KR950704294A - 축합 벤조화합물(fused benzo compounds) - Google Patents

축합 벤조화합물(fused benzo compounds)

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KR950704294A
KR950704294A KR1019950702356A KR19950702356A KR950704294A KR 950704294 A KR950704294 A KR 950704294A KR 1019950702356 A KR1019950702356 A KR 1019950702356A KR 19950702356 A KR19950702356 A KR 19950702356A KR 950704294 A KR950704294 A KR 950704294A
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케이. 몰첸 에이너
크리스티안 페리가르트 옌스
페데르센 헨리크
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존 메이달 피터센
하.룬크베크 아크티에 셀스카브
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Abstract

다음 식(I)의 축합 벤조화합물은 CNS칠환의 치료에 유용한 5-HT1A수용테 리간드이다.
이 화합물을 포함하는 약학적 조성물 및 그것의 약학적 제제의 제조를 위한 사용도 또한 개시되어 있다.
〔상기 식에서 A는 2내지 6원 탄화수소 스페이서기이고; B는 SO, SO2및 기(a)중에서 선택된 극성2가 기이고; U는 C,N 또는 CH이고; X는 한개 이상의 헤테로 원자를 임의로 포함하는 2가 3-4원 사슬이고; R1은 지방족 탄화수소기, 아릴알킬 또는 디페닐알킬이고; R2및 R3은 수소 또는 알킬이거나 또는 함께 에틸렌 또는 프로필렌다리를 형성하고; R4, R5및 R6은 수소 또는 치환기이고; R7및 R8은 수소 또는 기-COOR9및 -CONR10R11을 포함하는 치환기이다.〕

Description

축합 벤조화합물(FUSED BENZO COMPOUNDS)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 다음 일반식I의 화합물인 것을 특징으로 하는 축합 벤조화합물 및 그것의 약학적으로 허용되는 산부가염.
    〔상기 식에서 A는 각각 분지쇄 또는 직쇄일 수 있는 알킬렌, 알켄일렌 및 알킨일렌 중에서 선택되며 아릴 또는 히드록시로 임의로 치환된 2 내지 6원 스페이서기, 또는 3-7원 시클로알킬렌기이고, B는 SO, SO2및 식II
    의 기 중에서 선택된 극성2가 기이며, 이때 식II에서 W는 O또는 S이고 Z는 -(CH2)n-(n는 2또는 3이다), -CH=CH-, -COCH2-, -CSCH2-, 또는 할로겐 또는 트리플루오로메틸로 임의로 치환된 1,2-페닐렌이고, U는 N또는 CH이고 점선은 임의의 결합을 나타내는데, 만일 점선이 결합을 나타낸다면 U는 C이고, X는
    (여기서 점선은 임의의 결합을 나타낸다)으로 구성되는 2가 3-4원 기의 군에서 선택되어, 벤젠고리와 축합된 탄소환 또는 헤테로환 고리를 형성하고, R1은 알킬, 알케닐, 시클로알크(엔)일, 아릴, 시클로알크(엔)일알크(엔/인)일, 아릴알킬, 디페닐알킬인데, 알킬리는 어느 것이들 한개 또는 두개의 히드록시기로 임의로 치환되며, 단 Z가 1,2-페닐렌이고 U가 N이면 R1은 아릴 및 치환아릴 중에서 선택되고, R2및 R3은 독립적으로 수소, 저급 알킬이거나 또는 함께 결합되어 에틸렌 또는 프로필렌 다리를 형성할 수 있고, R4,R5및 R6은 독립적으로 수소, 할로겐, 저급알킬, 저급알콕시, 히드록시, 저급알킬티오, 저급알킬아미노 또는 디-저급-알킬아미노, 시아노, 니트로, 트리플루오로메틸 및 트리플루오로메틸티오로 구성되는 군에서 선택되고, R7및 R8은 독립적으로 수소, 할로겐, 트리플루오로메틸, 저급알킬, 한개 이상의 히드록시로 치환된 저급알킬, 아릴, 시아노, 기-COOR9및 기-XONR10R11(R9, R10및 R11은 수소 또는 저급알킬이다)로 구성되는 군에서 선택되는데, 존재하는 아릴기는 어느 것이든 할로겐, 저급알킬, 저급알콕시, 히드록시, 저급알킬티오, 저급알킬술포닐, 저급알킬 또는 디알킬아미노, 시아노, 트리플루오로메닐 또는 트리플루오로메틸티오 중에서 선택된 한개 이상의 치환기로 임의로 치환된다.〕
  2. 제1항에 있어서, A가 2 내지 6원 알킬렌기인 것을 특징으로 하는 화합물.
  3. 제1항에 있어서, B가 SO, SO2및 또는 제1항에 정의한 바와 같은 식II의 기이고 이때 식II에서 W는 O이고 Z는 -(CH2)n-(n는 2또는 3이다), -CH=CH-, 및 할로겐 또는 트리플루오로메틸로 임의로 치환된 1,2-페닐렌 중에서 선택되는 것을 특징으로 하는 화합물.
  4. 제1항에 있어서, X가
    으로 구성되는 2가 3-4원 기의 군에서 선택되는 것을 특징으로 하는 화합물.
  5. 제1항에 있어서, R1이 저급 알킬, 아릴, 시클로알킬 또는 아릴-저급알킬인 것을 특징으로 하는 화합물.
  6. 제5항에 있어서, R1이 저급 알킬, 제1항에 정의한 바와 같은 치환기중의 한개로 치환된 페닐, C5-C6시클로알킬, 아다만틸, 제1항에 정의한 바와 같은 치환기중의 한개로 임의로 치환된 페닐-저급 알킬 또는 나프틸인 것을 특징으로 하는 화합물.
  7. 제1항에 있어서, R2및 R3이 둘다 수소인 것을 특징으로 하는 화합물.
  8. 제1항에 있어서, R4,R5및 R6이 각각 수소 및 할로겐으로 구성되는 군에서 선택되는 것을 특징으로 하는 화합물.
  9. 제1항에 있어서, R7및 R8이 독립적으로 수소, 저급 알킬, 아릴, 기-COOR9(R9는 수소 또는 저급 알킬이다)및 기-CONH2로 구성되는 군에서 선택되는 것을 특징으로 하는 화합물.
  10. 제9항에 있어서, R7및 R8이 독립적으로 수소, 저급 알킬, 제1항에 정의한 바와 같은 치환기중의 한개로 임의로 치환된 페닐, 기-COOR9(R9는 수소 또는 저급 알킬이다)및 기-CONH2로 구성되는 군에서 선택되는 것을 특징으로 하는 화합물.
  11. 제1항 내지 제10중의 어느 한 항에 따른 적어도 하나의 신규의 축합 벤조유도체 또는 그것의 약학적으로 허용되는 산부가염을 치료 유효량으로 그리고 하나 이상의 약학적으로 허용되는 담체 또는 희석제와 조합하여 포함하는 것을 특징으로 하는 약학적 조성물.
  12. 불안증, 울병, 정신병, 욕망억제장애, 알코올남용, 고혈압증, 심장혈관질환, 종래의 항정신병약에 의해 유발되는 부장용 및 노인성 치매의 치료를 위한 약학적 제제의 제조를 위한 제1항에 따른 축합 벤조유도체 또는 그것의 산부가염의 사용.
    ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
KR1019950702356A 1992-12-09 1993-12-08 축합벤조화합물 KR100299624B1 (ko)

