KR900012890A - 환-치환된 2-아미노-1,2,3,4-테트라하이드로 나프탈렌 및 3-아미노크로만 - Google Patents

환-치환된 2-아미노-1,2,3,4-테트라하이드로 나프탈렌 및 3-아미노크로만 Download PDF

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KR900012890A
KR900012890A KR1019900002287A KR900002287A KR900012890A KR 900012890 A KR900012890 A KR 900012890A KR 1019900002287 A KR1019900002287 A KR 1019900002287A KR 900002287 A KR900002287 A KR 900002287A KR 900012890 A KR900012890 A KR 900012890A
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hydrogen
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allyl
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에드워드 플라우 마이클
메너트 샤우스 죤
다니엘 티투스 로버트
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레로이 화이터커
일라이 릴리 앤드 캄파니
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    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
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    • C07C317/32Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/36Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atoms of the amino groups bound to hydrogen atoms or to carbon atoms
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/31Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
    • C07C323/38Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton with the sulfur atom of the thio group bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
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    • C07C2602/00Systems containing two condensed rings
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    • C07C2602/04One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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Abstract

내용 없음

Description

환-치환된 2-아미노-1,2,3,4-테트라하이드로 나프탈렌 및 3-아미노크로만
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (24)

  1. 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 산부가염.
    상기식에서, R은 C1-C4알킬, 아릴 또는 사이클로프로필메틸이고, R1은 수소, C1-C4알킬, 알릴, 사이클로프로필메틸, 또는 아릴(C1-C4-알킬)이며, R2는 수소 또는 메틸이고, X는 -CH2-또는 -O-이며, R3는 C1-C8알킬, 아릴, 치환된 아릴, 아릴(C1-C4-아킬), 치환된 아릴(C1-C4아킬), 또는 C5-C7사이클로알킬이고, n은 0, 1, 또는 2이다.
  2. 제1항에 있어서, n이 0인 화합물.
  3. 제1항 또는 2항에 있어서, R2가 수소인 화합물.
  4. 제1항 내지 3항중 어느 한 항에 있어서, X가 -CH2-인 화합물.
  5. 제1항 내지 4항중 어느 한 항에 있어서, R3가 C1-C8아킬, 치환된 아릴, 및 치환된 아릴(C1-C4-알킬)중에서 선택된 화합물.
  6. 제1항 내지 5항중 어느 한 항에 있어서, R 및 R1이 둘다 C1-C4알킬인 화합물.
  7. 제1항 내지 6항중 어느 한 항에 있어서, R3가 C1-C8알킬인 화합물.
  8. 제1항 내지 7항중 어느 한 항에 있어서, R 및 R1이 둘다n-프로필인 화합물.
  9. 제1항 내지 8항중 어느 한 항에 있어서, R3이 메틸인 화합물.
  10. 5-HT1A수용체에서 길항작용을 필요로 하는 포유동물에게 제1항 내지 9항중 어느 한 항에서 청구된 약제학적 유효량의 화합물을 투여함을 특징으로 하여, 포유동물의 5-HT1A수용체에서 길항작용을 수행하는 방법.
  11. 제10항에 있어서, 화합물이 2-디-n-프로필아미노-8-메틸티오-1,2,3,4-테트라하이드로나프탈렌 또는 약제학적으로 허용되는 이의 산부가염인 방법.
  12. 활성성분으로서 제1항 내지 9항중 어느 한 항에서 청구된 화합물 또는 약제학적으로 허용되는 이의 산부가염을 하나 이상의 약제학적으로 허용되는 담체와 함께 함유하는 약제학적 제제.
  13. 제12항에 있어서, 화합물이 2-디-n-프로필아미노-8-메틸티오-1,2,3,4-테트라하이드로나프탈렌 또는 약제학적으로 허용되는 이의 산부가염인 방법.
  14. 상응하는 2-테트랄론 또는 3-크로마논을 광학적으로 활성인p-니트로펜에틸아민과 반응시키고, 생성된 2-(??-메틸-p-니트로벤질)-아미노테트랄린 또는 3-(??-메틸-p-니트로벤질)아미노크로만을 이의 광학 이성체로 분리시키며, 이성체로부터p-니트로펜에틸 그룹을 분해하여 광학적으로 활성인 테트라하이드 로나프탈렌 또는 크로만 생성물을 수득함을 특징으로 하여, 광학적으로 활성인 2-아미노-1,2,3,4-테트라하이드로나프탈렌 또는 3-아미노크로만을 제조하는 방법.
  15. 일반식(Ⅰa)의 화합물.
    상기식에서, R은 수소, C1-C4알킬, 알릴, 또는 사이클로프로필 메틸이고, R1은 수소, C1-C4알킬 , 알릴, 사이클로프로필메틸, 또는 아릴(C1-C|4-알킬)이다.
  16. 제15항에 있어서, R 및 R1이 둘다 수소인 화합물.
  17. 제15항에 있어서, R 및 R1이 둘다n-프로필인 화합물.
  18. 일반식(Ⅰb)의 화합물.
    상기식에서, R은 수소, C1-C4알킬, 알릴, 또는 사이클로프로필 메틸이고, R1은 수소, C1-C4알킬. 알릴 사이클로프로필메틸, 또는 아릴(C1-C4-알킬)이다.
  19. 제18항에 있어서, R 및 R1이 둘다 수소인 화합물.
  20. 제18항에 있어서, R 및 R1이 둘다n-프로필인 화합물.
  21. 일반식(Ⅱ)의 화합물.
    상기식에서, R은 수소, C1-C-4알킬, 알릴, 또는 사이클로프로필메틸이고, R1은 수소, C1-C4알킬, 알릴, 사이클로프로필메틸, 또는 아릴(C1-C-|4알킬)이며, R2는 수소 또는 메틸이다.
  22. 일반식(Ⅲ)의 화합물.
    상기식에서, R은 수소, C1-C4알킬, 알릴, 또는 사이클로프로필 메틸이고, R1수소, C1-C4알킬, 알릴, 사이클로프로필메틸, 또는 아릴(C1-C4알킬)이며, R2는 수소 또는 메틸이고, X는 -CH2-또는 -O-이다.
  23. 제22항에 있어서, R 및 R1n-프로필이고, R2가 수소이며, X가 -CH2-인 화합물.
  24. 일반식(Ⅱ)의 화합물을 알킬 리??과 반응시켜 상응하는 8-리티오 화합물을 수득하고, 8-리티오 화합물을 일반식(Ⅳ)의 화합물을 알킬 리튬과 반응시켜 상응하는 8-리티오 화합물을 수득하고, 8-리티오 화합물을 일반식(Ⅳ)의 화합물과 반응시켜 n이 0인 화합물을 수득하며, 임의로 n인 화합물을 산화시켜 n이 1 또는 2인 화합물을 수득함을 특징으로 하여, 일반식(Ⅰ)의 화합물을 제조하는 방법.
    상기식에서, R은 C1-C4알킬, 알릴, 또는 사이클로프로필 메틸이고, R1은 수소, C1-C4알킬, 알릴, 사이클로프로필메틸, 또는 아릴(C1-C4알킬)이며, R2는 수소 또는 메틸이고, X는 -CH2-또는-O-이며, R3는 C1-C4알킬, 아릴, 치환된 아릴, 아릴(C1-C4알킬), 치환된 아릴(C1-C4알킬), 또는 C5-C7사이크로알킬이고, n은 0, 1, 또는 2이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900002287A 1989-02-27 1990-02-23 환-치환된 2-아미노-1,2,3,4-테트라하이드로 나프탈렌 및 3-아미노크로만 KR900012890A (ko)

