US4503072A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihypercholesterolemic compounds
Assignee: Merck and Co Inc
•
Filing: 1984-06-18
•
Granted: 1985-03-05
•
Expires: 2004-06-18
Abstract
Abstract Compounds of general structural formula: <IMAGE> wherein Q is: <IMAGE> or pharmaceutically acceptable salts, C1-3 alkyl esters or alpha -monoglyceride when Q is a dihydroxy acid are useful as antihypercholesterolemic agents for the treatment of atherosclerosis, familial hypercholesterolemia, hyperlipemia and like diseases. They also have useful antifungal activity.
Inventors
- 👤 William F. Hoffman
- 👤 Ta-Jyh Lee
- 👤 Robert L. Smith
- 👤 Alvin K. Willard
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 01:44
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
174 words
The compound of structural formula: ##STR51## wherein Q is: ##STR52## or a pharmaceutically acceptable salt, C 1-3 alkyl ester or α-monoglyceride of the dihydroxy acid wherein R 2 is hydrogen or methyl; R is (1) C 1-10 alkyl, either straight or branched chain, (2) C 3-6 cycloalkyl, (3) C 2-10 alkenyl, (4) halo-C 1-10 alkyl, (5) phenyl, (6) phenyl substituted by one or more of halo, C 1-3 alkyl, or C 1-3 alkoxy, (7) phenyl-C 1-3 alkyl, (8) phenyl-C 1-3 alkyl wherein the phenyl group is substituted by one or more of halo, C 1-3 alkyl, or C 1-3 alkoxy; R 1 is (1) hydrogen, (2) C 1-3 alkyl, (3) C 3-6 cycloalkyl, (4) C 2-5 alkenyl, (5) halo-C 1-3 alkyl, (6) benzyl, or (7) benzyl, substituted by one or more of halo, C 1-3 alkyl, or C 1-3 alkoxy; and the dotted lines X, Y and Z, represent possible double bonds, the double bonds, when any are present being either X and Z in combination or one of X, Y or Z alone.
Claim 2
Dependent Claim
174 words
The compound of structural formula: ##STR51## wherein Q is: ##STR52## or a pharmaceutically acceptable salt, C 1-3 alkyl ester or α-monoglyceride of the dihydroxy acid wherein R 2 is hydrogen or methyl; R is (1) C 1-10 alkyl, either straight or branched chain, (2) C 3-6 cycloalkyl, (3) C 2-10 alkenyl, (4) halo-C 1-10 alkyl, (5) phenyl, (6) phenyl substituted by one or more of halo, C 1-3 alkyl, or C 1-3 alkoxy, (7) phenyl-C 1-3 alkyl, (8) phenyl-C 1-3 alkyl wherein the phenyl group is substituted by one or more of halo, C 1-3 alkyl, or C 1-3 alkoxy; R 1 is (1) hydrogen, (2) C 1-3 alkyl, (3) C 3-6 cycloalkyl, (4) C 2-5 alkenyl, (5) halo-C 1-3 alkyl, (6) benzyl, or (7) benzyl, substituted by one or more of halo, C 1-3 alkyl, or C 1-3 alkoxy; and the dotted lines X, Y and Z, represent possible double bonds, the double bonds, when any are present being either X and Z in combination or one of X, Y or Z alone.
Claim 3
Dependent Claim
51 words
The compound of claim 1 wherein R is 1-methylpropyl, 1,1-dimethylpropyl or 1-ethyl-1-methyl-propyl; R 1 is hydrogen or methyl; X and Z are double bonds; or X, Y and Z are all single bonds; or a pharmaceutically acceptable salt, C 1-3 alkyl ester or α monoglyceride of structure of the dihydroxy acid.
Claim 4
Dependent Claim
23 words
The compound of claim 2, which is ##STR53## or a pharmaceutically acceptable salt, C 1-3 alkyl ester, or α-monoglyceride of the dihydroxy acid.
Claim 5
Dependent Claim
34 words
An antihypercholesterolemic pharmaceutical composition comprising a pharmaceutical carrier and an effective antihypercholesterolemic amount of the compound of claim 1, or a pharmaceutically acceptable salt, C 1-3 alkyl ester or α-monoglyceride of the dihydroxy acid.
Claim 6
Dependent Claim
27 words
The composition of claim 4 wherein the compound is that of claim 3, or a pharmaceutically acceptable salt, C 1-3 alkyl or α-monoglyceride of the dihydroxy acid.
Claim 7
Dependent Claim
27 words
The composition of claim 5 wherein the compound is that of claim 4, or a pharmaceutically acceptable salt, C 1-3 alkyl or α-monoglyceride of the dihydroxy acid.
Claim 8
Dependent Claim
43 words
A method of treating atherosclerosis, familial hypercholesterolemia or hyperlipemia comprising administering to a patient in need of such treatment an effective antihypercholesterolemic amount of the compound of claim 1, or a pharmaceutically acceptable salt, C 1-3 alkyl or α-monoglyceride of the dihydroxy acid.
Claim 9
Dependent Claim
27 words
The method of claim 7 wherein the compound is that of claim 3, or a pharmaceutically acceptable salt, C 1-3 alkyl or α-monoglyceride of the dihydroxy acid.
Claim 10
Dependent Claim
27 words
The method of claim 8 wherein the compound is that of claim 4, or a pharmaceutically acceptable salt, C 1-3 alkyl or α-monoglyceride of the dihydroxy acid.
References Cited (Backward Citations)
US3983140A
Cited
US4231938A
Cited
US4294846A
Cited
US4282155A
Cited
EP0033538A2
Cited
US4293496A
Cited
US4351844A
Cited
US4343814A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-03-04 | 1988-09-03 | 1989-03-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-03-04 | 1992-09-03 | 1993-03-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-03-04 | 1996-09-03 | 1997-03-05 | $7700.00 | Window Closed / Lapsed |