Ml-236b derivatives, a process for their preparation and...

Details Ml-236b derivatives, a process for their preparation and... Ml-236b derivatives, a process for their preparation and...

C - Chemistry, Metallurgy

12

P

195/129, 260/357

C12P 17/06 (2006.01) C07D 309/30 (2006.01)

Patent

CA 1185199

ABSTRACT A compound of formula (1): Image (I) (called 6-methoxy-IsoML-236B lactone) and its corresponding free hydroxy-carboxylic acid and salts and esters of said acid may be prepared by the enzymatic alkoxylation of an ML-236B compound, preferably using a microorganism of the genus Syncephalastrum, Absidia or Cunninghamella, e.g. Absidia coerulea, or a cell-free enzyme-containing extract from said microorganism. If desired, the lactone or carboxylic acid may be converted by conventional salification or esterification techniques to the desired salt or ester. These compounds have the ability to inhibit the bio- synthesis of cholesterol and are thus of value in the treatment of hypercholesteraemia, for which purpose they may be formulated as compositions in admixture with conventional pharmaceutical carriers or diluents.

406984

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