논을 다음 일반식(4)의 아민과 용매 내에서 반응시키는 것으로 구성되는 하기 일반식(3)의 화합물들의 제조방법.
    여기서 R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
    여기서 R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
  7. 하기 일반식(6)의 화합물을 하기 일반식(7)의 페닐이 소시아네이트와 유기용매내에서 반응시키는 것으로 구성되는 하기 일반식(5)의 화합물의 제조 방법.
    여기서 R2은 수소 또는 알킬(C1-C4)이고; R3및 R4는 개별적으로 알킬(C1-C4)이거나, 함께 결합하여 -(CH2)n- (n은 2 또는 3인 정수)가 되고; X는 할로겐이거나 트리플루오로메틸이다.
    여기서 R2, R3및 R4는 전술한 바와 같다.
    여기서 X는 전술한 바와 같다.
  8. 하기 일반식(9)의 화합물과 일반식 ClCOY (10)의 염화 카르보닐을 유기용매내에서 반응시키는 것으로 구성되는 하기 알반식(8)의 화합물의 제조방법.
    여기서 R2는 수소 혹은 알킬(C1-C4);R3및 R4는 개별적으로 알킬(C1-C4)이거나, 혹은 함께 결합하여 -(CH2)n- (여기서 n은 2 또는 3의 정수)이 되고; Y는 0-알킬(C1-C6), 디메틸 아미노, 치환페닐[여기서 치환체는 할로겐 혹은 알킬(C1-C4)가 될 것이다], 0-벤질, -OCH2(할로겐)3또는 -(CH2)7CH=CH(CH)2)7CH3이다
    여기서 R2,R3및 R4는 전술한 바와 같다.
    (10) ClCOY
    여기서 Y는 전술한 바와 같다.
  9. 2,3-에폭시-2-메틸-1,4-나프로퀴논을 다음 일반식(12)의 아민과 유기용매내에서 반응시키는 것으로 구성되는 하기 일반식(11)의 화합물들과 약리학적으로 허용되는 그 산부 가염의 제조방법.
    여기서 R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
    여기서 R2,R3,R4및 R5는 전술한 바와 같다.
  10. 2,3-에폭시-2,3-디히드로-1,4-나프로퀴논을 다음 일반식(14)의 아민과 유기용매내에서 반응시키는 것으로 구성되는 하기 일반식(13)의 화합물들과 약리학적으로 허용되는 그 산부 가염의 제조방법.
    여기서 R2,R3,R4및 R5은 제1항에서 정의한 바와 같다.
    여기서 R2,R3,R4및 R5는 전술한 바와 같다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019860010896A 1985-12-19 1986-12-18 치환 피페라진-1,4-나프탈렌디온과 그 산부가염 및 그들의 제조방법. KR900001189B1 (ko)

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US06/811,122 US4686220A (en) 1985-12-19 1985-12-19 Substituted 2-[b-substituted-amino)-ethylamino]-1,4-naphthalenediones for treating asthma, allergic diseases and inflammation in warm-blooded animals

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US4882339A (en) * 1987-07-10 1989-11-21 Ciba-Geigy Corporation 4-Amino-substituted 1,2-dihydroxynaphthalene derivatives useful in inhibiting 5-lipoxygenase activity in mammals
US4808586A (en) * 1987-11-23 1989-02-28 American Cyanamid Company Substituted benzimidazoles and benzothidiazoles having anti-asthmatic and/or anti-inflammatory activities
FR2635105B1 (fr) * 1988-08-03 1991-01-25 Synthelabo Derives de piperazine et leur procede de preparation
AU5341699A (en) * 1998-08-06 2000-02-28 University Of Pittsburgh Antiproliferative naphthoquinones, derivatives, compositions, and uses thereof
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CA2433090A1 (en) * 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
KR101062376B1 (ko) 2008-04-10 2011-09-06 한국화학연구원 신규 인돌 카르복실산 비스피리딜 카르복사마이드 유도체,이의 제조방법 및 이를 유효성분으로 함유하는 조성물

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JPS5640651A (en) * 1979-09-12 1981-04-16 Takeda Chem Ind Ltd Quinone compound and its preparation
JPS58177934A (ja) * 1982-04-13 1983-10-18 Takeda Chem Ind Ltd ベンゾキノン誘導体
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HU198293B (en) 1989-09-28
KR900001189B1 (ko) 1990-02-27
NO166530C (no) 1991-08-14
CA1263650A (en) 1989-12-05
FI86060C (fi) 1992-07-10
NO865139D0 (no) 1986-12-18

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