| 摘要 |
Arylidene-1-aza-cycloalkane derivs. of formula (I) and their enantiomers, diastereomers and salts are new. n = 0-1; m = 1-2; p = 0-1; A = a single bond, opt. branched 1-17C alkylene, 2-17C alkenylene or 2-4C alkynylene; X = CO or SO2; Y = O, S or NR"; R1-R6 = each H or 1, 2 or 3 of R1-R6 = opt. branched 1-4C alkyl, (opt. mono substd. by OH, alkoxy, alkylthio, dialkylamino or Ph itself opt. mono-substd. with halogen or alkyl), or alkoxycarbonyl and the other R1-R6 gps. = each H; and 1,2 or 3 of R1, R3 and R5 can also be Ph (opt. mono-substd. by alkyl, or halogen); R7 = R9 = H or alkyl; R10 = H, 3-6C cycloalkyl, Ph (opt. mono or di-substd. with halogen or mono-substd. with alkyl or CF3 or di-substd. by halogen and 1 alkyl gp. naphthyl or tetrahydronaphthyl or thienyl (opt. mono-substd. by halo or alkyl); R11 = H or alkyl; provided that A is not a single bond if X = SO2 and R10 = H; and if not otherwise stated all alkyl, alkoxy and alkylthio gps. contain 1-3C and the halogen atoms are F, Cl or Br. USE - (I) inhibit cholesterol biosynthesis esp. they inhibit the enzyme 2,3-epoxysqualene lanosterol cyclase. (I) can therefore be used in the treatment and prophylaxis of hyperlipidaemia, hyperproteinaemia, hypertriglyceridaemia and the resulting atherosclerosis and coronary heart disease, cerebral ischaemia, claudicatio intermittens, gangrene etc. (I) can also be used to treat hyperproliferative skin and vascular disease, gall stones and mycoses, caused by e.g. Candida albicans, aspergillus niger, trichophyton mentagrophytes, penicillium sp. cladosporium sp. etc. |
