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DrugPatentWatch concentrates deep knowledge on more than 6,400 small-molecule drugs and 2,300 generic ingredients from 1,700 branded and generic pharmaceutical companies and 700 suppliers, and more than 4,400 active and expired US patents and 74,000 international patents spanning 93 countries and regional patent offices. |
Patent: 5,354,772
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; |
Glossary
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | Type | RLD | Patent No. | Patent Expiration | Patented / Exclusive Use | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Novartis | LESCOL | fluvastatin sodium | Capsule; Oral | 020261 | DEC 31, 1993 | RX | No | 5,354,772 | <disabled> | USE OF THE ACTIVE INGREDIENT FOR INHIBITING THE BIOSYNTHESIS OF CHOLESTEROL AND TREATMENT OF ATHEROSCLEROSIS | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Novartis | LESCOL | fluvastatin sodium | Capsule; Oral | 020261 | DEC 31, 1993 | RX | No | 5,354,772 | <disabled> | ADJUNCT DIET IN THE TX OF ELEVATED TOTAL CHOLESTEROL AND LDL-C LEVELS IN PTS W/PRIMARY HYPERCHOLESTEROLEMIA WHOSE RESPONSE TO DIETARY RESTRICTION OF SAT FAT AND CHOLESTEROL AND OTHER NONPHARMACOLOGICAL MEASURES HAS NOT BEEN ADEQUATE | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Novartis | LESCOL | fluvastatin sodium | Capsule; Oral | 020261 | DEC 31, 1993 | RX | Yes | 5,354,772 | <disabled> | USE OF THE ACTIVE INGREDIENT FOR INHIBITING THE BIOSYNTHESIS OF CHOLESTEROL AND TREATMENT OF ATHEROSCLEROSIS | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Novartis | LESCOL | fluvastatin sodium | Capsule; Oral | 020261 | DEC 31, 1993 | RX | Yes | 5,354,772 | <disabled> | ADJUNCT DIET IN THE TX OF ELEVATED TOTAL CHOLESTEROL AND LDL-C LEVELS IN PTS W/PRIMARY HYPERCHOLESTEROLEMIA WHOSE RESPONSE TO DIETARY RESTRICTION OF SAT FAT AND CHOLESTEROL AND OTHER NONPHARMACOLOGICAL MEASURES HAS NOT BEEN ADEQUATE | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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International Patent Family for Patent: 5,354,772
| Country | Document Number | Publication Date | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Austria | 31718 | Jan 15, 1988 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Australia | 2261283 | Jun 18, 1984 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Australia | 570021 | Mar 03, 1988 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Canada | 1210405 | Aug 26, 1986 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The preview shows a limited data set. Complete access is available with a Subscription | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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