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NOUVEAUX ANALOGUES DE 3-O-ACETYL-11-CETO-BETA-ACIDE BOSWELLIQUE
- 专利权人:
- LAILA NUTRACEUTICALS
- 发明人:
- 申请号：
- EP04745123.2
- 公开号：
- EP1765761B1
- 申请日:
- 2004.06.18
- 申请国别(地区):
- EP
- 年份:
- 2013
- 代理人:
- 摘要：
- This invention relates to novel AKBA analogs of the formula I given below: Where in R1, R2, R3, R4 and R5 in each of the said analogs are: 1. R1-OCHO, R2-H, R3-COOH, R4 & R5-O 2. R1-OCOCH2Cl, R2-H, R3-COOH, R4 & R5-O 3. R1-5'-O-methylgalloyloxy, R2-H, R3-COOH, R4 & R5-O 4. R1-OCOCH2CH2COOH, R2-H, R3-COOH, R4 & R5-O 5. R1-8',9'-Dihydro-4'-hydroxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 6. R1-4'-Hydroxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 7. R1-3',4'-Dimethoxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 8. R1-3',4'-Dihydroxy-5'-methoxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 9. R1-OCOCH2NH(tert-BOC), R2-H, R3-COOCH3, R4 & R5-O 10. R1-OCOCH2NH2HCl, R2-H, R3-COOH, R4 & R5-O 11. R1-OCOCH(CH3)NH2HCl, R2-H, R3-COOH, R4 & R5-O 12. R1-H, R2-OH, R3-COOCH3, R4 & R5-O 13. R1-H, R2-Br, R3 COOCH3, R4 & R5-O 14. R1-CN, R2-H, R3-COOCH3, R4 & R5-O 15. R1-SH, R2-H, R3-COOCH3, R4& R5-O 16. R1 & R2-N(OH), R3-COOCH3, R4 & R5-O 17. R1 & R2-H & OCOCH3 R3-H, R4 & R5-O 18. R1-OCOCH3, R2-H R3-COOCH2CH2N(CH3)2, R4 & R5-O 19. R1-OCOCH3, R2-H R3-CONH2, R4 & R5-O 20. R1-OCOCH3, R2-H, R3-CONHNH2, R4 & R5-O 21. R1-OCOCH3, R2-H, R3-CONHCH2CH2NH2, R4 & R5-O 22. R1-OCOCH3, R2-H, R3-CONHCH2CH2OH, R4 & R5-O 23. R1-OCOCH3, R2-H, R3-CON(CH2CH2)2NH, R4 & R5-O 24. R1-OCOCH3, R2-H R3-NCO, R4 & R5-O 25. R1-OCOCH3, R2-H R3-NH2, R4 & R5-O 26. R1-OCOCH3, R2-H R3-CN, R4 & R5-O 27. R1-OH, R2-H R3-COOH, R4 & R5-OH & H These compounds exhibited 5-Lipoxigenase inhibitory properties and these compounds may be used in pharmaceutical compositions for therapeutic applications against a variety of inflammations and hypersensitivity-based human diseases including asthma, arthritis, bowel diseases such as ulcerative colitis and circulatory disorders such as shock and ischaemia. These compounds also inhibited the growth of Brine Shrimp in cultures, which may be considered as a positive indication for cytotoxicity and antitumor activity.
- 来源网站：
- 中国工程科技知识中心
- 来源网址：
- http://www.ckcest.cn/home/
