KR910004543A - Acat 억제제 - Google Patents

Acat 억제제 Download PDF

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KR910004543A
KR910004543A KR1019900013485A KR900013485A KR910004543A KR 910004543 A KR910004543 A KR 910004543A KR 1019900013485 A KR1019900013485 A KR 1019900013485A KR 900013485 A KR900013485 A KR 900013485A KR 910004543 A KR910004543 A KR 910004543A
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phenyl
amino
bis
methylethyl
alkyl
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빌헬름 츄콜로브스키 알렉산더
윌레이스 크레스웰 마크
하워드 로크 윌리암
시르카 일라
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로널드 에이. 다이놀트
워너-램버트 캄파니
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Abstract

내용 없음.

Description

ACAT 억제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (23)

  1. 하기 일반식 I로 표시되는 화합물.
    R은 a)페닐(CH2)n-[여기서 n은 0 내지 2이고, 페닐 고리는 비치환이거나, 또는 직쇄 또는 분지쇄 C1-C6알킬, 직쇄 또는 분지쇄 C1-C6알콕시, 페녹시, 히드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, -COOH, -COO알킬 (여기서, 알킬은 C1-C4알킬임), -NR5N6중에서 선택되는 1 내지 3개의 치환체를 가짐] b) 1-또는 2-나프틸기 [이는 비치환이거나, 또는 직쇄 또는 분지쇄 C1-C6알킬, 직쇄 또는 분지쇄 C1-C6알콕시, 히드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, -COOH, -COO알킬 (여기서, 알킬은 C1-C4알킬임), -NR5N6중에서 선택되는 1 내지 3개의 치환체를 가짐] R1은 (a)수소원자, 또는 (b)직쇄 또는 분지쇄인 C1-C6알킬기이고, R2는 (a)수소원자, (b)포화되거나 또는 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄 C1-C20탄화수소, (c)p-페닐메톡시벤질기.
    (e)-CH2CH2S(O)c-2-CH3, (f)비치환되거나 또는 직쇄 또는 분지쇄인 C1-C4알킬, C1-C4알콕시, 히드록시, 염소, 불소, 브롬, 트리플루오로메틸 또는 아미노 중에서 선택되는 1 또는 2개의 치환체를 갖는 페닐기, 1- 또는 2-나프틸기.
    (식중, t는 0 내지 4이고, w는 0 내지 4인데, 단 t와 w의 합이 5보다 크지 않아야 함) (h) R1및 R2가 이들이 결합된 탄소원자와 함께 C3-C7인 포화 카르보시클릭고리를 형성하고, R3은 (a)수소원자 (b)포화되거나 또는 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄 C1-C20탄화수소,
    [여기서, q는 0 내지 3이고, r은 0내지 2이고, s는 2내지 6이며, Ar은 페닐기, 1-또는 2-나프틸기, 이들 기는 비치환이거나 또는 직쇄 또는 분지쇄인 C1-C6알킬, 직쇄 또는 분지쇄인 C1-C6알콕시, 히드록시, 벤질옥시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, -NH-COCH3, -CONH2, -COOH, -COO알킬 (여기서, 알킬은 직쇄 또는 분지쇄인 C1-C4알킬임), -CH2COOH, -CH2CONH2, -NR7R8, -CH2NR78, -CH2OR9, -COO 알킬(여기서, 알킬은 직쇄 또는 분지쇄인 C1-C6알킬이며, 임의로 이 알킬기의 말단에 위치하는 탄소가 -OR9기 또는 -NR7R8기로 치환됨), -NH-(CH2)-COO-알킬 (여기서, 알킬은 직쇄 또는 분지쇄인 C1-C6알킬임), -SO2NR7R9또는 -NHSO2R10, N-옥시드 중에서 선택되는 치환체를 가짐]
    (e)9-플루오레닐기, 1 또는 2개의 치환체로 치환된 9-플루오레닐기 (여기서, 치환체는 염소, 브룸 또는 불소임) 또는 1, 2, 또는 4 위치에서 1개의 치환체를 갖는 9-플루오레닐기 (여기서, 치환체는 직쇄 또는 분지쇄인 C1-C6알킬, 직쇄 또는 분지쇄인 C1-C6알콕시, 히드록시, 히드록시메틸, -COOH, -COO알킬(여기서, 알킬은 직쇄 또는 분지쇄인 C1-C6알킬임), 또는 -CONR5R6임), R4는 (a)수소원자 (b)포화되거나 또는 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄 C1-C20탄화수소.
