KR920006322A - 벤젠, 피리딘 및 피리미딘 유도체 - Google Patents

벤젠, 피리딘 및 피리미딘 유도체 Download PDF

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KR920006322A
KR920006322A KR1019910016674A KR910016674A KR920006322A KR 920006322 A KR920006322 A KR 920006322A KR 1019910016674 A KR1019910016674 A KR 1019910016674A KR 910016674 A KR910016674 A KR 910016674A KR 920006322 A KR920006322 A KR 920006322A
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phenyl
pharmacologically acceptable
benzene
acceptable salt
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KR940003494B1 (ko
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데이지 기무라
노부히사 와다나베
야스다까 다까세
겐지 하야시
마꼬또 마쓰이
히로노리 이꾸다
유우지 야마기시
고오조오 아까사까
히로시 다나까
잇세이 오오쯔까
다까오 사에끼
모또지 고구시
도오루 후지모리
이사오 사이또오
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나이또오 하루오
에자이 가부시끼가이샤
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Abstract

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Description

벤젠, 피리딘 및 피리미딘 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (23)

  1. 일반식(I) :
    의 벤젠, 피리딘 또는 피리미딘 유도체 또는 이들의 약리학적 허용염, 상기 식에서 R1은 수소 또는 할로겐 원자, 저급알킬, 저급알콕시, 니트로 또는 시아노기, 식 :의 기(여기서, R7및 R8은 서로 같거나 다를 수 있고 각각은 수소원자 또는 저급알킬 또는 저급알킬 술포닐기를 표시하고 u는 0이거나 1 또는 2의 정수이고; 달리, R7과 R8은 이들이 결합된 질소원자와 함께 고리를 형성한다), 식 : CH2OR9의 기(R9는 수소원자 또는 저급 알킬기를 표시한다), 식 : -COOR10의 기(R10은 수소원자 또는 저급알킬기를 표시한다), 식의 기(R11및 R12는 서로 같거나 달라질 수 있고 각각은 수소원자 또는 저급 알킬기를 표시한다), 또는 식의 기(t는 0이거나 1 또는 2의 정수이고, R13은 수소원자 또는 저급알킬기를 표시한다)를 표시하고; R2는 식 :의 기(R14, R15및 R16은 서로 같거나 다를 수 있고 각각은 수소원자, 또는 알킬, 시클로알킬, 알케닐 또는 알킬옥시알킬기를 표시하고, 달리, R15와 R16은 이들이 결합되는 질소원자와 함께 고리를 형성한다), 식 :의 기(R17은 알킬기를 표시한다), -NH-R18의 기(R18은 알킬기를 표시한다) 또는 식:의 기(R19는 알킬기를 표시하고 n은 1 내지 3의 정수이다)를 표시하고; R3은식 : -(CH2)p-X-(CH2)m-Y의 기(X는 식 :기를 표시하고, p는 0 또는 1이고; m은 1 내지 6의 정수이고; Y는 치환기를 가질수도 있는 1 내지 4개의 질소원자를 가지는 5- 또는 6-원 방향족 헤테로시클릭기, 치환기를 가질수도 있는 1 내지 3개의 질소원자를 가지는 5- 또는 6-원 포화 헤테로 시클릭기 또는 저급 알콕시기이다), 식 :의 기(V는 식 :의 기를 표시하고 ; q와 s는 각각 1 내지 6의 정수이고; R20은 수소원자 또는 저급알킬기를 표시하고; W는 Y의 정의와 같다)를 표시하고; A는 식 :의 기(R6은 수소원자, 저급알킬기, 할로겐원자 또는 식 : -(CH2)p-X-(CH2)m-Y의 기(p, X, m 및 Y는 상기에서 정의한 바와 같다)를 표시한다]또는 식: -N=의 기를 표시하고; B는 식:의 기[R4은 수소 또는 할로겐원자 또는 식; -(CH2)p-X-(CH2)m-Y의 기(p, X, m 및 y는 상기에서 정의한 바와 같다)의 크기를 표시한다] 또는 식 : -N=의 표시하고; 그리고 R5는 수소원자, 저급알킬기 또는 -(CH2)p - X-(CH2)m-Y의 기(p, X, m 및 Y는 상기에서 정의한 바와 같다)의 기를 표시하고; R1, 및 R4, R5및 R6에 대한 상기의 정의이외에 R1, R4, R6은 이들이 결합된 상호 인접한 탄소원자와 함께 치환될 수도 있는 벤젠고리를 형성한다.
  2. 제 1항에 있어서, A는 -CR6=이고 B는 -CR4=이고 벤젠유도체인 것을 특징으로 하는 유도체 또는 약리학적 허용 염.
  3. 제 1항에 있어서, A는 -CR6=이고 B는 -N=이고 피리딘 유도체인 것을 특징으로 하는 유도체 또는 약리학적 허용 염.
  4. 제 1항에 있어서, A와 B는 -N=이고 피리미딘 유도체인 특징으로 하는 유도체 또는 약리학적 허용 염.
  5. 제 1항에 있어서, 일반식:
    의 벤젠 유도체인 것을 특징으로 하는 유도체 또는 약리학적 허용 염.
    상기 식에서 Ra는 식: -NR7R8의 기 또는 저급 알킬을 표시하고 여기서 R7과 R8은 서로 같거나 다를 수 있고 각각은 수소원자 또는 저급 알킬기를 표시하고 : R16은 수소원자, 알킬, 시클로알킬, 알케닐 또는 알킬옥시알킬기를 표시하고: M은 1 내지 6의 정수이고: 그리고 Y는 치환될 수 있는, 1 내지 4개의 질소원자를 가지는 5- 또는 6- 원방향족 헤테로-모노시클릭, 치환될 수 있는, 1 내지 3개의 질소원자를 가지는 5- 또는 6원 포화 헤테로-모노시클릭기 또는 저급알콕시기를 표시한다.
