| 摘要 |
<p>The invention comprises compounds of general formula A.CH2-COOR in which A represents the farnesyl group (CH3)2.C : CH. <FORM:0938712/IV(a)/1> and R represents an alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, aralkenyl or heterocyclyl-alkyl group; and their preparation by reacting a compound of formula A.CH2.CO.X with a compound of formula RY, where X and Y are reactive groups which are capable of reacting together to form the compounds of the invention, in particular by reacting, as appropriate, acid with alcohol or diazoaliphatic compound, anhydride with alcohol, halide with alcohol, salt with halide, sulphate or sulphonate, or ester with alcohol; and by decarboxylation by heating of an acid-ester of formula A.CH(COOH). COOR, optionally prepared by hydrolysis of a diester A.CH.(COOR)2; and by hydrolysis of an ester of formula CH3.CO.CH(A).COOR. Farnesyl-acetic acid derivatives formed are the anhydride with ketene and with acetyl chloride, the chloride formed with thionyl chloride, and the silver salt. In the Provisional Specification R is defined as an organic group. Pharmaceutical compositions comprise a compound of the invention as active ingredient in association with a pharmaceutical carrier or excipient. Forms suitable for oral (tablets, capsules, cachets, syrups, elixirs), topical (ointments), rectal (suppositories) or parenteral (liquids) administration are mentioned and may be as dosage units. The compounds act against ulcers and other diseases of the gastro-intestinal mucosa.</p> |
