US4311694A
Expired / Lapsed
US
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Amorphous coprecipitates of 4-(monoalkylamino) benzoic acid and derivatives and certain water-soluble materials
Assignee: Wyeth Holdings LLC
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Filing: 1979-12-31
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Granted: 1982-01-19
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Expires: 1999-12-31
Abstract
Abstract A composition of matter in pharmaceutical dosage form comprising an amorphous coprecipitate of water-soluble polyhydroxylic organic compounds and 4-(monoalkylamino)-benzoic acid and derivatives for the treatment of atherosclerosis and hyperlipidemia.
Inventors
- 👤 James E. Krueger
- 👤 Eugene A. Carpentier
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 06:19
CPC Classifications
C; C07; C07H; C07H3/00; C07H3/04; A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K9/00; A61K9/14; A61K9/141; A61K9/145; A61K9/146; C07H3/02
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
108 words
An amorphous coprecipitate providing for substantially enhanced blood levels of a hypolipidemic and anti-atherosclerotic compound consisting essentially of a hypolipidemic and anti-atherosclerotic effective amount of a compound selected from those of the formula: ##STR2## wherein R 1 is an unbranced or branched alkyl group C n H 2n+1 wherein n is 8 to 19 and R 2 is selected from the group consisting of hydrogen, lower alkyl, benzyl, dilower alkylaminoethyl and lower alkoxyethyl together with the pharmaceutically acceptable salts thereof and a coprecipitating amount of a pharmaceutically acceptable water-soluble polyhydroxylic organic compound selected from the group consisting of mono. and di-saccharides, starches, gums and polyglycols or combination thereof.
Claim 2
Dependent Claim
108 words
An amorphous coprecipitate providing for substantially enhanced blood levels of a hypolipidemic and anti-atherosclerotic compound consisting essentially of a hypolipidemic and anti-atherosclerotic effective amount of a compound selected from those of the formula: ##STR2## wherein R 1 is an unbranced or branched alkyl group C n H 2n+1 wherein n is 8 to 19 and R 2 is selected from the group consisting of hydrogen, lower alkyl, benzyl, dilower alkylaminoethyl and lower alkoxyethyl together with the pharmaceutically acceptable salts thereof and a coprecipitating amount of a pharmaceutically acceptable water-soluble polyhydroxylic organic compound selected from the group consisting of mono. and di-saccharides, starches, gums and polyglycols or combination thereof.
Claim 3
Dependent Claim
19 words
The amorphous coprecipitate of claim 1 wherein the compound to polyhydroxylic organic compound ratio is about 1:0.5 to 1:10.
Claim 4
Dependent Claim
14 words
The amorphous coprecipitate of claim 2 wherein the ratio is about 1:1 to 1:5.
Claim 5
Dependent Claim
18 words
The composition of claim 1 or 2 or 3 wherein the water-soluble polyhydroxylic organic compound is a sugar.
Claim 6
Dependent Claim
10 words
The composition of claim 4 wherein the sugar is lactose.
Claim 7
Dependent Claim
10 words
The composition of claim 4 wherein the sugar is dextrose.
Claim 8
Dependent Claim
18 words
The composition of claim 1 or 2 or 3 wherein the water-soluble polyhydroxylic organic compound is a glycol.
Claim 9
Dependent Claim
11 words
The composition of claim 7 wherein the glycol is polyethylene glycol.
Claim 10
Independent Claim
124 words
The method of treating hyperlipidemia and atherosclerosis in warm-blooded animals by providing for substantially enhanced blood levels of a hypolipidemic and anti-atherosclerotic compound comprising administering to said animal an amorphous coprecipitate consisting essentially of a hypolipidemic and anti-atherosclerotic effective amount of a compound selected from those of the formula: ##STR3## wherein R 1 is an unbranched or branched alkyl group C n H 2n+1 wherein n is 8 to 19 and R 2 is selected from the group consisting of hydrogen, lower alkyl, benzyl, dilower alkylaminoethyl and lower alkoxyethyl together with the pharmaceutically acceptable salts thereof and a coprecipitating amount of a pharmaceutically acceptable water-soluble polyhydroxylic organic compound selected from the group consisting of mono- and di-saccharides, starches, gums and polyglycols or combination thereof.
Claim 11
Independent Claim
124 words
The method of treating hyperlipidemia and atherosclerosis in warm-blooded animals by providing for substantially enhanced blood levels of a hypolipidemic and anti-atherosclerotic compound comprising administering to said animal an amorphous coprecipitate consisting essentially of a hypolipidemic and anti-atherosclerotic effective amount of a compound selected from those of the formula: ##STR3## wherein R 1 is an unbranched or branched alkyl group C n H 2n+1 wherein n is 8 to 19 and R 2 is selected from the group consisting of hydrogen, lower alkyl, benzyl, dilower alkylaminoethyl and lower alkoxyethyl together with the pharmaceutically acceptable salts thereof and a coprecipitating amount of a pharmaceutically acceptable water-soluble polyhydroxylic organic compound selected from the group consisting of mono- and di-saccharides, starches, gums and polyglycols or combination thereof.
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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) | 1985-01-18 | 1985-07-20 | 1986-01-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-01-18 | 1989-07-20 | 1990-01-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-01-18 | 1993-07-20 | 1994-01-19 | $7700.00 | Window Closed / Lapsed |