KR950704234A - 아미노메틸인단, -벤조푸란 및 -벤조티오펜(aminomethylindans, -benzofuranes and -benzothiophenes) - Google Patents

아미노메틸인단, -벤조푸란 및 -벤조티오펜(aminomethylindans, -benzofuranes and -benzothiophenes)

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KR950704234A
KR950704234A KR1019950702357A KR19950702357A KR950704234A KR 950704234 A KR950704234 A KR 950704234A KR 1019950702357 A KR1019950702357 A KR 1019950702357A KR 19950702357 A KR19950702357 A KR 19950702357A KR 950704234 A KR950704234 A KR 950704234A
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lower alkyl
hydrogen
cycloalk
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크리스티안 페리가르트 옌스
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존 메이달 피터센
하.룬트베크 아크티에 셀스카브
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Abstract

일반식(I):
상기식에서 X 및 Y중 하나는 CH2이고, 다른 하나는 CH2, O 또는 S이고；R1은 지방족 탄화수소기, 아릴알킬, 아실, 술포닐기, 카르보네이트기 또는 R11R12NCO-(식중 R11및 R12는 수소 및 탄화수소기로부터 선택된다)이고；R2은 수소 또는 탄화수소기이고；R3내지 R5는 독립적으로 수소, 할로겐, 알킬, 알콕시, 알킬티오, 히드록시, 알킬술포닐, 시아노, 트리플루오로메틸, 시클로알킬, 시클로알킬알킬, 또는 니트로로부터 선택되며；R6및 R7은 각각 수소 또는 저급알킬이거나 함께 결합하여 탄소환 고리를 구성하며；R8및 R9은 독립적으로 수소, 탄화수소기 또는
(식중 R13은 수소 또는 탄화수소기이고, W는 O 또는 S이고 r은 2 내지 6이다)이다]을 갖는 화합물은 중심 5-HT1A리셉터에서 효능을 가지며 정신병, 불안장애, 우울, 충동제어 장애, 알코올중독, 공격성, 빈혈증, 종래 항정신성 약계 의해 유발되는 부작용 또는 심장 혈관장애의 치료에 유용하다.

