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KR880001561A - 유효한 치료성을 갖는 신규 8-(저급알킬)비시클로[4.2.0] 옥탄 유도체 - Google Patents

유효한 치료성을 갖는 신규 8-(저급알킬)비시클로[4.2.0] 옥탄 유도체 Download PDF

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KR880001561A
KR880001561A KR1019870008179A KR870008179A KR880001561A KR 880001561 A KR880001561 A KR 880001561A KR 1019870008179 A KR1019870008179 A KR 1019870008179A KR 870008179 A KR870008179 A KR 870008179A KR 880001561 A KR880001561 A KR 880001561A
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compound
pharmaceutically acceptable
hydroxy
acceptable non
endo
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KR1019870008179A
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에프. 클러지 아더
엔-휴이 우 헬렌
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원본미기재
산텍스(미합중국) 인코포레이티드
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Publication of KR880001561A publication Critical patent/KR880001561A/ko

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Abstract

내용 없음

Description

유효한 치료성을 갖는신규 8-(저급알킬)비시클로[4.2.0]옥탄 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (25)

  1. 하기 일반식(1),(2)또는 (3)의 화합물, 제약상 허용되는 그의 비득성염 및 에스테르.
    식중, Y는 액소-(저급 알킬)또는 앤도-(저급 알킬)기이고, n은 2또는 3이고, R1은 CH2OH, CHO, CO2R 또는 CO2H이고, R2는 수소 또는 메틸기 이고, R3는 5-10개의 탄소원자를 갖는 직선형 또는 가지달린 알킬,
    또는 -(CH2)m-페닐(이 기들은 임의로 저급 알킬, 저급 알콕시, 트리플루우로메틸 또는 할로겐으로 치환되며, 식 중 a는 0.1 또는 2이고 b는 3-7이고, m은 1또는 2임)이고, 상기 R1의 정의에서 R는여기에서 (X는
    또는(R4는 독립적으로 수소, 또는 1-6개의 탄소 원자를 갖는 저급 알킬기임)이다
  2. 제 1항에 있어서, Y가 엑소-메틸, 엑소-에틸 또는 앤도-에틸이고, R1,CO2H,CO2R 또는 CHO 이고, R3가 5-10개의탄소 원자를 갖는 직선형 또는 가지달린 알킬,또는화합물, 제약상 허용되는 그의 비독성염 및 에스테르.
  3. 제 2항에 있어서, R3가 5-7개의 탄소 원자를 갖는 직선형 또는 가지달린 알킬, (CH2)a-CH(CH2)b,또는인 화합물, 제약상 허용되는 그의 비독성염 및 에스테르.
  4. 제 3항에 있어서,R1이 C02H이고 R3가 n-펜틸기인 화합물, 제약상 허용되는 그의 비독성 염 및 에스테르.
  5. 제 3항에 있어서, R1이 CO2R또는 CH2H이고, R3가 수소이고 R3가인 화합물, 제약상 허용되는 그의 비독성염 및 에스테르.
  6. 제 5항에 있어서 n이 2이고 R1이 CO2H이고 R2가 수소이고, R3가인 화합물제약상 허용되는 그의 비독성염 및 에스테르.
  7. 제 6항에 있어서, a가 0 또는 1인 화합물, 제약상 허용되는 그의 비독성염 및 에스테르.
  8. 제 7항에 있어서, a가 0이고, b가 5인 화합물, 제약상 허용되는 그의 비독성염 및 에스테르.
  9. 제 5항에 있어서, n이 3이고, a가 0또는 1인 화합물, 제약상 허용되는 그의 비독성염 및 에스테르.
  10. 제 8항에 있어서, Y가 엔도-메틸기인 화합물, 즉 (Z)-(3'S,1S,2S,3R,6S)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]부티르산,(Z)-(3S,1R,2R,3R,6R)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]부티르산,또는 (E)-(3'S,1S,2S,3R,6S)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]부티르산 및 제약상 허용되는 그의 비독성염 및 에스테르.
  11. 제 10항의 화합물의 라세미 변형체, 즉 (a)(3'S*,1S*,2S*,3R*,6S*)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]부티르산 Z)-(3S*,1R*,2R*,3R*,6R*)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]부티르산, 또는(E)-(3'S*0,1S*,2S*,3R*,6S*)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]부티르산 및 제약상 허용되는 그의 비독성염 및 에스테르.
