KR920019770A - 포스포리파제 a₂억제제로서의 테트론산 및 티오테트론산 유도체 - Google Patents

포스포리파제 a₂억제제로서의 테트론산 및 티오테트론산 유도체 Download PDF

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KR920019770A
KR920019770A KR1019920005991A KR920005991A KR920019770A KR 920019770 A KR920019770 A KR 920019770A KR 1019920005991 A KR1019920005991 A KR 1019920005991A KR 920005991 A KR920005991 A KR 920005991A KR 920019770 A KR920019770 A KR 920019770A
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compound
hydroxy
furanone
oxo
thiophenone
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유진 커필드 크레이그
마이클 린커 제임스
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이곤 이. 버그
아메리칸 홈 프로덕츠 코포레이션
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Abstract

내용 없음

Description

포스포리파제 A2억제제로서의 테트론산 및 티오테트론산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (61)

  1. 일반식(I)의 화합물.
    상기식에서, X는 -CH2R이고,
    R은이며, 추가로 Y가 S인 경우, R은 -(CH2)eCH3일 수 있고, Y는 -O-또는 -S-이며, R1및 R2는 각각 독립적으로 수소 또는 저급 알킬이고, R3은 인돌릴, 푸릴, 페닐 또는 독립적으로 탄소수 1 내지 7의 알킬, -C(CH3)3, -C(CH3)2CH2C(CH3)3, -C(CH3)2CH2CH3, 할로저급알킬, 퍼플루오로알킬, 저급알콕시, 아릴알콕시, 할로 또는 니트로에 의해 임의로 일-또는 이치환된 페닐이며, R4및 R5는 독립적으로 -COCH2R7, -CO2R7, -CONHR7, 게라닐 또는 CH2R3이고, R6는 수소 또는 저급 알킬이며, R7은 게라닐 및이외의 R의 정의 중에서 선택된 잔기이고, A 및 B는 독립적으로 -O-, -S- 또는 -NR6-이며, a는 0 내지 8이고, b는 Y가 S인 경우 1 내지 10이며, Y가 0인 경우 2 내지 10이고, c는 1 내지 3이며, d는 0 내지 9이고, e는 3 내지 18이다.
  2. 제1항에 있어서, 4-하이드록시-3-[(페틸메톡시)아세틸]-2(5H)-푸란온인 화합물.
  3. 제1항에 있어서, (Z)-4-하이드록시-3-(1-옥소-9-옥타데세닐)-2(5H)-푸란온인 화합물.
  4. 제1항에 있어서, (Z,Z)-4-하이드록시-3-(1-옥소-9,12-옥타데카디에틸)-2(5H)-푸란온인 화합물.
  5. 제1항에 있어서, (Z,Z,Z)-4-하이드록시-3-(1-옥소-9,12,15-옥소데카트리에닐)-2(5H)-푸란온인 화합물.
  6. 제1항에 있어서, (Z)-4-하이드록시-5,5-디메틸-3-(1-옥소-9-옥타데세닐)-2(5H)-푸란온인 화합물.
  7. 제1항에 있어서, (Z)-4-하이드록시-3-(1-옥소-6-옥타데세닐)-2-2(5H)-푸란온인 화합물.
  8. 제1항에 있어서, (Z)-4-하이드록시-3-(1-옥소-8-(2'-옥틸사이클로프로필)옥타닐)-2(5H)-푸란온인 화합물.
  9. 제1항에 있어서, (Z,Z,Z)-4-하이드록시-3-(1-옥소-6,9,12-옥타데카트리에닐)-2(5H)-푸란온인 화합물.
  10. 제1항에 있어서, 4-하이드록시-3-[6-(4-클로로펜옥시)-1-옥소헥실]-2(5H)-푸란온인 화합물.
