KR950701323A - 1-피페라지노-1,2-디히드로인덴 유도체(1-Piperazino-1,2-dihydroindene Derivatives) - Google Patents

1-피페라지노-1,2-디히드로인덴 유도체(1-Piperazino-1,2-dihydroindene Derivatives)

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KR950701323A
KR950701323A KR1019940703815A KR19940703815A KR950701323A KR 950701323 A KR950701323 A KR 950701323A KR 1019940703815 A KR1019940703815 A KR 1019940703815A KR 19940703815 A KR19940703815 A KR 19940703815A KR 950701323 A KR950701323 A KR 950701323A
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뵈게소 클라우스
브레그네달 피터
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존 메이달 피터센
하.룬트베크 아크티에 셀스카브
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Abstract

일반식 Ⅰ
(상기식에서 X 및 Y는 수소, 할로겐, 트리플루오로메틸, 알킬, 알킬티오, 트리플루오로메틸티오, 알콕시, 히드록시, 알킬술포닐, 아미노, 알킬아미노, 니트로 또는 시아노이며; Ar은 각각 임의적으로 치환된 페닐, 티에닐 또는 푸릴기이며; R1은 수소, 또는 임의적으로 히드록시 치환된 알킬, 알케닐, 시클로알킬 또는 시클로 알킬알킬이며, R2는 알킬, 알케닐, 또는 시클로알킬알킬이거나; 또는 R1과 R2는 함께 피페라진고리와 융합된 5 내지 7원 헤테로환 고리를 형성하는데, 이 고리는 히드록시로치환될 수도 있으며; R3는 수소, 알킬, 알케닐, 시클로알킬 또는 시클로알킬알킬이거나; 또는 R2와 R3는 함께 피페라진고리에 스피로 융합된 3 내지 7원 탄소환 고리를 형성하며; R4는 수소 또는 알킬이다)을 갖는 1-피페라지노-1, 2-디히드로인덴화합물의 트랜스 이성질체는 도파민 D1리셉터에 대한 효능 있는 길항제 작용을 갖는다. 화합물은 중후신경계의 질환, 특히 정신병, 정신분열병(네거티브증상 뿐만아니라 포지티브증상), 불안, 억울증, 수면장해, 편두통, 파킨슨 증후군 또는 코카인 남용의 치료에 유용하다.

