KR900018048A - 환 치환된 2-아미노-1,2,3,4-테트라하이드로나프탈렌 - Google Patents

환 치환된 2-아미노-1,2,3,4-테트라하이드로나프탈렌 Download PDF

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KR900018048A
KR900018048A KR1019890006780A KR890006780A KR900018048A KR 900018048 A KR900018048 A KR 900018048A KR 1019890006780 A KR1019890006780 A KR 1019890006780A KR 890006780 A KR890006780 A KR 890006780A KR 900018048 A KR900018048 A KR 900018048A
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compound
hydrogen
halo
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methyl
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아더 닉슨 제임스
파울 포치 리차드
메너트 샤우스 존
다이엘 티투스 로버트
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매리 앤 터커
일라이 릴리 앤드 캄파니
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Abstract

내용 없음

Description

환 치환된 2-아미노-1,2,3,4-테트라하이드로나프탈렌
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (27)

  1. 일반식(Ⅰ)의 화합물 및 이의 약제학적으로 허용되는 산부가염.
    상기식에서, R은 수소 또는 메틸이고, R1은 수소 또는 메틸이며, X는 -CH2CH2- 또는 -CH2CH2CH2-이고, R2는 수소, 할로, C1-C알3콕시, C1-C3티오알킬, C1-C3일킬 및 히드록시로 이루어진 그룹중에서 선택되고, R3는 수소와 할로로 이루어진 그룹중에서 선택되며, R4는 수소, 할로, C1-C3알킬, C1-C3알콕시, C1-C3티오알킬 및 히드록실로 이루어진 그룹중에서 선택되고, R5는 수소, 할로, C1-C3알킬, C1-C3알콕시, C1-C3아실, 플루오로치환C2-C3아실, 플루오로치환 C1--C3알킬, 시아노, 카르복시아미도, 카르복실 및 C1-C3히드록시알킬 중에서 선택되며, 단(a) R1이 메틸인 경우, R2와 R4는 모두 수소이고, (b) R1이 수소인 경우, R2와 R4중 어느 하나는 수소이고 나머지 하나는 수소이외의 것이며, (c) R2가 수소가 아닌 경우에만 R5는 수소이외의 것일 수 있고, (d) R4가 수소가 아닌 경우에만 R3는 할로일 수 있다.
  2. 제1항에 있어서, R5가 수소, 할로, C1-C3알킬, C1-C3알콕시, C1-C3아실, 플루오로치환C2-C3아실, 플루오로치환 C1--C3알킬, 시아노로 이루어진그룹중에서 선택되는 화합물.
  3. 제1항 또는 3항에 있어서, R2가 할로, C1-C알3콕시, C1-C3티오알킬, C1-C3일킬 및 히드록시로 이루어진 그룹중에서 선택되는 화합물.
  4. 제1항 내지 3항중 어느 한 항에 있어서, X가 -CH2CH3-인 화합물
  5. 제1항 내지 4항중 어느 한 항에 있어서, R1이 수소인 화합물.
  6. 제1항 내지 5항중 어느 한 항에 있어서,R이 메틸인 화합물.
  7. 제1항 내지 6항중 어느 한 항에 있어서, R2가 C1-C3알콕시 또는 할로인 화합물.
  8. 제1항 내지 6항중 어느 한 항에 있어서,R2가 할로인 화합물.
  9. 제1항 내지 6항중 어느 한 항에 있어서, R2가 클로로인 화합물.
  10. 제1항 내지 6항중 어느 한 항에 있어서, R2가 C1-C3알콕시인 화합물.
  11. 제1항 내지 6항중 어느 한 항에 있어서, R2가 메톡시인 화합물.
  12. 제1항 내지 11항중 어느 한 항에 있어서,R5가 수소이외의 것인 화합물.
  13. 제1항 내지 11항중 어느 한 항에 있어서, R5가 할로인 화합물.
  14. 제1항 내지 11항중 어느 한 항에 있어서, R5가 브로모인 화합물.
  15. 제1항에 있어서, R4가 할로C1-C3알킬, C1-C3알콕시, C1-C3티오알킬, 및 히드록시로 이루어진 그룹중에서 선택되는 화합물.
  16. 제15항에 있어서, X가 -CH2CH2-인 화합물.
  17. 제15항 내지 16항중 어느 한 항에 있어서, R1이 메틸인 화합물.
  18. 제15항 내지 17항중 어느 한 항에 있어서, R이 수소인 화합물.
  19. 제15항 내지 18항중 어느 한 항에 있어서, R4가 할로인 화합물.
  20. 제15항 내지 19항중 어느 한 항에 있어서,R4가 클로로인 화합물.
  21. 제15항 내지 20항중 어느 한 항에 있어서, R3가 수소인 화합물.
  22. 1-메틸-2-피페라지릴-6-클로로-1,2,3,4-테트라히들로나프탈렌, 또는 이의 약제학적으로 허용되는 산부가염.
  23. A) 일반식(Ⅱ)의 화합물을 환원적으로 알킬화하거나, B) 일반식(Ⅲ)의 화합물로부터 브로모그룹을 치환시킴을 특징으로 하는, 제1항 내지 22항중 어느 한 항에 따른 일반식(Ⅰ)의 화합물의 제조방법.
    상기식에서, R1,R2,R3,R4및 R5는 제1항에서 정의한 바와 같고, R2a',R3a',R4a'및 R4a'중 하나이상은 브로모이다.
  24. 제22항에 있어서 일반식(Ⅱ)의 화합물과 일반식(A)화합물을 반응시키고, 생성물을 환원 시킴을 특징으로 하는 제조방법.
    상기식에서, R은 수소 또는 메틸이다.
  25. 제1항 내지 22항중 어느 한항에 따른 일반식(Ⅰ)의 화합물을 포유동물에게 투여함을 특징으로하여, 포유동물의 세로토닌 재흡수를 억제하는 방법.
  26. 제25항에 있어서, 화합물이 1-메틸2-피페라지닐-6-클로로-1,2,3,4-테트라히드로나프탈렌 또는 이의 약제학적으로 허용되는 산부가염인 방법.
  27. 활성성분으로서, 제1항 내지 22항중 어느 한 항에 따른 일반식(Ⅰ)의 화합물, 또는 이의 약제학적으로 허용되는 산부가염을 이의 약제학적으로 허용되는 하나이상의 담체와 함께 함유함을 특징으로 하는 약제학적 제제.
    ※ 참고사항 : 최초출원내용에 의하여 공개하는 것임.
KR1019890006780A 1988-05-23 1989-05-20 환 치환된 2-아미노-1,2,3,4-테트라하이드로나프탈렌 KR900018048A (ko)