  12. 9항에 있어서, a가 0이고 b가 5이고, Y가 엔도 -메틸기인 화합물, 즉 (Z)-(3'S,1S,2S,3R,6S)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]펜타산, (Z)-(3S*,1R*,2R*,3R*, 6R*)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]펜탄산, 또는(E)-)(3'S*0,1S*,2S*,3R*,6S*)-4-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]펜타산 및 제약상 허용되는 그의 비독성염 및 에스테르.
  13. 제 12항의 화합물의 라세미 변형체, 즉 (Z)-(3'S*,1S*,2S*,3*,6S*)-5-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]펜타산, Z)-(3S*,1R*,2R*,3R*,6R*)-5-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]펜타산, 또는(E)-(3'S*,1S*,2S*,3R*,6S*)-5-[2-(3'-히드록시-3'-시클로헥실프로프-1'-이닐)-3-히드록시-8-엔도-메틸비시클로[4.2.0]옥트-7-일리덴]펜타산 및 제약상 허용되는 그의 비독성염 및 에스테르.
  14. 제 1항의 화합물, 또는 제약상 허용되는 그의 비독성염 또는 에스테르의 치료 유효량을 치료를 필요로 하는 대상물에 투여하여, 포유류 동물의 심장혈관계 질환을 치료하는 방법.
  15. 제 14항에 있어서, 질환이 죽상경화중인 방법.
  16. 제 14항에 있어서, 질환이 혈전중인 방법.
  17. 제 14항에 있어서, 질환이 바소파스틱중인 방법.
  18. 제 14항에 있어서, 질환이 고혈압증인 방법.
  19. 제 14항에 있어서, 질환이 콜레스테롤 고농도증인 방법.
  20. 제 1항의 화합물, 또는 제약상 허용되는 그의 비독성염 또는 에스테르의 치료 유효량을 치료를 필요로 하는 대상물에 투여하여, 포유류 동물의 위산 분비를 억제시키는 방법.
  21. 적어도 1개의 제약상 적합한 부형제와 제 1항의 화합물, 또는 제약상 허용되는 그의 비독성염 또는 에스테르로 되는 제약 조성물.
  22. 하기 일반식 (1)(2) 및 (3)의 화합물, 제약상 허용되는 그의 비독성염 및 에스테르의 제조에 있어서,
    식 중, 식중, Y는 엑소-(저급 알킬)또는 엔도-(저급 알킬)이고, n은 2또는 3이고, R1은 CH2OH, CHO, CO2R 또는 CO2H이고, R2는 수소 또는 메틸기이고, R3는 5-10개의 탄소원자를 갖는 직선형 또는 가지달린 알킬,
    (이 기들은 임의로 저급알킬, 저급 알콕시, 트리플루오로 메틸 또는 할로겐으로 치환되며, 식 중 a는 0,1 또는 2이고 , b는 3-7이고, m은 0,1 또는 2임)이고 ,상기 R1의 정의에서 R는(여기에서 X는
    (R4는 독립적으로 수소, 또는 1-6개의 탄소원자를 갖는 저급 알킬기임)
    (a)하기 구조식
    의 화합물을 하기 구조식
    (식중 P'는 통상으로 올레핀 반응에 관련된 잔기이고, n은 2또는 3이고, R1은 상기 정의한 바와 같거나, 또는 보호된 유도체 또는 그의 염임)의 적당히 선택된 안정화 음이온 또는 일리드와 반응시켜서 상기 일반식 (1) 및 (2)의 혼합물 또는 상기 일반식 (3)의 화합물과 그의 대응하는 E-화합물의 혼합물을 얻고, 이어서 이 혼합물을 분리시키거나, 또는
    (b)하기 구조식
    의 화합물의 보호기를 제거해서 상기 일반식(1),(2), 또는 (3)의 화합물을 얻거나, 또는
    (c)하기 구조식
    의 화합물의 보호기를 제거해서 상기 일반식(1),(2), 또는 (3)(여기에서 R1은 CH2OH임)의 화합물을 얻고, 이어서 하기 임의 공정을 행하고, (d)상기 일반식(1),(2), 또는 (3) (여기에서 R1은 CH2OH임)의 화합물을 대응하는 화합물(R1CH2OH)으로 전환시키거나, 또는 (e)상기 일반식(1),(2), 또는 (3) (여기에서 R1은 CH2OH임)의 화합물을 대응하는 화합물(R1이 CHO임)으로 전환시키거나, 또는 (f)상기 일반식(1),(2) 또는 (3)(여기에서 R1은 CH2OH임)의 화합물 대응하는 화합물(R1이 CO2R임)으로 전환시키고, 이어서 하기 임의 공정을 행하고, (g)상기 일반식(1),(2) 또는 (3)의 산을 제약상 허용되는 그의 비독성염으로 전환시키고, (h)상기 일반식 (1),(2) 또는 (3)의 화합물의 제약상 허용되는 비독성염을 그의 대응하는 산 또는 에스테르로 전환시키고, (i)상기 일반식(1),(2) 또는 (3)의 산을 제약상 허용되는 그의 비독성 에스테르로 전환시키고, (j)상기 일반식 (1),(2) 또는 (3)의 화합물의 제약상 허용되는 비독성 에스테르를, 그의 대응하는 산 또는 염으로 전환시키고, (k)상기 일반식(1),(2) 또는 (3)의 화합물의 제약상 허용되는 비독성 에스테르를 제약상 허용되는 다른 비독성 에스테르로 전환시키고, (1)상기 일반식(1),(2) 또는 (3)의 화합물의 제약상 허용되는 비독성염을 제약상 허용되는 다른 비독성염으로 전환시킴을 특징으로 하는 방법.
  23. 제 21항에 의해서 제조된 생성물.
  24. 제 21항에 있어서, 제 21항에 의해서 제조한 유효 성분을 제약상 허용되는 담체와 혼합시키는 방법.
  25. 제약 조성물을 제조하기 위한 제 1항 화합물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870008179A 1986-07-28 1987-07-27 유효한 치료성을 갖는 신규 8-(저급알킬)비시클로[4.2.0] 옥탄 유도체 KR880001561A (ko)

