Patent US4450171A successfully refreshed from Google Patents.
US4450171A
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Antihypercholesterolemic compounds
Assignee: Merck and Co Inc
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Filing: 1982-06-14
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Granted: 1984-05-22
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Expires: 2002-06-14
Abstract
Abstract 6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro -2H-pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
Inventors
- 👤 William F. Hoffman
- 👤 Robert L. Smith
- 👤 Alvin K. Willard
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 08:59
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
91 words
A compound of the formula: ##STR81## wherein R' is H or CH 3 ; R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl, 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; or the corresponding dihydroxy acid of the formula: ##STR82## or a pharmaceutically acceptable salt of said acid, a C 1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C 1-4 alkyl ester or α-monoglyceride of said acid.
Claim 2
Dependent Claim
91 words
A compound of the formula: ##STR81## wherein R' is H or CH 3 ; R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl, 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; or the corresponding dihydroxy acid of the formula: ##STR82## or a pharmaceutically acceptable salt of said acid, a C 1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C 1-4 alkyl ester or α-monoglyceride of said acid.
Claim 3
Dependent Claim
11 words
The compound of claim 1 wherein R' is CH 3 .
Claim 4
Dependent Claim
18 words
The compound of claims 1 or 2, wherein none of X, Y or Z is a double bond.
Claim 5
Dependent Claim
106 words
A pharmaceutical antihypercholesterolemic composition comprising a pharmaceutical carrier and an antihypercholesterolemic effective amount of a compound of structural formula: ##STR83## in which R' is H, or CH 3 ; R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl, 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; or the corresponding dihydroxy acid of the formula: ##STR84## or a pharmaceutically acceptable salt of said acid, a C 1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C 1-4 alkyl ester or α-monoglyceride of said acid.
Claim 6
Dependent Claim
106 words
A pharmaceutical antihypercholesterolemic composition comprising a pharmaceutical carrier and an antihypercholesterolemic effective amount of a compound of structural formula: ##STR83## in which R' is H, or CH 3 ; R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl, 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; or the corresponding dihydroxy acid of the formula: ##STR84## or a pharmaceutically acceptable salt of said acid, a C 1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C 1-4 alkyl ester or α-monoglyceride of said acid.
Claim 7
Dependent Claim
11 words
The composition of claim 4 wherein R' is CH 3 .
Claim 8
Dependent Claim
18 words
The composition of claim 4 or 5, wherein none of X, Y or Z is a double bond.
Claim 9
Independent Claim
113 words
A method of treating hypercholesterolemia in a patient in need of such treatment which comprises administration of an antihyperchloesterolemic effective amount of a compound of structural formula: ##STR85## wherein R' is H or CH 3 ; R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl, 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; or the corresponding dihydroxy acid of the formula: ##STR86## or a pharmaceutically acceptable salt of said acid, a C 1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C 1-4 alkyl ester or α-monoglyceride of said acid.
Claim 10
Independent Claim
113 words
A method of treating hypercholesterolemia in a patient in need of such treatment which comprises administration of an antihyperchloesterolemic effective amount of a compound of structural formula: ##STR85## wherein R' is H or CH 3 ; R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl, 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; or the corresponding dihydroxy acid of the formula: ##STR86## or a pharmaceutically acceptable salt of said acid, a C 1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C 1-4 alkyl ester or α-monoglyceride of said acid.
Claim 11
Dependent Claim
11 words
The method of claim 7 wherein R' is CH 3 .
Claim 12
Dependent Claim
18 words
The method of claim 7 or 8, wherein none of X, Y or Z is a double bond.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-05-22 | 1987-11-21 | 1988-05-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-05-22 | 1991-11-21 | 1992-05-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-05-22 | 1995-11-21 | 1996-05-22 | $7700.00 | Window Closed / Lapsed |