Patent US4771071A successfully refreshed from Google Patents.
US4771071A
Expired / Lapsed
US
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Antihypercholesterolemic compounds
Assignee: Merck and Co Inc
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Filing: 1986-05-05
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Granted: 1988-09-13
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Expires: 2006-05-05
Abstract
Abstract Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): <IMAGE> (I) <IMAGE> (II) and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.
Inventors
- 👤 William F. Hoffman
- 👤 Clarence S. Rooney
- 👤 Ta J. Lee
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 19:46
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
95 words
A compound represented by the following general structural formula (I'): ##STR31## wherein n is 0 to 1; R 1 is C 1-3 alkyl; R 2 is hydrogen or C 1-3 alkyl; R 3 is selected from hydrogen or C 1-3 alkyl; R 4 is selected from hydrogen or C 1-3 alkyl; R 6 is hydrogen or C 1-3 alkyl; A is ##STR32## and a, b, c and d represent single bonds, one of a, b, c, or d represents a double bond, or both a and c or both b and d represent double bonds.
Claim 2
Dependent Claim
95 words
A compound represented by the following general structural formula (I'): ##STR31## wherein n is 0 to 1; R 1 is C 1-3 alkyl; R 2 is hydrogen or C 1-3 alkyl; R 3 is selected from hydrogen or C 1-3 alkyl; R 4 is selected from hydrogen or C 1-3 alkyl; R 6 is hydrogen or C 1-3 alkyl; A is ##STR32## and a, b, c and d represent single bonds, one of a, b, c, or d represents a double bond, or both a and c or both b and d represent double bonds.
Claim 3
Dependent Claim
33 words
A compound according to claim 1 wherein R 3 and R 4 are C 1-3 alkyl; and a, b, c and d represent single bonds or both b and d represent double bonds.
Claim 4
Dependent Claim
23 words
A compound according to claim 1 wherein R 1 is methyl; R 2 is methyl; and R 3 and R 4 are hydrogen.
Claim 5
Dependent Claim
9 words
A compound according to claim 3 which is 6(R)-[2-[8(S)-(2,2-dimethyl-3-methoxy-3-oxopropionyloxy)-2(S),6(R)-dimethyl-1,2,6,7,8,8a(R)-hexahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
Claim 6
Dependent Claim
9 words
A compound according to claim 3 which is 6(R)-[2-[8(S)-(2,2-dimethyl-3-methoxycarbonylpropionyloxy)-2(S),6(R)-dimethyl-1,2,6,7,8,8a-(R)-hexahydronaphthyl-1(S)]-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
Claim 7
Dependent Claim
22 words
A hypocholesterolemic, hypolipidemic pharmaceutical composition comprising a nontoxic therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
Claim 8
Dependent Claim
33 words
A composition according to claim 6 wherein R 3 and R 4 are C 1-3 alkyl; and a, b, c, and d represent single bonds or both b and d represent double bonds.
Claim 9
Dependent Claim
22 words
A composition according to claim 6 wherein R 1 is methyl; R 2 is methyl; R 3 and R 4 are hydrogen.
Claim 10
Dependent Claim
18 words
A composition according to claim 8 in which the therapeutically active ingredient is selected from 6(R)-[2-[8(S)-(2,2-dimethyl-3-methoxy-3-oxopropionyloxy)-2(S),6(R)-dimethyl-1,2,6,7,8a(R)-hexahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one; and 6(R)-[2-[8(S)-(2,2-dimethyl-3-methoxycarbonylpropionyloxy)-2(S),6(R)-dimethyl-1,2,6,7,8,8a(R)-hexahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
Claim 11
Dependent Claim
45 words
A hypocholesterolemic, hypolipidemic pharmaceutical composition comprising a nontoxic therapeutically effective amount of a compound of claim 1 in combination with a pharmaceutically acceptable nontoxic cationic polymer capable of binding bile acids in a a non-reabsorbable form in the gastrointestinal tract and a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
28 words
A method of inhibiting cholesterol biosynthesis comprising the administration to a subject in need of such treatment a nontoxic therapeutically effective amount of a compound of claim 1.
Claim 13
Dependent Claim
33 words
A method according to claim 11 wherein R 3 and R 4 are C 1-3 alkyl; and a, b, c, and d represent single bonds or both b and d represent double bonds.
Claim 14
Dependent Claim
22 words
A method according to claim 11 wherein R 1 is methyl; R 2 is methyl; R 3 and R 4 are hydrogen.
Claim 15
Dependent Claim
18 words
A method according to claim 13 in which the therapeutically active ingredient is selected from 6(R)-[2-[8(S)-(2,2-dimethyl-3-methoxy-3-oxopropionyloxy)-2(S),6(R)-dimethyl-1,2,6,7,8,8a(R)-hexahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one; and 6(R)-[2-[8(S)-(2,2-dimethyl-3-methoxycarbonylpropionyloxy)-2(S),6(R)-dimethyl-1,2,6,7,8,8a(R)-hexahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
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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) | 1991-09-13 | 1992-03-14 | 1992-09-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-09-13 | 1996-03-14 | 1996-09-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-09-13 | 2000-03-14 | 2000-09-13 | $7700.00 | Window Closed / Lapsed |