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US5030653A Expired / Lapsed US ⏱️ 0.0 years remaining

Antihyperlipidemic and antiatherosclerotic compounds and compositions

Assignee: Warner Lambert Co LLC
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Filing: 1990-10-23
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Granted: 1991-07-09
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Expires: 2010-10-23
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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 17:12
CPC Classifications
C; C07; C07C; C07C275/00; C07C275/28; C07D; C07D311/00; C07D311/02; C07D311/04; C07D311/58; 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: 5
Claim 1
Independent Claim 143 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## Z is a direct bond, >CH 2 , --CH═CH-- --CH 2 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 143 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## Z is a direct bond, >CH 2 , --CH═CH-- --CH 2 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 12 words
A compound as defined by claim 1 having the same N-[2,6-bis(1-methylethyl)phenyl]-N-40 -(9H-fluoren-9-ylmethyl)urea.
Claim 4
Dependent Claim 28 words
A pharmaceutical composition for treating hyperchlesterolemia or atherosclerosis comprising an ACAT-inhibitory effective amount of a compound as defined by claim 1 in combination with a pharmaceutically acceptable carrier.
Claim 5
Dependent Claim 29 words
A method of treating hypercholesterolemia or athersclerosis comprising administering to a mammal in need of such treatment an ACAT-inhibitory effective amount of a compound as defined by claim 1.

References Cited (Backward Citations)

GB935187A Cited
US3555086A Cited
US4868210A Cited
EP0335374A2 Cited
US4981865A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1994-07-08 1995-01-07 1995-07-09 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1998-07-08 1999-01-07 1999-07-09 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2002-07-08 2003-01-07 2003-07-09 $7700.00 Window Closed / Lapsed

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