Description

1-피페라지노-1,2-디히드로인덴 유도체(1-Piperazino-1,2-dihydroindene Derivatives)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 일반식 Ⅰ을 갖는 1-피페라지노-1,2-디히드로인덴화합물의 트랜스 이성질체, 그것에 대한 프로드럭 및 약학적으로 허용되는 그것의 산부가염.
    상기식에서 X 및 Y는 독립적으로 수소, 할로겐, 트리플루오로메틸, 저급알킬, 저급알킬티오, 트리플루오로메틸티오, 저급알콕시, 히드록시, 저급알킬술포닐, 아미노, 저급알킬아미노, 저급디알킬아미노, 니트로 및 시아노로부터 선택되며, Ar은 페닐기, 그리고 할로겐, 트리플루오로메틸, 히드록시, 저급알콕시 및 저급알킬로 이루어지는 군으로부터 선택된 하나 이상의 치환기로 치환된 페닐기이거나, 또는 Ar은 티에닐기, 푸릴기 또는 할로겐 또는 저급알킬로 치환된 티에닐 또는 푸릴기이며, R1은 수소, 각각 하나 또는 두 개의 히드록시기로 임의적으로 치환된 저급알킬, 저급 알케닐, 시클로알킬 또는 시클로알킬알킬이며, R2는 저급알킬, 저급알케닐, 시클로알킬 또는 시클로알킬알킬이거나, 또는 R1과 R2가 그것들이 붙어 있는 각각 질소 및 탄소원자와 함께 피페라진 고리와 융합된 5 내지 7원 헤테로환 고리를 형성하는데, 이 헤테로환 고리는 임의적으로 히드록시로 치환될 수도 있으며, R3는 수소, 저급알킬, 저급알케닐, 시클로알킬 또는 시클로알킬알킬이거나, 또는 R2와 R3가 그것들이 붙어 있는 탄소원자와 함께 피페라진 고리에 스피로 융합된 3 내지 7원 탄소환 고리를 형성하며, R4는 수소 또는 저급 알킬이며, 단, R1과 R2가 함께 고리를 형성할때는 R2와 R3는 고리를 형성하지 않는다.
  2. 제1항에 있어서, X가 수소, 할로겐, 저급알킬 또는 트리플루오로메틸이며, Y가 수소 또는 할로겐이며, Ar이 페닐, 할로겐으로 치환된 페닐, 또는 티에닐이며, R1이 수소, 저급알킬, 또는 히드록시로 치환된 저급알킬이며, R2는 저급알킬이거나, 또는 R1과 R2가 그것들이 붙어 있는 각각 질소 및 탄소원자와 함께 피페라진고리와 융합된 피페리디노고리를 형성하는데, 이 피페리디노고리는 임의적으로 히드록시로 치환될 수도 있으며, R3가 수소 또는 저급알킬이거나, 또는 R2와 R3가 그것들이 붙어 있는 탄소원자와 함께 스피로시클로알킬고리를 형성하며, R4가 수소 또는 메틸인 것을 특징으로 하는 화합물.
  3. 제1항에 있어서, X가 수소, 클로로, 브로모, 플루오로원자, 메틸 또는 트리플루오로메틸이며, Y가 수소원자이며, Ar이 페닐, 플루오로페닐 또는 티에닐이며, R1이 수소, 메틸, 2-프로필, 히드록시프로필 또는 히드록시에틸이며, R2는 CH3, 에틸 또는 2-프로필이며 R3는 H, 에틸 또는 메틸이거나, 또는 R2와 R3가 그것들이 붙어 있는 탄소원자와 함께 스피로시클로부틸 또는 스피로시클로펜틸 고리를 형성하며, R4가 수소인 것을 특징으로 하는 화합물.
  4. 약학적으로 허용되는 담체 또는 희석제와 함께 제1항에 따르는 화합물 적어도 한가지로 이루어지는 것을 특징으로 하는 약학제제.
  5. 제4항에 있어서, 제1항에 따르는 화합물이 순수한 거울상체, 라세미체 또는 두 거울 상체의 어떤 다른 혼합물로서 존재하는 것을 특징으로 하는 약학제제.
  6. 치료학적 유효투여량의 제1항에 따르는 화합물을 적합한 담체 또는 희석제와 함께 그것을 필요로 하는 환자에 투여하는 단계로 이루어지는 정신병, 정신분열병(네거티브 증상 뿐만아니라 포지티브증상), 불안, 억울증, 수면장해, 편두통, 파킨슨 증후군 또는 코카인 남용의 치료를 위한 방법.
  7. 정신병, 정신분열병(네거티브 증상 뿐만아니라 포지티브증상), 불안, 억울증, 수면장해, 편두통, 파킨슨증후군 또는 코카인 남용의 치료를 위한 약학제제의 제조를 위한 제1항에 따르는 화합물의 사용.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940703815A 1992-04-28 1993-04-23 1-피페라지노-1, 2-디히드로인덴 유도체 KR100267635B1 (ko)

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DK92551A DK55192D0 (da) 1992-04-28 1992-04-28 1-piperazino-1,2-dihydroindenderivater
DK551/92 1992-04-28
DK0551/92 1992-04-28
PCT/DK1993/000136 WO1993022293A1 (en) 1992-04-28 1993-04-23 1-piperazino-1,2-dihydroindene derivatives

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KR950701323A true KR950701323A (ko) 1995-03-23
KR100267635B1 KR100267635B1 (ko) 2000-11-01

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PT638073E (pt) 2000-11-30
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