USES OF ANALOGS OF 3-O-ACETYL-11-KETO-BETA-BOSWELLIC ACID

    公开(公告)号:US20090318551A1

    公开(公告)日:2009-12-24

    申请号:US12549663

    申请日:2009-08-28

    CPC分类号: C07J63/008

    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 & R550 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.

    Analogs of 3-O-acetyl-11-keto-β-boswellic acid

    公开(公告)号:US07625947B2

    公开(公告)日:2009-12-01

    申请号:US10540257

    申请日:2004-06-18

    CPC分类号: C07J63/008

    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.