KR900004680A - 사이클로알킬-치환된 글루타르아미드 고혈압 치료제 - Google Patents

사이클로알킬-치환된 글루타르아미드 고혈압 치료제 Download PDF

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KR900004680A
KR900004680A KR1019890012735A KR890012735A KR900004680A KR 900004680 A KR900004680 A KR 900004680A KR 1019890012735 A KR1019890012735 A KR 1019890012735A KR 890012735 A KR890012735 A KR 890012735A KR 900004680 A KR900004680 A KR 900004680A
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크리스토퍼 데나일윅츠 존
쥬릭 코바일리키 리스자드
제임스 케이트
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데이비드 존 우드
화이자 인코포레이티드
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Abstract

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Description

사이클로알킬-치환된 글루타르아미드 고혈압 치료제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
    상기식에서 A는 포화되거나 단일불포화될 수 있는 5 또는 6원 카보사이클릭환을 나타내고; R1은 H 또는 (C1-C4) 알킬이며; R 및 R4는 각각 H, (C1-C6)알킬, (C3-C7) 사이클로알킬, 벤질 또는 생물학적으로 불안정한 에스케르-형성 그룹이고; Y는 직접결합이거나 탄소수 1 내지 6의 직쇄 또는 측쇄 알킬렌그룹이며; R2는 H, 아릴, 헤테로사이클릴, R6CONR5-, R7NR5CO-, R7NR5SO2- 또는 R8SO2NR5- 그룹이고, 단 R2가 H, 아릴 또는 헤테로사이클리일 경우, Y는 직접 결함이 아니며; R5는 H, (C1-C6)알킬 또는 아릴 (C1-C6)알킬 또는 일반식의 그룹이며; R9는 H, OH, (C1-C6)알콕시, (C1-C6)알킬, 하이드록시 (C1-C6)알킬, 아릴 (C1-C6)알킬, (C2-C6)알케닐, 헤테로사이클릴, 헤테로사이클릴 (C1-C6)알킬, R12CONH-, R12SO2NH-, 또는 (R13)2N-이고; R10및 R11은 각각 H 또는 (C1-C6)알킬이거나, R10이 H이고 R11이 아미노 (C1-C6)알킬, 이미다졸릴메틸, 아릴, 아릴 (C1-C6)알킬, 아릴 (C1-C6) 알콕 (C1-C6)알콕시, 하이드록시(C1-C6)알킬 또는 메틸티오 (C1-C6) 알킬이거나, 결합된 탄소원자와 함께 두 그룹 R10및 R11은 3 내지 6원 카보사이클릭환 또는, 아미노, (C2-C4) 알카노일 또는 아로일에 의해 임의로 치환될 수 있는 피롤리딘 또는 피페리딘환을 형성하며; R12는 (C1-C6)알킬, (C3-C7)사이클로알킬, 아릴, 아릴(C1-C6)알킬, 헤테로사이클릴 또는 헤테로사이클릴 (C1-C6)알킬이고; R13은 각각 H, (C1-C6)알킬 또는 아릴 (C1-C6) 알킬이거나, 결합된 질소원자와 함께 두개의 R13그룹은 피롤리디닐, 피페리디노, 모르폴리노, 피레라지닐 또는 N-(C1-C4)알킬 피페라지닐 그룹을 형성하며; R7은 (C1-C6)알킬, 아릴, 아릴 (C1-C6)알킬, 헤테로사이클릴, 헤테로사이클릴 (C1-C6)알킬 이고; R6은 (C1-C6)알킬, 아릴, 아릴(C1-C6)알킬, 헤테로사이클릴, 헤테로사이클릴 (C1-C6)알킬 또는 일반식의 그룹이며; (여기서, R10및 R11은 상기 정의한 바와 같다)의 그룹이고; R14는 (R13)2NCO-, R13OCH2- 또는 R15OCO-(여기서, R12및 R13은 상기 정의한 바와 같다)이며; R15는 (C1-C6)알킬, (C3-C7)사이클로알킬 또는 아릴 (C1-C6)알킬이고; R8은 (C1-C6)알킬, 아릴, 아릴(C1-C6)알킬, 헤테로사이클릴 또는 헤테로 사이클릴(C1-C6)알킬이며; R3은 일반식의 그룹이거나, 일반식
    그룹[여기서, 이룹들은 융합된 벤젠환에서 (C1-C4)알킬, (C1-C4)알콕시, OH, 할로 또는 CF3에 의해 임의로 치환될 수 있다]이고; R16은 H, 할로, 4-OH, 4-(C1-C6알콕시), 4-(C3-C7사이클로알콕시), 4-(C2-C6알케닐옥시) 4-[((C1-C6알콕시) 카보닐옥시], 4-[(C3-C7사이클로 알콕시) 카보닐옥시] 또는 3-(C1-C4알킬) SO2NH-이며; R20은 H, (C1-C4)알킬, (C1-C4)알콕시, (C2-C6)알카노일 또는 할로이다.
  2. 제1항에 있어서, A가 (CH2)4이고 R1이 H인 일반식(Ⅱ)의 화합물 및 약제학적으로 허용되는 이의 생물학적 전구체.
    상기식에서,R,R2,R3,R4및 Y는 제1항에서 정의한 바와 같다.
