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Summary for Patent: 4,058,552
|Title:||Esters of p-carbonylphenoxy-isobutyric acids|
|Abstract:||This invention is concerned with esters of p-carbonylphenoxy-isobutyric acids of the general formulae: ##STR1## WHEREIN R is a phenyl group substituted by one or two halogen atoms; R' is H, CH.sub.3, C.sub.6 H.sub.5, SCH.sub.3, OCH.sub.3, or, SO.sub.2 CH.sub.3 ; R" is CH.sub.3 or C.sub.2 H.sub.5 ; Y is C.sub.1 -C.sub.4 alkoxy, phenoxy, phenoxy substituted by one or two halogen atoms, or, OCH.sub.2 O--CO--C(CH.sub.3).sub.3 ; Z is C.sub.1 -C.sub.4 alkyl, phenyl or R; Nr.sub.1 r.sub.2 is N(CH.sub.3).sub.2 N(C.sub.2 H.sub.5).sub.2, morpholino, piperidino, azepino, pyrrolidino. This invention is also concerned with acid addition salts obtained from formula Ia compounds with acids. Compounds of formulae I and Ia are useful as hypocholesterolemiant and hypolipidemiant agents.|
|Inventor(s):||Mieville; Andre (Lausanne, CH)|
|Assignee:||Orchimed SA (CH)|
1. A novel ester of p-carbonylphenoxy-isobutyric acid having the formula ##STR18## wherein R is a phenyl group substituted by one or two halogen atoms;
R' is H, CH.sub.3, C.sub.6 H.sub.5, SCH.sub.3, OCH.sub.3, or, SO.sub.2 CH.sub.3 ;
R" is CH.sub.3 or C.sub.2 H.sub.5 ; and
Y is C.sub.1- C.sub.4 alkoxy, phenoxy, phenoxy substituted by one or two halogen atoms, or, OCH.sub.2 O-CO-C (CH.sub.3).sub.3.
2. A novel ester according to claim 1 having the formula ##STR19## wherein R is 4-ClC.sub.6 H.sub.4, 3-ClC.sub.6 H.sub.4, 3,4-(Cl).sub.2 - C.sub.6 H.sub.3 and 2,6-(Cl).sub.2 - C.sub.6 H.sub.3, and, Y is OCH.sub.3, OC.sub.2 H.sub.5, OCH(CH.sub.3).sub.2.
3. An ester of p-carbonylphenoxy-isobutyric acid according to claim 1 wherein R is 4-chlorophenyl.
4. An ester of p-carbonylphenoxy-isobutyric acid according to claim 1 wherein R is 3,4-dichlorophenyl.
5. Isopropyl p-(4-chlorobenzoyl)phenoxy-isobutyrate.
6. A therapeutic composition useful for treating patients in order to reduce their blood cholesterol and lipids content, which comprises, in association with a pharmaceutically acceptable excipient, a therapeutically effective amount of at least a compound according to claim 1.
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