  11. 제1항에 있어서, 4-하이드록시-3-[1-옥소-8-[2-[(2-펜틸사이클로프로필)메틸]클로로프로필]옥틸-2(5H)-푸란온인 화합물.
  12. 제1항에 있어서, 4-하이드록시-3-((Z)-1-옥소-10-테트라데세닐)-2(5H)-푸란온인 화합물.
  13. 제1항에 있어서, (Z)-9-옥타데카노산 5-(2,5-디하이드로-4-하이드록시-3-푸라닐)-5-옥소-1,2-펜탄디일에스테르인 화합물.
  14. 제1항에 있어서, 4-하이드록시-3-((Z)-1-옥소-9-테트라데세닐)-2-2(5H)-푸란온인 화합물.
  15. 제1항에 있어서, 4-하이드록시-3-((Z)-1-옥소-9-헥사데세닐)-2(5H)-푸란온인 화합물.
  16. 제1항에 있어서, 4-하이드록시-3-(1-옥소-9-옥타데시닐)-2(5H)-푸란온인 화합물.
  17. 제1항에 있어서, 4-하이드록시-3-(1-옥소옥타데실)-2(5H)-푸란온인 화합물.
  18. 제1항에 있어서, 3-[9-(4-클로로펜옥시)-1-옥소노닐]-4-하이드록시-2(5H)-푸란온인 화합물.
  19. 제1항에 있어서, 헥시카밤산 5-(2,5-디하이드로-4-하이드록시-2-옥소-3-푸라닐)-5-옥소-1,2-펜탄디일에스테르인 화합물.
  20. 제1항에 있어서, 도데실카밤산 5-(2,5-디하이드로-4-하이드-2-옥소-3-푸라닐)-5-옥소-1,2-펜탄디일에스테르인 화합물.
  21. 제1항에 있어서, 4-하이드록시-3-[6-[4-[4-클로로페닐)메톡시펜옥시]]-1-옥소헥실]-2(5H)-푸란온인 화합물.
  22. 제1항에 있어서, 4-하이드록시-3-[6-[4-(헥실옥시)펜옥시]-1-옥소헥실]-2(5H)-푸란온인 화합물.
  23. 제1항에 있어서, 4-하이드록시-3-[7-[4-클로로펜옥시)-1-옥소헵틸]-2(5H)-푸란온인 화합물.
  24. 제1항에 있어서, 3-[(Z)-10-(4-클로로페닐)-1-옥소-9-데세닐]-4-하이드록시-2(5H)-푸란온인 화합물.
  25. 제1항에 있어서, 4-하이드록시-3-((E)-1-옥소-9-옥타데세닐)-2(5H)-푸란온인 화합물.
  26. 제1항에 있어서, 3-[6-(4-헵틸펜옥시)-1-옥소헥실]-4-하이드록시-2(5H)-푸란온인 화합물.
  27. 제1항에 있어서, (Z)-9-옥타데카노산 4-(2,5-디하이드로-4-하이드록시-2-옥소-3-푸라닐)-4-옥소부타노산 에스테르인 화합물.
  28. 제1항에 있어서, 4-하이드록시-3-[6(1,1,3,3,-테트라메틸부틸)펜옥시)-1-옥소헥실]-2(5H)-푸란온인 화합물.
  29. 제1항에 있어서, ((Z)-9-옥타데시닐)카밤산 1-[[((E)-3,7-디메틸-2,6-옥타데카디에닐)옥시]메틸]-4-(2,5-디하이드로-4-하이드록시-2-옥소-3-푸라닐)-4-옥소부틸 에스테르인 화합물.
  30. 제1항에 있어서, 4-하이드록시-3-[10-(4-클로로페닐)-1-옥소데실]-2(5H)-푸란온인 화합물.
  31. 제1항에 있어서, 4-하이드록시-3-[10-(3,4-디클로로페닐)-1-옥소데실]-2(5H)-푸란온인 화합물.
  32. 제1항에 있어서, 4-하이드록시-3-[10-[4-(1,1,-디메틸에틸)페닐]1-옥소데실]-2(5H)-푸란온인 화합물.
  33. 제1항에 있어서, 4-하이드록시-3-[10-(4-브로모페닐)-1-옥소데실]-2(5H)-푸란온인 화합물.
  34. 제1항에 있어서, 4-하이드록시-3-[10-(4-트리플루오로메틸)-페닐]-2(5H)-푸란온인 화합물.
  35. 제1항에 있어서, 4-하이드록시-3-[(Z,Z)-1-옥소-9,12-옥타데카디에닐]-2(5H)-티오펜온인 화합물.
  36. 제1항에 있어서, 4-하이드록시-3-[(Z)-1-옥소-9-테트라데세닐]-2(5H)-티오펜온인 화합물.
  37. 제1항에 있어서, 4-하이드록시-3-[(Z)-1-옥소-9-테트라데세닐]-2(5H)-티오펜온인 화합물.
  38. 제1항에 있어서, 4-하이드록시-3-[5-(4-클로로펜옥시)-1-옥소펜틸]-2(5H)-티오펜온인 화합물.
  39. 제1항에 있어서, 4-하이드록시-3-[(Z,Z,Z)-1-옥소-6,9,12-옥타데카트리에닐]-2(5H)-티오펜온인 화합물.