    (여기서 t, w는 상기 정의한 바와 같음) (d) -SO2R14, (e), (f)-CO2R15, (g)-COR18, (h), (i)R3이 수소원자 또는 C1-C4인 포화 직쇄 탄화수소인 경우, R4는 트리틸기이고, (j)9-플루오레닐기 또는 1 내지 3개의 치환체로 치환된 9-플루오레닐기 [여기서, 치환체로는 불소, 염소, 브룸, 직쇄 또는 분지쇄인 C1-C4알킬, -NHCO알킬 또는 -CO2알킬(여기서, 알킬은 직쇄 또는 분지쇄인 C1-C4알킬임)임], (k)페닐기 또는 1 또는 2개의 치환체로 치환된 페닐기 (여기서, 치환체는 직쇄 또는 분지쇄인 C1-C4알킬, 염소, 브롬, 불소, 트리플루오로메틸, 히드록시, 직쇄 또는 분지쇄인 C1-C4알콕시, 아미노 또는 니트로임), (l) -(CH2)p-COOR20, R5및 R6은 각각 독립적으로 수소 원자 또는 직쇄 또는 분지쇄인 C1-C4알킬기이고, R7및 R8은 각각 독립적으로 수소 원자이거나 또는 말단에 위치하는 탄소가 임의로 OR9기로 치환된 C1-C6알킬기이거나, 또는 R7및 R5는 이들이 결합된 질소 원자와 함께 5원 또는 6원 고리를 형성하며, 임의로 이 고리에는 산소 또는 -NR9가 포함되고, R9는 산소원자, C1-C6알킬기, C2-C5알카노일기, 벤조일기이고, R10은 C1-C6알킬기 또는 페닐기이고, R11및 R12는 각각 독립적으로 수소 원자 또는 C1-C6알킬이거나, 또는 R11이 수소원자일 때 R12는 하기하는 R13에서 정의된 기 중에서 선택될 수 있으며, R13은 1 내지 3개의 산소, 황 또는 질소 원자를 갖는 방향족 모노시클릭 헤테로시클릭기, 비치환 또는 1 내지 3개의 치환체를 갖는 페닐기, 1- 또는 2-나프틸기, [여기서, 치환체는 직쇄 또는 분지쇄인 C1-C6알킬, 직쇄 또는 분지쇄인 C1-C6알콕시, 페녹시, 히드록시, 불소, 염소, 브롬, 니트로, 트리플루오로메틸, -COOH, -COO알킬 (여기서, 알킬은 C1-C4알킬임), 또는 -NR5R6, -CH2NR5R6일 수 있음], R14는 모르폴리노기, 페닐기 또는 치환페닐기 (여기서, 치환체는 직쇄 또는 분지쇄인 C1-C4알킬임) 또는 포화되거나 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄인 C1-C20탄화수소, 페닐(CH2)p-COOR20(여기서, p는 0, 1 또는 2임) 중에서 선택되는 1 내지 3개의 치환체로 치환됨]이고, R16은 페닐기 또는 1 또는 2개의 치환체로 치환된 페닐기 (여기서, 치환체는 직쇄 또는 분지쇄인 C1-C4알킬, 불소, 염소 또는 브롬임), R17은 직쇄 또는 분지쇄인 저급 C1-C4알킬기이고, R18은 상기 R15에 대해 정의된 군 중에서 선택되거나 또는 1 내지 7개의 할로겐 원자로 치환된 직쇄 또는 분지쇄 C1-C10알킬기 (여기서, 할로겐 원자는 염소, 불소 또는 브롬임), 9-플루오닐메틸기, 피롤리디노기 또는 하기의 기이고,
    (식중, R16및 R17은 상기 정의한 바와 같음), R20은 수소 원자 또는 직쇄 또는 분지쇄 C1-C4알킬기이고, 단 R1, R2, R3및 R4가 동시에 모두 수소 원자는 아니고, R2, R3및 R4가 동시에 모두 포화되거나 또는 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄 C1-C20탄화수소는 아니며, R2, R3및 R4가 하기의 기인 경우
    R12는 R13과 동일하지 않고, R12및 R13이 모두 동시에 9-플루오레닐치환체는 아니다.
