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    • 61. 发明申请
      US20090318551A1 USES OF ANALOGS OF 3-O-ACETYL-11-KETO-BETA-BOSWELLIC ACID 审中-公开
    • USES OF ANALOGS OF 3-O-ACETYL-11-KETO-BETA-BOSWELLIC ACID
    • US20090318551A1
    • 2009-12-24
    • US12549663
    • 2009-08-28
    • Ganga Raju Gokaraju , Rama Raju Gokaraju , Venkata Subbaraju Gottumukkala , Trimurtulu Golakoti
    • Ganga Raju Gokaraju , Rama Raju Gokaraju , Venkata Subbaraju Gottumukkala , Trimurtulu Golakoti
    • A61K31/215 , C07C61/29 , C07C69/757 , C07C255/47 , C07C69/78 , C07C229/02 , A61K31/19 , A61K31/235 , A61P35/00 , A61P29/00
    • C07J63/008
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 63. 发明授权
      US07288671B2 Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators 有权
    • Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
    • US07288671B2
    • 2007-10-30
    • US11417906
    • 2006-05-03
    • Michael Palladino , Emmanuel A. Theodorakis
    • Michael Palladino , Emmanuel A. Theodorakis
    • C07C61/29 , C07C69/74
    • C07C33/14 , A61K31/12 , A61K31/16 , A61K31/215 , C07B2200/05 , C07B2200/07 , C07C57/26 , C07C61/29 , C07C61/35 , C07C62/30 , C07C62/32 , C07C69/753 , C07C69/757 , C07C233/58 , C07C2603/26 , C07D295/15 , C07D295/185 , C07D295/26 , Y02A50/463
    • Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R3-R5, R7, R8, R11-R13 is not hydrogen, R2 or R6 or R9 is not methyl, or R10 is not CH2, then R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C1-C12 esters, C1-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, (C1-C12)(C1-C12) cyclic amides, (C1-C12) amines, C1-C12 alcohols, (C1-C12)(C1-C12) ethers, C1-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls, and C5-C12 aryls. If all R3-R5, R7, R8, R11-R13 are hydrogen, R2, R6, and R9 are each methyl, and R10 is CH2, then R1 is selected from hydrogen, a halogen, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C2-C12 esters, C2-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, C2-C12 alcohols, (C1-C12)(C1-C12) ethers other than methyl-acetyl ether, C2-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls, and C2-C12 aryls. R2 and R9 are each separately selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, C2-C12 alkynyl, C1-C12 acyl, C1-C12 alcohol, and C5-C12 aryl. R3-R5, R7, R8, and R11-R13 are each separately selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, C2-C12 alkynyl, and C5-C12 aryl. R6 is selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, and C2-C12 alkynyl. R10 is selected from hydrogen, a halogen, CH2, C1-C6 alkyl, C1-C6 substituted alkyl, C2-C6 alkenyl, C2-C6 substituted alkenyl, C1-C12 alcohol, and C5-C12 aryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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