Claims for Patent: 5,753,675

Summary for Patent: 5,753,675

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):	Sompong Wattanasin
Assignee:	Novartis Pharmaceuticals Corp
Application Number:	US07/498,301
Patent Claims:	1. A compound of the formula ##STR38## wherein each of R and Ro is, independently, C1-6 alkyl, C3-7 cycloalkyl or ##STR39## each of R1, R2, R3, R4 and R5 is, independently, hydrogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, benzyloxy or hydroxy;with the provisos that not more than one of R1 and R2 is trifluoromethyl, not more than one of R1 and R2 is phenoxy, not more than one of R1 and R2 is benzyloxy, not more than one of R1 and R2 is hydroxy, not more than one of R3 -R5 is trifluoromethyl, not more than one of R3 -R5 is phenoxy, not more than one of R3 -R5 is benzyloxy, and not more than one of R3 -R5 is hydroxy; X is --(CH2)2 -- or --CH═CH--; ##STR40## with the proviso that Q may be ##STR41## only when X is --CH═CH or R6 is C1-3 alkyl or both, R6 is hydrogen or C1-3 alkyl; R7 is hydrogen, R8 or M; R8 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 Ro are independently CH3, 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.