  2. 제1항에 있어서, R1이 수소 원자인 화합물.
  3. 제1항에 있어서, R1, R2및 R3중 2개가 수소 원자인 화합물.
  4. 제3항에 있어서, R4가 하기의 화합물
  5. 제4항에 있어서, R13이 비치환페닐기이거나 또는 직쇄 또는 분자쇄인 C1-C6알킬, 직쇄 또는 분지쇄인 C1-C6인 알콕시, 페녹시, 히드록시, 불소, 염소, 브롬, 니트로, 히드록시메틸 트리플루오로메틸, -COOH, -COO 알킬(여기서, 알킬은 직쇄 또는 분지쇄인 C1-C4알킬임), -NR5R6(여기서, R5및 R6각각은 수소 원자 또는 C1-C4알킬임), 또는 -CH2NR5R6(여기서 R5및 R6은 상기 정의한 바와 같음)중에서 선택된 1 내지 3개의 치환체를 갖는 페닐기인 화합물.
  6. 제5항에 있어서, 다음 군 중에서 선택되는 화합물. N-[2,6-비스(1-메틸에틸)페닐]-2-[(디페닐메틸)아미노]아세트아미드, N-2,6-비스(1-메틸에틸)페닐]-2-[(1,1-디메틸-2-페닐에틸)아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[디페닐메틸)아미노]아세트아미드, 2-[(디페닐메틸)아미노]-N-(2,4,6-트리메톡시페닐)아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(페닐메틸)아미노]벤젠아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[(2,2-디페닐에틸)아미노]프로판아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[(2,2-디페닐에틸)아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[(디페닐에틸)아미노]아세트아미드, N-(2,6-디플루오로페닐)-2-[(디페닐메틸)아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[[[(4-(디메틸아미노)페닐]메틸]아미노]아세트아미드, N-(2,6-디에틸페닐)-2-[(페닐메틸)아미노]아세트아미드, 2-[(디페닐메틸)아미노]-N-[2,4,6-트리메톡시페닐]아세트아미드, N-[2,6-디메틸페닐)-2-[(디페닐메틸)아미노]아세트아미드, 2-[아세틸(1,1-디메틸-2-페닐에틸)아미노-N-[2,6-비스(1-메틸에틸)페닐]아세트아미드, N-[[[2-2[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸](2,2-디페닐에틸)아미노]카르보닐]글리신, 에틸 에스테르, 2-[아세틸[[4-(디메틸아미노)페닐]메틸]아미노]-N-[2,6-비스(1-메틸에틸)페닐]아세트아미드, N-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸-N-(메닐메틸)아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[디페닐메틸)-[[(2-메톡시페닐)아미노]카르보닐]아미노]아세트아미드, N-(2,6-디에틸페닐)-2-[[[(2,6-디메틸페닐)아미노]카보닐](디페닐메탈)아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[[[4-디메틸아미노)페닐]아미노]티옥소메틸](2,2-디페닐에틸]아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[(디메틸아미노)-[[4-메톡시페닐]아미노]티옥소메틸]아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[[[4-(디메틸아미노)페닐]아미노]티옥소메틸](디페닐메틸)아미노]아세트아미드, N-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]-N-(디페닐메틸)-2-메톡시벤즈아미드, 4-[[[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸](디페닐메틸)아미노]카르보닐]벤조산 메틸에스테르, N-[2[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]-N-(디페닐메틸)-2-(트리플루오로메틸)-벤즈아미드, N-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]-N-(디페닐메틸)-2,2,3,3,4,4,4-헵타-플루오로부탄아미드, N-(2,6-디메틸페닐(-2-[[N-(디페닐메틸)-N-(페닐아미노)카르보닐]아미노]아세트아미드, N-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]-N-(디페닐메틸)-4-니트로 벤즈아미드, N-[2-[[2,6-비스(1-에틸에틸)아미노]-2-옥소에틸]-N-(디페닐메틸)-2,5-벤즈아미드, 