  3. 제1항 또는 2항에 있어서, R 및 R4중 하나가 생물학적으로 불안정한 에스케르-형성 그룹인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  4. 제3항에 있어서, 생물학적으로 불안정한 에스테르-형성그룹이 에틸, 인다닐, 이소프로필, M-부틸, 2급-부틸, 3급-부틸, 사이클로헥실, 벤질, 펜에틸, 페프로필, 아세토닐, 글리세릴, 피발로일옥시메틸, 5-(4-메틸-1,3-디옥솔렌-2-오닐)메틸, 사이클로헥실메틸, 사이클로헥실카복시에틸, 사이클로헥실 아세톡시에틸, 프로피오닐옥시이소부틸, 헥사노일옥시에틸, 펜타노일옥시에틸, 아세톡시에틸, 아세톡시벤질, 펜타노일옥시벤질, 사이클로헥실옥시카보닐옥시에틸, 부틸옥시카보닐옥시에틸, 이소부틸옥시카보닐에틸 및 에톡시카보닐옥시에틸 중에서 선택되는 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  5. 제4항에 있어서, 생물학적으로 불안정한 에스케르 그룹이 피발로일옥시메틸인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  6. 제1항 내지 5항중 어느 한 항에 있어서, R3이 4-하이드록시벤질, 4-메톡시벤질 또는 3-메탄설폰아미도벤질이며, R3이 결합되어 있는 탄소원자의 입체화학적 배열이 (S)인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  7. 제1항 내지 5항중 어느 한 항에 있어서, Y가 CH2인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  8. 제1항 내지 7항중 어느 한 항에 있어서, R2가 일반식 R6CONR5의 그룹인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  9. 제8항에 있어서, R6은 일반식 R9R10R11C-[여기서, R9는 일반식(R13)2N-, R12SO2NH- 또는 R12CONH-(여기서, R12및 R13은 제1항에서 정의한 바와 같다)의 그룹이며, R10은 아미노 (C1-C6)알킬이고, R11은 H이다]의 그룹인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  10. 제9항에 있어서, R6CO가 일반식 R9R10R11CO[여기서, R9는 NH2, R12CONH 또는 R12SO2NH(여기서, R12는 제1항에서 정의한 바와 같다)이며, R10은 4-아미노 부틸이고, R11은 H이다]의 (S)-리실 또는 N2-치환된 (S)-리실인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  11. 제10항에 있어서, R6CO가 (S)-리실, N2-메탄설포닐 -(S)-리실, N2-페닐설포닐-(S)-리실 또는 N2-아세틸-(S)-리실인 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적 전구체.
  12. 제1항에 있어서, N-[1-(2-(S)-카복시-3-(S)-리실아미노프로필)-1-사이클로-펜탄카보닐]-(S)-티로신, N-{1-[2(S)-카복시-3-(N2-메탄설포닐-(S)-리실아미노)프로필]-1-사이클로펜탄카보닐}-(S)-티로신, N-{1-[2(S)-카복시-3-(N2-2-푸로일-(S)-리실아미노)프로필]-1-1-사이클로펜탄카보닐}-(S)-티로신, N-{1-[2(S)-카복시-3-(N2-아세틸-(S)-리실아미노)프로필]-1-사이클로펜탄카보닐}-(S)-4-메톡시페닐알라닌, N-[1-(2-카복시-3-(S)-리실아미노프로필-1-사이클로펜탄카보닐]-3-메탄설포아미도페닐알라닌, N-{1-[2(S)-카복시-3-(N2-메탄설포닐-(S)-리실아미노)프로필]-1-사이클로펜탄카보닐}-3-메탄설폰아미도페닐알라닌, 및 N-{1-[2(S)-카복시-3-(N2-페닐설포닐-(S)-리실아미노)프로필]-1-사이클로펜탄 카보닐}-(S)-티로신중에서 선택된 화합물 및 약제학적으로 허용되는 이의 염, 및 이의 생물학적으로 불안정한 에스테르 유도체.
  13. 제1항 내지 12항중 어느 한 항에 청구된 일반식(Ⅰ) 또는 (Ⅱ)의 화합물 또는 약제학적으로 허용되는 이의 염, 또는 이의 생물학적 전구체를 약제학적으로 허용되는 희석제 또는 담체와 함께 함유함을 특징으로 하는 약제학적 조성물.
  14. 약제, 특히 고혈압, 심부전증 또는 신부전증을 치료하기 위한 약제로 사용하기 위한, 제1항 내지 12항중 어느 한 항에 청구된 일반식(Ⅰ) 또는 (Ⅱ)의 화합물 또는 약제학적으로 허용되는 이의 염, 또는 이의 생물학적 전구체.
  15. 고혈압, 심부전증 또는 신부전증을 치료하는 약제를 제조하기 위한, 제1항 내지 12항중 어느 한항에 청구된 일반식(Ⅰ) 또는 (Ⅱ)의 화합물 또는 약제학적으로 허용되는 이의 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890012735A 1988-09-05 1989-09-04 사이클로알킬-치환된 글루타르아미드 고혈압 치료제 KR920007230B1 (ko)

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