KR900701734A - 아민의 아릴옥시- 아릴티오-, 헤테로아릴옥시-, 헤테로아릴티오-알케닐렌 유도체 - Google Patents

아민의 아릴옥시- 아릴티오-, 헤테로아릴옥시-, 헤테로아릴티오-알케닐렌 유도체

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KR900701734A
KR900701734A KR1019900701173A KR900701173A KR900701734A KR 900701734 A KR900701734 A KR 900701734A KR 1019900701173 A KR1019900701173 A KR 1019900701173A KR 900701173 A KR900701173 A KR 900701173A KR 900701734 A KR900701734 A KR 900701734A
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phenyl
methylaminomethylethylene
alkyl
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group
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멜로니 피에로
도스터트 필리페
델라 토레 아르투로
본시그노리 알베르토
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비토리노 페라리오
팜이탈리아 카를로 에르바 에스. 알. 엘.
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Publication of KR900701734A publication Critical patent/KR900701734A/ko

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Abstract

내용 없음

Description

아민의 아릴옥시-아릴티오-, 헤테로아릴옥시-, 헤테로아릴티오-알케닐렌 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 다음 일반식(Ⅰ)의 화합물 및 약제학적으로 허용가능한 이의 염
    상기식에서, A및 B는 각각 독립적으로 일반식(ⅰ)및
    (iii)의 그룹이고;여기에서, Y는 -O-, -S- 또는 -NR- (이때, R은 수소 또는 C1-6알킬이다)이고; R3,R4,R5및 R6은 각각 동일하거나 상이할 수 있으며, 독립적으로 (a)수소, 할로겐, 히드록시, 시아노 또는 니트로, (b)할로겐에 의해 치환되거나 비치환된 C1-6알킬, C1-6알콕시 또는 C1-6알킬티오, (d)C1-6알킬-설포닐, (e)-NR7R8그룹〔이때, R7및 R8은 각각 독립적으로 수소 또는 C1-6알킬이거나; R7과 R8중의 하나가 수소 또는 C1-6알킬이고 나머지 하나는 -COR9그룹{이때, R9는 소수, C1-6알킬, C1-6알콕시 또는 -NR10R11(이때, R10및 R11은 각각 독립적으로 수소 또는 C1-6알킬이다)이다}이다〕, 또는 (f)-COR12그룹{이때, R12는 C1-6알콕시, C1-6알킬 또는 -NR10R11(이때, R10및 R11은 상기에서 정외한 바와 같다)이다}이거나; (g) R3,R4,R5및 R6중 인접한 두개는 함께 C1-4알킬렌디옥시그룹을 형성하고; R1및 R2는 각각 독립적으로 수소, C3-6알키닐, C3-6-알케닐, 또는 페닐에 의해 치환되거나 비치환된 C1-6알킬이거나; R1과 R2는 이들이 연결되는 질소원자와 함께, 산소, 황 및 질소중에서 선택된 추가의 헤테로원자를 임의로 함유하는 치환되거나 비치환된 포화 헤테로모노시클릭 환을 형성한다.
  2. 제1항에 있어서, A및 B가 각각 독립적으로 일반식 (a)및 (aaa)의 그룹이고;여기에서, R3,R4,R5및 R6은 각각 독립적으로수소, 할로겐, 히드록시, 시아노, C1-4알킬설포닐, 니트로, C1-4알킬, C1-4알콕시, -NR7R8그룹〔이때, R7및 R8은 독립적으로 수소 또는 C1-4알킬이거나; R7과 R8중의 하나가 수소 또는 C1-4알킬이고 나머지 하나는 -COR9그룹{이때, R9는 소수, C1-4알킬, C1-4알콕시 또는 -NR10R11(이때, R10및 R11은 각각 수소 또는C1-4알킬이다)이다}이다〕, 또는 -C0R12그룹{이때, R12는 C1-4알콕시, C1-4알킬 또는 -NR10R11(이때, R10및 R11은 상기에서 정의한 바와 같다)이다}이거나; R3,R4,R5및 R6중 인접한 두개는 함께 C1-2알킬렌디옥시그룹을 형성하고; R1및 R2는 각각 독립적으로 수소, C3-4알케닐, C3-4알키닐, 또는 페닐에 의해 치환되거나 비치환된 C1-4알킬이거나; R1및 R2는 이들이 연결되는 질소원자와 함께, 히드록시에 의해 치환되거나 비치환된 C1-4알킬에 의해 N-치환되거나 비치환된 피페라진 환을 형성하거나, 피페리딘, 모르폴린, 티오모르폴린 및 피롤리딘중에서 선택된 환을 형성하는 일반식(Ⅰ)의 화합물 및 약제학적으로 허용가능한 이의 염.
