KR950011408A - 사이클릭 아민 유도체 - Google Patents

사이클릭 아민 유도체 Download PDF

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KR950011408A
KR950011408A KR1019940026700A KR19940026700A KR950011408A KR 950011408 A KR950011408 A KR 950011408A KR 1019940026700 A KR1019940026700 A KR 1019940026700A KR 19940026700 A KR19940026700 A KR 19940026700A KR 950011408 A KR950011408 A KR 950011408A
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carbon atoms
methylsulfonamidophenylethyl
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바움가르트 만프레드
루에스 잉게
밍크 클라우스-옷토
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위르겐 호이만, 라인하르트 슈틀러
메르크 파텐트 게젤샤프트 미트 베쉬랭크터 하프퉁
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Abstract

하기 일반식(Ⅰ)의 사이클릭 아민 유도체 및 그의 생리학적으로 허용가능한 염은 항부정맥 효과를 나타낸다 :
상기식에서, Ar 및 Ar'는 각각 서로 독립적으로, 비치한되거나 또는 NO2, NH2, Hal, CF3, A, NHSo2A 또는 NHAc에 의해 한번 또는 두번 치환된 페닐이고, X 및 Y는 각각 서로 독립적으로, 0 또는 결합이고, m은 0 또는 1이고, n은 0, 1 또는 2이고, p은 0,1,2 또는 3이고, q은 2 또는 3이고, A는 탄소원자수 1 내지 6개의 알킬이고, Hal은 F, Cl, Br 또는 1이고, Ac는 탄소원자수 1 내지 8개의 알카노일, 탄소원자수 8 내지 10개의 아르알카노일 또는 탄소원자수 7 내지 11개의 아로일이다.

