KR910700251A - 5-ht 선택제 - Google Patents

5-ht 선택제

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KR910700251A
KR910700251A KR1019900701796A KR900701796A KR910700251A KR 910700251 A KR910700251 A KR 910700251A KR 1019900701796 A KR1019900701796 A KR 1019900701796A KR 900701796 A KR900701796 A KR 900701796A KR 910700251 A KR910700251 A KR 910700251A
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methoxy
hexahydro
benzo
trans
isoindole
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KR1019900701796A
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에프. 드버나디스 죤
디. 마이어 마이클
비. 십피 케빈
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원본미기재
애보트 래보러토리즈
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Publication of KR910700251A publication Critical patent/KR910700251A/ko

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/62—Naphtho [c] pyrroles; Hydrogenated naphtho [c] pyrroles
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D209/56—Ring systems containing three or more rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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Abstract

내용 없음.

Description

5-HT 선택제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 하기 일반식(I)의 화합물 및 약제학적으로 허용되는 이의 염.
    상기 식에서, R1은 수소이거나 전자흡인성 그룹이고, R2는 수소, 저급알킬 또는 아르알킬이며, m 및 n은 1 내지 3의 값을 갖는 정수이고; R4는 수소, 할로겐, 저급알킬, 저급알콕시 및 아릴(저급알킬)중에서 선택되는 원소이며, R2및 R4는 함께 알킬렌디옥시 가교를 형성하고; R3은 수소, 저급알킬, 저급알콕시, 아릴(저급알킬), 아릴아미도알킬리덴, 아릴알킬렌, 아릴(저급알킬) 아미도알킬리덴, 아릴(저급 알킬)아미도알킬렌, 벤조 알킬렌디옥시알킬렌, a) 일반식
    (여기서, B는 벤조, 사이클로헥실 또는 바이사이클로 환이고, A는 CO, SO 또는 SO2이며, R7은 2가 지방족 탄화수소이다)의 그룹, b) 일반식
    (여기서, q는 0 내지 3의 정수이고 R8및 R9는 수소 또는 저급알킬이거나, R8및 R9는 5 내지 7원 환을 형성하며, A 및 R7은 상기에서 정의한 바와 같다)의 그룹 및 c) 일반식
    (여기서, S 및 t는 1 내지 3의 정수이고; q, A 및 R7은 상기에서 정의한 바와 같다)의 그룹중에서 선택되는 원소이며, 또 R3이 수소, 저급알킬 또는 벤조(알킬렌디옥시) 알킬렌이고 n이 1인 겨우에, m은 2가 아니다.
  2. 제1항에 있어서, 하기 일반식으로 표현되는 화합물.
    상기식에서, R1, R2및 R3는 제1항에서 정의한 바와 같다.
  3. 제1항에 있어서, 하기 일반식으로 표현되는 화합물.
    상기식에서, R1, R2및 R3는 제1항에서 정의한 바와 같다.
  4. 제1항에 있어서, 하기 일반식으로 표현되는 화합물.
    상기식에서, R1, R2및 R3는 제1항에서 정의한 바와 같다.
  5. 제1항에 있어서, R3가
    (여기서, R7, R8및 R9는 제1항에서 정의한 바와 같다)으로 이루어진 그룹중에서 선택되는 화합물.
  6. 제2항에 있어서, 8-하드록시-2-메틸-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-메톡시-2-메틸-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-히드록시-2-에톤-1,2,3,3a,8,8a-히드록시-2-피롤-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-메톡시-2-아미노메틸-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-메톡시-2-시아노메틸-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(S-1,4-벤조디옥사닐-2-메틸)-8-메톡시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-메톡시-2-((2-페닐)에틸)-