KR880012549A - 신규의 치환된 아닐리드 유도체 - Google Patents

신규의 치환된 아닐리드 유도체 Download PDF

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KR880012549A
KR880012549A KR1019880004060A KR880004060A KR880012549A KR 880012549 A KR880012549 A KR 880012549A KR 1019880004060 A KR1019880004060 A KR 1019880004060A KR 880004060 A KR880004060 A KR 880004060A KR 880012549 A KR880012549 A KR 880012549A
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group
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lower alkyl
phenyl
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기미유끼 시부야
요시오 다까하시
세이이찌 사또오
히로미찌 시교
도미오 오오따
야스미 우찌다
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미와 다까야스
고오와 가부시끼가이샤
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Publication of KR880012549A publication Critical patent/KR880012549A/ko

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Abstract

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Description

신규의 치환된 아닐리드 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (23)

  1. 하기 일반식(Ⅰ)의 치환된 아닐리드 유도체 또는 그의 산부가염.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하며 치환체를 가질 수도 있는 단핵 또는 2헥헤테로환식기를 표시하고, A는 단일 결합, 카르보닐기, 황원자이거나, 또는 히드록실기로 치환될 수도 있는 저급 알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 돌일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유 복소환식기를 형성할 수도 있고, B는 단일 결합이나 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  2. 제1항에 있어서, R1이 1~3질소원자를 고리구성원으로 함유하며, 및 저급알콕시카르보닐기, 니트로옥시-저급알킬-아미노카르보닐기, 저급알킬-아미노카르보닐기, 저급 알킬티오기 및 저급 알킬술피닐기로 구성된 군에서 선택되는 치환체를 가질 수도 있는 4- 내지 10-원 단핵 또는 2핵 헤테로환식기 또는 그의 N-옥사이드를 표시함을 특징으로 하는 화합물.
  3. 제2항에 있어서, 헤테로환식기가 피리딜, 이미다졸릴 또는 이미다졸피리딜기임을 특징으로 하는 화합물.
  4. 제3항에 있어서, 헤테로환식기가 피리딜기임을 특징으로 하는 화합물.
  5. 제1항에 있어서, R1이 피리딜기임을 특징으로 하는 화합물.
  6. 제1항에 있어서, A가 단일 결합임을 특징으로 하는 화합물.
  7. 제1항에 있어서, R2가 저급알킬기, 알릴옥시기, 저급알콕시기, 또는 2,2,2-트리플루오로에톡시기임을 특징으로 하는 화합물.
  8. 제1항에 있어서, R2가 저급알콕시기임을 특징으로 하는 화합물.
  9. 제1항에 있어서,가 아미노기, 디(저급알킬)아미노기, 페닐아미노기 또는 (저급알콕시-치환된 페닐)저급알킬기이거나, 또는 4- 내지 7-원 포화질소-함유복소환식기를 표시함을 특징으로 하는 화합물.
  10. 제1항에 있어서, R3및 R4양자가 수소원자임을 특징으로 하는 화합물.
  11. 제1항에 있어서, B가 직쇄 또는 측쇄 저급 알킬렌기임을 특징으로 하는 화합물.
  12. 제1항에 있어서, B가 @임을 특징으로 하는 화합물.
  13. 제1항에 있어서, 기 R1-A- 및 R2-각각이 기 -NHCH-B-N에 대해 오르토-또는 메타-위치에 존재함을 특징으로 하는 화합물.
  14. 제1항에 있어서, 기 R1-A가 기 R2에 대해 따라-위치에 존재함을 특징으로 하는 화합물.
  15. 3-아미노-5'-에톡시-2'-(3-피리딜)부티르아닐리드 및 약학적으로 허용 가능한 그의 산부가염.
  16. 3-아미노-5'-알릴톡시-2'-(3-피리딜)부티르아닐리드 및 약학적으로 허용 가능한 그의 산부가염.
  17. 하기 일반식(Ⅱ)로 표시되는 아닐린 유도체를 하기 일반식(Ⅲ)으로 표시되는 아미노알킬카르복실산 또는 그 반응성 유도체와 반응시키고, 필요에 따라 결과로 생성된 화합물을 그의 산부가염으로 전환시킴을 특징으로 하는 하기 일반식(Ⅰ)의 치환된 아닐리드 유도체 및 그의 산부가염의 제조방법.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단책 또는 2핵 헤테로환식기를 표시하고, A는 단일결합, 카르보닐기, 황원자이거나, 또는 히드록실기로 치환될 수도 있는 저급알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급 알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유복소환기를 형성할 수도 있고, B는 단일결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  18. 