  6. 제 5항에 있어서, Ra는 메틸기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  7. 제 5항에 있어서, Ra는 디메틸아미노기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  8. 제 5항에 있어서, R16은 탄소수가 1 내지 6인 알킬기인 것을 특징으로 하는 벤젠 유도체 또는 약리학적 허용 염.
  9. 제 5항에 있어서, R16은 탄소수가 2 내지 4인 알킬기인 것을 특징으로 하는 벤젠 유도체 또는 약리학적 허용 염.
  10. 제 5항에 있어서, Y는 치환될 수 있는 아미다졸릴기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  11. 제 5항에 있어서, Y는 저급 알킬기, 할로겐원자 또는 페닐기로 치환될 수 있는 이미다졸릴기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  12. 제 5항에 있어서, Y는 탄소수가 1 내지 6인 저급알킬기, 할로겐원자 및 페닐기로 구성되는 군으로부터 선택되는 치환기를 가지는 이치환-이미다졸릴기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  13. 제 5항에 있어서, Ra는 메틸이고, R16은 탄소수가 1 내지 6인 알킬기이고, M은 1 내지 6의 정수이고, Y는 치환기를 가질 수 있는 이미다졸릴기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  14. 제 5항에 있어서, Ra는 메틸이고, R16은 탄소수가 2 내지 4인 알킬기이고, M은 1 내지 6의 정수이고, Y는 탄소수가 1 내지 6인 저급알킬기, 할로겐원자 및 페닐기로 구성되는 군으로부터 선택되는 하나 또는 그 이상의 치환기를 가질 수 있는 이미다졸릴기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  15. 제 5항에 있어서, Y는 치환기를 가지는 피페라지닐기인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  16. 제 5항에 있어서, 식:
    으로 표시되고 N-[2-{3-(5-에틸-4-페닐-1H-이미다졸-1-일)프로폭시}-6-메틸]페닐-N'-부틸우레아인 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  17. 제 5항에 있어서, N-[6-N, N-디메틸아미노-2-{3-(4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-펜틸우레아
    N-[6-N, N-디메틸아미노-2-{3-(4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-부틸우레아
    N-[6-N, N-디메틸아미노-2-{3-(5-메틸-4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-부틸우레아
    N-[6-N, N-디메틸아미노-2-{3-(4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-헥실우레아
    N-[6-(4-(4-페닐-1H-이미다졸-1-일)부틸}-2-N, N-디메틸아미노]페닐-N'-부틸우레아
    N-[6-메틸-2-{3-(4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-부틸우레아
    N-[6-N, N-디메틸아미노-2-{3-(4-페닐피페라진-1-일)프로폭시}]페닐-N'-펜틸우레아
    N-[6-메틸-2-[3-{5-(1-메틸에틸)-4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-부틸우레아
    N-[6-메틸-2-[3-{5-클로로-4-이미다졸-1-일)프로폭시}]페닐-N'-펜틸우레아
    N-[6-메틸-2-[3{5-메틸-4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-펜틸우레아
    N-[6-에틸-2-[3-{5-메틸-4-페닐-1H-이미다졸-1-일)프로폭시}]페닐-N'-펜틸우레아
    로 구성된 군으로부터 선택된 것을 특징으로 하는 벤젠 유도체 또는 그것의 약리학적 허용 염.
  18. 제 1항의 벤젠, 피리딘, 또는 피리미딘 유도체 또는 이들의 약리학적 허용 염 및 약리학적 허용 담체로 이루어진 것을 특징으로 하는 약학적 조성물.
  19. 유효성분으로서 제 1항의 벤젠, 피리딘 또는 피리미딘 유도체 또는 약리학적 허용염을 함유하는 것을 특징으로 하는 ACAT효소 저해제.
  20. 유효성분으로서 제 1항의 벤젠, 피리딘 또는 피리미딘 유도체 또는 약리학적 허용염을 함유하는 것을 특징으로 하는, ACAT효소 저해작용이 효과적인 질병의 치료제.
  21. 유효성분으로서 제 1항의 벤젠, 피리딘 또는 피리미딘 유도체 또는 약리학적 허용염을 함유하는 것을 특징으로 하는, ACAT효소 저해작용이 효과적인 질병의 치료방법.
  22. 제 1항이 벤젠, 피리딘 또는 피리미딘 유도체 또는 이들의 약리학적 허용 염의 치료효과량을 투여하는 것으로 이루어지는 것을 특징으로 하는, ACAT효소 저해작용이 효과적인 질병의 치료방법.
  23. 제 22항에 있어서, 질병이 동맥경화인 것을 특징으로 하는 질병의 치료방법.
    ※ 참고사항: 최초출원 내용에 의하여 공개하는 것임.
KR1019910016674A 1990-09-25 1991-09-25 벤젠, 피리딘 및 피리미딘 유도체 KR940003494B1 (ko)

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US5668136A (en) 1997-09-16
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PH31028A (en) 1997-12-29
IE75733B1 (en) 1997-09-24
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