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(3-(3,3-테트라메틸렌)글루타리미틸)프로필)-8-히드록시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(4-(3,3-테트라메틸렌)글루타리미틸)부틸)-8-히드록시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(4-(3,3-디메틸)글루타리미딜)부틸)-8-메톡시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(4-(3,3-테트라메틸렌)글루타리미딜)부틸)-5-클로로-8-메톡시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(5-(3,3-테트라메틸렌)글루타리미딜)시스-부텐-2-일-8-메톡시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 2-(4-(3,3-테트라메틸렌)글루타리미딜)트랜스-부텐-2-일-8-메톡시-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-히드록시-2-(4-플루오로벤즈아미도)메틸)-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-히드록시-2-(4-(2-91,2-벤조이소티아졸린-3-온-1,1-디옥시드))부틸-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-메톡시-2-(4-(2-(1,2-벤조이소티아졸린-3-온-1,1-디옥시드))부틸)-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕피롤; 8-히드록시-2-)2-(2-프탈이미도)부틸)-1,2,3,3a,8,8a-헥사히드로인데노〔1,2-c〕 피롤중에서 선택된 화합물 및 약제학적으로 허용가능한 이의 염.
  7. 제3항에 있어서, 시스-2-(4-(3,3-테트라메틸렌)글루타르이미딜)부틸-9-하이드록시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 시스-2-(4-(3,3-테트라메틸렌)글루타르이미딜)부틸-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스-2-(4-(2-91,2-벤즈이소티아졸릴-3-온-1,1-디옥사이드))부틸-9-메톡시-2,3,3a-4,5,9b-헥사하이드로-1H-벤조〔e〕-이소인돌; 트랜스-2-(4-(3ad,4a,5,6,7,7ad-헥사하이드로-4,7-메타노-1H-이소인돌-1,3(2H)-디오닐-부틸-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕-이소인돌; 트랜스-2-(4-(3,3-테트라메틸렌)글루타르이미딜)-프로필-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스-2-(4-Ba,4,4a,6a,7,7a-헥사하이드로-4,7-에탄노-1H-사이클로부트〔f〕이소인돌-1,3-디오닐)-부틸)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스-2-(2-아미노에틸)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스-2-(2-아미노에틸)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스-2-(3-아미노프로필)-9-메톡시-2,3,3a-4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스 9-메톡시-2-(4-플루오로벤즈아미도)에틸)-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스 9-메톡시-2-(3-(4-플루오로벤즈아미도)프로필)-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트랜스-2-(3-(2-(1,2-벤즈이소티아졸린-3-온-1,1-디옥사이드))프로필)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 시스-2-(4-2-(1,2-벤즈이소티아졸릴-3-온-1,1-디옥사이드))부틸)-9-메톡시-2,3,3a,4,5,9b-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 시스-2-(3-(3-(3,3-테트라메틸렌)글루타르이미딜)-프로필-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 시스-2-(3-(2-(1,2-벤즈이소티아졸릴-3-온-1,1-디옥사이드))프로필)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; 트렌스-2-(4-(3a,4,4a,5,6,6a,7,7a-옥타하이드로-4,7-에타노-1H-사이클로부트〔f〕이소인돌-1,3-디모닐)-부틸)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤조〔e〕이소인돌; (-)-트랜스-2-(4-(3a,4,4a,6a,7,7a-헥사하이드로-4,7-에타노-1h-사이클로부트〔f〕인소인돌-1,3-디모닐)-부틸)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-1H-벤즈〔e〕이소인돌; 및 (f) -트랜스-2-(4-(3a,4,4a,6a,7,7a-헥사하이드로-4,7-에타노-1H-사이클로부트〔f〕인소인돌-1,3-디모닐)-부틸)-9-메톡시-2,3,3a,4,5,9b-헥사하이드로-헥사하이드로-1H-벤즈〔e〕이소인돌; 중에서 선택된 화합물 및 이의 약제학적으로 허용되는 염.
