Back to results
US 6,274,559 B1Granted
Liver protection or treatment agents comprising asiatic acid derivatives as the active component
AssigneeDong Kook Pharmaceutical Co., Ltd.
InventorsSang Sup Jew, Hyeung Geun Park, Hee Doo Kim, Young Hoon Jung, Young Choong Kim, Hong Pyo Kim, Mi Kyeong Lee, Hee Sung Choi, Eung Seok Lee, Chi Hyoung Yoo, Doo Yeon Lim, Jeong Hoon Kim, Hee Man Kim
Life of this patent
Estimating the term…
Abstract
Compositions and methods of treating or preventing hepatotoxicity utilizing asiatic acid derivatives of Formula 1 are disclosed.
Claims3
A method of treating or preventing hepatotoxicity, said method comprising administering to a patient in need of such treatment, a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, represented by Formula 1
- wherein:
- R1 is chosen from —H, a hydroxy group, a hydroxy group protected by an acetyl or benzoyl group, a methyl group, an ethyl group, a methoxy group, an ethoxy group, a vinyl group, an ethinyl group, a cyano group, an azide group, an ethoxymethyloxy group, an octyloxymethyloxy group, a methanesulfonyloxy group, a phenylthio group and a (methylthio)thiocarbonyloxy group, or
- R1 and R2 taken together may form an oxo group;
- R2 is chosen from —H, a methoxy group, an ethoxy group, a hydroxy group and a hydroxy group protected by an acetyl or benzoyl group, or
- R2 and R4 taken together may form an epoxy group;
- R3 is chosen from —H, a vinyl group, a methyl group, an ethyl group, a hydroxy group and a hydroxy group protected by an acetyl or benzoyl group or
- R3 and R4 taken together may form an oxo group;
- R4 is chosen from —H, a methyl group, an ethyl group, a vinyl group, a hydroxy group and a hydroxy group protected by an acetyl or benzoyl group;
- R5 is chosen from a methyl group, a hydroxymethyl group wherein the hydroxy group may be protected by an acetyl or benzoyl group, a t-butyldimethylsilyloxymethyl group, a carboxylic group, a carboxylic ester moiety, a carboxylic amide moiety and an aldehyde group, or
- R4 and R5 taken together may form —OCR6R7OCH2—, wherein
- R6 is chosen from —H, a lower alkyl group having 1-4 carbon atoms and a phenyl group;
- R7 is chosen from —H, a lower alkyl group having 1-4 carbon atoms and a phenyl group, or
- R6 and R7 taken together may form —(CH2)5;
- R8 is chosen from —H and a methyl group;
- R9 is chosen from —CH2COOR and —COOR, wherein
- R is chosen from —H, a lower alkyl group having 1-4 carbon atoms, a 2-tetrahydropyranyl group, CH(OR11)R10, CH(OR13)CH2R12, wherein
- R10 is chosen from —H, a methyl group and an ethyl group;
- R11 is chosen from a lower alkyl group having 1-4 carbon atoms, an octyl group, a benzyl group, a methoxymethyl group and a methoxyethyl group;
- R12 is chosen from —H, a methyl group and an ethyl group;
- and
- R13 is chosen from a methyl group and an ethyl group, or
- R12 and R13 taken together may form —CH2CH2CH2—,
- a glucosyl or a rhamnosyl group, wherein the hydroxy group may be protected by an acetyl or benzoyl group,
- a hydroxymethyl group wherein the hydroxy group may be protected by an acetyl or a benzoyl group, a methanesulfonyloxymethyl group and a cyanomethyl group;
- and
- R14 and R15 are independently —H, or R14 and R,5 taken together form an oxo group, with the provisos that:
- when R1 and R4 are hydroxy, R2 and R3 are —H, R5 is hydroxymethyl and R8 is methyl,
- R is not —H or methyl and R10 is not —H;
- and
- when R1 is —OH, R2 is —H, R3 or R4 form with R5 —OC(R6)(R7)OCH2—, and R6 is methyl,
- R is not methyl,
- and a pharmaceutically acceptable carrier.
29 more elements
Dependencies are inferred from the claim text.