KR970703324A - 신규한 피리미딘 유도체(novel pyrimidine derivative) - Google Patents

신규한 피리미딘 유도체(novel pyrimidine derivative) Download PDF

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KR970703324A
KR970703324A KR1019960706565A KR19960706565A KR970703324A KR 970703324 A KR970703324 A KR 970703324A KR 1019960706565 A KR1019960706565 A KR 1019960706565A KR 19960706565 A KR19960706565 A KR 19960706565A KR 970703324 A KR970703324 A KR 970703324A
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alkyl group
phenyl
alkyl
hydrogen atom
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하루히꼬 기꾸찌
히로아끼 사또오
류우따 후꾸또미
고헤이 이노마따
마사시 스즈끼
고이찌로 하기하라
다께오 아라이
세쯔꼬 미노
하루꼬 에구찌
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쇼오다 오사무
닛신세이훈 가부시끼가이샤
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Abstract

상기 화학식(I)로 표현되고 위장성 운동 가속제로서 유용한 피리미딘유도체 또는 약제학적으로 허용 가능한 그의 염(식 중, X는 O 또는 NR5를 나타내고; Y는 O, S 또는 NR5를 나타내며, 이때 R5는 수소원자, C1-C6알킬기등이고; R1및 R2는 각각 독립적으로 수소원자, C1-C 6 알킬기 등을 나타내며; R3는 CN 또는 COOR6을 나타내고, 이때 R6은 C1-C6알킬기, C3-C6시클로알킬기, 아릴기 등이며; R4는 -SR7또는 -NR8R9을 나타내고, 이때 R7는 C1-C6알킬기를 나타내며, R8은 C1-C6알킬기 등을 나타내고, R9는 수소원자, C1-C6알킬기 등을 나타내고 R8및 R9는 부착되어 있는 질소원자와 함께 상기 화학식(X) (식 중, R10은 C1-C6알킬기 등을 나타낸다)로 나타난 N- 치환된 피페라진 고리를 나타낸다).

