Patent ID: 6518274
Filing Date: 2003-02-11
Classification: A61K,A61P,Y10S

Abstract:
A method of treating a nuclear factor &kgr;B-dependent disease selected from the group consisting of immunological disorders, septic shock, transplant rejection, radiation damage, reperfusion injuries after ischemia, arteriosclerosis and neurodegenerative diseases, comprising administering to a mammal in need of such treatment an effective amount of a cyclopentabenzofuran derivative of the formula (I): in which[A] R1 represents hydrogen, R2 represents methoxy, R3 represents hydrogen or R2 and R3 together represent â€”OCH2Oâ€”, R4 represents methoxy, R5 represents hydroxyl, OCHO or acetoxy, R6 and R7 in each case represent hydrogen or R5 and R6 together represent oxygen (oxo) or hydroxyimino, R8 represents â€”COOR12 or â€”CONR13R14, in which R12 and R13 represent hydrogen or methyl and R14 represents hydrogen, methyl, 4-hydroxybutyl or 2-tetrahydrofuryl, or R8 represents a radical of the formula: R5 and R8 together represent a group of the formulae (a) or (b): where the linkage site adjacent to the N atom corresponds to R5 and moreover R6 and R7 together represent a direct bond, R9 represents phenyl, R10 represents methoxy, R11 represents hydrogen, hydroxyl, methoxy or 2-rhamnosyl, or R10 and R11 are adjacent and together represent â€”OCH2Oâ€”, or R15 represents hydroxyl, methoxy or ethoxy, R16 represents hydrogen, hydroxyl or methoxy, [B] R1, R3 and R8 in each case represent hydrogen, R2 and R4 in each case represent methoxy, R5 represents hydroxyl, R6 and R7 in each case represent hydrogen or R5 and R6 together represent oxygen (oxo group), R9 represents phenyl, R10 represents methoxy, R11 represents 2-methoxy or 2-rhamnosyl, or R10 and R11 are adjacent and together represent â€”OCH2Oâ€”, R15 represents hydroxyl, methoxy or ethoxy, R16 represents hydrogen, hydroxyl or methoxy.