KR890009923A - 헤테로사이클릭 화합물 - Google Patents

헤테로사이클릭 화합물 Download PDF

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KR890009923A
KR890009923A KR1019880017218A KR880017218A KR890009923A KR 890009923 A KR890009923 A KR 890009923A KR 1019880017218 A KR1019880017218 A KR 1019880017218A KR 880017218 A KR880017218 A KR 880017218A KR 890009923 A KR890009923 A KR 890009923A
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azabicyclo
octan
amino
alkyl
carbonyl
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제임스 워드 테렌스
크리스틴 화이트 자네트
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폴 에이 리쳐
존 와이어스 앤드 브라더 리미티드
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Priority claimed from GB888819728A external-priority patent/GB8819728D0/en
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Abstract

내용 없음

Description

헤테로사이클릭 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 일반식(Ⅰ)의 헤테로사이클릭 화합물 또는 약제학적 허용되는 이의 산부가염.
    A-X-NHCW-Y-B (Ⅰ)
    상기식에서 A는
    의 방향족 라디칼 [여기에서, 자유 원자가는 일반식(a)의 융합 환 또는 일반식(b)의 융합환에 결합된다]이고, R1은 수소, 또는 저급알킬, 저급알콕시, 하이드록시, 할로겐, 할로(저급알킬), 아미노, 니트로, 카복스, 아미도, 페닐(저급)알킬옥시(여기에서 페닐그룹은 임의로 하나 이상의 저급알킬, 저급알킬옥시 또는 할로치환체에 의해 치환될 수 있다), (저급)알킬아미노, 디(저급)알킬아미노, 디(저급)알킬아미노 및 아실아미노중에서 선택된 하나 이상의 동일하거나 상이한 치환체이고, Z1및 Z2는 CH2-CH, NR2-CH, O-CH, S-CH, CH2-N, O-N, S-N, NR2-N, CH-NR2또는 N-NR2[여기에서 R2는 수소, (저급)알킬, 또는 페닐 또는 페닐 (저급)알킬(여기에서 페닐그룹은 하나 이상의 저급알킬, 저급알킬옥시 또는 할로치환체에 의해 임의로 치환될 수 있다)]이고, Z3및 Z4는 CH=CH, O-CH2또는 N=CH이고, Z5는 N 또는 CH이고, Z6는 O, S 또는 NH이고, X는 직접결합이거나, CO이고, W는 산소 또는 황이고, Y는 NH 또는 산소이고, B는 일반식
    의 포화 아자사이클릭 환이고, 여기에서 n은 2,3 또는 4이고, m은 1,2 또는 3이고, p는 0,1 또는 2이고, R3은 수소, 또는 (저급)알킬이고, R4및 R5는 각각 수소 또는 저급알킬이며 단, X가 직접결합일 경우, A는 일반식(c) 또는 (d)의 그룹이고 W는 산소이며, 환(c) 또는 (d)는 -X-NHCW-Y-B 측쇄에 대해 오르토 위치에 치환체를 함유하지 않는다.
  2. 제1항에 있어서, X가 CO인 화합물.
  3. 제1항에 있어서, A가 일반식()인 화합물,
    상기식에서 R6내지 R9은 독립적으로 수소 또는 제1항에서 정의한 치환체 R1이다.
  4. 제3항에 있어서, R6은 저급알콕시이고 R7, R8및 R9가 수소이거나 R6가 저급 알킬옥시 또는 사이클로(저급)알킬(저급)알킬옥시이고 R7이 수소이고, R8이 아미노 또는 저급알킬아미노이며 R9가 할로이거나 R7및 R9가 클로로이며 R6및 R8이 수소인 화합물.
  5. 제1항 내지 제3항중 어느 한 항에 있어서, B가 트로판 3-일인 화합물.
  6. 제1항에 있어서, A가 R1이 수소, 또는 하나의 할로(저급)알킬, 저급알콕시, 저급알킬, 아미노, (저급)알킬아미노, 디(저급)알킬아미노 또는 (저급)알카노일아미노 치환체인 일반식(a) 또는 (b)의 라디칼이거나 Z5가 CH치고 R1이 수소 또는 저급알킬, 저급알콕시, 하이드록시, 할로겐, 할로(저급)알킬, 아미노, 니트로, 카복스아미노(저급)알킬아미노, 디(저급)알킬아미노 및 (저급)알카노일아미노로부터 선택되는 하나 이상의 동일하거나 상이한 치환체인 일반식(c)의 라디칼인 화합물.
  7. 제1항에 있어서, N-(1-아자비사이클로)[2.2.2]옥탄-3-일)-N'-(3,5-디클로로페닐)우레아 또는 약제학적으로 허용되는 이의 염인 화합물.
  8. 제1항에 있어서, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-메톡시벤즈아미드 또는 약제학적으로 허용되는 이의 염인 화합물.
  9. 제1항에 있어서, N[[[1-아자비사이클르로[2.2.2]옥탄-3-일]아미노]카보닐]-3,5-디클로로벤즈아미드, (엔도)-N-(3,5-디클로로벤조일)-O-(8-메틸-8-아자비사이클로[3.2.1]옥트-3-일)카바메이트 또는 N-(3,5-디클로로페닐)-N'-(1,2-디메틸피라졸리딘-4-일)우레아 또는 약제학적으로 허용되는 이의 염인 화합물.
