KR930000518A - 메타노 교량 결합된 퀴놀리진의 아미드 동족체 유도체 - Google Patents

메타노 교량 결합된 퀴놀리진의 아미드 동족체 유도체 Download PDF

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KR930000518A
KR930000518A KR1019920010016A KR920010016A KR930000518A KR 930000518 A KR930000518 A KR 930000518A KR 1019920010016 A KR1019920010016 A KR 1019920010016A KR 920010016 A KR920010016 A KR 920010016A KR 930000518 A KR930000518 A KR 930000518A
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워드 기토스 모리스
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스티븐 엘. 네스비트
메텔 다우 파마슈티칼스 인크.
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Abstract

내용 없음

Description

메타노 교량 결합된 퀴놀리진의 아미드 동족체 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(Ⅰ)의 화합물, 그의 수화물, 호변이성체, 입체이성체, 기하 이성체 및 그의 제약상 허용되는 산부가염 및 4급 암모늄염.
    상기식에서, A는 =H2, =O, =(H)(OH), =NOR1, 또는(여기에서, n은 2 또는 3이고, X 및 Y는 0또는 S임)이고, 각각의 R1은 독립적으로 H 또는 C1-4알킬이며, R2는 H, 할로게노, C1-4알킬, C1-4알콕시, C3-6시클로알킬메톡시, OH, -CN 또는 C(O)NH2이고, Z는 O,S 또는 NR1이며, Q는 하기 일반식의 헤테로사이클릭 또는 카르보사이클릭 잔기이다.
  2. 제1항에 있어서, Q가 잔기(c)인 화합물.
  3. 제1항에 있어서, Q가 잔기(c)인 화합물.
  4. 제1항에 있어서, 잔기 Q가 (a),(d)및 (1)로 이루어진 군의 잔기 중에서 선택되는 화합물.
  5. 제1항에 있어서, 잔기(e)가 위치 3에서 두개의 R1치환체들을 갖는 화합물.
  6. 제1항에 있어서, A가 =NOR1[여기에서 R1은 H, =O, =(H)(OH) 또는(여기에서, X 및 Y는 각각 0이고, n은 Z임)]으로 이루어진 군중에서 선택된 화합물.
  7. 제1항에 있어서, (Z-트랜스)-1-메틸-N-(옥타하이드로-3-하이드록시이미노-2,6-메타노-2H-퀴놀리진-8-일)-1H-인다졸-3-카르복스아미드; 트랜스-2,3-디하이드로-3,3-디메틸-N-[옥타하이드로스피로[(1,3)-디옥솔란-2,3'-(2,6)-메타노-2'H-퀴놀리진]-8'-일]-1H-인돌-1-카르복스아미드; (E-트랜스)-1-메틸-N-(옥타하이드로-3-하이드록시이미노-2,6-메타노-2H-쾨놀리진-8-일)-1H-인다졸-3-카르복스아미드; 트랜스-5-클로로-2,3-디하이드로-2,2-디메틸-N-[옥타하이드로스피로-[1,3-디옥솔란-2,3'-(2,6)-메타노-2'H-퀴놀리진]-8'-일]-7-벤조푸란카르복스아미드; 트랜스-2,3-디하이드로-3,3-디메틸-N-(옥타하이드로-3-옥소-2,6-메타노-2H-퀴놀리진-8-일)-1H-인돌-1-카르복스아미드; 트랜스-1-메틸-N-(옥타하이드로-3-옥소-2,6-메타노-2H-키놀리진-8-일)-1H-인디롤-3-카르복스아미드; 트랜스-N-(옥타하이드로-3-하이드록시-2,6-메타노-2H-퀴놀리진-8-일)-1H-인돌-3-카르복스아미드; 시스-1-메틸-N-(옥타하이드로-3-옥소-2,6-메타노-2H-퀴놀리진-8-일)-1H-인다졸-3-카르복스아미드; 