  3. 제1항에 있어서, A및 B가 각각 일반식 (b)의 그룹이고; 여기에서, 동일하거나 상이할 수 있는 R3및 R4는 각각 수소, 할로겐, C1-4알록시, C1-4알킬, 시아노 니트로, 아미노, 트로플루오로메틸, C1-4알킬설포닐 또는 C2-5알카노일이거나; 인접한 R3과R4는 함께 메틸렌디옥시그룹을 형성하고; R1, 및 R2는 각각 독립적으로 수소 또는 C1-4알킬인 일반식(Ⅰ)의 화합물 및 약제학적으로 허용가능한 이의 염.
  4. 제1항에 있어서, α-페녹시-α-페닐-β-메틸아미노메틸에틸렌, α-(-2-에톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(-2-클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2,6-디클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(3,4-디클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-트리플루오로메틸페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-니트로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-아미노페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-우레이도페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-티에닐옥시)-α-페닐-β-메틸아미노메틸에틸렌,α-(1-나프틸옥시)-α-페닐-β-메틸아미노메틸에틸렌,α-(2-나프틸옥시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-시아노페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(3-클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-메틸페녹시)-α-페닐-β-메틸아미노메틸에틸렌, (E)-α-(2,6-디메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, (E)-α-(4-니드로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(3,4-디메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-아세틸페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(3-메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌-α-(4-메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-시아노-3-메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-시아노페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(3-시아노메톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-메틸설포닐페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-페녹시-α-(2-티에닐)-β-메틸아미노메틸에틸렌, α-페녹시-α-(3-클로로페닐)-β-메틸아미노메틸에틸렌, α-페녹시-α-(4-클로로페닐)-β-메틸아미노메틸에틸렌, α-페녹시-α-(2-히드록시페닐)-β-메틸아미노메틸에틸렌, α-페녹시-α-(3,4-에틸렌디옥시페닐)-β-메틸아미노메틸에틸렌, α-페녹시-α-(3-메톡시페닐)-β-메틸아미노메틸에틸렌, (E)-α-(3-히드록시메녹시)-α-페닐-β-메틸아미메틸에틸렌, α-(3,4-메틸렌디옥시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-페녹시-α-페닐-3-메틸아미노메틸에틸렌, α-(2-에톡시페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(3.4-디클로로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-트리플루오로메틸페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(4-니트로페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-아미노페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-우레이도페녹시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-티에닐옥시)-α-페닐-β-메틸아미노메틸에틸렌, α-(1-나프틸옥시)-α-페닐-β-메틸아미노메틸에틸렌, α-(2-나프틸옥시)-α-페닐-β-메틸아미노메틸에틸렌, α-페녹시-α-(2-티에닐)-β-디메틸아미노메틸에틸렌, α-페녹시-α-(3-클로로페닐)-β디-메틸아미노메틸에틸렌, α-페녹시-α-(4-클로로페닐)-β-디메틸아미노메틸에틸렌, α-페녹시--(3,4-메틸렌디옥시페닐)-β-디메틸아미노메틸에틸렌, α-페녹시-α-(3-메톡시페닐)-p-디메틸아미노메틸에틸렌, -α-(3,4-메틸렌디옥시페녹시)-α-페닐-β-디메틸아미노메틸에틸렌 및 α-페녹시-α-페닐-β-디메틸아미노메틸에틸렌중에서, 선택되며, 별다른 언급이 없는 한은 단일한 Z 및 E 이성체, 및 이들의 혼합물둘다로서인 화합물 및 약제학적으로 허용가능한 이의 염.
