KR910014350A - 3-아미노피페리딘 유도체 및 관련 질소 함유 헤테로사이클릭 화합물 - Google Patents

3-아미노피페리딘 유도체 및 관련 질소 함유 헤테로사이클릭 화합물 Download PDF

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KR910014350A
KR910014350A KR1019910000001A KR910000001A KR910014350A KR 910014350 A KR910014350 A KR 910014350A KR 1019910000001 A KR1019910000001 A KR 1019910000001A KR 910000001 A KR910000001 A KR 910000001A KR 910014350 A KR910014350 A KR 910014350A
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씨.데자이 마노즈
제이.로젠 테리
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알렌 제이.스피겔
화이자 인코포레이티드
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Abstract

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Description

3-아미노피페리딘 유도체 및 관련 질소 함유 헤테로사이클릭 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용되는 산 부가염 :
    상기식에서, Y는 (CH2)14(여기서 n은 1내지 4의 정수이다)이고, 여기에서, 상기 (CH2)14의 탄소-탄소 단일결합중 어느 하나는 탄소-탄소 이중결합에 의해 임의로 대체될 수 있고, 상기 (CH2)14의 탄소원자중 어느 하나는 R7로 임의로 치환될 수 있으며, 상기 (CH2)14의 탄소원자중 어느 하나는 R7로 임의로 치횐될 수 있고; m은 0 내지 6의 정수이며, 상기 (CH2)14의 탄소-탄소 단일 결합중 어느 하나는 탄소-탄소 이중결합 또는 탄소-탄소 3중결합으로 임의로 대체될 수 있고, 상기 (CH2)14의 탄소의 원자중 어느 하나는 R8로 임의로 치환될 수 있으며, R1은 수소이거나 또는 하이드록시, 알콕시 또는 플루오로로 임의로 치환된 (C1-C8)알킬이고; R2는 수소, (C1-C6)직쇄 또는 측쇄알킬, (C3-C7)사이클로알킬(여기서, 탄소원자중 하나는 질소, 산소 또는 황으로 임의로 대체될수 있다)중에서 선택되는 라디칼, 페닐 및 나프틸중에서 선택되는 아릴, 인다닐, 티에닐, 푸릴, 피리딜, 티아졸릴, 이소티아졸릴, 옥사졸릴; 이속사졸릴, 트리아졸릴, 테트라졸릴, 및 퀴놀릴중에서 선택되는 헤테로아릴; 페닐(C2-C6)알킬, 벤즈하이드릴 및 벤질이며, 여기에서, 상기 아릴 및 헤테로아릴 그룹 각각과 상기 벤질, 페닐(C2-C6)알킬 및 벤즈하이드릴의 페닐 잔기는 할로, 나트로, (C1-C6)알킬, (C1-C6)알콕시, 트리플루오로메틸, 아미노, (C1-C6)알킬아미노, (C1-C6)알킬(C1-C8)알킬알킬,
    알킬중에서 독립적으로 선택된 하나 이상의 치환체로 임의로 치환될 수 있고, 여기에서, 상기 벤즈하이드릴의 페닐 잔기중 하나는 나프틸, 티에닐, 푸릴 또는 피리딜로 임의로 대체될 수 있으며, R5는 수소, 페닐 또는 (C1-C6)알킬이거나, 또는 R2및 R5는 그들이 결합되어 있는 탄소와 함께 3내지 7개의 탄소원자를 갖는 포화 카보사이클릭 고리(여기에서, 상기 탄소원자중 하나는 산소, 질소 또는 황으로 임의로 대체될 수 있다)를 형성하고, R3은 페닐 및 나프틸중에서 선택되는 아릴, 인다닐, 티에닐, 푸릴, 피리딜, 티아졸릴, 이소티아졸릴, 옥사졸릴, 이속사졸릴, 트리아졸릴, 테트라졸릴 및 퀴놀릴중에서 선택되는 헤테로아릴, 및 3내지 7개의 탄소 원자를 갖는 사이클로알킬(여기에서, 상기 탄소원자중 하나는 질소, 산소 또는 황으로 임의로 대체될 수 있다)이며, 여기에서, 상기 아릴 및 헤테로아릴 그룹 각각은 하나 이상의 치환체로 임의로 치환될 수 있고, 상기 (C3-C7)사이클로알킬은 할로, 니트로, (C1-C6)알킬, (C1-C6)알콕시, 메틸, 트리플루오로메틸, 아미노, (C1-C6)알킬아미노,알킬, -(C1-C8)알킬알킬,및알킬중에서 독립적으로 선택된 1 또는 2개의 치환체로 임의로 치환될 수 있으며, R4및 R7은 각각 수소, 하이드록시, 할로, 아미노, 옥소(=O), 니트릴, (C1-C6)알킬아미노, 디-(C1-C8)알킬아미노, (C1-C6)알콕시, (C1-C6)알킬 및 R2의 정의에서 언급한 라디칼중에서 독립적으로 선택되며, R6는NHCH2R9, SO2R2, 또는 R2, R4및 R7의 정의에서 언급한 라디칼 중 하나이고, R8는 옥스이미노(=NOH) 또는 R2, R4및 R7의 정의에서 언급한 라디칼 중 하나이며, R9은 (C1-C6)알킬, 수소, 페닐 또는 페닐(C1-C6)알킬이나; 단, (a) m이 0이고 R8이 부재하는 경우, (b) R4,R6, 또는 R7중 어느 것도 그들이 결합된 탄소와 함께 R5를 갖는 고리를 형성할 수 없는 경우, 및 (c)R4및 R8이 동일한 탄소원자에 결합되어 있는 경우에는, R4및 R7각각은 수소, 플루오로 및 (C1-C6)알킬중에서 독립적으로 선택되거나, 또는 R4및 R7은 그들이 결합되어 있는 탄소와 함께 (C3-C6) 포화 카보사이클릭 고리(이것은 그들이 결합되어 있는 질소-함유 고리를 갖는 스피로 화합물을 형성한다)를 형성한다.
