KR920703513A - 단백질 활성효소 c(protein kinase c)를 방해하는 비스-(하이드록시알킬아미노)-안트라퀴논 - Google Patents

단백질 활성효소 c(protein kinase c)를 방해하는 비스-(하이드록시알킬아미노)-안트라퀴논

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KR920703513A
KR920703513A KR1019920701572A KR920701572A KR920703513A KR 920703513 A KR920703513 A KR 920703513A KR 1019920701572 A KR1019920701572 A KR 1019920701572A KR 920701572 A KR920701572 A KR 920701572A KR 920703513 A KR920703513 A KR 920703513A
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비이. 지앙 잭
조지 존슨 매리
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클레이턴 아이. 턴칸
스핑크스 파마슈티칼스, 코포레이션
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Abstract

내용 없음

Description

단백질 활성효소 C(PROTEIN KINASE C)를 방해하는 비스-(하이드록시알킬아미노)-안트라퀴논
[도면의 간단한 설명]
제1도는 본 발명의 화합물의 합성에 이용되는 도표 I의 합성 루트를 보여준다.
제2도는 본 발명의 화합물의 합성에 이용되는 도표 II의 합성 루트를 보여준다.
제3도는 본 발명의 화합물의 합성에 이용되는 도표 III의 합성 루트를 보여준다.
제4도는 대조구의 MCF-7종양무게와 화합물 1b-1로 처리된 생쥐(mice)대 날마다의 이식 종양의 평균값에 대한 그래프를 보여준다. 생쥐 대조구용의 종양 크기는 검은 원이다; 시험된 생쥐의 종양무게는 검은 사각형이다.
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. 하기의 식을 가지는 치환 안트라퀴논
    식에서 R1과 R2는 독립적인 H, C1-C10알킬, 아릴, 아릴알킬, 알킬아릴, 또는 질소를 포함하는 부가적인 헤테로원자들을 함유하는 치환되거나 치환되지 않은 사이클릭 링(cyclic ring)을 형성하는 주위의 질소 원자를 가지는 R1과 R2; m과 n은 독립적인 1,2 또는 3; A는 할로겐, OH, 알콕시, OCO(NR3R4), S-C(NH2)=NR5, 또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4, 및 R5는 독립적으로 H, 알킬, 또는 아릴; X는 H, OH, NR6R7, Cl, Br, I, F, 알킬, 아릴, 알콕시, 아릴록시, COOR8또는 CONR9R10; 그리고 R6, R7, R8, R9및 R10은 독립적인 H, 저가 알킬 또는 아릴인 것을 특징으로 하는 치환 안트라퀴논.
  2. 제1항에 있어서, R1과 R2는 독립적으로 H, 또는 저가 알킬; m 과 n은 독립적인 1, 또는 2; A는 할로겐, OCO(NR3R4), S-C(NH2)=NR5, 또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4, 및 R5는 독립적으로 H, 또는 알킬; X는 H, OH, Cl, Br, I, F 또는 알콕시인 것을 특징으로 하는 치환 안트라퀴논.
  3. 제2항에 있어서, R1과 R2는 독립적으로 H, 또는 아릴알킬; m과 n은 1;A는 Cl, Br, OCO(NR3R4), S-C(NH2)=NR5또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4및 R5는 독립적으로 H; X는 H, OH인 것을 특징으로 하는 치환 안트라퀴논.
  4. 제1항의 치환된 안트라퀴논으로 구성되는 단백질 활성효소 C를 방해하는 약제적 조성물과 약제적으로 수용가능한 운반체 또는 희석제.
  5. 제2항의 치환된 안트라퀴논으로 구성되는 단백질 활성효소 C를 방해하는 약제적 조성물과 약제적으로 수용가능한 운반체 또는 희석제.
  6. 제3항의 치환된 안트라퀴논으로 구성되는 단백질 활성효소 C를 방해하는 약제적 조성물과 약제적으로 수용가능한 운반체 또는 희석제.
  7. 하기식으로 이루어지는 치환된 안트라퀴논의 방해량을 가지는 단백질 활성 효소 C와 접촉하는 것으로 구성된 단백질 활성 효소 C의 방해 방법.
    식에서 R1과 R2는 독립적인 H, C1-C10알킬, 아릴, 아릴알킬, 알킬아릴, 또는 질소를 포함하는 부가적인 헤테로원자들을 함유하는 치환되거나 치환되지 않은 사이클릭 링(cyclic ring)을 형성하는 주위의 질소 원자를 가지는 R1과 R2; m과 n은 독립적인 1,2 또는 3; A는 할로겐, OH, 알콕시, OCO(NR3R4), S-C(NH2)=NR5, 또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4, 및 R5는 독립적으로 H, 알킬, 또는 아릴; X는 H, OH, NR6R7, Cl, Br, I, F, 알킬, 아릴, 알콕시, 아릴록시, COOR8또는 CONR9R10; 그리고 R6, R7, R8, R9및 R10은 독립적인 H, 저가 알킬 또는 아릴인 것을 특징으로 하는 치환 안트라퀴논을 이용한 단백질 활성효소 C의 방해방법.
