Hypolipidemic 1,4-benzothiazepine-1,1-dioxides
AssigneeHoechst Aktiengesellschaft
InventorsAlfons Enhsen, Eugen Falk, Heiner Glombik, Siegfried Stengelin
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Abstract
The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis. Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are a defined in the specification and are useful as hypolipidemic compounds.
Claims18
A compound of formula (I) ##STR13## wherein R.sup.1 is a straight chain C.sub.1-6 alkyl group;
- R.sup.2 is a straight chain C.sub.1-6 alkyl group;
- R.sup.3 is hydrogen or a group OR.sup.11 in which R.sup.11 is hydrogen, optionally substituted C.sub.1-6 alkyl or a C.sub.1-6 alkylcarbonyl group;
- R.sup.4 is pyridyl or an optionally substituted phenyl;
- R.sup.5, R.sup.6 and R.sup.8 are the same or different and each is selected from:
- hydrogen, halogen, cyano, R.sup.15 -acetylide, OR.sup.15, optionally substituted C.sub.1-6 alkyl, COR.sup.15, CH(OH)R.sup.15, S(O).sub.n R.sup.15, P(O)(OR.sup.15).sub.2, OCOR.sup.15, OCF.sub.3, OCN, SCN, NHCN, CH.sub.2 OR.sup.15, CHO, (CH.sub.2).sub.p CN, CONR.sup.12 R.sup.13, (CH.sub.2).sub.p CO.sub.2 R.sup.15, (CH.sub.2).sub.p NR.sup.12 R.sup.13, CO.sub.2 R.sup.15, NHCOCF.sub.3, NHSO.sub.2 R.sup.15, OCH.sub.2 OR.sup.15, OCH.dbd.CHR.sup.15, O(CH.sub.2 CH.sub.2 O).sub.n R.sup.15, O(CH.sub.2).sub.p SO.sub.3 R.sup.15, O(CH.sub.2).sub.p NR.sup.12 R.sup.13 and O(CH.sub.2).sub.p N.sup.+ R.sup.12 R.sup.13 R.sup.14 wherein
- p is an integer from 1-4,
- n is an integer from 0-3 and
- R.sup.12, R.sup.13, R.sup.14 and R.sup.15 are independently selected from hydrogen and optionally substituted C.sub.1-6 alkyl;
- R.sup.7 is a group of the formula ##STR14## wherein the hydroxyl groups may be substituted by acetyl, benzyl,
- or --(C.sub.1 -C.sub.6)-alkyl-R.sup.17,
- wherein the alkyl group may be substituted with one or more hydroxyl groups;
- R.sup.16 is --COOH, --CH.sub.2 --OH, --CH.sub.2 --O-Acetyl, --COOMe or --COOEt;
- R.sup.17 is H, --OH, --NH.sub.2, --COOH or COOR.sup.18 ;
- R.sup.18 is (C.sub.1 -C.sub.4)-alkyl or --NH--(C.sub.1 -C.sub.4)-alkyl;
- X is --NH--or --O--;
- and
- R.sup.9 and R.sup.10 are the same or different and each is hydrogen or C.sub.1-6 alkyl;
- and salts thereof.
A compound of formula (II):
- or a salt thereof.
Dependencies are inferred from the claim text.