4-[[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]-(2,2-디페닐에틸)아미노]-4-옥소 부탄산, N-[2,6-비스(1-메틸에틸)페닐]-2-[비스(페닐메틸)아미노]아세트아미드, N-(2,6-디에틸페닐)-2-[[[[4-(디메틸아미노)페닐]아미노]티옥소메틸](디페닐메틸)아미노]아세트아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(페닐메틸)아미노]벤젠프로판아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-4-(페닐메톡시)-α[(페닐메틸]아미노]벤젠프로판아미드, (S)-N-[2,6-비스(1-메틸메틸)페닐]2-[(디페닐메틸)아미노]벤젠프로판아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(디페닐메틸)아미노]-4-(페닐메톡시)프로판아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[(4-메톡시페닐)페닐메틸]아미노 아세트아미드,(±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[[4-(디메틸아미노)페닐]페닐메틸]아미노 아세트아미드, (R)-N-[2,6-비스(1-메틸에틸)페닐]-2-[(1-페닐에틸)아미노]아세트아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-2-[(1-페닐에틸)아미노]아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[4-히드록시페닐)페닐메틸]아미노 아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[1-(2-메톡시페닐)에틸]아미노 아세트아미노, N-[2,6-비스(1-메틸에틸)페닐)-2-[(비스(4-클로로페닐)메틸아미노]아세트아미노, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[[(4-플루오로페닐)페닐메틸]아미노]아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[((2-메톡시페닐)페닐메틸]아미노 아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[((3-메틸페닐)페닐메틸]아미노]아세트아미드, N-(2,6-비스(1-메틸에틸)페닐]-2-[[비스(4-플루오로페닐)아미노]아세트아미노,
    N-(2,6-비스(1-메틸에틸)페닐]-2-[(비스(4-메톡시페닐)메틸]아미노]아세트아미노, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[((3-(매틸페닐)페닐메틸]아미노]아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[((2-클로로페닐)페닐메틸]아미노]아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[((2-메틸페닐)페닐메틸]아미노]아세트아미드,(±)-N-[2,6-비스(1-메틸에틸]페닐)-2-[[(4-니트로-페닐)페닐메틸]아미노]아세트아미드, N-(2,6-비스(1-메틸에틸)페닐]-2-[(비스(3-트리플루오로메틸)페닐(메틸]아미노]아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[((3,5-디메톡시페닐)페닐메틸]아미노]아세트아미드, (±)-3-[[[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]아미노]페닐메틸]벤조산 메틸 에스테르, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[[[3-(히드록시메틸)페닐]페닐메틸]아미노]아세트아미드, (±)-3-[[[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]아미노]페닐메틸]벤조산, (±)-4-[[[2-[[2,6-비스(1-메틸에틸)페닐]-2-옥소에틸]아미노]페닐메틸]벤조산 에틸 에스테르, (±)-4-[[[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]아미노]페닐메틸]벤조산, (±)-N-[2,6-비스(1-메틸에틸]페닐]-2-[[(3,5-디메톡시페닐)(2-메틸페닐)메틸]아미노]아세트아미드, (±)-2-[아세틸[(3,5-디메톡시페닐)(2-메틸페닐)메틸]아미노-N-[2,6-비스(1-메틸에틸)페닐]아세트아미드, N-(2,6-비스(1-메틸에틸)페닐]-(±)-[(2,2-디페닐에틸)아미노]벤젠아세트아미드, N-(2,6-비스(1-메틸에틸)페닐]-(±)-[(2-페닐에틸)아미노)벤젠아세트아미드.
