BioPatents

Document Number: 20060089409

Abstract:

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.

Application Number: 10540257

Primary Class: 514532000

Sub-Classes: 514548000, 560005000, 560055000

Inventors: Ganga Gokaraju, Andhra Pradesh, IN; Rama Gokaraju, Andhra Pradesh, IN; Venkata Subbaraju, Andhra Pradesh, IN; Trimurtulu Golakoti, Andhra Pradesh, IN

Assignee: LAILA NUTRACEUTICALS, ANDHRA PRADESH, IN

Attorney, Agent or Firm: RADER FISHMAN & GRAUER PLLC, LION BUILDING, WASHINGTON, DC, 20036, US

PCT: WO PCT/IN04/00176, 2004-06-18

Filing Date: 2004-06-18

Publication Date: 2006-04-27

PDF: 20060089409

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