KR960041168A - 베타-아드레날린 효능성 작용물질 - Google Patents

베타-아드레날린 효능성 작용물질 Download PDF

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KR960041168A
KR960041168A KR1019960015262A KR19960015262A KR960041168A KR 960041168 A KR960041168 A KR 960041168A KR 1019960015262 A KR1019960015262 A KR 1019960015262A KR 19960015262 A KR19960015262 A KR 19960015262A KR 960041168 A KR960041168 A KR 960041168A
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리 다우 로버트
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알렌 제이. 스피겔
화이자 인코포레이티드
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Abstract

본 발명은 비만증 및 당뇨병과 같은 질환/증상의 치료를 위한 β-아드레날린 효능성 작용물질에 관한 것이다. 화합물은 하기 일반식(Ⅰ)을 갖는다.
상기 식에서, R1, R2, R3, R4, R5, R6, R7, W, X, Y 및 Z는 명세서에 정의한 바와 같다.

Description

β-아드레날린 효능성 작용물질
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (21)

  1. 하기 일반식을 갖는 화합물, 상기 화합물의 약학적으로 허용가능한 약물 전구체 및 상기 화합물 및 상기 약물 전구체의 약학적으로 허용가능한 염:
    상기 식에서, R1, R2, R4및 R5는 독립적으로 수소 또는 (C1-C6)알킬이고; R3, R6 및 R7은 독립적으로 수소, 할로겐, (C1-C6)알킬, 니트로, 시아노, 트리플루오로메틸, SO2R8, SO2NR9R10, NR9R10, COR11, CO2R9, (C1-C6)알콕시, NR9SO2R8, NR9COR11, NR9CO2R9또는 OR9이고; R8은 독립적으로 (C1-C6)알킬 또는 (C1-C6)알콕시(C1-C6)알킬이고; R9및 R10은 독립적으로 수소, (C1-C6)알킬, (C3-C8)사이클로알킬 또는 (C1-C6)알콕시(C1-C6)알킬이고; R11은 독립적으로 수소, (C1-C6)알킬, NR9R10, (C3-C8)사이클로알킬 또는 (C1-C6)알콕시(C1-C6)알킬이고; W는 N 또는 CH이거나, 또는 R3가 W에 결합되는 경우에는 CR3(여기서, R3는 H 뿐아니라 R3에 대해 상기 나타낸 어떠한 정의일 수 있다)이고; X 및 Y는 독립적으로 직접 결합이거나, 산소, 황 또는 NR1이고(여기서, R1는 상기 정의된 바와 같다); Z는 (CH2)mOR9, (CH2)nCO2H, (CH2)nCOR11, (CH2)nSO2NR9R10, (CH2)n-NR9SO2R8, (CH2)nP(O)(OR1)(OR2), (CH2)n-O-(CH2)m-, CO2H, (CH2)nO-(CH2)mCOR11, (CH2)nO-(CH2)mP(O)(OR1)-(OR2), (CH2)nO-(CH2)mSO2NR9R10또는 (CH2)n-O-(CH2)m-NR9SO2R8(여기서, R1, R2, R8, R9, R10및 R11은 상기 정의한 바와 같다)이고; m은 1 내지 6이고; n은 0 내지 6이나, 단 Y가 O 또는 S인 경우, n은 0이 아니다.
  2. 제1항에 있어서, 유리 카복실산인 화합물.
  3. 제2항에 있어서, X가 산소인 화합물.
  4. 제3항에 있어서, W가 CH인 화합물.
  5. 제4항에 있어서, 각 R1, R2, R3, R4, R5, R6및 R7이 H인 화합물.
  6. 제5항에 있어서, Y가 산소 또는 직접 결합인 화합물.
  7. 제1항에 있어서, 하기 화합물로 구성되는 그룹으로부터 선택되는 화합물 및 상기 각 화합물의 약학적으로 허용가능한 염: (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)페닐)아세트산; (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)페닐)아세트산; (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)벤조산: 및 4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)페닐)프로피온산.
  8. 제7항에 있어서, (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)페닐)아세트산인 화합물 및 그의 약학적으로 허용가능한 염.
  9. 제7항에 있어서, (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)페녹시)아세트산인 화합물 및 그의 약학적으로 허용가능한 염.
