KR920019357A - 설폰아미드 및 이의 약제로서의 용도 - Google Patents

설폰아미드 및 이의 약제로서의 용도 Download PDF

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KR920019357A
KR920019357A KR1019920007084A KR920007084A KR920019357A KR 920019357 A KR920019357 A KR 920019357A KR 1019920007084 A KR1019920007084 A KR 1019920007084A KR 920007084 A KR920007084 A KR 920007084A KR 920019357 A KR920019357 A KR 920019357A
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pyrimidinyl
hydroxyethoxy
benzenesulfonamide
chlorophenyl
tolyl
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뷰리 카스파
끌로젤 마르띤느
피쉴 발터
이르트 조르쥬
미카엘 뢰플러 베른트
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프리돌린 클라우스너,롤란트 보러
에프. 호프만-라 로슈 에이지
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Abstract

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Description

설폰아미드 및 이의 약제로서의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 순환계 질환, 특히 고혈압, 허혈증, 혈관 경련 및 협심증 치료용 약제의 제조를 위한 활성 성분으로서의 일반식(Ⅰ) 화합물 및 이의 염의 용도.
    상기식에서, R1은 수소, 저급 알킬, 저급 알콕시, 저급 알킬티오, 할로겐 또는 트리플루오로메틸이고; R2는 수소 할로겐, 저급 알콕시, 하이드록시-저급 알콕시 또는 트리플루오로메틸이며; R3은 수소, 하이드록시, 할로겐, 알킬티오, 사이클로알킬, 하이드록시-저급알킬, 하이드록시-저급 알콕시, 하이드록시아미노-저급 알킬, 저급 알케닐, 옥소-저급 알킬, 트리플루오로메틸, 트리플루오로메톡시, 저급 알콕시, 저급 알콕시-저급 알콕시 또는 아릴-저급 알콕시이거나, 또는 R2및 R3은 함께 부타디에닐을 나타내며; R4는 수소, 저급 알킬, 아릴 또는 헤테로아릴이고; R5는 수소, 저급 알카노일, 벤조일, 헤테로사이클릴-카보닐 또는 테트라하이드로피란-2-일이며; R6은 하기 일반식(a) 또는 (b)의 잔기를 나타내고;
    R7은 수소, 저급 알킬, 또는 니트로이며; R8은 수소, 할로겐, 저급 알킬, 저급 알콕시, 저급 알킬티오, 니트로, 하이드록시, 아미노 또는 트리플루오로 메틸이거나, R7및 R8은 함께 부타디에닐을 나타내고; R9는 수소, 할로겐, 저급 알킬, 저급 알콕시, 저급 알킬티오 또는 트리플루오로메틸이며; R10는 수소, 할로겐, 저급 알킬, 저급 알콕시, 또는 저급 알킬티오이고; X 및 Y는 각각 독립적으로 O, S 또는 NH를 나타내며; n은 2,3 또는 4이다.
  2. 제1항에 있어서, R4는 수소, 저급 알킬 또는 아릴이고, 나머지 라디칼은 제1항에서 정의된 바와 같은 일반식(Ⅰ)의 화합물 및 이의 염의 용도.
  3. R6이 하기 일반식(c)의 잔기를 나타내고 라디칼 R1내지 R5, X, Y 및 n은 제1항에서 정의된 바와 같은 제1항의 일반식(Ⅰ)의 화합물 및 이의 염.
    상기식에서, R11은 할로겐, 저급 알콕시, 저급 알킬티오, 또는 트리플루오로메틸이고; R12는 수소 또는 저급 알콕시이다.
  4. R4는 수소, 저급 알킬 또는 아릴이며, 나머지 라디칼은 제3항에서 정의된 바와 같은 일반식(Ⅰ)의 화합물 및 이의 염.
  5. N-〔5-(2,6-디메톡시벤질)-6-(3-하이드록시프로필)-4-피리미디닐〕-p-비닐벤젠설폰아미드, α,α,α-트리플루오로-N-〔6-(2-하이드록시에톡시)-6-(o-트리플루오로메틸)벤질〕피리미디닐〕-p-톨루엔설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-트리플루오로메틸)벤질〕-4-피리미디닐〕-p-메톡시벤젠설폰아미드, p-클로로-N-〔6-(2-하이드록시에톡시)-5-(o-트리플루오로메틸)벤질〕-4-피리미디닐〕벤젠설폰이미드, N-〔6-(2-하이드록시에톡시)-5-(0-메톡시벤질)-4-피리미디닐〕-P-비닐벤젠설폰아미드,N-〔6-(2-하이드록시에톡시)-5-(0-트리플루오로메틸)벤질〕-4-피리미디닐〕-p-(메틸티오)벤젠설폰아미드, N-〔5-(2,4-디메톡시벤질)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, rac-N-〔5-(o-메톡시 벤질)-6-〔2-〔(테트라하이드로-2H-피란-2-일)옥시〕에톡시〕-4-피리미디닐〕-p-비닐벤젠설폰아미드, rac-N-〔〔5-(o-메톡시벤질)-6-〔2-〔(테트라하이드로-2H-피란-2-일)옥시〕에톡시〕-4-피리미디닐〕설파모일〕벤즈알데히드, p-〔(RS)-1-하이드록시에틸〕-N-〔5-(메톡시벤질)6-〔2-〔〔(RS)-테트라하이드로-2H-피란-2-일)옥시〕에톡시〕-4-피리미디닐〕벤젠설폰아미드, rac-α-하이드록시-N-〔5-(o-메톡시벤질)-6-〔2-〔(테트라하이드로-2H-피란-2-일)옥시〕에톡시〕-4-피리미디닐〕-p-톨루엔설폰아미드, rac-α-하이드록시이미노-N-〔5-(o-메톡시벤질)-6-〔2-〔(테트라하이드로-2H-피란-2-일)옥시〕에톡시〕-4-피리미디닐〕-p-톨루엔설폰아미드, rac-N-6(2-하이드록시에톡시)-5-(o-메톡시벤질)-p-(1-하이드록시에틸)벤젠셀폰아미드, α-〔(E/Z)-하이드록시이미노〕-N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-p-톨루엔설폰아미드, p-〔〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕설파모일〕벤즈알데히드, 2-〔〔5-(o-메톡시벤질)-6-〔(p-비닐페닐)설파모일〕-4-피리미디닐〕옥시〕에틸 