  8. 제7항에 있어서, 상기한 식의 화합물의 R1과 R2는 독립적으로 H, 또는 저가 알킬; m과 n은 독립적인 1, 또는 2; A는 할로겐, OCO(NR3R4), S-C(NH2)=NR5, 또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4, 및 R5는 독립적으로 H, 또는 알킬; X는 H, OH, Cl, Br, I, F 또는 알콕시인 것을 특징으로 하는 치환 안트라퀴논을 이용한 단백질 활성효소 C의 방해방법.
  9. 제8항에 있어서, 상기한 식의 화합물의 R1과 R2는 독립적으로 H, 또는 저가 알킬; m과 n은 1; A는 Br, Cl, OCO(NR3R4), S-C(NH2)=NR5또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4및 R5는 독립적으로 H; X는 H, 또는 OH인 것을 특징으로 하는 치환 안트라퀴논을 이용한 단백질 활성효소의 C의 방해방법.
  10. 하기 식의 화합물을 이용하여
    식에서 R1과 R3는 독립적인 H, C1-C10알킬, 아릴, 아릴알킬, 알킬아릴, 또는 질소를 포함하는 부가적인 헤테로원자들을 함유하는 치환되거나 치환되지 않은 사이클릭 링(cyclic ring)을 형성하는 주위의 질소 원자를 가지는 R1과 R2; m과 n은 독립적인 1,2 또는 3; A는 할로겐, OH, 알콕시, OCO(NR3R4), S-C(NH2)=NR5, 또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4, 및 R5는 독립적으로 H, 알킬, 또는 아릴; X는 H, OH, NR6R7, Cl, Br, I, F, 알킬, 아릴 알콕시, 아릴록시, COOR8, 또는 CONR9R10; 그리고 R6, R7, R8, R9및 R10은 독립적인 H, 저가 알킬 또는 아릴을 단백질 활성효소 C용의 약제의 준비에 이용하는 것을 특징으로 하는 치환 안트라퀴논.
  11. 제10항에 있어서, 식에서 R1과 R2는 독립적으로 H, 또는 저가 알킬; m과 n은 독립적인 1, 또는 2; A는 할로겐, OCO(NR3R4), S-C(NH2)=NR5, 또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4, 및 R5는 독립적으로 H, 또는 알킬; X는 H, OH, Cl, Br, I, F 알콕시를 이용하는 것을 특징으로 하는 치환 안트라퀴논.
  12. 제11항에 있어서, 식에서 R1과 R2는 저가 알킬; m과 n은 1; A는 Cl, Br, OCO(NR3R4), S-C(NH2)=NR5또는 m=1일때 부가적인 산소원자를 갖는 옥시란 링(oxiran ring); R3, R4및 R5는 H; X는 H, 또는 OH를 이용하는 것을 것을 특징으로 하는 치환 안트라퀴논.
  13. 제10항에 있어서, 상기 화합물은 치료적인 양 내에서 약제 내에 존재하는 것을 특징으로 하는 치환 안트라퀴논.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920701572A 1990-11-02 1991-10-30 단백질 활성효소 c(protein kinase c)를 방해하는 비스-(하이드록시알킬아미노)-안트라퀴논 KR920703513A (ko)

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US60917990A 1990-11-02 1990-11-02
US609,179 1990-11-02
US07/609,252 US5204370A (en) 1990-11-05 1990-11-05 Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase C
US609,252 1990-11-05
PCT/US1991/008026 WO1992007557A1 (en) 1990-11-02 1991-10-30 Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase c

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AU9039891A (en) 1992-05-26
WO1992007557A1 (en) 1992-05-14
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CA2072889A1 (en) 1992-05-03
AU637014B2 (en) 1993-05-13
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EP0507938A1 (en) 1992-10-14
EP0507938A4 (en) 1993-03-10

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