  5. (a)다음 일반식(Ⅱ)의 화합물을 환원제의 존재하에 다음 일반식(Ⅲ)의 아민과 반응시키거나, (b)다음 일반식(Ⅳ)의 화합물을 환원시키거나, (c)다음 일반식(V)의 화합물을 다음 일반식(Ⅵ)의 아민과 반응시켜, R1이 제1항에서 정의한 바와 같고 R2는 수소인 다음 일반식(Ⅰ)의 화합물을 수득하고, 경우에 따라, 다음 일반식(Ⅰ)의 화합믈을 다음 일반식(Ⅰ)의 또다른 화합물로 전환시키고/거나, 경우에 따라, 다음 일반식(Ⅰ)의 화합물을 약제학적으로 허용가능한 이의 염으로 전환시키고/거나, 경우에 따라, 이 염을 유리 화합물로 전환시키고/거나, 경우에 따라, 이성체 혼합물을 단일 이성체로 분리시키는 단계를 포함함을 특징으로 하여, 제1항에 따른 다음 일반식(Ⅰ)의 화합물 및 약제학적으로 허용가능한 이의 염을 제조하는 방법;
    상기식에서, A, B, R1및 R2는 제1항에서 정의한 바와 같고; Z는 이탈기이다.
  6. 적합한 담체 및/또는 희석제, 및 활성성분으로서 제1항에 따른 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용가능한 이의 염을 함유하는 약제학적 조성물.
  7. 우울증 억제제로서 사용하기 위한, 제1항에 따른 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용가능한 이의 염
  8. 비만방지제로서 사용하기 위한, 제1항에 따른 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용가능한 이의 염.
  9. 우울증, 비만증 또는 알콜중독증에 걸리거나 흡연하는 인간에게 제1항에 정의한 바와 같은 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용가능한 이의 염 유효량을 투여하는 단계를 포함하여. 인간의 우울증을 치료하거나 인체 외관을 좋게 하거나 흡연을 중간시키거나 알콜 남용을 중간시키는 방법.
  10. 다음 일반식(Ⅱ)의 화합물;
    상기식에서, A 및 B는 각각 독립적으로 일반식 (ⅰ)및
    (iii)의 그룹이고; 여기에서, Y는 -O-, -S- 또는 -NR-(이때, R은 수소 C1-6알킬이다)이고: R3,R4,R5및 R6은 각각 독립적으로 (a)수소, 할로겐, 히드록시, 시아노 또는 니트로, (b)할로겐에 외해 치환되거나 비치환된 C1-6알킬, (c)C1-6알콕시 또는 C1-6알킬티오, (d)C1-6알킬-설포닐, (e)-NR|7R8그룹〔이때, R7및 R8은 각각 독립적으로 수소 또는 C1-6알킬이거나; R7과 R8중의 하나가 수소 또는 C1-6알킬이고 나머지 하나는 -COR9그룹{이때, R9는 소수, C1-6알킬, C1-6알콕시 또는 -NR10R11(이때, R10및 R11은 각각 독립적으로 수소 또는 C1-6알킬이다)이다}이다〕, 또는 (f)-COR12그룹{이때, R12는 C1-6알콕시. C1-6알킬 또는 -NR10R11(이때, R10및 R11은 상기에서 정의한 바와 같다)이다}이거나; (g) R3,R4,R|5및 R6중 인접한 두개는 함께 C1-4알킬렌디옥시그룹을 형성하고; A와 B가 둘다 일반식(i) 하에 정의한 바와 같고 A가 p-NO2에 의해 치환되거나 비치환된 페닐환인 경우, A 또는 B환상에 남아 있는 치환체중 하나 이상의 치환제는 수소가 아니다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900701173A 1988-10-05 1989-10-02 아민의 아릴옥시- 아릴티오-, 헤테로아릴옥시-, 헤테로아릴티오-알케닐렌 유도체 KR900701734A (ko)

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YU46941B (sh) 1994-06-24
PH27293A (en) 1993-05-04
ATE99670T1 (de) 1994-01-15
NZ230628A (en) 1991-06-25
EP0363782A1 (en) 1990-04-18
CN1022828C (zh) 1993-11-24
CZ279655B6 (cs) 1995-05-17
AU4507989A (en) 1990-05-01
DK137490A (da) 1990-07-30
PT91880B (pt) 1995-05-31
PT91880A (pt) 1990-04-30
CN1041755A (zh) 1990-05-02
MY106236A (en) 1995-04-29
IL91541A0 (en) 1990-04-29
ZA897590B (en) 1991-06-26
IE893171L (en) 1990-04-05
FI902775A0 (fi) 1990-06-04
GB8823405D0 (en) 1988-11-09

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