| abstract |
The present invention relates to compounds of formula I in which U is O or a solitary electron pair V is a single bond, O, S, -CH2-, -CH = CH-, -CH = CH-CH2-O- or -C <C- ; W is CO, COO, CONR1, CSO, CSNR1, SO2 or SO2 NR1; m and n are independently 0-7; and m + n is from 0 to 7; with the proviso that when V is O or S, it is different from m 0, A1 is hydrogen, lower alkyl, hydroxy (lower alkyl), or lower alkenyl; A2 is a lower alkyl group substituted with cycloalkyl, cycloalkyl-lower alkyl, lower-alkenyl, lower-alkynyl, heteroaryl-substituted; or A1 and A2 together form a lower alkylene or lower alkenylene group as defined for -A1-A2 as R2; wherein one of -CH2- in the -A1-A2 group is optionally NR3, S or Olehet; or -A1-A2- is -CH = N-CH = CH-, which may be substituted by a lower alkyl group; A3 and A4 are independently hydrogen or lower alkyl; or A3 and A4 together with the carbon atom to which they are attached form a ring and -A3-A4 is - (CH2) 2-5; A5, A6, A7 and A8 are independently hydrogen or lower alkyl; A9 is hydrogen, lower alkyl, lower alkenyl or arylalkyl; A10 is lower alkyl, cycloalkyl, aryl, aryl-lower alkyl, heteroaryl or heteroaryl-lower alkyl; p is 0 or 1; R2 is hydroxy, lower alkyl, lower alkoxy, lower alkoxycarbonyl, N (R4, R5), thioalkoxy or halogen; and R 1, R 3, R 4 and R 5 are each independently hydrogen or lower alkyl and pharmaceutically acceptable salts thereof, with the exception of transrannaphthalene-1-sulfonic acid methyl (4-methylaminomethyl-cyclohexylmethyl) -amide. The compounds of the invention are inhibitors of 2,3-oxido-squalene-lanosterol cyclase, including related diseases (e.g., hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasitic infections, gallstones, tumors and / or hyperproliferative disorders and / or impaired glucose tolerance and diabetes) ) for treatment and / or prophylaxis. HE |