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PCT/DK1993/000414 WO1994013659A1 (en) 1992-12-09 1993-12-08 Fused benzo compounds

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DK148392D0 (da) 1992-12-09
RU2141959C1 (ru) 1999-11-27
NO952275L (no) 1995-08-03
FI109697B (fi) 2002-09-30
EP0673375A1 (en) 1995-09-27
GR3030200T3 (en) 1999-08-31
NO952275D0 (no) 1995-06-08
ES2127912T3 (es) 1999-05-01
HUT73632A (en) 1996-08-28
JPH08504410A (ja) 1996-05-14
ATE176909T1 (de) 1999-03-15
DE69323630D1 (de) 1999-04-01
KR100299624B1 (ko) 2001-11-05
IL107923A (en) 1999-08-17
AU5561894A (en) 1994-07-04
DE69323630T2 (de) 1999-10-14
EP0673375B1 (en) 1999-02-24
ZA939203B (en) 1994-08-08
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US6140331A (en) 2000-10-31
SK280779B6 (sk) 2000-07-11
FI952824A (fi) 1995-06-08
CA2151378A1 (en) 1994-06-23
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IL107923A0 (en) 1994-04-12
CZ151795A3 (en) 1996-01-17
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NZ258117A (en) 1996-08-27
AU675263B2 (en) 1997-01-30
MX9307779A (es) 1994-06-30
CZ283143B6 (cs) 1998-01-14
HU9501668D0 (en) 1995-08-28
NO311617B1 (no) 2001-12-17
RU95117096A (ru) 1997-06-10
FI952824A0 (fi) 1995-06-08
SG52722A1 (en) 1998-09-28

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