하기 일반식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 산부가염을 함유함을 특징으로 하는 약제.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단핵 또는 2헥 헤테로환식기를 표시하고, A는 단일결합, 카르보닐기, 황원자이거나, 또는 히드록실기로 치환될 수 있는 저급 알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 크리플루오로메틸기, 저급 알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1-C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유복소환식기를 형성할 수도 있고, B는 단일결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  19. 하기 일반식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 산부가염을 함유함을 특징으로 하는 항-부정맥제.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단핵 또는 2헥 헤테로환식기를 표시하고 A는 단일결합, 카르보닐기, 황원자이거나이것이는 히드록실기로 치환될 수도 있는 저급 알킬렌기를 표시, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 치환체를 가질 수도 있는 페닐(저급을 알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포활질소-함유복소환식기를 형성할 수도 있고, B는 단일 결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  20. 하기 일반식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 산부가염을 유효량 및 약학적으로 허용가능한 희석제 또는 담체로 구성됨을 특징으로 하는 약학 조성물.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단핵 또는 2헥 헤테로환식기를 표시하고 A는 단일결합, 카르보닐기, 황원자이거나 또는 히드록실기로 치환될 수도 있는 저급 알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유복소환식기를 형성할 수도 있고, B는 단일 결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  21. 하기 일반식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 산부가염들의 질병 또는 억제 또는 방지의 용도.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단핵 또는 2헥 헤테로환식기를 표시하고 A는 단일결합, 카르보닐기, 황원자이거나 또는 히드록실기로 치환될 수도 있는 저급 알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유복소환식기를 형성할 수도 있고, B는 단일결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  22. 하기 일반식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 산부가염을 부정맥 억제 또는 방지의 용도.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단핵 또는 2헥 헤테로환식기를 표시하고 A는 단일결합, 카르보닐기, 황원자이거나 또는 히드록실기로 치환될 수도 있는 저급 알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유복소환식기를 형성할 수도 있고, B는 단일결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
  23. 하기 일반식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 그의 산부가염을 항-부정맥 활성 약제의 제조용용도.
    상기식에서 R1은 1 내지 3질소원자를 고리구성원으로 함유하고 치환체를 가질 수도 있는 단핵 또는 2헥 헤테로환식기를 표시하고 A는 단일결합, 카르보닐기, 황원자이거나 또는 히드록실기로 치환될 수도 있는 저급 알킬렌기를 표시하고, R2는 수소원자, 할로겐원자, 저급알킬기, 트리플루오로메틸기, 저급알케닐옥시기이거나, 또는 치환체를 가질 수도 있는 C1~C14알콕시기를 표시하고, R3및 R4는 동일하거나 상이하며, 각각은 수소원자, 저급알킬기, 페닐기이거나, 또는 치환체를 가질 수도 있는 페닐(저급알킬)기를 표시하거나, 또는 함께 취하여져서 이들이 결합되는 질소원자와 함께 포화질소-함유복소환식기를 형성할 수도 있고, B는 단일결합 또는 치환체를 가질 수도 있는 저급 알킬렌기를 표시한다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880004060A 1987-04-10 1988-04-09 신규의 치환된 아닐리드 유도체 KR880012549A (ko)

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BRPI0706610A2 (pt) * 2006-01-18 2011-04-05 Siena Biotech Spa moduladores de receptores alfa 7 nicotìnico acetilcolina e usos terapêuticos destes
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