New cyclodextrin derivs. used as bile acid adsorption agents - useful for treating hyperlipidaemia, can be administered at lower does than cholestyramine or colestipol resin

Cyclodextrin derivs. of formula (I) are new. Where R1 = OH; a 6-30C fatty acid bonded via a carboxy gp.; 6-30C alcohol bonded via the alcohol function; an amino acid bonded via the carboxy gp.; bile acid bonded via a 2-12C alkyl or alkoxy gp. in position 3; and/or X-A-N(R3)R4; X = O or OC(=O)-; A =...

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Main Authors AHLERS, MICHAEL., 6500 MAINZ, DE, NEUBAUER, HORST PAUL., 6240 KOENIGSTEIN, DE, WIESNER, MATTHIAS., 6500 MAINZ, DE, MUELLNER, STEFAN., 6203 HOCHHEIM, DE
Format Patent
LanguageEnglish
German
Published 13.05.1993
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Summary:Cyclodextrin derivs. of formula (I) are new. Where R1 = OH; a 6-30C fatty acid bonded via a carboxy gp.; 6-30C alcohol bonded via the alcohol function; an amino acid bonded via the carboxy gp.; bile acid bonded via a 2-12C alkyl or alkoxy gp. in position 3; and/or X-A-N(R3)R4; X = O or OC(=O)-; A = 2-15 (pref. 2-8C) alkylene, alkenylene or alkynylene (pref. branched); R3, R4 = H or 1-6C alkyl; pref. 1-3C alkyl; R2 = CH2R1 or C(=O)YAB; Y = O or NH; B = H, NH2, a bile acid bonded via position 3 or a mono-or di(1-3C alkyl) amino; and n = 6-8. Also claimed is a conjugate contg. (I) and a bile acid. (I) has a mol. wt. of 600-2000. The conjugate has a substitution percent DS of 0.01-1 pref. 0.3-0. USE/ADVANTAGE - (I) are bile acid adsorption agents useful for treating hyperlipidaemia. They are administered at lower doses than cholestyramine or cholesterol resin, e.g. 0.5-10 g/kg/day. The conjugate can be used in food and fruit juice. They can be used to treat blood plasma, serum, urine or bile.
Bibliography:Application Number: DE19914136325