US4766145A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihypercholesterolemic compounds
Assignee: Merck and Co Inc
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Filing: 1986-05-05
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Granted: 1988-08-23
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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) +TR <IMAGE> (II) and pharmaceutically acceptable salts of the compound (II) in which Z is hydrogen are disclosed.
Inventors
- 👤 Ta J. Lee
- 👤 Clarence S. Rooney
- 👤 William F. Hoffman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:02
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
40 words
A compound represented by the following general structural formula (I'): ##STR34## wherein: n is 2 to 7; R 1 is C 1-6 alkyl, A is ##STR35## b and d represent single bonds, or both b and d represent double bonds.
Claim 2
Dependent Claim
40 words
A compound represented by the following general structural formula (I'): ##STR34## wherein: n is 2 to 7; R 1 is C 1-6 alkyl, A is ##STR35## b and d represent single bonds, or both b and d represent double bonds.
Claim 3
Dependent Claim
11 words
A compound of claim 1 wherein n is 2 to 5.
Claim 4
Dependent Claim
9 words
A compound of claim 2 wherein n is 2.
Claim 5
Dependent Claim
8 words
A compound of claim 3 which is 6(R)-[2-[8(S)-(1-Ethoxycarbonylcyclopropanecarbonyloxy)-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 of claim 2 wherein n is 3.
Claim 7
Dependent Claim
8 words
A compound of claim 5 which is 6(R)-[2-[8(S)-(1-Ethoxycarbonylcyclobutanecarbonyloxy)-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 8
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 9
Dependent Claim
12 words
A composition according to claim 7 wherein n is 2 to 5.
Claim 10
Dependent Claim
20 words
A composition according to claim 8 wherein the therapeutically active ingredient is selected from the group consisting of: 6(R)-[2-[8(S)-(1-Ethoxycarbonylcyclopropanecarbonyloxy)-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; 6(R)-[2-[8(S)-(1-Ethoxycarbonylcyclobutanecarbonyloxy)-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
44 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 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
11 words
A method of claim 11 wherein n is 2 to 5.
Claim 14
Dependent Claim
19 words
A method of claim 12 wherein the therapeutically active ingredient is selected from the group consisting of: 6(R)-[2-[8(S)-(1-Ethoxycarbonylcyclopropanecarbonyloxy)-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; 6(R)-[2-[8(S)-(1-Ethoxycarbonylcyclobutanecarbonyloxy)-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-2one.
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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) | 1991-08-23 | 1992-02-22 | 1992-08-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-08-23 | 1996-02-22 | 1996-08-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-08-23 | 2000-02-22 | 2000-08-23 | $7700.00 | Window Closed / Lapsed |