  7. 제4항에 있어서, R13이 직쇄 또는 분지쇄인 C1-C6알킬, 직쇄 또는 분지쇄인 C1-C6알콕시, 페녹시, 히드록시, 불소, 염소, 브롬, 니트로, 히드록시메틸, 트리플루오로메틸, -COOH, -COO-알킬(여기서, 알킬은 직쇄 또는 분지쇄인 C1-C4알킬임), -NR5R6(여기서, R5및 R6각각은 수소 원자 또는 C1-C4알킬임), 또는 -CH2NR5R6(여기서, R5및 R6는 상기 정의한 바와 같음)중에서 선택된 1개 내지 3개의 치환체로 치환된 1- 또는 2-나프틸기인 화합물.
  8. 제7항에 있어서, 다음 군 중에서 선택되는 화합물. (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[(1-나프탈레닐)페닐메틸]아미노 아세트아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-2-[1-[(1-나프탈레닐)에틸]아미노]아세트아미드, (R)-N-[2,6-비스(1-메틸에틸)페닐]-2-[(1-나프탈레닐)에틸]아미노]아세트아미드.
  9. 제4항에 있어서, R13이 1 내지 3개의 질소, 산소, 또는 황원자를 갖는 방향족 모노시클릭 헤테로시클릭기인 화합물.
  10. 제9항에 있어서, 다음 군 중에서 선택되는 화합물. (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[페닐-(2-티에닐)메틸]아미노아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[페닐-(2-피리디닐)메틸]아미노아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[비스(2-피리디닐)페닐]아미노아세트아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-2-[1-(2-피리디닐)에틸]아미노아세트아미드.
  11. 제3항에 있어서, R4가 -COR18인 화합물. [여기서, R18은 직쇄 또는 분지쇄인 C1-C10알킬기, 페닐( CH2)x-(여기서, x는 0 내지 2이고, 페닐고리는 비치환이거나, 또는 치환되며, 그 치환체로는 직쇄 또는 분지쇄인 C1-C4알킬, 염소, 브롬, 불소, 트리플루오로메틸, -NR6R6(여기서, R5및 R6은 상기 정의한 바와 같음), -CH2NR5R6(여기서, R5및 R6은 상기 정의한 바와 같음), -NH(CH2b Ph(여기서, b는 0 또는 1이고, Ph는 페닐임). 직쇄 또는 분지쇄인 C1-C4알콕시, 디페닐메틸, 니트로-(CH2p-COOR20(여기서 p는 0, 1 또는 2이고, R20은 수소 또는 직쇄 또는 분지쇄인 C1-C4알킬임), 1내지7개의 할로겐 원자로 직쇄 또는 분지쇄인 C1-C10알킬(여기서, 할로겐은 염소, 불소 또는 브롬은 d원자임)중에서 선택됨), q-플루오레닐메틸렌, 피롤리디노 또는 하기식의 기임(하기식중 R16은 비치환되거나 또는 직쇄 또는 분지쇄인 C1-C4알킬, 불소, 염소, 또는 브롬중에서 선택되는 1 내지 2개의 치환체를 갖는, R17은 직쇄 또는 분지쇄인 C1-C4알킬임).