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US06/891,509 US4678805A (en) 1985-03-27 1986-07-28 Novel 8-(lower alkyl)bicyclo[4.2.0]octane derivatives with valuable therapeutic properties

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US4735966A (en) * 1986-08-25 1988-04-05 Syntex (U.S.A.) Inc. Novel substituted (4.2.0)bicyclooctane derivatives with valuable therapeutic properties
US5049497A (en) * 1986-08-25 1991-09-17 Syntex (U.S.A.) Inc. Novel process for the synthesis of the enantiomers of bicyclo(4.2.0)oct-2-en-7-one and derivatives
US4730078A (en) * 1987-05-13 1988-03-08 G. D. Searle & Co. Allenic prostacyclins
US4983627A (en) * 1988-11-10 1991-01-08 Syntex (U.S.A.) Inc. Novel 6-alkyl and 6.8-dialkylbicyclo(4.2.0)octane derivatives
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US4705806A (en) * 1978-02-13 1987-11-10 Morton Jr Douglas R Prostacyclin analogs
US4306076A (en) * 1980-04-23 1981-12-15 The Upjohn Company Inter-phenylene CBA compounds
US4608388A (en) * 1985-03-27 1986-08-26 Syntex (U.S.A.) Inc. Novel [4,2,0]bicyclooctane derivatives with valuable therapeutic properties
US4735966A (en) * 1986-08-25 1988-04-05 Syntex (U.S.A.) Inc. Novel substituted (4.2.0)bicyclooctane derivatives with valuable therapeutic properties

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IL83339A0 (en) 1987-12-31
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NO166442C (no) 1991-07-24
NO873131D0 (no) 1987-07-27
NO166442B (no) 1991-04-15
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GR3002024T3 (en) 1992-12-30
AU7612587A (en) 1988-02-11
HUT44471A (en) 1988-03-28
EP0255098B1 (en) 1991-05-29
JPS6345232A (ja) 1988-02-26
AU605493B2 (en) 1991-01-17
EP0255098A1 (en) 1988-02-03
FI873271A (fi) 1988-01-29
ATE63899T1 (de) 1991-06-15
NZ221197A (en) 1990-01-29
NO873131L (no) 1988-01-29
PH24200A (en) 1990-04-10
DK391087A (da) 1988-01-29
HU197870B (en) 1989-06-28

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