  2. 제1항에 있어서, R1, R4, R5, R6및 R7이 수소이고, R2가 페닐이며, R3이 2-메톡시페닐(여기서, 페닐 잔기는 염소, 불소, (C1-C6)알콕시 또는 트리플루오로 메탄으로 임의로 치환될 수 있다)이고, n이 3 또는 4이며, m이 0인 화합물.
  3. 하기 일반식(Ⅶ)의 화합물 :
    상기식에서 R1, R2, R3, R4, R5, 및 R7은 제1항에서 정의한 바와 같다.
  4. 제1내기 제3항중 어느 한 항에 따른 화합물의 3중 수소 및14C-동위원소로 이루어진 그룹중에서 선택되는 상기 화합물의 방사성 동위원소.
  5. 3-아미노-2-페닐피페리딘.
  6. (2S, 3S)-3-아미노-2-페닐피페리딘.
  7. 염증 질환, 불안증, 대장염, 우울증 또는 기분변조 질환, 정신변, 동통, 알러지, 만성 폐색성 기도 질병, 과민성 질환, 혈관수축 질환, 섬유화 및 콜라겐성 질환, 반사교감신경 디스트로피, 중독 질환, 스트레스 관련 신체장애, 말초신경장애, 신경통, 신경병리학적 질환, 면역 증대 또는 억제와 관련된 질병 및 류마티스성 질환으로 이루러진 그룹중에서 선택된 질환을 예방 또는 치료하는데 효과적인 양의 제1항 또는 2항에 따르는 화합물 및 약학적으로 허용되는 담체를 포함하는, 포유동물에 있어서 상기 질환을 치료 또는 예방하기 위한 약학 조성물.
  8. 염증 질환, 불안증, 대장염, 우울증 또는 기분변조 질환, 정신병, 동통, 알러지, 만성 폐색성 기도 질병, 과민성 질환, 혈관수축 질환, 섬유화 및 콜라겐성 질환, 반사교감신경 디스트로피, 중독 질환, 스트레스 관련 신체장애, 말초신경장애, 신경통, 신경병리학적 질환, 면역 증대 또는 억제와 관련된 질병 및 류마티스성 질환으로 이루러진 그룹중에서 선택된 질환을 예방 또는 치료하는데 효과적인 양의 제1항 또는 2항에 따르는 화합물을 상기와 같은 치료 또는 예방을 필요로 하는 포유동물에게 투여함을 포함하는, 포유동물에 있어서 상기 질환을 치료 또는 예방하는 방법.
  9. 물질 P의 수용체 부위에서의 작용에 길항작용하기에 효과적인 양의 제1항 또는 제2항에 따르는 화합물 및 약학적으로 담체를 포함하는, 포유동물에 있어서 물질 P매개 신경 전달의 감소에 의해 치료 또는 예방되거나, 또는 치료 또는 예방이 촉진되는 질환을 치료 또는 예방하는 방법.
  10. 물질 P의 수용체 부위에서의 작용에 길항작용하기에 효과적인 양의 제1항 또는 제2항에 따르는 화합물 또는 그의 약학적으로 허용되는 염을, 물질 P매개 신경 전달의 감소에 의해 치료 또는 예방되거나, 또는 치료 또는 예방이 촉진되는 질환의 치료 또는 예방을 필요로 하는 포유동물에게 투여함을 포함하는, 포유동물에 있어서 상기 질환을 치료 또는 에방하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910000001A 1990-01-04 1991-01-03 3-아미노피페리딘 유도체 및 관련 질소 함유 헤테로사이클릭 화합물 KR930009441B1 (ko)

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CN1045595C (zh) 1999-10-13
IL112348A0 (en) 1995-03-30
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IL96821A0 (en) 1991-09-16
HUT68179A (en) 1995-05-29
PL164205B1 (en) 1994-06-30
CZ289485B6 (cs) 2002-02-13
HU220602B1 (hu) 2002-03-28
MY105438A (en) 1994-10-31
HU222724B1 (hu) 2003-09-29
EP0436334A3 (en) 1992-05-27
IE63770B1 (en) 1995-06-14
IL96821A (en) 1997-03-18
NO178187C (no) 1996-02-07
PL164244B1 (en) 1994-07-29
FI114096B (fi) 2004-08-13
CA2033497C (en) 1997-01-07
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PL288592A1 (en) 1992-06-15
CA2033497A1 (en) 1991-07-05
CN1053060A (zh) 1991-07-17
IL112348A (en) 1998-06-15
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UA41251C2 (uk) 2001-09-17
PL293392A1 (en) 1992-07-13
PL293389A1 (en) 1992-07-13
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HUT60719A (en) 1992-10-28
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