US4868210A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihyperlipidemic and antiatherosclerotic compounds and compositions
Assignee: Warner Lambert Co LLC
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Filing: 1988-03-30
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Granted: 1989-09-19
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Expires: 2008-03-30
Abstract
Abstract Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
Inventors
- 👤 Bharat K. Trivedi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 12:00
CPC Classifications
C; C07; C07D; C07D311/00; C07D311/02; C07D311/04; C07D311/58; A; A61; A61P; A61P3/00; A61P3/06; A61P9/00; A61P9/10; C07C; C07C275/00; C07C275/28; C07D311/78; C07D311/80; C07D311/82; C07D311/90; C07D313/00; C07D313/02; C07D313/06; C07D313/08; C07C2602/00; C07C2602/02; C07C2602/04; C07C2602/08; C07C2602/10; C07C2603/00; C07C2603/02; C07C2603/04; C07C2603/06; C07C2603/10; C07C2603/12; C07C2603/18
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
144 words
A compound having the formula ##STR6## wherein R 1 and R 2 are independently selected from alkyl or alkoxy of from one to six carbon atoms; R 3 is hydrogen, alkyl of from one to seven carbon atoms, or phenylmethyl; X is oxygen or sulfur; n is zero, one or two; A is selected from ##STR7## where n' is one or two; Y is a direct bond, or >CH 2 ; R 4 is selected from hydrogen, alkyl of from one to six carbon atoms, hydroxy, acetoxy, alkoxy of from one to six carbon atoms, phenoxy, fluorine, chlorine, bromine, nitro, trifluoromethyl, carboxyl, --COO--alkyl in which the alkyl portion contains from one to four carbon atoms, amino, alkylamino of from one to six carbon atoms, dialkylamino in which the alkyl groups contain from one to six carbon atoms, --NH--acetyl; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
144 words
A compound having the formula ##STR6## wherein R 1 and R 2 are independently selected from alkyl or alkoxy of from one to six carbon atoms; R 3 is hydrogen, alkyl of from one to seven carbon atoms, or phenylmethyl; X is oxygen or sulfur; n is zero, one or two; A is selected from ##STR7## where n' is one or two; Y is a direct bond, or >CH 2 ; R 4 is selected from hydrogen, alkyl of from one to six carbon atoms, hydroxy, acetoxy, alkoxy of from one to six carbon atoms, phenoxy, fluorine, chlorine, bromine, nitro, trifluoromethyl, carboxyl, --COO--alkyl in which the alkyl portion contains from one to four carbon atoms, amino, alkylamino of from one to six carbon atoms, dialkylamino in which the alkyl groups contain from one to six carbon atoms, --NH--acetyl; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
27 words
A compound as defined by claim 1 wherein A is selected from unsubstituted or substituted 2,3-dihydro-1H-inden-1-yl; 2,3-dihydro-1H-inden-2-yl; 2,3-dihydro-1-hydroxy-1-indenyl; 1,2,3,4-tetrahydronaphth-1-yl; 1,2,3,4-tetrahydronaphth-2-yl; 1,2,3,4-tetrahydro-1-hydroxy-1-naphthyl; 6,7,8,9-tetrahydro-5H-benzocycloheptan-8-yl; 6,7,8,9-tetrahydro-5H-benzocycloheptan-9-yl; 9-fluorenyl; 10,11-dibenzo[a,d]cycloheptan-5-yl; and 1,2,3,4-tetrahydro-1,1,4,4-tetramethylnaphthen-2-yl.
Claim 4
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-Methylethyl)phenyl]-N'-[(2,3-dihydro-1H-inden-1-yl)methyl]urea.
Claim 5
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-N'-1,2,3,4-tetrahydro-2-naphthalenyl)urea.
Claim 6
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-N'-[(1,2,3,4-tetrahydro-1-naphthalenyl)methyl]urea.
Claim 7
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-N'-[(3,4-dihydro-1-naphthalenyl)methyl]urea.
Claim 8
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-N'-[(2,3-dihydro-1-hydroxy-1H-inden-1-yl)methyl]urea.
Claim 9
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-N'-[(1,2,3,4-tetrahydro-1-hydroxy-1-naphthalenyl)methyl]urea.
Claim 10
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-(2,6-dimethylphenyl)-N'-(1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-2-naphthalenyl)urea.
Claim 11
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-n-(1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-2-naphthalenyl)urea.
Claim 12
Dependent Claim
11 words
A compound as defined by claim 2 having the name N-[2,6-bis(1-methylethyl)phenyl]-N'-[(1,2,3,4-tetrahydro-7-methoxy-2-naphthalenyl)methyl]urea.
Claim 13
Dependent Claim
28 words
A pharmaceutical composition for treating hypercholesterolemia or atherosclerosis comprising an ACAT-inhibitory effective amount of a compound as defined by claim 1 in combination with a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
29 words
A method of treating hypercholesterolemia or atherosclerosis comprising administering to a mammal in need of such treatment an ACAT-inhibitory effective amount of a compound as defined by claim 1.
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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) | 1992-09-18 | 1993-03-20 | 1993-09-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-09-18 | 1997-03-20 | 1997-09-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-09-18 | 2001-03-20 | 2001-09-19 | $7700.00 | Window Closed / Lapsed |