  10. 제1항에 있어서, N-(아자비사이클로[2.2.2]옥탄-3-일-N'-(3,5-디클로로페닐)티오우레아, (엔도)-N-(3,5-디클로로페닐)-N'(8-메틸-8-아자비사이클로[3.2.1]옥탄-3-일)우레아, N-(1-아자비사이클로[2.2.2]옥탄-3-일)-N'-(3-트리플루오로메틸페닐)우레아, N-(1-아자비사이클로[2.2.2]옥탄-3-일)-N'-(4-클로로페닐)우레아, N-(아자비사이클로[2.2.2]옥탄-3-일)-N'-(1-메틸-1H-인돌-3-일)우레아, N-(아자비사이클로[2.2.2]옥탄-3-일)-N'-(2-벤조티에닐)우레아, (S)-(-)-N-(1-아자비사이클로[2.2.2]옥탄-3-일)-N'-(3,5-디클로로페닐)우레아, (R)-(+)-N-(1-아자비사이클로[2.2.2]옥탄-3-일)-N'-(3,5-디클로로페닐)우레아, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-트리플루오로메틸벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-4-메톡시벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]나프탈렌-2-카복스아미드 또는 약제학적으로 허용되는 이의 염인 화합물.
  11. 제1항에 있어서, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-푸란카복스아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2,6-디메틸벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-티오펜카복스아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-플루오로벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-에톡시벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-이소프로폭시벤즈아미드, 2-알릴옥시-N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-피리딘카복스아미드, (엔도)-N-[[[8-메틱-8-아자비사이클로[3.2.1]옥탄-3-일]아미노]카보닐]-2-메톡시벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-메틸벤즈아미드, N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-(사이클로프로필)메톡시)벤즈아미드, (S)-N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-메톡시아미드, (R)-N-[[[1-아자비사이클로[2.2.2]옥탄-3-일]아미노]카보닐]-2-메톡시벤즈아미드 또는 (엔도)-O-N-[[[8-메틸-8-아자비사이클로[3.2.1]옥탄-3-일]-N-(3,5디클로로포닐)카바메이트 또는 약제학적으로 허용되는 이의 연인 화합물.
  12. 유효량의 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 이의 산부가염을 편두통, 구토, 불안증, 위장병 또는 정신병 치료를 필요로 하는 온혈동물에게 투여함을 특징으로 하여 상기 질명을 치료하는 방법.
    A-X-NHCW-Y-B (Ⅰ)
    상기식에서 A는
    의 방향족 라디칼 [여기에서, 자유 원자가는 일반식(a)의 융합 환 또는 일반식(b)의 융합환에 결합된다]이고 R1은 수소, 또는 저급알킬, 저급알콕시, 하이드록시, 할로겐, 할로(저급)알킬, 아미노, 니트로, 카복스아미도, 페닐(저급)알킬옥시(여기에서 페닐그룹은 임의로 하나 이상의 저급알킬, 저급알킬옥시 또는 할로치환체에 의해 치환될 수 있다), (저급)알킬아미노, 디(저급)알킬아미노, 디(저급)알킬아미노 및 아실아미노중에서 선택된 하나 이상의 동일하거나 상이한 치환체이고, Z1및 Z2는 CH2-CH, NR2-CH, O-CH, S-CH, CH2-N, O-N, S-N, NR2-N, CH-NR2또는 N-NR2[여기에서 R2는 수소, (저급)알킬, 또는 페닐 또는 페닐 (저급)알킬(여기에서 페닐그룹은 하나 이상의 저급알킬, 저급알킬옥시 또는 할로치환체에 의해 임의로 치환될 수 있다)이다]이고, Z3및 Z4는 CH=CH, O-CH2또는 N=CH이고, Z5는 N 또는 CH이고, Z6는 O, S 또는 NH이고, X는 직접 결합이거나, CO이고, W는 산소 또는 황이고, Y는 NH 또는 산소이고, B는 일반식
    또는 이의 N-옥사이드,
    의 포화 아자사이클릭 환이고, 여기에서 n은 2,3 또는 4이고, m은 1,2 또는 3이고, p는 0,1 또는 2이고, R3은 수소, 또는 (저급)알킬이고, R4및 R5는 각각 수소 또는 저급알킬이며 단, X가 직접결합일 경우, A는 일반식(c) 또는 (d)의 그룹이고 W는 산소이며, 환 (c) 또는 (d)는 -X-NHCW-Y-B 측쇄에 대해 오르토 위치에 치환체를 함유하지 않는다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880017218A 1987-12-24 1988-12-22 헤테로사이클릭 화합물 KR970009588B1 (ko)

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