| 摘要 |
<p>Long chain fatty acid derivs. of formula (I) are new: (where A is (i) 7-23 unsatd. fatty acid residue (minus the carboxyl) having 1-4 ethylenic double bonds or (ii) a similar residue in which the -CH=CH- is replaced by a cyclopropylene(-CH(-CH2-)-CH-) and (a) R1 = H and R2 = a residue of formula (II), (III), (IV) or (V), h, g, j, f= 0 or 1, R4, Y=H, F, Cl, Br, 1-3C alkyl or 1-3C alkoxy, R5, Y1=H, F, Cl, 1-3C alkyl or 1-3C alkoxy, R3 = H, 1-8C alkyl or a Gp. (VI), R6=H, F, Cl, Br, 1-3C alkyl, 1-3C alkoxy or a Gp. (VII), B = -CH2- or -O-, X = H or -COOR7, R7 = 1-8C alkyl or benzyl, R8 = H, 1-8C alkyl or benzyl, k = 1, 2, 3 or 4, With the conditions that A is alternatively (ii) when R2 = (II) or (III) where h = 0, x = -COOR7 when R2 = (IV) where h = 0 and X = H, when R2 = (IV) where h = 1. or b) R1 and R2 together with the N atom form a Gp. (VIII) where R9, R10 independently = H, F, Cl, CF3, 1-4c alkyl or 1-4C alkoxy and R11 = H or 1-4C alkoxy with the condition that >=1 of the substituents R9 and R10 = alkoxy when R11 = alkoxy and neither R9 or R10 = H, or, R9 and R10 on two adjacent C atoms form a gp. -(CH2)m-, -CH=CH-CH=CH- or -O-CH2-B-, m = 3 or 4, and R11 = H, F, Cl, CF3, 1-4C alkyl or 1-4C alkoxy). (I) lower the level of esterified cholesterol in artery walls and may be used therapeutically and prophylactically in the treatment of arteriosclerosis. (I) are free from side-effects and are administered orally, rectally or parenterally in daily doses of 100-5000 mg, pref. as 2-4 unit doses or in a retarded release form.</p> |
