KR970701698A - 프로스타글란딘 i₂작용물질로서의 나프탈렌 유도체(naphthalene derivatives as prostaglandin i₂agonists) - Google Patents

프로스타글란딘 i₂작용물질로서의 나프탈렌 유도체(naphthalene derivatives as prostaglandin i₂agonists)

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KR970701698A
KR970701698A KR1019960704963A KR19960704963A KR970701698A KR 970701698 A KR970701698 A KR 970701698A KR 1019960704963 A KR1019960704963 A KR 1019960704963A KR 19960704963 A KR19960704963 A KR 19960704963A KR 970701698 A KR970701698 A KR 970701698A
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기요시 다니구치
마사노부 나가노
고지 핫토리
가즈노리 츠바키
오사무 오키츠
세이이치로 다부치
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후지야마 아키라
후지사와 야쿠힝 고교 가부시키가이샤
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Abstract

본 발명은 약제로서 유용한 하기 화학식 (1)의 화합물 및 이의 약학적으로 허용가능한 염에 관한 것이다 :
상기 식에서, R1은 카르복시 또는 보호된 카르복시이며; R2는 수소, 히드록시 또는 보호된 히드록시이며; R3는 수소, 히드록시, 보호된 히드록시 등이며; R4는 수소 또는 할로겐이며; A1은 저급 알킬렌이며; A2는 결합 또는 저급 알킬렌이며; ㅡR5는(이때, R6는 모노(또는 디 또는 트리) 아릴(저급)알킬이며, Z는 N 또는 CH임)이며;은