  12. 제11항에 있어서, 다음 군 중에서 선택되는 화합물. (S)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(3,3-디메틸-1-옥소부틸)아미노]-4-(페닐메톡시)벤젠프로판아미드, (S)-α-[(3-다메틸-1-옥소부틸)-아미노]-4-(페니레톡시)-N-(2,4,6-트리플루오로페닐)벤젠프로판아미드, (S)-α-N-(2,6-디이소프로필페닐)벤젠프로판아미드, (S)-α-(아세틸아미노)-N-(2,6-디에틸페닐)벤젠프로판아미드, (S)-α-(아세틸아미노)-N-[2,6-비스(1-메틸에틸)페닐]벤젠프로판아미드, (S)-α-(아세틸아미노)-N-[2,6-디메틸페닐]벤젠프로판아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(4-클로로-1-옥소부틸)아미노]벤젠프로판아미드, (±)-α-(벤지오일아미노)-N-[2,6-비스(1-메틸에틸)페닐]벤젠프로판아미드, (±)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(1-옥소펜틸)아미노]벤젠프로판아미드, (±)-시스-N-[2,6-비스(1-메틸에틸)페닐]-α-[(1-옥소-9-옥타데세닐)벤젠프로판아미드, 2-[아세틸(디페닐메틸)아미노]-N-[2,6-비스(1-메틸에틸)페닐]아세트아미드, N-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸-N-(디페닐메틸)-벤즈아미드, (S) - N-[2-[2,6-비스(1-메틸에틸)페닐]아미노]-1-메틸-2-옥소에틸]-α-페닐벤젠아세트아미드.
  13. 제3항에 있어서, R4가 -CO2R15인 화합물.[여기서, R15는 포화되거나 또는 1 내지 3개의 이중결합을 갖는 직쇄 또는 분지쇄인 C1-C20탄화수소, 페닐(CH2)x-임(여기서, x는 0 내지 2이고, 페닐고리는 비치환이거나, 또는 직쇄 또는 분지쇄인 C1-C4알킬, 염소, 브롬, 불소, 트리플루오로메틸, -NR5R6(여기서, R5및 R6은 상기 정의한 바와 같음), -CH2NR5R6(여기서, R5및 R6상기 정의한 바와 같음), 직쇄 또는 분지쇄인 C1-C4알콕시, 디페닐메틸, 니트로, -(CH2)p-COOR20(여기서, p는 0, 1 또는 2이고 R20은 수소 원자 또는 직쇄 또는 분지쇄인 C1-C4알킬임)중에서 선택되는 1 내지 3개의 치환체로 치환됨)].
  14. 제13항에 있어서, 다음 군 중에서 선택되는 화합물. (S)-1,1-디메틸에틸[2-[(2,6-비스-(1-메틸에틸)페닐]아미노]-2-옥소-1-[[4-(페닐메톡시)페닐]메틸]에틸]카르바메이트, (S)-1,1-디메틸에틸[2-[[2,6-비스-(1-메틸에틸)페닐]아미노]-1-[[[4히드록시페닐)-메틸]-2-옥소에틸]카르바메이트, (S)-1,1-디메틸에틸[2-옥소-1-[[4-(페닐메톡시)페닐]메틸-2-[(2,4,6-트리플루오로페닐)아미노]에틸]카르바메이트, (S)-1,1-디메틸에틸[2-[[2,6-비스-(1-메틸에틸)페닐]아미노]-1-(1H-인돌-3-일메틸)-2-옥소에틸]카르바메이트, (S)-(1,1-디메틸에틸[1-(1H-인돌-3-일메틸)-2-옥소-2-[2,4,6-트리플루오로페닐)아미노]에틸]카르바메이트, (S)-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-1-페닐에틸]카르밤산, 페닐메틸 에스테르, (S)-[1-[[2,6-비스(1-메틸에틸)페닐]아미노]카르보닐]-3-(메틸티오)프로필]카르밤산, 1,1-디메틸에틸 에스테르, (S)-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-1-메틸에틸]카르밤산, 1,1-디메틸에틸 에스테르, (S)-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-1-[[4-(페닐메톡시)페닐]메틸]에틸]카르밤산, 9H-플루오렌-9-일메틸 에스테르, (S)-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-1-[[4-(페닐메톡시)페닐]에틸]카르밤산, 9H-플루오렌-9-일메틸 에스테르, 페닐메틸 (±)-2-[(2,6-디메틸페닐)아미노]-2-옥소-1-(페닐메틸)에틸]카르바메이트, 