아세테이트, N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-p-메톡시벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-p-톨루엔설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-p-메틸티오벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-α,α,α-트리플루오로-p-톨루엔설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, p-3급-부틸-N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-클로로벤질)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-메틸티오벤질)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-클로로벤질)-4-피리미디닐〕-p-이소부틸벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(o-클로로벤질)-4-피리미디닐〕-p-이소펜틸벤젠설폰아미드, 또는 N-〔6-(2-하이드록시에톡시)-5-(o-메톡시벤질)-4-피리미디닐〕-p-이소프로필티오벤젠설폰아미드인 일반식(Ⅰ)의 화합물.
  6. R6이 하기 일반식(d)의 잔기를 나타내고,R1내지 R5, X, Y 및 n이 제1항에서 정의된 바와 같은 제1항의 일반식(Ⅰ) 화합물.
    상기식에서, R13은 수소, 저급알콕시 또는 니트로이고, R14는 수소, 할로겐, 저급 알킬, 저급 알콕시, 저급 알킬티오 또는 니트로이거나, 또는 R13및 R14는 함께 부티디에닐을 나타낸다.
  7. R4가 수소, 저급 알킬 또는 아릴이고, 나머지 라디칼은 제6항에서 정의된 바와 같은 일반식(Ⅰ)의 화합물 및 이의 염.
  8. N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-α,α,α-트리플루오로-p-톨루엔설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-(트리플루오로메톡시)벤젠설폰아미드, p-클로로-N-〔5-(p-플루오로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-플루오로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-플루오로벤젠설폰아미드, N-[5-(p플루오로페닐)-6-(2-하이드록시에폭시)-4-피리미디닐]-p-플루오로벤젠설폰아미드, o-클로로-N-〔5-(p-클로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, p-클로로-N-〔5-(3,4-디메톡시페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, 3,4-디클로로-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-α,α,α-α′,α′,α′-헥사플루오로-3,5-크실렌설폰아미드, 3-클로로-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-4-(2-하이드록시에톡시)벤젠설폰아미드, p-클로로-N-〔6-(2-하이드록시에톡시)-5-(p-니트로페닐)-4-피리미디닐〕벤젠설폰아미드, p-부톡시-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-3,4-디메톡시벤젠설폰아미드, 2-클로로-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-α,α,α-트리플루오로-p-톨루엔설폰아미드, 6-클로로-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-α,α,α-트리플루오로-m-톨루엔설폰아미드, 2,3,4-트리클로로-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, m-클로로-N-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, 2,4-디클로로-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-α,α,α-트리플루오로-m-톨루엔설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-α,α,α-트리플루오로-o-톨루엔설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-2-나프탈렌설폰아미드, p-클로로-N-〔6-(2-하이드록시에톡시)-5-(m-니트로페닐)-4-피리미디닐〕벤젠설폰아미드, α,α,α-트리플루오로-N-〔6-(2-하이드록시에톡시)-5-(m-니트로페닐)-4-피리미디닐〕-p-톨루엔설폰아미드, p-(벤질옥시)-N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-클로로페닐)-4-피리미디닐〕-p하이드록시벤젠설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-(2-메톡시에톡시)벤젠설폰아미드, N-〔5-(p-브로모페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-클로로벤젠설폰아미드, p-클로-N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-α,α,α-트리플루오로-p-톨루엔설폰아미드 나트륨염, N-〔6-(2-하이드록시에톡시)-5-(p-메톡시페닐)-4-피리미디닐〕-p-톨루엔설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(p-메톡시페닐)-4-피리미디닐〕-p-메톡시설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(p-메톡시페닐)-4-피리미디닐〕-p-(메틸티오)벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(p-메톡시페닐)-2-4-피리미디닐〕-p-메톡시벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(p-메톡시페닐)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, p-3급-부틸-N-〔6-(2-하이드록시에톡시)-5-(p-니트로페닐)-4-피리미디닐〕벤젠설폰아미드, rec-p-2급-부틸-N-〔6-(2-하이드록시에톡시)-5-(p-클로로페닐)-4-피리미디닐〕벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-〔p-(메틸티오)페닐〕-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-〔p-(메틸티오)페닐〕-4-피리미디닐〕-α,α,α-트리플루오-p-톨루엔설폰아미드, p-클로로-N-〔5-(p-메톡시페닐)-6-(2-하이드록시에톡시)-2-메틸-4-피리미디닐〕벤젠설폰아미드, p-클로로-N-〔6-(2-하이드록시에톡시)-5-(p-메톡시페닐)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-메톡시페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-클로로벤젠설폰아미드 