Description

신규한 피리미딘 유도체(NOVEL PYRIMIDINE DERIVATIVE)
[도면의 간단한 설명]
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 하기 화학식(I)
    식 중, X는 O 또는 NR5이고; Y는 O, S 또는 NR5이며, 이때, R5는 C1-C6알킬기, C1-C6알킬카르보닐, 아릴기, 아릴 C1-C6알킬기, 아릴아미노카르보닐기, 아릴 C1-C4알킬아미노카르보닐기, 또는 C1-C6알킬아미노카르보닐기이고; R1및 R2는 동일하거나 다를 수 있고 각각 수소원자, C1-C6알킬기, C3-C6시클로알킬기, 아릴기, C3-C6시클로알킬 C1-C4알킬기, 또는 아릴 C1-C4알킬기이며; R3는 CN 또는 COOR6, 이때 R6은 C1-C6알킬기, C3-C6시클로알킬기, 아릴기, 또는 아릴 C1-C4알킬기이고; R4는 -SR7또는 -NR8R9이때, R7는 C1-C6알킬기이며; R8은 C1-C6알킬기, 아릴 C1-C4알킬기, 헤테로아릴 C1-C4알킬기, 아릴옥시 C2-C6알킬기이며, 이때, 아릴 또는 헤테로아릴 부분은 임의로 할로겐원자, C1-C6알킬기, 할로 C1-C6알킬기, C1-C6알콕시기, C1-C6알콕시카르보닐기 또는 페닐기로써 모노- 내지 트리-치환될 수 있거나, 또는 R8는 하기 화학식(II)-(IX)
    (식 중, R10은 C1-C6알킬기, 아릴 C1-C6알킬기, 헤테로아릴 C1-C6알킬기, 아릴옥시 C2-C6알킬기, 피롤리디닐카르보닐 C1-C4알킬기이며, 아릴부분은 임의로 할로겐원자, C1-C6알킬기, 할로 C1-C6알킬기, C1-C6알콕시기, C1-C6알콕시카르보닐기, 페닐기 또는 아미노기로써 치환될 수 있다)의 기로 나타나고; R11은 수소원자, C1-C6알킬기, 아릴 C1-C4알킬기 또는 아릴기이며; Z1가 및 Z2는 O, S, N(C1-C6알킬) 또는 CH2이며; Z3는 N 또는 CH이고; 1은 0-2이며; m이 0일 때, n은 4이고, m이 1일 때, n은 l 또는 3이며, m은 2일때 n은 2이고; p는 1-2이고; j는 0-3이고; k는 0-3이고; j 및 k의 합은 l-6이고; h는 1-6이며; Q는 O, NR13, CHOR14또는 OCH2CH2O이며; R12및 R13은 동일하거나 다를 수 있으며 각각 수소원자, C1-C6알킬기 또는 C2-C4알콕시 C2-C6알킬기이고; R14는 수소원자 또는 C1-C6알킬기이며; R9는 수소원자, C1-C6알킬기 또는 C1-C6알콕시 C2-C6알킬기이고; 또는 R8및 R9는 부착되어 있는 질소원자와 함께 하기 화학식(X)
    (식 중, R10은 상기 정의된 바와 같은 기를 나타낸다)의 N-치환된 피페라진 고리를 나타낼 수 있는 피리미딘 유도체 또는 약제학적으로 허용 가능한 그의 염.
  2. 제1항에 있어서, 화학식(I)에서, 식 중, X는 O 또는 NR5이고 이때, R5는 수소원자, C1-C6알킬기, C1-C6알킬카르보닐기, 페닐기, 페닐 C1-C6알킬기, 페닐아미노카르보닐기, 페닐 C1-C4알킬아미노카르보닐기, 또는 C1-C4알킬아미노카르보닐기이고; Y는 O 또는 S이고; R1및 R2는 동일하거나 다를 수 있으며 각각은 수소원자, C1-C6알킬기, C3-C6시클로알킬기, 페닐기, 나프틸기, C3-C6시클로알킬, C1-C4알킬기, 또는 페닐 C1-C4알킬기이며; R3는 CN 또는 COOR6이고, 이때 R6은 C1-C6알킬기, C3-C6시클로알킬기, 페닐기, 또는 페닐 C1-C4알킬기이고; R4는 -NR8R9이며; R8은 C1-C6알킬기, 페닐 C1-C4알킬기, 나프틸 C1-C4알킬기, 피리딜 C1-C4알킬기, 페녹시 C2-C6알킬기, 1H-인돌-3-일 C1-C4알킬기, 이때 페닐, 페녹시, 나프틸 및 1H-인돌-3-일 부분은 임의로 할로겐원자, C1-C6알킬기, 할로 C1-C6알킬기, C1-C6알콕시기, C1-C6알콕시카르보닐기 또는 페닐기로써 모노- 내지 트리-치환될 수 있으며, 또는 R8는 화학식(II)-(IX)(식 