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DE3718317A1 (de) * 1986-12-10 1988-06-16 Bayer Ag Substituierte basische 2-aminotetraline

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PT90569B (pt) 1994-08-31
HU208818B (en) 1994-01-28
JP2795677B2 (ja) 1998-09-10
EP0343830A2 (en) 1989-11-29
RU2014330C1 (ru) 1994-06-15
EP0343830A3 (en) 1990-11-28
HUT50799A (en) 1990-03-28
CA1335591C (en) 1995-05-16
IL90292A0 (en) 1989-12-15
CN1038644A (zh) 1990-01-10
ZA893619B (en) 1991-01-30
PT90569A (pt) 1989-11-30
AU615747B2 (en) 1991-10-10
RU2001911C1 (ru) 1993-10-30
DK243989D0 (da) 1989-05-19
MX16046A (es) 1993-10-01
DE68916705D1 (de) 1994-08-18
ES2058518T3 (es) 1994-11-01
DE68916705T2 (de) 1994-11-24
PH26986A (en) 1992-12-28
AU3482089A (en) 1989-11-23
NZ229141A (en) 1991-08-27
JPH0217179A (ja) 1990-01-22
DK243989A (da) 1989-11-24
CN1024665C (zh) 1994-05-25
ATE108446T1 (de) 1994-07-15
EP0343830B1 (en) 1994-07-13

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