| 摘要 |
New carboxamides of formula (I): (where R1-3=same or different, saturated or unsaturated, straight branched or cyclic hydrocarbyl the carbon chain of which may be interrupted by heteroatoms or divalent groups e.g. O,S, -SO-, -SO2-, -CO- or phenylene and may be substituted by substituents such as halo, alkoxy, acyloxy, aryl, aryloxy, arylmercapto, aroyl, alkylmercapto, alkylsulphenyl, alkylsulphonyl, acylamino, aroylamino, cyano, alkoxycarbonyl, aryloxycarbonyl or carbamoyl (opt. substd. by alkyl); R4,R5=same or different H, opt. substd. aryl or saturated or unsaturated, straight, branched or cyclic hydrocarbyl the carbon chain of which is opt. interrupted by heteroatoms or groups such as O,S,SO2,SO,CO and phenylene and may be substd. by hydroxy, alkoxy, halo, acyloxy, acylamino, aryl, aryloxy, aroyl, alkylmercapto, alkylsulphonyl, alkylsulphinyl, cyano, alkoxycarbonyl, aryloxycarbonyl or carbamoul (opt. substd. by alkyl or aryl) radicals or R4 and R5 together may form an alkylene chain; when n=0, R4 and R5 together = alkylene thus form a heterocyclic containing the two N atoms; X=saturated or unsaturated, straight, branched or cyclic hydrocarbon chain which may be interrupted by heteroatoms or groups such as O,S,SO,SO2, arylaza, alkylaza, carbonyl or phenylene and may be substd. by halo, alkoxy, aryloxy, hydroxy, cyano, carboxy, carbalkoxy, acylamino, carbaryloxy, alkylmercapto, alkylsulphinyl, alkylsulphonyl, arylmercapto, aryl or carbamoyl (opt. substd. by alkyl or aryl), radicals and n=0-4. All aryl radicals defined in R1-5 and X have 6-10C atoms and are opt. substd. (I) are hypolipemics which reduce hyperlipemia and the absorption of cholesterol and is administered orally, parenthelly or rectally in the treatment of lipid metabolism troubles e.g. adiposity and hyperlipoproteinemia. The cpds. have low toxicity oral LD50 in mice >2000mg/kg. |