페닐메틸(±)-2-[(2,6-디에틸페닐)아미노]-2-옥소-1-(페닐메틸)에틸]카르바메이트 페닐메틸(±)-2-[(2,6-비스(1-메틸에틸)아미노]-2-옥소-1-(페닐메틸)페닐)에틸]카르바메이트, 1,1-디메틸에틸 (S-2-옥소-1-(페닐메틸)-2-[(2,4,6-트리플루오로페닐)아미노]에틸]카르바메이트, [2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-에틸](디페닐메틸)카르밤산 메틸 에스테르, 1,1-디메틸에틸-[2-[(2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸]카르바메이트, (±)-1,1-디메틸에틸-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-1-페닐메틸]에틸]메틸카르바메이트, (S)-1,1-디메틸에틸-[2-[(2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-1-페닐메틸]에틸]메틸카르바메이트, (S)-[1-[[[2,6-비스(1-메틸에틸)페닐]아미노]카르보닐]-3-페닐프로필]카르밤산, 1,1-디메틸에틸 에스테르, [2-[(2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소-1-[[4-(페닐메톡시)페닐]메틸]에틸]카르밤산, 메틸 에스테르, (S)-[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-1-메틸-2-옥소에틸]메틸]카르밤산, 1,1-디메틸에틸 에스테르, (S)-2-옥소-1-[[4-(페닐메톡시)페닐]메틸]-2-[(2,4,6-트리메톡시페닐)아미노]에틸]카르밤산, 1,1-디메틸에틸 에스테르, (S)-[1-(1H-인돌-3-일메틸)-2-옥소-2-[2,4,6-트리메톡시-페닐)아미노]에틸]카르밤산, 1,1-디메틸에틸 에스테르.
  15. 제3항에 있어서, R4가 -CONHR15인 화합물.[여기서, R15는 포화되거나 또는 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄인 C1-C20탄화수소, 페닐(CH2)x-임(여기서, x는 0 내지 2이고, 페닐고리는 비치환이거나, 또는 직쇄 또는 분지쇄인 C1-C4알킬, 염소, 브롬, 불소, 트리플루오로메틸, -NR5R6(여기서, R5및 R6은 상기 정의한 바와 같음), -CH2NR5R6(여기서, R5및 R6상기 정의한 바와 같음), 직쇄 또는 분지쇄인 C1-C4알콕시, 디페닐메틸, 니트로, -(CH2)p-COOR20(여기서, p는 0, 1 또는 2이고 R20은 수소 원자 또는 직쇄 또는 분지쇄인 C1-C4알킬임)중에서 선택되는 1 내지 3개의 치환체로 치환됨)].
  16. 제15항에 있어서, 다음 군 중에서 선택되는 화합물.[S)-N-[2,6-비스(1-메틸에틸페닐]-α-[[[(1,1-디메틸에틸)아미노]카르보닐]아미노-4-페닐-메톡시)벤젠프로판아미드, (S)-α-[[[(1,1-디메틸에틸)아미노]카르보닐]아미노-4-(페닐메톡시)-N-(2,4,6-트리플루오로페닐)벤젠프로판아미드, N-[2,6-비스(1-메틸에틸)페닐]-α-[[(페닐아미노)에틸)아미노]카르보닐]아미노]벤젠프로판아미드, N-[2,6-비스(1-메틸에틸)페닐],-α-[[[(1,1-디메틸에틸)아미노]카르보닐]아미노]벤젠프로판아미드, (S)-α-[[(페닐아미노)카르보닐]아미노]-N-(2,4,6-트리플루오로페닐)벤젠프로판아미드, (S)-α-[[[(1,1-디메틸에틸)아미노]카르보닐]아미노]-N-2,4,6-트리플루오로페닐)벤젠프로판아미드, (S)-N-[2,6-비스(1-메틸에틸페닐]-α-[[[(페닐메틸)아미노]카르보닐)아미노]벤젠프로판아미드, (S)-α-[[(부틸아미노)카르보닐)아미노]-N-(2,4,6-트리플루오로메틸)벤젠프로판아미드, N-[[[2-[[2,6-비스(1-메틸에틸)페닐]아미노]-2-옥소에틸](디페닐메틸)이미노]카르보닐]글리신 에틸 에스테르, N-[2,6-비스(1-메틸에틸)페닐]-2-[(디페닐메틸)-[(페닐아미노)카르보닐]아미노]아세트아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-[(디페닐아미노)카르보닐](페닐메틸)아미노]아세트아미드.