  40. 제1항에 있어서, 4-하이드록시-3-[(Z)-1-옥소-6-옥타데세닐-2(5H)-티오펜온인 화합물.
  41. 제1항에 있어서, 4-하이드록시-3-[(Z)-8-(2-옥틸 사이클로프로필)-1-옥소옥틸]-2(5H)-티오펜온인 화합물.
  42. 제1항에 있어서, 4-하이드록시-3-[(Z)-1-옥소-2-(2-펜틸사이클로프로필)에틸]-2(5H)-푸란온인 화합물.
  43. 제1항에 있어서, 4-하이드록시-3-[(Z)-]8-(2-부틸 사이클로 플필)-1-옥소옥틸]-2(5H)-푸란온인 화합물.
  44. 제1항에 있어서, 4-하이드록시-3-[(Z)-1-옥소-5-(2-운데실사이크롤프로필)펜틸]-2(5H)-푸란온인 화합물.
  45. 제1항에 있어서, 4-하이드록시-3-[(Z)-1-옥소-2-(2-펜틸사이크로프로필)에틸]-2(5H)-티오펜온인 화합물.
  46. 병에 걸린 포유동물에 일반식(I)의 화합물의 유효량을 투여함을 특징으로 하여, 포유동물에서 면역염증 상태를 치료하는 방법.
    상기식에서, Y는 -O- 또는 -S-이고, X는 Y가 0인 경우 -(CH2)aCH3, -(CH2 bZ 또는 -(CH=CH)bZ이며, Y가 S인 경우 -(CH2)aCH3이고, R1및 R2는 각각 독립적으로 수소 또는 저급 알킬이며, Z는 인돌릴, 푸릴, 페닐 또는 독립적으로 탄소수 1 내지 7의 알킬, 할로저급알킬, 퍼플루오로알킬, 저급알콕시, 아르알콕시, 할로 또는 니트로에 의해 임의로 일- 또는 이치환된 페닐이고, a는 Y가 0인 경우 0 내지 20이며, Y가 S인 경우 1 내지 3이고, b는 1 내지 2이다.
  47. 제46항에 있어서, 화합물이 4-하이드록시-3-(1-옥소데실)-2(5H)-푸란온인 방법.
  48. 제46항에 있어서, 화합물이 4-하이드록시-3-(1-옥소-3-페닐프로필)-2(5H)-푸란온인 방법.
  49. 제46항에 있어서, 화합물이 4-하이드록시-3-[3-(1H-인돌-3-일)-]1-옥소프로필]-2(5H)-푸란온인 방법.
  50. 제46항에 있어서, 화합물이 4-하이드록시-3-[4-(1H-인돌-3-일)-]1-옥소부틸]-2(5H)-푸란온인 방법.
  51. 제46항에 있어서, 화합물이 (E)-4-하이드록시-3-(3-(4-메톡시페닐)-1-옥소-2-프로페닐)-2(5H)-푸란온인 방법.
  52. 제46항에 있어서, 화합물이 (E)-4-하이드록시-3-(3-(4-클로로페닐)-1-옥소-2-프로페닐)-2(5H)-푸란온인 방법.
  53. 제46항에 있어서, 화합물이 (E)-4-하이드록시-3-(3-(페닐)-1-옥소-2-프로페닐)-2(5H)-푸란온인 방법.
  54. 제46항에 있어서, 화합물이 (E)-4-하이드록시-3-(1-옥소-3-(3-트리플루오로메틸)페닐)-2-프로페닐)-2(5H)-푸란온인 방법.
  55. 제46항에 있어서, 화합물이 4-하이드록시-3-(1-옥소에이코사노일)-2(5H)-푸란온인 방법.
  56. 제46항에 있어서, 화합물이 (E)-4-하이드록시-3-(3-(3-니트로페닐)-1-옥소-2-프로페닐)-2(5H)-푸란온인 방법.
  57. 제46항에 있어서, 화합물이 (E)-3-3-(3-(2,5-디메톡시페닐)-1-옥소-2-프로페닐)-4-하이드록시-2(5H)-푸란온인 방법.
  58. 제46항에 있어서, 화합물이 (E)-3-3-(3-(2,5-디메톡시페닐)-1-옥소-2-프로페닐)-4-하이드록시-2(5H)-푸란온인 방법.
  59. 제46항에 있어서, 화합물이 (E)-3-3-(3-(2,5-디메톡시페닐)-1-옥소-2-프로페닐)-4-하이드록시-2(5H)-푸란온인 방법.
  60. 제46항에 있어서, 화합물이 3-[9-(4-클로로펜옥시)-1-옥소노닐]-4-하이드록시-2(5H)-푸란온인 방법.
  61. 제46항에 있어서, 화합물이 4-하이드록시-3-[1-옥소헥사데실]-2(5H)-푸란온인 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920005991A 1991-04-12 1992-04-10 포스포리파제 a₂억제제로서의 테트론산 및 티오테트론산 유도체 KR920019770A (ko)