하이드로클로라이드, N-〔5-(4-비페닐릴)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-클로로벤젠설폰아미드, p-클로-N-〔(6-하이드록시에톡시)-5-(α,α,α-트리플루오-p-톨릴)-4-피리미디닐〕벤젠설폰아미드, p-클로-N-〔5-(p-하이드록시페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕벤젠설폰아미드, N-〔5-(p-벤질옥시)페닐〕-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-클로로벤젠설폰아미드, -N-〔(6-하이드록시에톡시)-5-(α,α,α-트리플루오-p-톨릴)-4-피리미디닐〕α,α,α-트리플루오-p-톨루엔설폰아미드, N-〔5-(p-클로로페닐)-6-(2-하이드록시에톡시)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, N-〔(6-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, p-3급-부틸-N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-p-(2-메톡시에톡시)벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-p-(트리플루오로메톡시)벤젠설폰아미드, p-부틸-N-〔6-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕벤젠서폰아미드, N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-2-나프탈렌설폰아미드, N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕p-톨루엔설폰아미드, -N-〔(6-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕α,α,α-트리플루오-p-톨루엔설폰아미드, p-(2-하이드록시에톡시)-N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕벤젠설폰아미드, N-〔(6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-p-프로필벤젠설폰아미드, N-〔(6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-o-프로필벤젠설폰아미드, p-에틸-N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕벤젠설폰아미드, o-에틸-N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕벤젠설폰아미드, p-사이클로펜틸-N-〔6-(2-하이드록시에톡시)-5-p-톨릴〕벤젠설폰아미드, α,α,α-트리플루오로-N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-o-톨루엔설폰아미드, N-〔6-(2-하이드록시에톡시)-5-p-톨릴-4-피리미디닐〕-o-톨루엔설폰아미드, p-클로로-N-〔6-(2-하이드록시에톡시)-5-(α,α,α-트리플루오-p-톨릴)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, N-〔-5-(p-브로모페닐)-6-(-하이드록시에톡시)-4-피리미디닐〕-p-이소프로필벤젠설폰아미드, N-〔6-(2-하이드록시에톡시)-5-(p-에틸페닐)-4-피리미디닐〕-p-이소프로필〕벤젠설폰아미드, 또는 p-사이클로펜틸-N-〔6-(2-하이드록시에톡)-5-(p-에틸페닐)-4-피리미디닐〕벤젠설폰아미드인 일반식(Ⅰ)의 화합물.
  9. 제3항 내지 제8항중 어느 한 항의 일반식(Ⅰ) 화합물 및 통상적인 약제학적 보호제를 함유하는 약제학적 제제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920007084A 1991-04-25 1992-04-24 설폰아미드 및 이를 함유하는 약제학적 제제 KR100238366B1 (ko)

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KR100238366B1 (ko) 2000-02-01
NO300874B1 (no) 1997-08-11
FI921850A0 (fi) 1992-04-24
IE921341A1 (en) 1992-11-04
GR3022571T3 (en) 1997-05-31
IL101650A (en) 1996-10-16
JPH0670021B2 (ja) 1994-09-07
NO921609D0 (no) 1992-04-24
US5270313A (en) 1993-12-14
JPH05155864A (ja) 1993-06-22
ES2096673T3 (es) 1997-03-16
NZ242396A (en) 1994-12-22
HRP931531B1 (en) 2000-10-31
HUT61289A (en) 1992-12-28
AU1497692A (en) 1992-10-29
ATE145898T1 (de) 1996-12-15
DE59207601D1 (de) 1997-01-16
HU9201329D0 (en) 1992-07-28
TW270116B (ko) 1996-02-11
AU652238B2 (en) 1994-08-18
EP0510526B1 (de) 1996-12-04
FI921850A (fi) 1992-10-26
HRP931531A2 (en) 1997-10-31
DK0510526T3 (da) 1997-05-26
NO921609L (no) 1992-10-26
IL101650A0 (en) 1992-12-30
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