트랜스-5-클로로-2,3-디하이드로-2,2-디메틸-N-(옥타하이드로-3-옥소-2,6-메타노-2H-퀴놀리진-8-일)-7-벤조푸란카르복스아미드; 트랜스-5-클로로-2,3-디하이드로-N-(옥타하이드로-3-하이드록시-2,6-메타노-2H-퀴놀리진-8-일)-7-벤조푸란카르복스아미드; 시스-1-메틸-N-(옥타하이드로-3-하이드록시-2,6-메타노-2H-퀴놀리진-8-일)-1H-인다졸-3-카르복스아미드; (-)및 (+)-트랜스-5-클로로-2,3-디하이드로-2,2-디메틸-N-(옥타하이드로-3-하이드록시-2,6-메타노-2H-퀴놀리진-8-일)-7-벤조푸란카르복스아미드; 및 (+)-트랜스-1-메틸-N-(옥타하이드로-3-하이드록시-2,6-메타노-2H-퀴놀리진-8-일)-1H-인다졸-3-카르복스아미드로 이루어진 군 중에서 선택된 화합물.
  8. 하기 일반식의 화합물.
    상기식에서, A'는 =H2또는 -X-(CH2)2-Y -X-(CH2)3-Y (여기에서, X 및 Y는 O또는 S임)이다.
  9. 하기 일반식(6)의 디아민 또는 그의 반응성 유도체를 일반식 QCOOH의 산의 반응성 등가물과 반응시키고, 임의로 반응시에 적합한 보호기를 사용하여 Q의 적합한 잔기를 보호하고, 이 반응에 이어서 임의로 보호기를 제거하는 것을 특징으로 하는, 일반식(Ⅰ)의 화합물의 제조 방법.
    상기 식들에서 A는 =H2, =O, =(H)(OH), =NOR1또는(여기에서, n은 2 또는 3이고, X 및 Y는 O 또는 S임)이고, A'은 =H2또는 "-X-(CH2)2-Y 또는 -X(CH2)3-Y (여기에서, X 및 Y는 상기 정의한 바와 같음)이며, 각각의 R1은 독립적으로 H 또는 C1-4알킬이고, R2는 H, 할로게노, C1-4알킬, C1-4알콕시, C3-6시클로알킬메톡시, OH, -CN 또는 C(O)NH2이며, Z는 O,S 또는 NR1이고 Q는 하기 일반식의 헤테로사이클릭 또는 카르보사이클릭 잔기이다.
  10. 제1항에 따른 화합물 및 제약상 허용되는 담체로 이루어지는, 화학 요법상 유반되는 구역질 및 구토, 편두통, 부정맥, 인식 장애, 정신 분열증, 광중, 녹내장, 위 운동성, 약물 중독증, 수면 질식증 또는 급성 설사중의 치료를 위한 제약 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920010016A 1991-06-11 1992-06-10 메타노교량 결합된 퀴놀리진의 아미드 동족체 유도체 KR100234926B1 (ko)

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EP91401550A EP0517984A1 (en) 1991-06-11 1991-06-11 Derivatives of amide analogs of certain methano bridged quinolizines

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EP0518767A3 (en) 1993-05-05
HUT61549A (en) 1993-01-28
HU212735B (en) 1996-10-28
JPH05202044A (ja) 1993-08-10
EP0518767B1 (en) 2002-03-13
AU649836B2 (en) 1994-06-02
DK0518767T3 (da) 2002-07-01
KR100234926B1 (ko) 1999-12-15
PT518767E (pt) 2002-09-30
ES2173863T3 (es) 2002-11-01
FI112866B (fi) 2004-01-30
FI922695A0 (fi) 1992-06-10
EP0517984A1 (en) 1992-12-16
EP0518767A2 (en) 1992-12-16
DE69232473T2 (de) 2002-11-21
IL102132A (en) 1996-10-31
FI922695A (fi) 1992-12-12

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