중, R10은 C1-C6알킬기, 페닐 C1-C4알킬기, 나프틸 C1-C4알킬기, 피리딜 C1-C4알킬기, 페녹시 C2-C6알킬기, 피롤리디닐카르보닐 C1-C4알킬기이며, 페닐, 페녹시 및 나프틸부분은 임의로 할로겐원자, C1-C6알킬기, 할로 C1-C6알킬기, C1-C6알콕시기, C1-C6알콕시카르보닐기 또는 페닐기로써 모노- 내지 트리- 치환될 수 있다)의 기로 나타나고; R11은 수소원자, C1-C6알킬기 또는 페닐 C1-C4알킬기, 페닐기 또는 나프틸기이며; Z1는 O, S, N(C1-C6알킬) 또는 CH2이며; Z2는 O, N(C1-C6알킬) 또는 CH2이며; Z3는 N 또는 CH이고; 1은 0-2이며; m이 0일 때, n은 4이고, m이 1일때, n은 1 또는 3이며, m은 2일때 n은 2이고; p는 l-2이고; j는 0-3이고; k는 0-3이고; j 및 k의 합은 1-6이고; h는 1-6이며; Q는 O, NR13, CHOR14또는 OCH2CH2O이며; R12및 R13은 동일하거나 다를 수 있으며 각각은 수소원자, C1-C6알킬기 또는 C1-C4알콕시 C2-C4알킬기이고; R14는 수소원자 또는 C1-C6알킬기이며; R9는 수소원자, C1-C6알킬기 또는 C1-C6알콕시 C2-C6알킬기로 표현되는 화합물 또는 약리학적으로 허용 가능한 그의 염.
  3. 제1항에 있어서, 하기 화학식(I)에서, 식중, X는 O 또는 NR5이고 이때, R5는 수소원자, C1-C6알킬기, C1-C6알킬카르보닐기, 페닐기, 페닐 C1-C6알킬기, 페닐아미노카르보닐기, 페닐 C1-C4알킬아미노카르보닐기, 또는 C1-C6알킬아미노카르보닐기이고; Y는 O 또는 S이고; R1및 R2는 동일하거나 다를 수 있으며 각각은 수소원자, C1-C6알킬기, C3-C6시클로알킬기, 페닐기, 나프틸기, C3-C6시클로알킬 C1-C4알킬기, 또는 페닐 C1-C4알킬기이며; R3는 CN 또는 COOR6이고, 이때 R6은 C1-C6알킬기, C3-C6시클로알킬기, 페닐기, 또는 페닐 C1-C4알킬기이고; R4는 -NR8R9이며; R8및 R9는 그들이 부착된 질소원자와 함께 화학식(X)(식 중, R10은 제1항에 정의된 바와 같은 기를 나타낸다)의 N-치환된 피페라진 고리를 나타내는 화합물 또는 약제학적으로 허용 가능한 그의 염.
  4. 제1항에 있어서, 화학식(I)(식중, X는 O 또는 NR5이고 이때, R5는 수소원자, C1-C6알킬기, C1-C6알킬카르보닐기, 페닐기, 아릴 C1-C6알킬기, 페닐아미노카르보닐기, 페닐 C1-C4알킬아미노카르보닐기, 또는 C1-C6알킬아미노카르보닐기이고; Y는 O 또는 S이고; R1및 R2는 동일하거나 다를 수 있으며 각각은 수소원자, C1-C6알킬기, C3-C6시클로알킬기, 페닐기, 나프틸기, C3-C6시클로알킬 C1-C4알킬기, 또는 페닐 C1-C4알킬기이며; R3는 CN 또는 COOR6이고, 이때 R6은 C1-C6알킬기, C3-C6시클로알킬기, 페닐기, 또는 페닐 C1-C4알킬기이고; R4는 -SR7이고 이때, R7은 C1-C6알킬기를 나타낸다)로 나타내는 화합물 또는 약재학적으로 허용 가능한 그의 염.
  5. 활성 성분으로서, 제1항의 화학식(I)로 나타난 화합물 또는 약재학적으로 허용 가능한 그의 염 및 필요하다면, 약제학적으로 허용 가능한 첨가물의 혼합물로 이루어진 것을 특징으로 하는 위장 활성 촉진제.
  6. 제5항에 있어서, 만성 위염, 당뇨병, 후-위절제증 및 소화성 궤양으로부터 유래한 소화 관 장애 및 역류성 식도염, 과민성 장증후군 및 가성장폐색증을 포함하는 소화관 질병의 치료에 유용한 위장 활성촉진제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960706565A 1994-05-18 1995-05-17 신규한 피리미딘 유도체(novel pyrimidine derivative) KR970703324A (ko)

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