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US5453436A Expired / Lapsed US ⏱️ 0.0 years remaining

Treatment of athereosclerosis using, carbazolyl-(4)-oxypropanolamine compounds

Assignee: Roche Diagnostics Corp
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Filing: 1994-03-17
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Granted: 1995-09-26
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Expires: 2014-03-17
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Abstract

Abstract A new use of, and method of treatment of atherosclerosis using, a compound selected from the group consisting essentially of compounds of Formula I: ##STR1## wherein: R 1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R 2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R 3 is hydrogen or lower alkyl of up to 6 carbon atoms; R 4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R 4 together with R 5 can represent --CH 2 --O--; X is a valency bond, --CH 2 , oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R 5 and R 6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH 2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R 5 and R 6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, for inhibition of proliferation of smooth muscle cells.

Inventors

  • 👤 Eliot H. Ohlstein

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 13:22
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/403

Claims Analysis

Total Claims: 4
Claim 1
Independent Claim 199 words
A method of treating atherosclerosis in human patients, comprising internally administering to a patient in need thereof an effective dose of a pharmaceutical composition comprising a compound of Formula I: ##STR5## wherein: R 1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R 2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R 3 is hydrogen or lower alkyl of up to 6 carbon atoms; R 4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R 4 together with R 5 can represent --CH 2 --O--; X is a valency bond, --CH 2 , oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R 5 and R 6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH 2 --group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim 199 words
A method of treating atherosclerosis in human patients, comprising internally administering to a patient in need thereof an effective dose of a pharmaceutical composition comprising a compound of Formula I: ##STR5## wherein: R 1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R 2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R 3 is hydrogen or lower alkyl of up to 6 carbon atoms; R 4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R 4 together with R 5 can represent --CH 2 --O--; X is a valency bond, --CH 2 , oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R 5 and R 6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH 2 --group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 17 words
A method of treatment according to claim 1 wherein said pharmaceutical composition is suitable for parenteral administration.
Claim 4
Dependent Claim 13 words
A method of treatment according to claim 1 wherein said compound is carvedilol.

References Cited (Backward Citations)

US4503067A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1998-09-25 1999-03-27 1999-09-26 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2002-09-25 2003-03-27 2003-09-26 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2006-09-25 2007-03-27 2007-09-26 $7700.00 Window Closed / Lapsed

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