  8. 제4항에 있어서, 시스-2-벤질--5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노〔2,1-C〕피리딘; 트란스-2-벤질-5-메톡시-2,3,4,4a,9,9a-헥사하이드록-1H-인데노〔2,1-C〕피리딘; 시스-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노〔2,1-C〕피리딘; 트란스-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노〔2,1-C〕피리딘; 트란스-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노〔2,1-C〕피리딘; 시스-5-하이드록시-2-프로필-2,3,4,4a,9,9a-헥사하이드로-1H-인데노〔2,1-C〕피리딘; 시스-2-(2,3-테트라메틸렌)글루오로이미딜)푸로필-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노-〔2,1-C〕피리딘; 트란스-2-(3,3-테트라메틸렌)글루타르이미딜)프로필-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노-〔2,1-C〕피리딘; 트란스-2-(3-(2-(1,2-벤즈이소티아졸린-3-온-1,1-디옥사이드))프로필-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노-〔2,1-C〕피리딘; 트란스-2-(4-(2-(1,2-벤즈이소티아졸릴-3-온-1,1-디옥사이드))부틸-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노-〔2,1-C〕피리딘; 트란스-2-(2-(4-플루오로벤즈아미도)에틸)-5-메톡시-2,3,4,4a,9,9a-헥사하이드로-1H-인데노-〔2,1-C〕피리딘 하이드로클로라이드로 이루어진 그룹중에서 선택된 화합물 및 약제학적으로 허용되는 이의 염.
  9. 약제학적으로 허용되는 담체와 함께 고혈압억제에 유효한 양의 하기 일반식(I)의 화합물 및 이의 약제학적으로 허용되는 염을 함유함을 특징으로 하는 약제학적 조성물.
    상기 식에서, R1은 수소 또는 전자 흡인 그룹이며, R2는 수소, 저급 알킬 또는 아르알킬이고, m 및 n은 1 내지 3의 정수이며, R4는 수소, 할로겐, 저급알킬, 저급알콕시, 및 아릴(저급알릴)중에서 선택된 그룹이고, R2및 R4는 함께 알킬렌디옥시 가교그룹을 형성하며, R3은 수소, 저급 알킬, 저급 알콕시, 아릴(저급 알킬), 아릴아미도알킬리덴, 아릴알킬렌, 아릴(저급알킬) 아미도알킬리덴, 아릴(저급 알킬)아미도알킬렌, 벤조알킬렌디옥시알킬렌, a) 일반식
    (여기서, B는 벤조, 사이클로헥실, 또는 비사이클로환이며, A는 CO, SO, 또는 SO2이고, R7은 2가 지방족 탄화수소이다)의 그룹, b) 일반식
    (여기서, q는 0 내지 3의 정수이고, R8및 R9는 수소 또는 저급알킬이거나, R8과 R9는 함께 5 내지 7원환을 형성하며, A 및 R7은 상기 정의한 바와 같다)의 그룹, c) 일반식
    (여기서, s 및 t는 독립적으로 1 내지 3의 정수이며, q, A 및 R7은 상기 정의한 바와 같다)의 그룹 중에서 선택된 그룹이며, 단 R3이 수소, 저급알킬, 또는 벤조(알킬렌 디옥시)알킬렌이고 n이 1인 경우, m은 2가 아니다.
  10. 중추 5-HT1A수용체의 조절이 필요한 포유동물에게 제1항에서 정의한 바와 같은 화합물의 치료학적 유효량을 투여함을 특징으로 하여, 포유동물의 중추 5-HT1A 수용체를 조절하는 방법.
  11. 고혈압, 불안증 또는 우울증의 치료가 필요한 포유동물에게 제1항에서 정의한 바와 같은 화합물의 치료학적 유효량을 투여하는 특징으로 하여, 포유동물의 고혈압, 불안증 또는 우울증을 치료하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900701796A 1988-12-15 1989-12-07 5-ht 선택제 KR910700251A (ko)

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AU626621B2 (en) 1992-08-06
DK194490D0 (da) 1990-08-15
DK171061B1 (da) 1996-05-13
WO1990006927A1 (en) 1990-06-28
EP0422134A4 (en) 1992-05-06
DE68926673T2 (de) 1997-01-16
DK24595A (da) 1995-03-10
AU4746090A (en) 1990-07-10
DK194490A (da) 1990-10-12
JPH03502701A (ja) 1991-06-20
EP0422134B1 (en) 1996-06-12
ATE139230T1 (de) 1996-06-15
DE68926673D1 (de) 1996-07-18
ES2090119T3 (es) 1996-10-16

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