Patent US3143960A successfully refreshed from Google Patents.
US4916162A
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Antihypercholesterolemic compounds
Assignee: Merck and Co Inc
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Filing: 1988-07-18
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Granted: 1990-04-10
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Expires: 2008-07-18
Abstract
Abstract Novel 3-hydroxy-3-methylglutary-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.
Inventors
- 👤 William F. Hoffman
- 👤 Clarence S. Rooney
- 👤 Ta Jyh Lee
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 19:35
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
133 words
A compound represented by the following general structural formula (II ' ) ##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 hydrogen or C 1-3 alkyl; R 4 is hydrogen or C 1-3 alkyl; R 6 is hydrogen or C 1-3 alkyl; ##STR32## and a, b, c and d represent single bonds, one of a, b, c or d represent a double bond, or both a and c or both b and d represent double bonds; Z is hydrogen, C 1-5 alkyl, or C 1-5 alkyl substituted with a member of the group consisting of phenyl, dimethylamino or acetylamino; or a pharmaceutically acceptable salt of a compound of the formula (II 40 ) in which Z is hydrogen.
Claim 2
Dependent Claim
133 words
A compound represented by the following general structural formula (II ' ) ##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 hydrogen or C 1-3 alkyl; R 4 is hydrogen or C 1-3 alkyl; R 6 is hydrogen or C 1-3 alkyl; ##STR32## and a, b, c and d represent single bonds, one of a, b, c or d represent a double bond, or both a and c or both b and d represent double bonds; Z is hydrogen, C 1-5 alkyl, or C 1-5 alkyl substituted with a member of the group consisting of phenyl, dimethylamino or acetylamino; or a pharmaceutically acceptable salt of a compound of the formula (II 40 ) in which Z is hydrogen.
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
22 words
A hypocholesterolemic, hypolipidemic pharmaceutical composition comprising a nontoxic therapeutically effective amount of a compound of claim 3 and a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim
33 words
A composition according to claim 4 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 7
Dependent Claim
22 words
A composition according to claim 4 wherein R 1 is methyl; R 2 is methyl; R 3 and R 4 are hydrogen.
Claim 8
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 9
Dependent Claim
33 words
A method according to Claim 7 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 10
Dependent Claim
22 words
A method according to claim 7 wherein R 1 is methyl; R 2 is methyl; R 3 and R 4 are hydrogen.
Claim 11
Dependent Claim
9 words
A compound of Claim 3 which is 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2,2-dimethyl-3-methoxy-3-oxopropionyloxy-1(S)-naphthyl]-3(R),5(R)-dihydryoxyheptanoic acid.
Claim 12
Dependent Claim
9 words
A compound of Claim 3 which is 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2,2-dimethyl-3-methoxycarbonylpropionyloxy)-1(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid.
Claim 13
Dependent Claim
19 words
A composition according to claim 6 in which the therapeutically-active ingredient is selected from; 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2,2-dimethyl-3-methoxy-3-oxopropionyloxy)-1(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid, or 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-.8(S)-(2,2-dimethyl-3-methoxycarbonylpropionyl-oxy)-1(S)-naphthyl]-3(R),5(R)-dihydroxyheptanioc acid.
Claim 14
Dependent Claim
19 words
A method according to claim 7 in which the therapeutically-active ingredient is selected from: 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2,2-dimethyl-3-methoxy-3-oxopropionyloxy)-1(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid, or 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-.8(S)-(2,2-dimethyl-3-methoxycarbonylpropionyl-oxy)-1(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid.
References Cited (Backward Citations)
US4444784A
Cited
US4668699A
Cited
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