KR920700209A - 치환된 벤조[5,6]사이클로헵타피리딘의 헤테로사이클릭 n-옥사이드 유도체, 조성물 및 용도 - Google Patents

치환된 벤조[5,6]사이클로헵타피리딘의 헤테로사이클릭 n-옥사이드 유도체, 조성물 및 용도

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KR920700209A
KR920700209A KR1019900702706A KR900702706A KR920700209A KR 920700209 A KR920700209 A KR 920700209A KR 1019900702706 A KR1019900702706 A KR 1019900702706A KR 900702706 A KR900702706 A KR 900702706A KR 920700209 A KR920700209 A KR 920700209A
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제이. 피빈스키 존
제이. 그린 마이클
웡 제시
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제임스 알. 넬슨
쉐링 코포레이션
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Abstract

내용 없음

Description

치환된 벤조[5, 6]사이클로헵타피리딘의 헤테로사이클릭 N－옥사이드 유도체, 조성물 및 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. 일반식(Ⅰ)의 화합물, 약제학적으로 허용되는 이의 염 또는 이의 용매화물.
    상기식에서, R은 일반식 (ⅰ), (ⅱ), (ⅲ) 또는 (ⅳ)의 N-옥사이드 헤테로사이클릭 그룹을 나타내거나
    R은 상기한 일반식 (ⅰ), (ⅱ), (ⅲ) 또는 (ⅳ)의 헤테로사이클릭 N－옥사이드 그룹에 의해 치환된 알킬그룹이고, a, b, c 및 d 중의 하나는 N 또는 NR12〔여기서, R12는 0, －CH3또는 －(CH2)nCO2H(여기서, n은 1 내지 3이다)이다〕이고, 나머지 a, b, c 및 d그룹은 R1또는 R2에 의해 임의로 치환될 수 있으며, R1및 R2는 동일하거나 상이하며, 각각 독립적으로 할로, －CF3, －OR13, －COR13, －SR13, －S(O)eR14(여기서, e는 1 또는 2이다), －N(R13)2, －NO2, －OC(O)R13, －CO2R13, －OCO2R14, 알키닐, 알케닐 또는 알킬이고, 여기서 알킬그룹은 할로, －OR13또는－CO2R13에 의해 치환될 수 있으며 알케닐 그룹은 할로, －OR14또는 －CO2R13에 의해 치환될 수 있으며, R3및 R4는 동일하거나 상이하며 각각 독립적으로 H 또는 R1및 R2의 치환체를 나타내거나, R3및 R4는 함께 벤젠환에 융합된 포화 또는 불포화 C5－C7카보사이클릭환을 나타내고, R5, R6, R7및 R8은 각각 독립적으로 H, －CF3, 알킬 또는 아릴을 나타내고, 여기서 알킬 또는 아릴은 －OR13, －SR13또는 －N(R13)2에 의해 치환될 수 있으며, R5는 R6과 함께 = O 또는 =S를 나타낼 수 있고, 있거나 R7은 R8과 함께 = O 또는 = S를 나타낼 수 있고, R9, R10및 R11은 동일하거나 상이하며 각각 독립적으로 H, 할로, －CF3, －OR13, －C(O)R13, －SR13, －S(O)eR14(여기서, e는 1 내지 2이다), －N(R13)2, －NO2, －CO2R13, －OCO2R14, －OCOR13, 알킬, 아릴, 알케닐 또는 알키닐이고, 여기서 알킬 또는 알케닐은 －OR13, －SR13또는 －N(R13)에 의해 치환될 수 있으며 알케닐은 OR14또는 SR14에 의해 치환될 수 있으며, R13은 H, 알킬 또는 아릴이고 R14는 알킬 또는 아릴이고, R13는 H또는 알킬이고, X는 N, CH 또는 C이고, X가 C를 나타내는 경우, 탄소원자 11에 점선으로 나타낸 임의의 이중결합이 존재하며, X가 N 또는 CH인 경우, 이중결합은 존재하지 않으며, 탄소원자 5와 6사이의 점선은 임의의 이중결합을 나타내며, 이중결합이 존재하는 경우, A와 B는 각각 독립적으로 －R13, 할로, －OR14, －OC(O)R13또는 -OCO2R14를 나타내고, 탄소원자 5와 6사이에 이중결합이 존재하지 않는 경우, A와 B는 독립적으로 H2, －(OR14)2, 〔H 및 할로〕, 디할로, 〔알킬 및 H〕, (알킬)2, 〔－H 및 OC(O)R13〕, 〔H 및 －OR13〕, = 0, 〔아릴 및 H〕, =NOR15또는 －O－(CH2)p－O－(여기서, p는 2, 3 또는 4이고 R13은 상기에서 정의한 바와 같다)를 나타내고, Z는 =0 또는 =S를 나타낸다.
  2. 제1항에 있어서, 탄소원자 5와 6사이에 이중결합이 존재하는 않는 화합물.
  3. 제1항에 있어서, 탄소원자 5와 6사이에 이중결합이 존재하는 않는 화합물.
  4. 제1항 내지 제3항중의 어느 한 항에 있어서, R5및 R6이 H이고 R7및 R8이 각각 독립적으로 H 또는 알킬을 나타내는 화합물.
  5. 제1항 내지 제4항중의 어느 한 항에 있어서, R1및 R2가 각각 독립적으로 H, 알킬, OR13, NR13또는 할로를 나타내는 화합물.
