US4473579A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antiatherosclerotic tetrasubstituted ureas and thioureas
Assignee: Wyeth Holdings LLC
•
Filing: 1982-01-26
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Granted: 1984-09-25
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Expires: 2002-01-26
Abstract
Abstract Tetrasubstituted urea and thiourea compounds useful as antiatherosclerotic agents, compositions thereof and processes for their preparation.
Inventors
- 👤 Vern G. DeVries
- 👤 Ransom B. Conrow
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 21:51
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16; A61K31/17; A61P; A61P3/00; A61P3/06; A61P9/00; A61P9/10
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
239 words
A compound of the formula: ##STR5## wherein X represents at least one substituent selected from the group consisting of (C 1 -C 4 )alkyl, (C 1 -C 4 )alkenyl, (C 1 -C 4 )alkynyl, phenoxy, mercapto, amino, (C 1 -C 4 )alkylamino, di(C 1 -C 4 )alkylamino, halo, trihalomethyl, (C 1 -C 4 )alkanoyl, benzoyl, (C 1 -C 4 )alkanamido, nitro, cyano, carboxy, (C 1 -C 4 )-carboalkoxy, carbamoyl, sulfamyl, methylenedioxy, phenyl, ortho-phenylene, tolyl, benzyl, halobenzyl and the group ##STR6## R 1 and R 2 are the same or different and are independently selected from the group consisting of (C 4 -C 12 )alkyl, (C 4 -C 12 )alkenyl, (C 4 -C 12 )alkynyl, (C 4 -C 12 )cycloalkylalkyl, (C 7 -C 14 )aralkyl, and (C 7 -C 14 )aralkyl in which an aromatic ring bears at least one substituent selected from the group consisting of (C 1 -C 10 )alkyl, (C 1 -C 10 )alkoxy, phenoxy, benzyloxy, methylenedioxy, (C 1 -C 4 )alklthio, phenyl, halo, trihalomethyl, adamantyl, (C 1 -C 4 )carboalkoxy and nitro; R 3 is selected from the group consisting of (C 1 -C 4 )alkenyl, (C 1 C 4 )alkynyl, benzyl, benzyl bearing at least one substituent Z, naphthyl, phenyl and phenyl bearing at least one substituent Z, Z being selected independently of X from the group consisting of those from which X is selected with the proviso that X may not be alkyl only.
Claim 2
Dependent Claim
239 words
A compound of the formula: ##STR5## wherein X represents at least one substituent selected from the group consisting of (C 1 -C 4 )alkyl, (C 1 -C 4 )alkenyl, (C 1 -C 4 )alkynyl, phenoxy, mercapto, amino, (C 1 -C 4 )alkylamino, di(C 1 -C 4 )alkylamino, halo, trihalomethyl, (C 1 -C 4 )alkanoyl, benzoyl, (C 1 -C 4 )alkanamido, nitro, cyano, carboxy, (C 1 -C 4 )-carboalkoxy, carbamoyl, sulfamyl, methylenedioxy, phenyl, ortho-phenylene, tolyl, benzyl, halobenzyl and the group ##STR6## R 1 and R 2 are the same or different and are independently selected from the group consisting of (C 4 -C 12 )alkyl, (C 4 -C 12 )alkenyl, (C 4 -C 12 )alkynyl, (C 4 -C 12 )cycloalkylalkyl, (C 7 -C 14 )aralkyl, and (C 7 -C 14 )aralkyl in which an aromatic ring bears at least one substituent selected from the group consisting of (C 1 -C 10 )alkyl, (C 1 -C 10 )alkoxy, phenoxy, benzyloxy, methylenedioxy, (C 1 -C 4 )alklthio, phenyl, halo, trihalomethyl, adamantyl, (C 1 -C 4 )carboalkoxy and nitro; R 3 is selected from the group consisting of (C 1 -C 4 )alkenyl, (C 1 C 4 )alkynyl, benzyl, benzyl bearing at least one substituent Z, naphthyl, phenyl and phenyl bearing at least one substituent Z, Z being selected independently of X from the group consisting of those from which X is selected with the proviso that X may not be alkyl only.
