New beta,beta=di:methyl=4=piperidine=ethanol derivs - useful as cholesterol biosynthesis inhibitors for treating hypercholesterolaemia, atheroscloerosis and fungal infections

摘要

beta,beta-Dimethyl-4-piperidineethanol and 1,2,3,6-tetrahydro-beta,beta-dimethyl-4-pyridineethanol derivs. of formula (I) and their salts and N-oxides are new. In the formula, R = 4-20C alkyl, 9-13C alkenyl, 9-13C alkadienyl, 7-11C hydroxyalkyl, (CH2)nYR1, (Z)- or (E)-6,6-dimethyl-hept-2-en-4-yn-1-yl or 3-(3-isopropoxypropoxy)propyl; Y = S or O; R1 = Me or CH2CH2OH; n = 7-10. Also claimed are new intermediates. 1-(1,5,9-trimethyldecyl)-beta,beta-dimethyl-4-piperidineethanol; 1-(1,5,9-trimethyl-(E)-4,8-decadien-1-yl)-beta,beta-dimethyl- 4-piperidineethanol maleate (Ia); and 1-dodecyl-beta,beta-dimethyl-4-piperidineethanol are specifically claimed. USE - (I) are cholesterol biosynthesis inhibitors acting by inhibition of epoxysqualene cyclase in mammals and fungi. They may be used to treat hypercholesterolaemia, atherosclerosis and fungal infections.