  10. 제7항에 있어서, (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)벤조산인 화합물 및 그의 약학적으로 허용가능한 염.
  11. 제7항에 있어서, (4-(2-(2-(6-아미노피리딘-3-일)-2(R)-하이드록시에틸아미노)에톡시)페닐)프로피온산인 화합물 및 그의 약학적으로 허용가능한 염.
  12. 제1항에서 정의된 효과량의 화합물, 약물 전구체 또는 염, 및 약학적으로 허용가는한 담체를 포함하는 약학 조성물.
  13. 포유동물의 당뇨병, 과혈당증 및 비만증으로 구성된 그룹중에서 선택된 중상을 치료하는데 유용한 양으로 제1항에서 정의된 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 상기 증상의 치료를 필요로 하는 포유류동물에서 투여하는 것을 포함하는 상기 증상의 치료 방법.
  14. 식용 동물에서 살코기의 함량을 증가시키는데 유효량으로 제1항에서 정의된 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 식용 동물에게 투여하는 것을 포함하는, 상기 함량을 증가시키는 방법.
  15. 포유동물에게 전립선 질환을 치료하는데 유효한 양으로 제1항에서 정의된 바와 같은 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 상기 치료를 필요로 하는 포유동물에게 투여하는 것을 포함하는 상기 질환의 치료 방법.
  16. 포유동물의 장 운동 질환을 치료하는데 유효한 양으로 제1항에서 정의된 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 상기 치료를 필요로 하는 포유동물에게 투여하는 것을 포함하는 상기 질환의 치료 방법.
  17. 포유동물의 우울증을 치료하는데 유효한 양으로 제1항에서 정의된 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 상기 치료를 필요로 하는 포유동물에게 투여하는 것을 포함하는 상기 질환의 치료 방법.
  18. 포유동물의 이상 지혈증을 치료하는데 유효한 양으로 제1항에서 정의된 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 상기치료를 필요로 하는 포유동물에게 투여하는 것을 포함하는 상기 질환의 치료 방법.
  19. 포유동물의 기도 염증성 질환을 치료하는데 유효한 양으로 제1항에서 정의된 일반식(Ⅰ)의 화합물, 그의 약물 전구체 또는 이들 화합물 또는 약물 전구체의 약학적으로 허용가능한 염을 상기 치료를 필요로 하는 포유동물에게 투여하는 것을 포함하는 상기 질환의 치료 방법.
  20. 제19항에 있어서, 상기 기도 염증성 질환이 천식인 방법.
  21. 하기 화합물로 구성되는 그룹으로부터 선택되는 화합물:
    상기 식에서, PG는 통상적인 보호 그룹이고, R은 알킬 그룹이고, R1, R4및 R5는 독립적으로 수소 또는 (C1-C6)알킬이고, R3, R6및 R7은 독립적으로 수소, 할로겐, (C1-C6)알킬, 니트로, 시아노, 트리플루오로메틸, SO2R8, SO2NR9R10, NR9R10, COR11, CO2R9, (C1-C6)알콕시, NR9SO2R8, NR9COR11, NR9CO2R9또는 OR9이고; R8은 독립적으로 (C1-C6)알킬 또는 (C1-C6)알콕시(C1-C6)알킬이고; R9및 R10은 독립적으로 수소, (C1-C6)알킬, (C3-C8)사이클로알킬 또는 (C1-C6)알콕시(C1-C6)알킬이고; R11은 독립적으로 수소, (C1-C6)알킬, NR9R10, (C3-C8)사이클로알킬 또는 (C1-C6)알콕시(C1-C6)알킬이고 (여기서, R9및 R10은 상기 정의한 바와 같다); W는 N는 CH이거나, 또는 R3가 W에 결합되는 경우에는 CR3(여기서, R3는 H뿐아니라 R3에 대해 상기 나타낸 어떠한 정의일 수 있다)이고; X 및 Y는 독립적으로 직접 결합이거나, 산소, 황 또는 NR1이고; Z (CH2)mOR9, (CH2)nCO2H, (CH2)nCOR11, (CH2)nSO2NR9R10, (CH2)nNR9SO2R8, (CH2)nP(O)(OR1)(OR2), (CH2)n-O-(CH2)m-, CO2H, (CH2)nO-(CH2)mCOR11, (CH2)-nO-(CH2)mP(O)(OR1)-(OR2), (CH2)nO-(CH2)mSO2NR9R10또는 (CH2)n-O-(CH2)m-NR9SO2R8(여기서, R1, R2, R8, R9, R10및 R11은 상기 정의된 바와 같다)이고; m은 1 내지 6이고; n은 0 내지 6이나, 단 Y가 O 또는 S인 경우 n은 0이 아니다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960015262A 1995-05-10 1996-05-09 베타-아드레날린 효능성 작용물질 KR100190259B1 (ko)

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