KR900014365A - 신규의 벤즈이미다졸 및 아자벤즈이미다졸 유도체, 이들의 제조방법, 합성 중간체 및 이들을 함유하며 특히 심장 혈관계 질환과 십이지장 궤양의 치료에 유효한 약리적 조성물 - Google Patents

신규의 벤즈이미다졸 및 아자벤즈이미다졸 유도체, 이들의 제조방법, 합성 중간체 및 이들을 함유하며 특히 심장 혈관계 질환과 십이지장 궤양의 치료에 유효한 약리적 조성물 Download PDF

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KR900014365A
KR900014365A KR1019900002790A KR900002790A KR900014365A KR 900014365 A KR900014365 A KR 900014365A KR 1019900002790 A KR1019900002790 A KR 1019900002790A KR 900002790 A KR900002790 A KR 900002790A KR 900014365 A KR900014365 A KR 900014365A
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lower alkyl
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hydrogen atom
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브뤼-마니에 니꼴
귄고르 띠뮈르
라크랑쁘 쟝
로네이 미셀
뛸롱 쟝-마리
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기 부르댕
라보라또아르 위 뻬 에쓰 아
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    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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Abstract

내용 없음

Description

신규의 벤즈이미다졸 및 아자벤즈이미다졸 유도체, 이들의 제조방법, 합성 중간체 및 이들을 함유하며 특히 심장 혈관계 질환과 십이지장 궤양의 치료에 유효한 약리적 조성물.
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (25)