  17. 제3항에 있어서, R4가 포화되거나 또는 1 내지 3개의 이중 결합을 갖는, 직쇄 또는 분지쇄인 탄화수소인 화합물.
  18. 제17항에 있어서, 다음 군 중에서 선택되는 화합물. (Z)-2-[(9-옥타데세닐)(페닐메틸)아미노]-N-(2,4,6-트리메톡시페닐)아세트아미드, (Z)-2-[(9-옥타데세닐[[(2-페닐에틸)아미노]카르보닐]아미노-N-(2,4,6-트리메톡시페닐)아세트아미드, (Z)-[[[2,6-비스(1-메틸에틸)페닐]아미노)카르보닐]-9-옥타데세닐아미노]-N-(2,4,6-트리메톡시페닐)아세트아미드, (Z)-2-[[(4-메틸페닐)술포닐](9-옥타데세닐)아미노]-N-(2,4,6-트리메톡시페닐)아세트아미드, (Z)-2-[[(4-메틸페닐)술포닐](9-옥타데세닐)아미노]-N-(2,4,6-트리메톡시페닐)아세트아미드, (Z)-2-(9-옥타데세닐아미노)-N-(2. 46-트리메톡시페닐)아세트아미노, (Z) -N-)2. 6-디메틸페닐)-2-(9-옥타데세닐아미노)아세트아미드.
  19. 제3항에 있어서, R4가 -SO2R14인 화합물.[여기서, R14는 모르폴리노기, 페닐기, 또는 치환페닐기(여기서, 치환체를 직쇄 또는 분지쇄인 C1-C4알킬임), 또는 포화되거나 1 내지 3개의 이중 결합을 갖는 직쇄 또는 분지쇄인 C1-C20탄화수소임)].
  20. 제19항에 있어서, 다음 군 중에서 선택되는 화합물. (±)-N-[2,6-비스(1-메틸에틸)페닐]-α-[(4-모르폴리닐술포닐)아미노]벤젠프로판아미드, (S)-N-[2,6-비스(1-메틸에틸)페닐]-α-[[(4-메틸페닐)술포닐]아미노]벤젠프로판아미드, (S)-α-[((4-메틸페닐)술포닐]아미노]-N-(2,4,6-트리플루오로페닐)벤젠프로판아미드.
  21. 다음 군 중에서 선택되는 화합물. N-[2,6-비스(1-메틸에틸)페닐]-2-브로모프로판아미드, N-[2,6-비스(1-메틸에틸)페닐]-2-브로모아세트아미드. N-[2,6-비스(1-메틸에틸)페닐]-2-브로모페닐아세트아미드.
  22. 유효량의 제1항의 화합물 및 제약학적으로 허용되는 담체로 이루어진, 콜레스테롤 조절을 위한 제약학적 조성물.
  23. 유효량의 제1항의 화합물을 제약학적으로 허용되는 담체와 함께 환자에게 투여하여 과콜레스테린혈증 및 아테롬성 동맥 경화증을 치료하기 위한 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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