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|Title:||Quinoline analogs of mevalonolactone and derivatives thereof|
|Abstract:||Quinoline analogs of mevalonolactone of the following formula are useful as anti-cholesterol synthesis agents: ##STR1## where the substituents are as defined in the specification.|
|Inventor(s):||Wattanasin; Sompong (Hopatcong, NJ)|
|Assignee:||Novartis Pharmaceuticals Corporation (East Hanover, NJ)|
1. A compound of the formula ##STR38## wherein each of R and R.sub.o is, independently, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or ##STR39## each of R.sub.1, R.sub.2, R.sub.3,
R.sub.4 and R.sub.5 is, independently, hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, benzyloxy or hydroxy;
with the provisos that not more than one of R.sub.1 and R.sub.2 is trifluoromethyl, not more than one of R.sub.1 and R.sub.2 is phenoxy, not more than one of R.sub.1 and R.sub.2 is benzyloxy, not more than one of R.sub.1 and R.sub.2 is hydroxy, not more than one of R.sub.3 -R.sub.5 is trifluoromethyl, not more than one of R.sub.3 -R.sub.5 is phenoxy, not more than one of R.sub.3 -R.sub.5 is benzyloxy, and not more than one of R.sub.3 -R.sub.5 is hydroxy;
X is --(CH.sub.2).sub.2 -- or --CH.dbd.CH--; ##STR40## with the proviso that Q may be ##STR41## only when X is --CH.dbd.CH or R.sub.6 is C.sub.1-3 alkyl or both,
R.sub.6 is hydrogen or C.sub.1-3 alkyl;
R.sub.7 is hydrogen, R.sub.8 or M;
R.sub.8 is a physiologically acceptable and hydrolyzable ester group; and
M is a pharmaceutically acceptable cation.
2. A compound according to claim 1 wherein Z is (a) and Q is ##STR42##
3. A compound according to claim 2 which is a 3R,5S isomer.
4. A compound according to claim 2 wherein R and R.sub.o are independently CH.sub.3, isopropyl, phenyl, 3,5-dimethylphenyl or 4-fluorophenyl.
5. A compound according to claim 1 which is (E,)-6-heptenoic acid, 3,5-dihydroxy-7-[2-(1-methylethyl)-4-phenylquinolin-3-yl]-ethyl ester, or its sodium salt.
6. A compound according to claim 1 which is 7-[4-(3,5-dimethylphenyl)-2-methylquinolin-3-yl-3,5-dihydroxy-ethyl ester, or its sodium salt.
7. A compound according to claim 1 which is 6-[2-[4-(3,5-dimethylphenyl)-2-methylquinolin-3-yl]-ethenyl]tetrahydro-2H- pyran-2-one, or its sodium salt.
8. A method of inhibiting cholesterol biosynthesis comprising administering to a mammal in need of such treatment a cholesterol-biosynthesis-inhibiting amount of a compound of claim 1.
9. A method of treating atherosclerosis comprising administering to a mammal in need of such treatment an effective amount of a compound according to claim 1, said effective amount being an amount effective for the treatment of atherosclerosis.
10. A pharmaceutical composition comprising a cholesterol-biosynthesis inhibiting amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
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