Description

프로스타글란딘 I2작용물질로서의 나프탈렌 유도체 (NAPHTHALENE DERIVATIVES AS PROSTAGLANDINI2AGONISTS)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 하기 화학식 (1)의 화합물 및 이의 약학적으로 허용가능한 염:
    상기 식에서, R1은 카르복시 또는 보호된 카르복시이며; R2는 수소, 히드록시 또는 보호된 히드록시이며; R3는 수소, 히드록시, 보호된 히드록시, 저급 알킬 또는 할로겐이며; R4는 수소 또는 할로겐이며; A1은 저급 알킬렌이며; A2는 결합 또는 저급 알킬렌이며; ㅡR5는(이때, R6는 모노(또는 디 또는 트리) 아릴(저급)알킬이며, Z는 N 또는 CH임) 또는[이때, ㅡA3ㅡ은 또는(이때, R9은 수소 또는 저급 알킬임)이며, Q는 N 또는 CH이며, R7은 아릴이며; R8은 아릴임)]이며;은 또는이다.
  2. 제1항에 있어서, R1은 카르복시 또는 에스테르화된 카르복시이며; A1은 C1ㅡC3알킬렌이며; A2는 결합 또는 C1ㅡC3알킬렌이며; ㅡR5는(이때, R6은 디아릴(저급)알킬이며, Z는 N 또는 CH임) 또는[이때, ㅡA3ㅡ은,또는(이때, R9은 수소 또는 저급 알킬임)이며, Q는 N 또는 CH이며, R7은 아릴이며; R8은 아릴임)]인 화합물.
  3. 제2항에 있어서, ㅡR5는(이때, R6은 디페닐(저급) 알킬이며, Z는 N 또는 CH임) 또는[이때, ㅡA3ㅡ은,또는(이때, R9은 수소 또는 저급 알킬임)이며, Q는 N 또는 CH이며, R7은 페닐이며; R8은 페닐임)]인 화합물.
  4. 제3항에 있어서, R1은 카르복시 또는 저급 알콕시카르보닐이며; R2는 수소, 히드록시 또는 아실옥시이며; R3는 수소, 히드록시, 아실옥시, 저급 알킬 또는 할로겐이며; R4는 수소 또는 할로겐이며; A1은 메틸렌이며; A2는 결합, 메틸렌 또는 에틸렌이며; ㅡR5는(이때, R6은 디페닐메틸이며, Z는 N 또는 CH임) 또는[이때, ㅡA3ㅡ은,또는(이때, R9은 수소 또는 저급 알킬임)이며, Q는 N 또는 CH이며, R7은 페닐이며; R8은 페닐임)]인 화합물.
  5. 제4항에 있어서, 하기 화학식 (1h)를 갖는 화합물 :
    상기 식에서, R1은 카르복시 또는 저급 알콕시카르보닐이며; R2는 수소 또는 히드록시이며; R3는 수소, 히드록시, 저급 알킬 또는 할로겐이며; R4는 수소 또는 할로겐이며; A1은 메틸렌이며; A2는 메틸렌 또는 에틸렌이며; ㅡR5는또는이다.
  6. 제5항에 있어서, (1) (2R)ㅡ[5ㅡ(카르복시메톡시)ㅡ2ㅡ히드록시ㅡ1,2,3,4ㅡ테트라히드로ㅡ2ㅡ나프틸]메틸 N,Nㅡ디페닐카르바메이트의 나트륨 염, (2) (트랜스)ㅡ2ㅡ[5ㅡ(카르복시메톡시)ㅡ2ㅡ히드록시ㅡ1,2,3,4ㅡ테트라히드로ㅡ1ㅡ나프틸]에틸 N,Nㅡ디페닐카르바메이트의 나트륨 염 및 (3) (S)ㅡ2ㅡ[(1,2,3,4ㅡ테트라히드로ㅡ5ㅡ카르복시메톡시ㅡ2ㅡ나프틸)메틸]ㅡ6ㅡ디페닐메틸ㅡ3(2H)ㅡ디리다지논으로 구성된 군에서 선택되는 화합물.
  7. (1) 하기 화학식 (2)의 화합물 또는 이의 염을 하기 화학식 (3)의 화합물 또는 이의 염과 반응시켜 하기 화학식 (1)의 화합물 또는 이의 염을 수득하거나 또는 (2) 하기 화학식 (1a)의 화합물 또는 이의 염을 카르복시 보호기 제거 반응 처리하여 하기 화학식 (1b)의 화합물 또는 이의 염을 수득하거나 또는 (3) 하기 화학식 (4)의 화합물 또는 이의 염을 하기 화학식 (5)의 화합물 또는 이의 염과 반응시켜 하기 화학식 (1c)의 화합물 또는 이의 염을 수득하거나 또는 (4) 하기 화학식 (6)의 화합물 또는 이의 염을 하기 화학식 (7)의 화합물 또는 이의 염과 반응시켜 하기 화학식 (1d)의 화합물 또는 이의 염을 수득하거나 또는 (5) 하기 화학식 (8)의 화합물 또는 이의 염을 하기 화학식 (9)의 화합물 또는 이의 카르복시 기에서의 반응성 유도체 또는 이의 염과 반응시켜 하기 화학식 (1e)의 화합물 또는 이의 염을 수득하거나 또는 (6) 하기 화학식 (1f)의 화합물 또는 이의 염을 하기 화학식 (10)의 화합물 또는 이의 염과 반응시켜 하기 화학식 (1g)의 화합물 또는 이의 염을 수득하는 것을 포함하는 하기 화학식 (1)의 화합물 또는 이의 염을 제조하는 방법.
    상기 식에서, A1은 저급 알킬렌이며; A2는 결합 또는 저급 알킬렌이며; R1은 카르복시 또는 보호된 카르복시이며; R1 a는 보호된 카르복시이며; R2는 수소, 히드록시 또는 보호된 히드록시이며; R3는 수소, 히드록시, 보호된 히드록시, 저급 알킬 또는 할로겐이며; R4는 수소 또는 할로겐이며; ㅡR5는(이때, R6는 모노(또는 디 또는 트리)아릴(저급)알킬이며, Z는 N 또는 CH임) 또는[이때, ㅡA3ㅡ은또는(이때, R9은 수소 또는 저급 알킬임)이며, R9 a는 저급 알킬이며;
    은또는이다.
    X1은 산 잔기이며; X2, X3및 X4은 할로겐이다.
  8. 활성 성분으로서 제1항의 화합물 또는 이의 약학적으로 허용가능한 염 및 약학적으로 허용가능한 담체를 포함하는 약학적 조성물.
  9. 프로스타글란딘 I2작용물질로서 제1항의 화합물 또는 이의 약학적으로 허용가능한 염을 사용하는 방법.
  10. 제1항의 화합물 또는 이의 약학적으로 허용가능한 염을 사람 또는 동물에게 투여하는 것을 포함하는, 동맥폐색증, 경피 경강성 관상 혈관 성형술 이후의 재발협착증, 동맥경화, 대뇌 혈관 질환 또는 허혈성 심장 질환을 예방 또는 치료하는 방법.
  11. 제1항의 화합물 또는 이의 약학적으로 허용가능한 염을 약학적으로 허용가능한 담체와 혼합하는 것을 특징으로 하는 약학적 조성물의 제조 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960704963A 1994-03-10 1995-03-08 프로스타글란딘i₂작용물질로서의나프탈렌유도체 KR100383305B1 (ko)

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GB9404734A GB9404734D0 (en) 1994-03-10 1994-03-10 Heterocyclic compounds
GB9404734.7 1994-03-10
GB9407036.4 1994-04-08
GB9407036A GB9407036D0 (en) 1994-04-08 1994-04-08 Naphthalene derivatives

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EP0749424B1 (en) 2001-09-12
DE69522676D1 (de) 2001-10-18
KR100383305B1 (ko) 2003-11-01
CN1147250A (zh) 1997-04-09
WO1995024393A1 (en) 1995-09-14
JPH09509958A (ja) 1997-10-07
RU2155188C2 (ru) 2000-08-27
AU688871B2 (en) 1998-03-19
EP0749424A1 (en) 1996-12-27
HU9602466D0 (en) 1996-11-28
ES2160156T3 (es) 2001-11-01
CN1057522C (zh) 2000-10-18
US5763489A (en) 1998-06-09
HK1013289A1 (en) 1999-08-20
HUT75226A (en) 1997-04-28
DK0749424T3 (da) 2001-11-26
DE69522676T2 (de) 2002-04-18
HU224822B1 (en) 2006-02-28
US5863918A (en) 1999-01-26
JP3245864B2 (ja) 2002-01-15
PT749424E (pt) 2002-03-28
GR3037080T3 (en) 2002-01-31
ATE205479T1 (de) 2001-09-15
TW282456B (ko) 1996-08-01
CA2185104A1 (en) 1995-09-14
AU1861895A (en) 1995-09-25

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