  1. 다음 일반식(Ⅰ)로 표시되는 벤자이미다졸 및 아자벤즈이미다졸 유도체와 그의 호변이성체 형태 및 약리적으로 유리하게 허용되는 그의 산부가염:
    상기식중 -Y는 벤즈이미다졸 또는 아자벤즈이미다졸의 4-,5-,6- 또는 7-위에 위치하고 할로겐, OR2, SR5, COOR5, NHR5, NHCOR5또는 COR5기 (R5는 수소원자 또는 저급알킬래디칼임)로 치환되거나 치환되지않은 저급알킬래디칼, 할로겐, COR5, OR5, SR5또는 COOR5기(R5는 상기 정의한 바와 같음)로 치환되거나 치환되지 않은 이미다졸, 벤즈이미다졸, 트리아졸 또는 이미다조티아졸 유도체이고; -Z는 벤즈이미다졸 또는 아자벤즈이미다졸에 직접 결합하거나 또는 질소원자를 통해 간접결합되고 저급알킬래디칼도 치환되거나 치환되지 않은 페닐 또는 피리딜환, 특히 아닐린 또는 아미노피리딘, 특히 하나이상의 저급알킬래디칼, 하나이상의 할로겐원자, 하나이상의 OR5, SR5, SOR5NHCOR5또는 NHR5기(R5는 상기 정의한 바와 같음) 또는 질소, 산소 및 황중에서 선택된 헤테로원 1-3개를 함유하는 5-내지 10-원 헤테로환으로 치환되거나 치환되지 않은 페닐 또는 피리딜환이거나, 또는 Z는 OH,SH,SR6또는 SOR6기가 될 수 있고 이때 R6은 저급알킬, C2-C8-알케닐이며 특히 알릴, 또는 C2-C8-알키닐, 특히 프로파르길이다; -R1및 R2는 각각 수소원자, 할로겐원자, CF3, NO2, NHR4, NHCOR4, OR4또는 SR4기(R4수소원자 또는 저급 알킬래디칼임)또는 저급알킬이고 벤즈이미다졸 또는 아자벤즈이미다졸의 4-,5-,6- 또는 7-위에 위치할 수 있으며;-R3은 수소원자이고 만약 Z가 OH, SH, SR6또는 SOR6기라면 저급알킬래디칼 또는 벤질기가 될 수 있고; -A,B,T 및 W는 탄소원자 또는 질소와 같은 헤테로원일 수 있다.
  2. 제 1항에 있어서, Y가 이미다졸인 것이 특징인 유도체.
  3. 제 1항 또는 2항에 있어서, Z가 피리딜 래디칼, 특히 피리드 -4-일 인 것이 특징인 유도체.
  4. 제 1항 또는 2항에 있어서, Z가 아미노피리딘이고 특히 4-아미노피리딘인 것이 특징인 유도체.
  5. 제 1항 또는 2항에 있어서, Z가 OH기인 것이 특징인 유도체.
  6. 제 1항 또는 2항에 있어서, Z가 SH기인 것이 특징인 유도체.
  7. 제 1항 또는 6항중 어느 한 항에 있어서, R1이 수소인것이 특징인 유도체.
  8. 제 1항 또는 6항중 어느 한 항에 있어서, R1이 C1-C6저급알킬래디칼, 특히 바람직하게는 6-위 또는 7-위의 메틸인 것이 특징인 유도체.
  9. 제 1항 또는 6항중 어느 한 항에 있어서, R1이 염소 원자인 것이 특징인 유도체.
  10. 제 1항 또는 6항중 어느 한 항에 있어서, R1이 트리플루오로메틸기인 것이 특징인 유도체.
  11. 제 1항 또는 10항중 어느 한 항에 있어서, R2가 수소 원자인 것이 특징인 유도체.
  12. 제 1항 또는 10항중 어느 한 항에 있어서, R2가 메틸래디칼인 것이 특징인 유도체.
  13. 제 1항 내지 12항중 어느 한 항에 있어서, Z가 OH 또는 SH기인 경우 R3가 이소프로필 래디칼인 것이 특징인 유도체.
  14. 제 1항 내지 13항중 어느 한 항에 있어서, W가 질소원자인 것이 특징인 유도체.
  15. 제 1항 내지 14항중 어느 한 항에 있어서, B 및 W가 질소원자 것이 특징인 유도체.
  16. 제 1항, 2항, 3항, 8항, 11항 및 13항 내지 15항중 어느 한 항에 있어서, R1이 저급래디칼, 특히 7-위의 메틸이고, R2는 수소원자, Y는 이미다졸릴 래디칼이고 Z는 피리드-4-일 래디칼인 것이 특징인 유도체.
  17. 제 1항 내지 16항중 어느 한 항에 있어서, 다음 구조식의 생성물들로부터 선택됨을 특징으로 하는 유도체
  18. 다음의 화학 구조식을 갖는 신규의 벤즈이미다졸 유도체.
  19. 우레아, 티오우레아, 이황화탄소, 방향족 또는 피리딘 알데히드(이 경우 산화반응 수반), 방향족 또는 피리딘산 염화물, 벤조산 또는 피리딘산, 방향족 또는 피리딘 니트릴, 방향족 또는 피리딘 디티오카르바메이트, 방향족 또는 피리딘 이소티오시아네이트 또는 방향족 또는 피리딘 이미도디티오카르보네이트를 다음 일반식(Ⅱ)의 디아미노 화합물과 반응시킴을 특징으로 하는, 청구범위 제1항 내지 18항중 어느 한 항에 따른 일반식(Ⅰ)의 화합물의 제조방법:
    상기식중;R1및R2는 각각 수소원자, 할로겐원자, CF2, NO5, NHR4, NHCOR4, OR4또는 SR4기 (R4는 수소원자 또는 저급알킬래디칼) 또는 저급알킬이고;R3은 수소원자, 저급알킬 또는 벤질기이며;Y는 할로겐, OR5, SR5, COOR5, NHR5, NHCOR5또는 COR5기 (R5는 수소원자 또는 저급알킬래디칼임)로 치환되거나 치환되지 않은 저급알킬래디칼, 할로겐, COR5, OR5, SR5, 또는 COOR5(R5는 상기 정의한 바와 같음)에 의해 치환되거나 치환되지 않은 이미다졸, 벤즈이미다졸, 트리아졸 또는 이미다조티아졸 유도체임.
  20. 제 1항 내지 18항중 어느 한 항에 정의된 해당 화합물(Ⅰ)의 제조에 유용한, 제19항에 기재된 바와 같은 일반식(Ⅱ)의 합성 중간체.
  21. 제 1항 내지 18항중 어느 한 항에 정의된 일반식(Ⅰ)의 적어도 한가지 화합물 또는 약리적으로 허용되는 그의 산부가염의 약리적 유효량으로 이루어지며, 약리적으로 허용되는 부형제, 운반체 또는 담체에 혼입되거나 혼입되지 않는 약리적 조성물.
  22. 제 1항 내지 18항중 어느 한 항에 정의된 일반식(Ⅰ)의 적어도 한가지 화합물 또는 약리적으로 허용되는 그의 산부가염의 약리적 유효량으로 이루어지며, 약리적으로 허용되는 부형제, 운반체 또는 담체에 혼입되지 않은, 심장혈관계 활성을 갖는 약리적 조성물.
  23. 제 1항 내지 18항중 어느 한 항에 정의된 일반식(Ⅰ)의 적어도 한가지 화합물 또는 약리적으로 허용되는 그의 산부가염의 약리적 유효량으로 이루어지며, 약리적으로 허용되는 부형제, 운반체 또는 담체와 혼입되거나 혼입되지않은, 분비 및/또는 궤양 억제활성을 갖는 약리적 조성물.
  24. 제 1항 내지 18항중 어느 한 항에 정의된 일반식(Ⅰ)의 적어도 한가지 화합물 또는 적당한 경우 약리적으로 허용되는 그의 산부가염의 약리적 유효량을 허용하는 부형제, 운반체 또는 담체에 혼입시키는 것으로 되는, 치료 조성물의 제조방법.
  25. 제24항에 있어서, 심장혈관계, 강심, 혈관확장, 항고혈압 및 혈소판 응집 억제 활성이나 분비 또는 궤양 억제 활성을 갖는 약리적 조성물을 제조하는 것이 특징이 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900002790A 1989-03-03 1990-03-03 신규의 벤즈이미다졸 및 아자벤즈이미다졸 유도체, 이들의 제조방법, 합성 중간체 및 이들을 함유하며 특히 심장 혈관계 질환과 십이지장 궤양의 치료에 유효한 약리적 조성물 KR900014365A (ko)

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FR8902833 1989-03-03
FR8902833A FR2643903A1 (fr) 1989-03-03 1989-03-03 Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux

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AU5061190A (en) 1990-09-06
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NZ232621A (en) 1991-02-26
ZA901602B (en) 1990-12-28
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CA2011222A1 (en) 1990-09-03
IL93508A0 (en) 1990-11-29

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