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ZA901277B (en) 1991-10-30
CN1120532A (zh) 1996-04-17
HUT53354A (en) 1990-10-28
HU9202449D0 (en) 1992-12-28
JP2954255B2 (ja) 1999-09-27
CN1045099A (zh) 1990-09-05
NZ232628A (en) 1992-03-26
CA2362972A1 (en) 1990-08-27
GR3015136T3 (en) 1995-05-31
JPH02268151A (ja) 1990-11-01
DK0385658T3 (da) 1995-02-20
DE69015384T2 (de) 1995-05-18
AU630671B2 (en) 1992-11-05
CN1031262C (zh) 1996-03-13
PT93218A (pt) 1990-08-31
MX19637A (es) 1994-02-28
HUT65268A (en) 1994-05-02
IL93464A0 (en) 1990-11-29
JPH11315063A (ja) 1999-11-16
IL114715A0 (en) 1995-11-27
RU1826966C (ru) 1993-07-07
IL109647A (en) 1997-04-15
HU901048D0 (en) 1990-05-28
CA2010542C (en) 2002-05-14
EP0385658A1 (en) 1990-09-05
IL114715A (en) 1997-01-10
PH27444A (en) 1993-07-02
ES2065478T3 (es) 1995-02-16
IE65769B1 (en) 1995-11-15

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