Description

사이클릭 아민 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 하기 일반식(Ⅰ)의 사이클릭 아민 유도체 및 이들의 생리학적으로 허용가능한 염 :
    상기식에서, Ar 및 Ar'는 각각 서로 독립적으로, 비치한되거나 또는 NO2, NH2, Hal, CF3, A, NHSo2A 또는 NHAc에 의해 한번 또는 두번 치환된 페닐이고, X 및 Y는 각각 서로 독립적으로, 0 또는 결합이고, m은 0 또는 1이고, n은 0, 1 또는 2이고, p은 0,1,2 또는 3이고, q은 2 또는 3이고, A는 탄소원자수 1 내지 6개의 알킬이고, Hal은 F, Cl, Br 또는 1이고, Ac는 탄소원자수 1 내지 8개의 알카노일, 탄소원자수 8 내지 10개의 아르알카노일 또는 탄소원자수 7 내지 11개의 아로일이다.
  2. 제1항에 따르는 일반식(Ⅰ)화합물의 거울상이성질체.
  3. (a) 1-(2-p-메틸설폰아미도페닐에틸)-3-(p-메틸설폰아미도페녹시)피페리딘; (b) 1-(2-p-메틸설폰아미도페닐에틸)-2-(p-메틸설폰아미도페녹시메틸)피롤리딘; (c) 1-(2-p-메틸설폰아미도페닐에틸)-3-(p-니트로페녹시)피롤리딘; (d) 1-(2-p-아세트아미도페닐에틸)-3-(p-아세트아미도페녹시)피롤리딘; (e) 1-(2-p-메틸설폰아미도페닐에틸)-3-(p-메틸설폰아미도페녹시)피롤리딘; (f) 1-(2-p-니트로페닐에틸)-2-(p-니트로페녹시메틸)피페리딘; (g) 1-(2-p-니트로페닐에틸)-3-(p-니트로페녹시헥사하이드로아제핀; (h) 1-(2-p-메틸설폰아미도페닐에틸)-2-(p-메틸설폰아미도페녹시메틸)피페리딘; (i) 1-(2-p-메틸설폰아미도페닐에틸)-3-(p-메틸설폰아미도페녹시헥사하이드로아제핀; (j) 1-(2-p-메틸설폰아미도페닐에틸)-4-(p-메틸설폰아미도페녹시)피페리딘; (k) 1-(2-p-메틸설폰아미도페닐에틸)-3-(p-메틸설폰아미도페녹시메틸)피페리딘.
  4. 하기 일반식(Ⅱ)의 화합물을 하기 일반식(Ⅲ)의 화합물과 반응시키거나, 또는 Y가 산소인 제1항에 따르는 하기 일반식(Ⅰ)의 화합물을 제조하기 위해, 하기 일반식(Ⅳ)의 화합물을 하기 일반식(Ⅴ)의 화합물과 반응시키거나, 또는 하기 일반식(Ⅴa)의 화합물을 하기 일반식(Ⅵ)의 화합물과 반응시키거나, 또는 일반식(Ⅰ)에 상응하지만, 하나 이상의 CH2대신에 하나 이상의 환원가능한 그룹을 갖는 화합물을 환원에 의해 일반식(Ⅰ)의 화합물로 전환시키고/시키거나, 일반식(Ⅰ)의 화합물중의 Ar 및 Ar'그룹 중 하나 또는 두개 모두를 각각 다른 라디칼 Ar 및 Ar'로 전환시키고/시키거나, 일반식(I)의 염기성 화합물을 산으로 처리하여 그의 생리학적으로 허용가능한 산 부가염증의 하나로 전환시킴을 특징으로 하는, 제1항에 따르는 일반식(Ⅰ)의 화합물의 제조 방법 :
    Ar-X-(CH2)q-L (Ⅲ)
    Ar'-Z (Va)
    상기식에서, Ar 및 Ar'는 각각 서로 독립적으로, 비치한되거나 또는 NO2, NH2, Hal, CF3, A, NHSo2A 또는 NHAc에 의해 한번 또는 두번 치환된 페닐이고, X 및 Y는 각각 서로 독립적으로, 0 또는 결합이고, m은 0 또는 1이고, n은 0, 1 또는 2이고, p은 0,1,2 또는 3이고, q은 2 또는 3이고, A는 탄소원자수 1 내지 6개의 알킬이고, Hal은 F, Cl, Br 또는 1이고, Ac는 탄소원자수 1 내지 8개의 알카노일, 탄소원자수 8 내지 10개의 아르알카노일 또는 탄소원자수 7 내지 11개의 아로일이고, L은 OH, Cl, Br 또는 반응성, 작용성 변형 OH 그룹이고, Z는 OH 또는 염과 유사한 특성을 가진 그룹을 포함하는 반응성, 작용서 변형 OH 그룹이다.
  5. 적어도 하나의 고형, 액체 또는 반고체 비히클 또는 보조 물질과 함께 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 염중 하나를 적합한 투여 형태로 전환시킴을 특징으로 하는, 약학적 제제의 제조 방법.
  6. 일반식(Ⅰ)의 적어도 하나의 화합물 및/또는 그의 생리학적으로 허용가능한 염중 하나를 함유함을 특징으로 하는 약학적 제제.
  7. 약물을 제조하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용가능한 염의 용도.
  8. 질병을 치료하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용가능한 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940026700A 1993-10-20 1994-10-19 사이클릭 아민 유도체 KR950011408A (ko)

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ZA9610745B (en) * 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists
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RU94038254A (ru) 1996-09-10
NO943961D0 (no) 1994-10-19
EP0649838A1 (de) 1995-04-26
HU9403010D0 (en) 1994-12-28
AU7588394A (en) 1995-05-11
JPH07188162A (ja) 1995-07-25
HUT72294A (en) 1996-04-29
ZA948211B (en) 1995-06-12
CZ257794A3 (en) 1995-11-15
CA2118375A1 (en) 1995-04-21
PL305487A1 (en) 1995-05-02
DE4335718A1 (de) 1995-04-27
TW275062B (ko) 1996-05-01
SK125994A3 (en) 1995-05-10
CN1107469A (zh) 1995-08-30
NO943961L (no) 1995-04-21

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