  6. 제1항 내지 제5항중의 어느 한 항에 있어서, R3및 R4가 각각 독립적으로 H, 알킬, OR13, NR13또는 할로를 나타내는 화합물.
  7. 제1항 내지 제6항중의 어느 한 항에 있어서, X가 C를 나타내고 X에 대한 점선이 이중결합인 화합물.
  8. 제1항 내지 제6항중의 어느 한 항에 있어서, X가 CH를 나타내고 X에 대해 점선으로 나타낸 이중결합이 존재하지 않는 화합물.
  9. 제1항 내지 제6항중의 어느 한 항에 있어서, X가 N를 나타내고 X에 대해 점선으로 나타낸 이중결합이 존재하지 않는 화합물.
  10. 제1항 내지 제9항중의 어느 한 항에 있어서, Z가 O를 나타내는 화합물.
  11. 제1항 내지 제10항중의 어느 한 항에 있어서, R이〔여기서, R9및 R10은 각각 독립적으로 H, 알킬, 할로, OR13또는 N(R13)2를 나타낸다〕를 나타내는 화합물.
  12. 제1항 내지 제11항중 어느 한 항에 있어서, R이를 나타내는 화합물.
  13. 제1항에 있어서
    인 화합물.
  14. 제1항에 있어서,
    인 화합물.
  15. 약제학적으로 허용되는 담체와 배합하여 제1항의 일반식(Ⅰ)의 화합물을 포함함을 특징으로 하는 약제학적 조성물.
  16. 제1항의 일반식(Ⅰ)의 화합물을 알러지치료 유효량으로 치료를 요하는 포유류에게 투여함을 특징으로 하는 알러지를 치료하는 방법.
  17. 제1항의 일반식(Ⅰ)의 화합물을 염증치료 유효량으로 치료를 요하는 포유류에게 투여함을 특징으로 하는 알러지를 치료하는 방법.
  18. 알러지 또는 염증 치료용 약제학적 조성물을 제조하기 위한 제1항 내지 제14항중의 어느 한 항의 화합물의 용도.
  19. a)일반식(Ⅱ)의 화합물을 커플링제의 존재하에 일반식 RCOOH의 화합물과 반응시켜 일반식(Ⅰ)의 화합물을 수득하거나 b)일반식(Ⅱ)의 화합물을 염기의 존재하에 일반식(Ⅲ)의 화합물과 반응시켜 일반식(Ⅰ)의 화합물을 수득하거나, c)일반식(Ⅳ)의 화합물을 산화제와 반응시켜 일반식(Ⅰ)의 화합물을 수득함을 특징으로 하는, 일반식(Ⅰ)의 화합물을 제조하는 방법.
    상기식에서, L은 이탈그룹이고, R9는
    R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, a, b, c, d 및 Z는 제1항에서 정의한 바와 같다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900702706A 1989-05-01 1990-04-30 치환된 벤조[5,6]사이클로헵타피리딘의 헤테로사이클릭 n-옥사이드 유도체, 이의 제조방법 및 이를 함유하는 약제학적 조성물 Expired - Fee Related KR950009859B1 (ko)

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US89-345604 1989-05-01
US345604 1989-05-01
US07/345,604 US5089496A (en) 1986-10-31 1989-05-01 Benzo[5,6]cycloheptapyridine compounds, compositions and method of treating allergies
PCT/US1990/002251 WO1990013548A1 (en) 1989-05-01 1990-04-30 Heterocyclic n-oxide derivatives of substituted benzo[5,6]cycloheptapyridines, compositions and methods of use

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NO179674B (no) 1996-08-19
US5151423B1 (en) 1994-08-30
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US5151423A (en) 1992-09-29
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ES2064520T3 (es) 1995-02-01
CA2053903A1 (en) 1990-11-02
IE66392B1 (en) 1995-12-27
NO914270D0 (no) 1991-10-31
FI915138A0 (fi) 1991-10-31
NO914270L (no) 1991-12-23
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NO179674C (no) 1996-11-27
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ATE114650T1 (de) 1994-12-15
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IL94258A (en) 1994-10-07
JP2863629B2 (ja) 1999-03-03
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KR950009859B1 (ko) 1995-08-29
US5089496A (en) 1992-02-18
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