KR890000412A - 과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물 - Google Patents

과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물 Download PDF

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KR890000412A
KR890000412A KR1019880006438A KR880006438A KR890000412A KR 890000412 A KR890000412 A KR 890000412A KR 1019880006438 A KR1019880006438 A KR 1019880006438A KR 880006438 A KR880006438 A KR 880006438A KR 890000412 A KR890000412 A KR 890000412A
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trifluoromethyl
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칼리다스 트리비디 바래트
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워너-탐버트 컴퍼니
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Abstract

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Description

과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물
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Claims (34)

  1. 다음 구조식을 갖는 화합물 또는 그것의 제약학적으로 허용가능한 염.
    식중, Ar은 페닐; 나프틸; C1-v 알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 페닐; C1-6알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리츤루오로메틸 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 나프틸; X는 산소 또는 황; Y는 산소 또는 -NH-; n은 0 또는 1-3인 정수; n′는 2-6인 정수; 및 n″는 0,1 또는 2; Ar′는 페닐; 나프틸; 티에닐; 피리디닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 나프틸; C1-6알킬, C1-6알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-6알킬인 -NR1R2로 임의 치환된 티에닐; 또는 C1-6알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 피리디닐로부터 선택됨.
  2. 제1항에 있어서, X가 산소인 화합물.
  3. 제1항에 있어서, Y가 -NH-인 화합물.
  4. 제1항에 있어서, Ar이 페닐이거나 C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐인 화합물.
  5. 제1항에 있어서, Ar′가 티에닐; 페닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 티에닐; 또는 C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐로부터 선택된 화합물.
  6. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-(1-페닐사이클로펜틸)우레아인 화합물.
  7. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-(1-페닐사이클로부틸)우레아인 화합물.
  8. 제1항에 있어서, N-(2,6-디에틸페닐)-N′-(1-페닐사이클로펜틸)우레아인 화합물.
  9. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[(1-페닐사이클로펜틸) 메틸]우레아인 화합물.
  10. 제1항에 있어서, N-(페닐사이클로펜틸)-N′-(2,4,6-트리메톡시페닐)우레아인 화합물.
  11. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
  12. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
  13. 제1항에 있어서, N-[2,6-비스(1-메틸에틸)]-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
  14. 제1항에 있어서, N-(2,6-디에틸페닐)-N′-[(1-페닐사이클로헥실) 에틸]우레아인 화합물.
  15. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
  16. 제1항에 있어서, N-(2,6-디메틸페닐)-N′-[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
  17. 제1항에 있어서, N-(2,6-디에틸페닐)-N′-[(1-페닐사이클로펜틸) 메틸]우레아인 화합물.
  18. 제1항에 있어서, N-[2,6-비스(1-메틸에틸)페닐]-N′-[(1-페닐사이클로헥실) 에틸]우레아인 화합물.
  19. 제1항에 있어서, N-[2,6-비스(1-메틸에틸)페닐]-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
  20. 제1항에 있어서, N-[2-에틸-6-(1-메틸에틸)페닐]-N′-[1-(2-티에닐) 사이클로헥실]우레아인 화합물.
  21. 제1항에 있어서, N-[2-(1,1-디메틸에틸)-6-메틸페닐]-N′-[1-(2-티에닐)사이클로헥실]우레아인 화합물.
  22. 제1항에 있어서, N-[2-메틸-6-(1-메틸에틸페닐]-N′-[1-페닐사이클로헥실) 에틸]우레아인 화합물.
  23. 제1항에 있어서, N-[2-(1.1-디메틸에틸)-6-메틸페닐]-N′-[1-페닐사이클로헥실) 에틸]우레아인 화합물.
  24. 제1항에 있어서, N-[2-에틸-6-(1-에틸에틸)페닐]-N′-[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
  25. 제1항에 있어서, N-[2-메틸-6-(1-메틸에틸)페닐]-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
  26. 제1항에 있어서, N-[2-(1.1-디메틸에틸)-6-메틸페닐]-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
  27. 제1항에 있어서, N-[2-에틸-6-(1-메틸에틸)페닐]-N′-[1-(1-페닐사이클로펜틸) 메틸]우레아인 화합물.
  28. 제1항에 있어서, N-[2,4-디플루오로페닐)-N′-[1-(2-티에닐)사이클로헥실]우레아인 화합물.
  29. 제1항에 있어서, N-[2,4-디플루오로페닐)-N′-[(1-페닐사이클로펜틸) 에틸]우레아인 화합물.
  30. 제1항에 있어서, N-[2,4-디플루오로페닐)-N′-[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
  31. 제1항에 있어서, N-(2,6-디브로오-4-플루오로페닐)-N′[(1-페닐사이클로헥실) 메틸]우레아인 화합물.
  32. 제약학적으로 허용가능한 담체와 함께 제1항에 정의된 화합물의 ACAT-억제 효과량으로 구성되는, 콜레스테롤을 조절하는 제약학적 조성물.
  33. 제약학적으로 허용가능한 담체와 함께 제1항에 정의된 화합물의 ACAT-억제 효과량을 환자에게 투여하는 것으로 구성되는, 콜레스테롤의 조절방법.
  34. a) 다음 구조식의 화합물은 Ar-N=C=0
    식중 Ar은 상기 정의된 바와 같음. 극성인 중성 유기용매내 주변 온도에서 다음 구조식의 화합물과 반응시키고;
    식중, y, n, n′, n″및 Ar′는 상기 정의된 바와 같음.
    b) 그후에 상기 반응 단계의 생성무를 분리하며; c) 원한다면, 상기 분리한 생성물을 제약학적으로 허용가능한 염으로 전화시키는 단계로 구성되는, 다음 구조식의 화합물 또는 그것의 제약학적으로 허용 가능한 염의 제조방법.
    식중 Ar은 페닐; 나프틸; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 페닐; C1-v알킬, C1-2알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 치환된 나프틸; X는 산소 또는 황; Y는 산소 또는 -NH-; n은 0 또는 1-3인 정수; n′는 2-6인 정수; 및 n″는 0.1 또는 2; Ar′는 페닐; 나프틸; 티에닐; 피리디닐; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 페닐; C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 나프틸; C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 티에틸; 또는 C1-v알킬, C1-v알콕시, 하이드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, 또는 R1및 R2가 각각 수소, 또는 C1-v알킬인 -NR1R2로 임의 치환된 피리디닐로부터 선택됨.
    ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880006438A 1987-06-02 1988-05-31 과지지질혈증을 방지하고 아테롬성 동맥경화증을 방지하는 우레아 및 카바메이트 화합물 KR890000412A (ko)

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NO167200B (no) 1991-07-08
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NZ224670A (en) 1989-10-27
DK297988A (da) 1988-12-03
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PT87622B (pt) 1992-09-30
CA1296339C (en) 1992-02-25
DK175791B1 (da) 2005-02-21
IE881380L (en) 1988-12-02
GR3006297T3 (ko) 1993-06-21
NO882406L (no) 1988-12-05
EP0293880B1 (en) 1992-08-26
PT87622A (pt) 1988-06-01
FI882588A (fi) 1988-12-03
DK297988D0 (da) 1988-06-01
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JP2575183B2 (ja) 1997-01-22
AU601846B2 (en) 1990-09-20
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DE3873992T2 (de) 1992-12-17
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