KR890009870A - 피페리디닐 화합물 - Google Patents

피페리디닐 화합물 Download PDF

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KR890009870A
KR890009870A KR1019880016691A KR880016691A KR890009870A KR 890009870 A KR890009870 A KR 890009870A KR 1019880016691 A KR1019880016691 A KR 1019880016691A KR 880016691 A KR880016691 A KR 880016691A KR 890009870 A KR890009870 A KR 890009870A
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에이.카르 알버트
씨.데이지 리차드
이.코에르너 존
퉁리
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개리 디.스트리트
메렐다우 파마슈티칼스 인코포레이티드
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Abstract

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Description

피페리디닐 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. 다음 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 산부가염.
    상기식에서, Y는 H, CO(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다) 또는 S02(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다)이고; X는 CO, CHOH 또는 C=N-O-A(여기에서, A는 수소 또는 C1-4알킬이다)이며; R은 할로겐, 저급알킬그룹, 저급 알콕시그룹, 및 수소로 이루어진 그룹으로부터 선택되거나, 2가 치환체로 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시치환체를 나타내며; m은 1 내지 5의 정수이며, 단 X가 CO 또는 CHOH인 경우 Y는 S02(CH2)nCH3가 아니다.
  2. 부정맥 질환을 치료하거나 부정맥질환의 발명을 예방하기에 충분한 양의 제1항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 심부정맥을 예방하거나 치료하는 방법.
  3. 제1항에 있어서, X가 C=N-O-A인 화합물.
  4. 진통제로 유효한 양의 일반식(Ⅰ)화합물 및 약제학적으로 허용되는 이의 산부가염을, 이를 필요로 하는 환자에게 투여함을 특징을로 하여 통증을 해소하거나 경감시키는 방법:
    상기식에서 Y는 H,CO(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다) 또는 S02(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다)이고; X는 CO, CHOH 또는 C=N-O-A(여기에서, A는 수소 또는 C1-4알킬이다)이며; R은 할로겐, 저급알킬그룹, 저급 알콕시그룹, 및 수소로 이루어진 그룹으로부터 선택되거나, 이가 치환체로 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시치환체를 나타내며; m은 1 내지 5의 정수이다.
  5. 불안해소량의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 불안을 해소시키거나 경감시키는 방법.
  6. 협심증 치료량의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 여러가지 협심증을 치료하는 방법.
  7. 식욕 불량 치료량의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 신경성 식욕불량을 치료하는 방법.
  8. 환자의 증후군을 해소하거나 경감시키기에 충분한 양의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 레이노 현상을 치료하는 방법.
  9. 경련 치료량의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 관상 혈관 경련을 치료하는 방법.
  10. 혈전증치료량의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 혈전붕괴성질환을 치료하는 방법.
  11. 섬유성근통증의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 섬유성 근통증을 치료하는 방법.
  12. EPS치료량의 제4항에 따른 화합물을 이를 필요로 하는 환자에게 투여함을 특징으로 하여 신경이완 치료와 관련된 추체외로의 부작용을 치료하는 방법.
  13. 일반식(Ⅳ)의 중간체 화합물.
    상기식에서 Y는 H,CO(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다) 또는 S02(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다)이고; X는 CO, CHOH 또는 C=N-O-A(여기에서, A는 수소 또는 C1-4알킬이다)이며, 단 X가 CO 또는 CHOH인 경우 Y는 S02(CH2)nCH3가 아니다.
  14. 수축력을 증가시키는 양의 하기 일반식의 화합물을 이를 필요로하는 환자에게 투여함을 특징으로 하여 심장 수축력을 증가시키는 방법.
    상기식에서, R, m 및 n은 제1항에서 정의한 바와 같고, R1은 C1-6알킬이며, P는 1 내지 6의 정수이다.
  15. a) 일반식(Ⅱ)와 일반식(Ⅲ)의 화합물간에 프리델 크라프트(Friedel-Crafts)아실화 반응을 수행하고; b) 단계 (a)에서 수득된 생성물을 일반식(Ⅳ)의 화합물과 반응시킴을 특징으로하여, 일반식(Ⅰ-1)의 화합물 및 약제학적으로 허용되는 이의 산 부가염을 제조하는 방법.
    상기식에서 Y는 H, CO(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다) 또는 S02(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다)이고, R은 할로겐, 저급알킬그룹, 저급알콕시그룹, 및 수소로 이루어진 그룹으로부터 선택되거나, 2가 치환체로 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시그룹이며, m은 1 내지 5의 정수이고, Z는 브롬, 염소 및 요오드로부터 선택된 할로겐 원자이다.
  16. a) 일반식(Ⅰ-1)의 화합물을 환원시키거나, b) 일반식(Ⅳ)의 화합물을 환원시키고, 환원된 생성물을 일반식(Ⅴ)의 화합물과 반응시킴을 특징으로하여, 일반식 (Ⅱ-2)의 화합물 및 약제학적으로 허용되는 이의 산부가염을 제조하는 방법.
    상기식에서 Y는 H, CO(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다) 또는 S02(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다)이고, R은 할로겐, 저급알킬그룹, 저급알콕시그룹, 및 수소로 이루어진 그룹으로부터 선택되거나, 2가 치환체로 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시그룹이며, m은 1 내지 5의 정수이고, Z는 Br, C1 또는 Ⅰ이다.
  17. 일반식(Ⅰ-1)의 화합물과 NH2-O-A-화합물간에 친핵성 부가반응을 수행함을 특징으로 하여 일반식(Ⅰ-3)의 화합물 및 약제학적으로 허용되는 이의 산부가염을 제조하는 방법.
    상기식에서 Y는 H, CO(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다) 또는 S02(CH2)nCH3(여기에서 n은 0 내지 3의 정수이다)이고, A는 H 또는 C1-4알킬이며, R은 할로겐, 저급알킬그룹, 저급 알콕시그룹, 및 수소로 이루어진 그룹으로부터 선택되거나, 2가 치환체로 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시치환체를 나타내며; m은 1 내지 5의 정수이다.
  18. 일반식(Ⅰ-4)의 화합물을 가수분해시킴을 특징으로 하여 일반식(Ⅰ-5)의 화합물 및 약제학적으로 허용되는 이의 산부가염을 제조하는 방법.
    상기식에서 X는 CO, CHOH 또는 C=N-O-A(여기에서, A는 수소 또는 C1-4알킬이다)이고, R은 할로겐, 저급알킬그룹, 저급 알콕시그룹, 및 수소로 이루어진 그룹으로부터 선택되거나, 2가 치환체로 3,4-메틸렌디옥시 또는 3,4-에틸렌디옥시그룹이고, m은 1 내지 5의 정수이다.
    ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880016691A 1987-12-17 1988-12-15 피페리디닐 화합물 KR890009870A (ko)