Description

아미노메틸인단, -벤조푸란 및 -벤조티오펜(AMINOMETHYLINDANS, -BENZOFURANES AND -BENZOTHIOPHENES)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 다음 일반식 Ⅰ을 가진 화합물과 그것의 약학적으로 허용가능한 산부가염：
    상기식에서 X 및 Y중 하나는 CH2이고, 다른 하나는 CH2, O 및 S로 이루어진 군으로부터 선택되며；R1은 저급알킬, 저급 알켄일, 저급 알킨일, 시클로알크(엔)일, 시클로알크(엔)일-저급 알크(엔/인)일, 아릴-저급 알킬, 아실, 저급-알킬술포닐, 트리플루오로메틸술포닐, 아릴술포닐, R10ZCO-(식중 Z는 O 또는 S이고 R10은 알킬, 알켄일, 알킨일, 시클로알크(엔)일, 시클로알크(엔)일 알킬, 또는 알릴이다.) 또는 R11R12NCO-(식중 R11및 R12는 독립적으로 수소, 알킬, 알켄일, 알킨일, 시클로알크(엔)일, 시클로알크(엔)일 알크(엔/인)일, 또는 아릴이다.)로 이루어진 군으로부터 선택되며：R2는 수소, 저급알킬, 저급 알켄일, 저급 알킨일, 시클로알크(엔)일, 시클로알크(엔)일-저급 알크(엔/인)일, 아릴-저급 알킬로 이루어진 군으로부터 선택되며：R3내지 R5는 독립적으로 수소, 할로겐, 저급 알킬, 저급 알콕시, 아실, 저급 알킬티오, 히드록시, 저급 알킬술포닐, 시아노, 트리플루오로메틸, 시클로알킬, 시클로알킬알킬 또는 니트로로 이루어진 군으로부터 선택되며：R6및 R7은 각각 수소 또는 저급 알킬이거나 함께 결합하여 3-7-원 탄소환 고리를 구성하며：R8및 R9은 독립적으로 수소, 알킬, 알켄일, 알킨일, 시클로알크(엔)일, 시클로알크(엔)일, 시클로알크(엔)일-알크(엔/인)일, 아릴알킬 또는 다음 기
    (식중 R13은 수소, 저급알킬, 저급알켄일, 저급알킨일, 시클로알크(엔)일, 시클로알크(엔)일-저급 알크(엔/인)일, 아릴-저급 알킬 또는 아릴이고, W는 O 또는 S이고 r은 2 내지 6이다)이며；또는 R8및 R9는 함께 결합하여 한개의 질소원자를 함유하는 3-7원 고리를 형성하며；어떤 알킬, 시클로알킬 또는 시클로알킬알킬기는 한개 또는 두개의 히드록시기와 선택적으로 치환되고 다시 지방족 또는 방향족 카르복실 산으로 선택적으로 에스테르화 되어 있으며；그리고 어떤 아릴치환기는 할로겐, 저급알킬, 저급알콕시, 저급 알킬티오, 히드록시, 저급 알킬술포닐, 시아노, 트리플루오로메틸, 시클로알킬, 시클로알킬알킬 또는 니트로와 선택적으로 치환되어 있다.
  2. 제1항에 있어서, X는 CH2, O 또는 S이고 Y는 CH2인 것을 특징으로 하는 화합물.
  3. 제1항에 있어서, R1은 아릴-저급알킬기, 아실기, 저급 알킬술포닐기 또는 R11R12N-CO-기(식중 R11은 수소 또는 저급 알킬이고 R12는 수소, 알킬, 아릴 또는 시클로알킬이다.)이고 R2는 수소 또는 저급 알킬인 것을 특징으로 하는 화합물.
  4. 제3항에 있어서, R1은 벤질 또는 치환 벤질, 포르밀, 알킬카르보닐, 아릴카르보닐 또는 R11R2N-CO-기(식중 R11은 수소 또는 저급 알킬이고 R12는 수소, 저급 알킬, 페닐, 치환페닐, 또는 C5-6시클로알킬이다.)인 것을 특징으로 하는 화합물.
  5. 제1항 내지 제4항중 어느 한 항에 있어서, R3, R4및 R5는 수소 또는 할로겐이고 R6및 R7은 모두 수소인 것을 특징으로 하는 화합물.
  6. 제1항에 있어서, R8은 수소 또는 저급 알킬이고 R는 저급알킬, 아릴-저급알킬, 시클로알킬-저급알킬 또는 W가 0이고 R13이 수소, 저급알킬, 시클로알킬 또는 아릴인, 제1항에 정의된 바와같은 식 1a의 기이고, 또는 R8와 R9은 결합하여 한개의 질소 원자를 함유하는 3-7원 고리를 형성하는 것을 특징으로 하는 화합물.
  7. 제6항에 있어서, R9은 페닐-저급알킬, 치환페닐-저급알킬, 인돌일-저급알킬, 시클로헥실-저급알킬 또는 W가 0이고 R13이 수소, 저급알킬, 시클로알킬, 페닐 또는 치환페닐기인 식 1a의 기이고, 또는 R8와 R9은 결합하여 피롤리딘 또는 피페리딘 고리를 형성하는 것을 특징으로 하는 화합물.
  8. 치료학적으로 효과적인 양으로 및 하나 이상의 약학적으로 허용가능한 담체 또는 희석액과 조합하여 제1항의 적어도 하나의 신규화합물 또는 그것의 약학적으로 허용 가능한 산부가염으로 이루어진 것을 특징으로 하는 약학적 조성물.
  9. 정신병, 불안장애, 우울, 충동제어장재, 알코올중독, 공격성, 빈혈증, 종래의 항정신병 약에 의해 유발되는 부작용 또는 심장혈관장애의 치료를 위한 약학적 제제의 제조에 있어서 제1항의 화합물 또는 그것의 약학적으로 허용가능한 산부가염의 사용.
  10. 정신병, 불안장애, 우울, 충동제어장애, 알코올중독, 공격성, 빈혈증, 종래의 항정신병 약에 의해 유발되는 부작용 또는 심장혈관 장애의 치료방법에 있어서, 제1항의 화합물 또는 그것의 약학적으로 허용가능한 산부가염을 치료학적으로 효과적인 양으로 그것을 필요로하는 사람에게 투여하는 것을 특징으로 하는 방법.
    ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
KR1019950702357A 1992-12-09 1993-12-08 아미노메틸인단, -벤조푸란 및 -벤조티오펜 KR100357976B1 (ko)

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