Claim 3
Dependent Claim
34 words
A compound as recited in claim 1 wherein X represents at least one substituent selected from the group consisting of (C 1 -C 4 )alkyl, halo, carboxy, (C 1 -C 4 )carboalkoxy and benzyl.
Claim 4
Dependent Claim
25 words
A compound as recited in claim 2 wherein R 1 is (C 7 -C 14 )aralkyl and R 2 is (C 4 -C 12 )alkyl.
Claim 5
Dependent Claim
17 words
A compound as recited in claim 3 wherein R 1 is benzyl and R 2 is n-butyl.
Claim 6
Dependent Claim
8 words
The compound as recited in claim 1; 1,1-di-benzyl-3-(3-chloro-4-methylphenyl)-3-phenylurea.
Claim 7
Dependent Claim
8 words
The compound as recited in claim 1; 1,1-di-(n-butyl)-3-(3-chloro-4-methylphenyl)-3-phenylurea.
Claim 8
Dependent Claim
8 words
The compound as recited in claim 1; 1,1-di-benzyl-3,3-di-(3-chloro-4-methylphenyl(urea.
Claim 9
Dependent Claim
8 words
The compound as recited in claim 1; 1,1-di-(n-butyl)-3,3-di-(3-chloro-4-methylphenyl)urea.
Claim 10
Dependent Claim
8 words
The compound as recited in claim 1; 1-benzyl-1-(n-butyl)-3-(3-chloro-4-methylphenyl)-3-phenylurea.
Claim 11
Dependent Claim
8 words
The compound as recited in claim 1; 1-benzyl-1-(n-butyl)-3,3-di-(3-chloro-4-methylphenyl)urea.
Claim 12
Dependent Claim
8 words
The compound as recited in claim 1; 1-benzyl-1-(n-butyl)-3-(4-chlorophenyl)-3-phenylurea.
Claim 13
Dependent Claim
8 words
The compound as recited in claim 1; 1-benzyl-1-(n-butyl)-3-(3-chlorophenyl)-3-phenylurea.
Claim 14
Dependent Claim
44 words
A method of reducing the cholesterol ester content of an arterial wall, inhibiting atherosclerotic lesion development and treating hyperlipidemia in a mammal in need of such treatment which comprises administering to said mammal an effective amount of a compound as recited in claim 1.
Claim 15
Dependent Claim
38 words
A method of reducing the cholesterol ester content of an arterial wall in a mammal in need of such treatment which comprises administering to said mammal a cholesterol ester-reducing amount of a compound as recited in claim 1.
Claim 16
Dependent Claim
34 words
A method of inhibiting atherosclerotic lesion development in a mammal in need of such treatment which comprises administering to said mammal an atherosclerotic lesion development-inhibiting amount of a compound as recited in claim 1.
Claim 17
Dependent Claim
31 words
A method of treating hyperlipidemia in a mammal in need of such treatment which comprises administering to said mammal an effective lipid-altering amount of a compound as recited in claim 1.
Claim 18
Dependent Claim
43 words
A pharmaceutical composition suitable for reducing the cholesterol ester content of an arterial wall, inhibiting atherosclerotic lesion development and treating hyperlipidemia in a mammal which comprises an effective amount of a compound as recited in claim 1 and a non-toxic, pharmaceutically acceptable carrier.
Claim 19
Dependent Claim
37 words
A pharmaceutical composition suitable for reducing the cholesterol ester content of an arterial wall in a mammal which comprises a cholesterol ester-reducing amount of a compound as recited in claim 1 and a non-toxic pharmaceutically acceptable carrier.
Claim 20
Dependent Claim
33 words
A pharmaceutical composition suitable for inhibiting atherosclerotic lesion development in a mammal which comprises an atherosclerotic lesion development-inhibiting amount of a compound as recited in claim 1 and a non-toxic, pharmaceutically acceptable carrier.
Claim 21
Dependent Claim
30 words
A pharmaceutically composition suitable for treating hyperlipidemia in a mammal which comprises an effective lipid-lowering amount of a compound as recited in claim 1 and a non-toxic, pharmaceutically acceptable carrier.
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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) | 1987-09-25 | 1988-03-26 | 1988-09-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-09-25 | 1992-03-26 | 1992-09-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-09-25 | 1996-03-26 | 1996-09-25 | $7700.00 | Window Closed / Lapsed |