Patent US4282155A successfully refreshed from Google Patents.
US4282155A
Expired / Lapsed
US
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Antihypercholesterolemic compounds
Assignee: Merck and Co Inc
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Filing: 1980-08-05
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Granted: 1981-08-04
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Expires: 2000-08-05
Abstract
Abstract 6(R)-[2-(8'-Etherified-hydroxy-2',6'-dimethylpolyhydronaphthyl-1')-eth yl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones are prepared from the corresponding 8'-acyloxy compounds, some of which are naturally occurring, by protection of the 4(R)-hydroxyl and the 2-keto group, followed by reductive removal of the 8'-acyloxy group, etherification of the resulting 8'-hydroxyl and removal of the protecting groups. The products inhibit the biosynthesis of cholesterol.
Inventors
- 👤 Robert L. Smith
- 👤 Ta-Jyh Lee
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 13:48
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30; C07C; C07C59/00; C07C59/40; C07C59/58; C07C59/62; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
126 words
A compound of the structure: ##STR13## in which R is: C 1-18 alkyl, straight or branched chain, C 4-10 cycloalkyl, C 2-10 alkenyl, C 5-10 cycloalkenyl, C 2-10 alkynyl, phenyl C 1-3 alkyl, substituted phenyl C 1-3 alkyl in which the substituent is halogen, CF 3 or CN, and C 1-10 alkyl having one or more --O--, --S--, or ##STR14## in the chain, in which the dotted lines at X,Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone, and the corresponding hydroxy acids of the formula: ##STR15## and the pharmaceutically acceptable salts, the loweralkyl esters and the phenyl, dimethylamino and acetylamino substituted loweralkyl esters of said hydroxy acids.
Claim 2
Dependent Claim
126 words
A compound of the structure: ##STR13## in which R is: C 1-18 alkyl, straight or branched chain, C 4-10 cycloalkyl, C 2-10 alkenyl, C 5-10 cycloalkenyl, C 2-10 alkynyl, phenyl C 1-3 alkyl, substituted phenyl C 1-3 alkyl in which the substituent is halogen, CF 3 or CN, and C 1-10 alkyl having one or more --O--, --S--, or ##STR14## in the chain, in which the dotted lines at X,Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone, and the corresponding hydroxy acids of the formula: ##STR15## and the pharmaceutically acceptable salts, the loweralkyl esters and the phenyl, dimethylamino and acetylamino substituted loweralkyl esters of said hydroxy acids.
Claim 3
Dependent Claim
9 words
A compound of claim 1 in the lactone form.
Claim 4
Dependent Claim
17 words
A compound of claim 1 in the free hydroxy acid form or the salts or esters thereof.
Claim 5
Dependent Claim
13 words
A compound of claim 2 in which X and Z are double bonds.
Claim 6
Dependent Claim
10 words
A compound of claim 4 in which R is methyl.
Claim 7
Dependent Claim
10 words
A compound of claim 4 in which R is p-fluorobenzyl.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-08-03 | 1985-02-02 | 1985-08-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-08-03 | 1989-02-02 | 1989-08-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-08-03 | 1993-02-02 | 1993-08-04 | $7700.00 | Window Closed / Lapsed |