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US5428058A (en) * 1994-09-28 1995-06-27 American Home Products Corporation Phospholipase A2 inhibitors
US5508302A (en) * 1994-09-28 1996-04-16 American Home Products Corporation Phospholipase A2 inhibitors
CA2222471A1 (en) * 1996-03-27 1997-10-02 Toray Industries, Inc. Ketone derivatives and medical application thereof
AU721881B2 (en) * 1996-03-27 2000-07-13 Toray Industries, Inc. Ketone derivatives and medicinal use thereof
GB2321455A (en) * 1997-01-24 1998-07-29 Norsk Hydro As Lipophilic derivatives of biologically active compounds
EP1013178B2 (en) * 1998-12-22 2009-09-16 Unilever N.V. Cosmetic use of petroselinic acid
ES2315365T3 (es) * 2001-06-13 2009-04-01 Magnachem International Laboratories, Inc. Formulaciones de lactona y metodo de uso.
US7323495B2 (en) * 2002-11-05 2008-01-29 Magnachem International Laboratories, Inc. Synthetic lactone formulations and method of use
WO2005102315A1 (en) 2004-04-23 2005-11-03 Magnachem International Laboratories, Inc. Synthetic lactone formulations for pain control
MX2011004331A (es) * 2008-10-24 2011-09-21 Magnachem Int Lab Inc Metodo para busqueda de compuestos que interactuan selectivamente con rad9.
CN117802156A (zh) * 2024-02-29 2024-04-02 云南师范大学 硼酸转运蛋白基因在转基因植株筛选中的应用及筛选方法

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