KR950017928A - 아세트산 유도체 - Google Patents

아세트산 유도체 Download PDF

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KR950017928A
KR950017928A KR1019940032546A KR19940032546A KR950017928A KR 950017928 A KR950017928 A KR 950017928A KR 1019940032546 A KR1019940032546 A KR 1019940032546A KR 19940032546 A KR19940032546 A KR 19940032546A KR 950017928 A KR950017928 A KR 950017928A
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lower alkyl
group
hydrogen
alkoxy
alkyl
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KR100335541B1 (ko
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알리히 레오
하드바리 파울
휘르젤러 뮐러 마리안네
뮐러 마르셀
스타이너 베아트
벨러 토마스
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프리돌린 클라우스너, 롤란드 보러
에프. 호프만-라 롯슈 아크티엔게젤샤프트
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Abstract

하기 일반식( I )의 아세트산 유도체는 혈소판에 유착성 단백질의 결합 및 혈소판 응집 및 세포-세포 유착에 의해 야기된 질병의 치료 또는 예방에 유용할 수 있다. 이들은 상응하는 보호된 화합물의 보호 그룹을 분리하거나 또는 사용하는 니트릴에서 시아노 그룹을 아미디노 그룹으로 전환시키므로써 제조할 수 있다.
(상기식에서, L, M, T 및 Q는 명세서에 개시한 바와 같은 의미를 갖는다.

Description

아세트산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (2)

  1. 하기 일반식( I )의 아세트산 유도체, 그의 수화물 또는 용매화물 및 생리학적으로 유용한 그의 염;
    I
    상기식에서, L은 하기 일반식 L1내지 L5의 그룹이고,
    L1
    L2
    L3
    L4
    L5
    이때, L그룹 및/또는 아미드 형태로 결합되지 않은 L과 M그룹사이에 존재하는 카보닐 그룹은 또한 옥심으로 존재할 수 있고, A는 하기 일반식 A1내지 A4의 그룹이고;
    A1
    A2
    A3
    A4
    [이때, E1및 E2는 수소, 저급 알킬, 하이드록시, 저급 알콕시, 저급 알콕시-저급 알킬, 카복시-저급알킬, p(O)(O-저급 알킬)2,C(O)OR1, OC(O)R1, OC(O)OR1또는 C(O)SR1이나, 단 E1및 E2중 적어도 하나는 수소이거나, 또는 E1및 E2는 이들이 결합된 질소 원자와 함께 (5,5-디메틸 또는 5-옥소)-4,5-디하이드로-1,2,4-옥사디아졸-3-일 그룹을 형성하고, R1은 저급 알콕시-저급 알킬: 저급 알킬 OH, COOH, 저급 알콕시카보닐, 저급 알카노일옥시, 저급 알케노일옥시로 치환된 저급 알킬, 임의 치환 도니 벤조일옥시로 치환된 저급 알킬 도는 저급 알길-CONH에 의해 치환된 저급 알킬: 또는 임의 치환되고 저급 알킬렌에 의해 임의 결합된 페닐; 또는 0에 의해 임의로 차단된 사이클로알킬이고, 이때 X 및 Y중 하나는 CH이고, 다른 하나는 CH, C-저급 알킬, C-저급 알콕시 또는 N이고, D는 (CH2)s또는 (CH2)1O 그룹이고, s는 1 내지 4이과, m 및 n은 0 내지 5이고, t는 0 내지 3이나, m+n은 1 내지 5이고, m+t 및 n+t는 각각 적어도 1이고, p 및 q는 0 내지 5이나, p+q는 2 내지 5이고, W1은 CH2,알킬-CH, 저급 알킬-OC(O)CH, NH, 저급 알킬-N 또는 저급 알콕시-저급 알킬-N이고, W2는 O, NH, 아실-N 또는 저급 알킬-OC(O)-N이고, G는 H 또는 α-아미노카복실산의 특징 부여 그룹이다] M은 N원자에 의해 케토 그룹에 결합된 1,4-피페리디닐렌; 또는 저급 알킬, 저급 알콕시, OCH2COOH 또는 OCH2COO 저급 알킬로 임의 치환된 1,4-페닐렌이고, Q는 O, CH2, NH, 아실-N 또는 저급 알킬 OC(0)N이고, T는 NH2, NH-저급 알킬, NH-저급 알킬(COOH 또는 COO-저급 알킬); 저급 알콕시 COOH, COO-저급 알킬, 저급 알킬-COO 또는 저급 알킬-OCOO에 의해 치환된 저급 알콕시 또는 저급 알케닐옥시; 또는 OT' 그룹이고, T'는 수소; 저급 알킬; 저급 알킬렌에 의해 임의 결합된 페닐 또는 피리딜: 또는 저급 알킬렌에 의해 임의 결합되고, O, NH 또는 NCOO-저급 알킬로 임의의 차단된 사이클로알킬이나, 단, a) L이 하기 일반식(L')의 그룹이고:
    (이때, A는 하기 일반식(A')의 그룹이고:
    E1및 E2중 하나는 수소이고, 다른 하나는 수소, 1-부톡시카보닐 또는 벤질옥시카보닐이고, X 및 Y 중 하나는 CH이고, 다른 하나는 CH 또는 N이고, W1은 NH, 저급 알킬-N 또는 저급 알콕시-저급 알킬 -N이고, G는 상기와 갈은 의미를 갖는다) M이 N원자에 의해 케토 그룹에 곁합된 1,4-피페리디닐렌이고, Q가 O인 경우, T'는 수소, 저급 알킬 및 페닐-저급 알킬이 아니고, b) L이 L11, L31또는 L41의 그룹이과 :
    (이때, A는 하기 일반식(A1)의 그룹이고,
    E1및 E2중 하나는 수소이고, 다른 하나는 수소, t-부톡시카보닐 또는 벤질옥시카보닐이고, X 및 Y중 하나는 CH이고, 다른 하나는 CH, C- 저급 알킬, C- 저급 알콕시 또는 N이고, R0및 G0는 수소 또는 저급 알킬이고, W4는 C=O 또는 C=NOH이다.) M이 저급 알킬, 저급 알콕시, OCH2COOHO 또는 CH2COOH- 저급 알킬로 임의 치환된 1,4-페닐렌이고, Q가 O, CH2, 또는 NH인 경우, T'는 수소, 저급 아킬, 페닐 및 페닐-저급 알킬이 아니다.
  2. 활성 물질로 제1항의 화합물을 함유하는, 혈소판에 유착성 단백질의 결합 및 혈소판 응집 및 세포-세포 유착에 의해 야기되는 질병의 치료 또는 예방에 유용한 약제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940032546A 1993-12-03 1994-12-02 아세트산유도체 KR100335541B1 (ko)

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