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JPH02138214A (ja) * 1987-12-10 1990-05-28 Merrell Dow Pharmaceut Inc 不安を治療する方法
ZA891901B (en) * 1988-03-17 1989-11-29 Merrell Dow Pharma Method for the treatment of the extrapyramidal side effects associated with neuroleptic therapy
JP2969359B2 (ja) * 1989-01-13 1999-11-02 武田薬品工業株式会社 環状アミン化合物
NZ236501A (en) * 1989-12-21 1992-12-23 Merrell Dow Pharma Piperidine derivatives and antithrombotic compositions
US5292752A (en) * 1989-12-21 1994-03-08 Merrell Dow Pharmaceuticals Inc. Antithrombotic compounds
EP0531410B1 (en) * 1990-06-01 1994-11-30 Merrell Dow Pharmaceuticals Inc. (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(fluorophenyl)ethyl]-4-piperidinemethanol
US5478846A (en) * 1990-06-07 1995-12-26 Merrell Dow Pharmaceuticals Inc. 1-piperidinyl alkanoylanyl sulfonamides for treatment of cardiac arrhythmia
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US5254689A (en) * 1992-02-25 1993-10-19 American Home Products Corporation Piperdinyl and piperazinyl derivatives
US5202346A (en) * 1992-02-25 1993-04-13 American Home Products Corporation Piperidinyl and piperazinyl derivatives
EP0661266A1 (en) * 1993-12-27 1995-07-05 Toa Eiyo Ltd. Substituted cyclic amine compounds as 5HT2 antagonists
DE19934433A1 (de) * 1999-07-22 2001-01-25 Merck Patent Gmbh N-(Indolcarbonyl-)piperazinderivate
DE19939756A1 (de) * 1999-08-21 2001-02-22 Merck Patent Gmbh Piperidinalkohole
WO2001064670A1 (fr) 2000-02-29 2001-09-07 Mitsubishi Pharma Corporation Nouveaux derives amide cycliques
US6914142B2 (en) * 2001-10-15 2005-07-05 Schering Corporation Synthesis of (4-bromopnenyl)(4-piperidyl)methanone-(Z)-O-ethyloxime and salts
DE10201550A1 (de) * 2002-01-17 2003-07-31 Merck Patent Gmbh Phenoxy-Piperidine
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