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Details for Patent: 5,354,772

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Summary for Patent: 5,354,772

Title: Indole analogs of mevalonolactone and derivatives thereof
Abstract:Compounds of the formula ##STR1## wherein one of R and R.sub.o is ##STR2## and the other is primary or secondary C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-6 cycloalkyl or phenyl-(CH.sub.2).sub.m --, wherein R.sub.4 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R.sub.5 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R.sub.5a is hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R.sub.5 and R.sub.5a must be hydrogen when R.sub.4 is hydrogen, R.sub.5a must be hydrogen when R.sub.5 is hydrogen, not more than one of R.sub.4 and R.sub.5 is trifluoromethyl, not more than one of R.sub.4 and R.sub.5 is phenoxy, and not more than one of R.sub.4 and R.sub.5 is benzyloxy, R.sub.2 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.3-6 cycloalkyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R.sub.3 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R.sub.3 must be hydrogen when R.sub.2 is hydrogen, not more than one of R.sub.2 and R.sub.3 is trifluoromethyl, not more than one of R.sub.2 and R.sub.3 is phenoxy, and not more than one of R.sub.2 and R.sub.3 is benzyloxy, X is --(CH.sub.2).sub.n -- or --CH.dbd.CH--, wherein n is 0, 1, 2 or 3, and Z is ##STR3## wherein R.sub.6 is hydrogen or C.sub.1-3 alkyl, and R.sub.7 is hydrogen, R.sub.7b or M, wherein R.sub.7b is a physiologically acceptable and hydrolyzable ester group, and M is a pharmaceutically acceptable cation, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level, and therefore, in the treatment of hyperliopoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
Inventor(s): Kathawala; Faizulla G. (Mountain Lakes, NJ)
Assignee: Sandoz Pharm. Corp. (E. Hanover, NJ)
Application Number:08/157,595
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;

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International Patent Family for Patent: 5,354,772

Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria31718► subscribe
Australia2261283► subscribe
Australia570021► subscribe
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