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US3846541A Expired / Lapsed US ⏱️ 0.0 years remaining

Treatment of hypercholesteremia

Assignee: Pfizer Health AB
•
Filing: 1973-03-20
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Granted: 1974-11-05
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Expires: 1993-03-20
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Abstract

Abstract Hypercholesteremia in humans is treated by daily administrations of (a) para-chlorophenoxyisobutyric acid or a simple functional derivative thereof which, under the influence of substances present in the gastric juices, serum or tissues of a human being, acts as a source of that acid and (b) a solid non-toxic anion exchange resin in the weight ratio of 1:2 to 1:20. The resin is a dextran-epichlorohydrin polymer in which 6-50 percent of the hydroxyl groups have been replaced by lower dialkylaminoalkoxy groups, a copolymer of tetraethylene pentamine and epichlorohydrin which contains quaternary ammonium groups or a styrene-divinyl-benzene copolymer containing quaternary ammonium groups. When present in the indicated weight ratios synergism exists between the para-chlorophenoxy isobutyric acid and the anion exchange resins.

Inventors

  • 👤 A Howard

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 11:22
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/74; A61K31/785; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585; A61K9/00; A61K9/48; A61K9/50

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 252 words
A METHOD OF TREATING PATIENTS SUFFERING FROM HYPERCHOLESTEREMIA WHICH COMPRISES THE DAILY ORAL ADMINISTRATION THERETO OF A HYPOCHOLESTEREMIC EFFECTIVE AMOUNT OF A COMPOSITION COMPRISING (A) A COMPOUND SELECTED FROM THE GROUP CONSISTING OF PARA-CHLOROPHENOXYISOBUTYRIC ACID, THE ETHYL ESTER O SAID ACID AND SALTS OF SAID ACID WITH PHARMACOLOGICALLY ACCEPTABLE METALS AND (B) A PHARMACOLOGICALLY ACCEPTABLE GRADE OF A SOLID NON-TOXIC ANION EXCHANGE RESIN IN THE WEIGHT RATIO OF 1:2 TO 1:20, SAID RESIN BEING SELECTED FROM THE GROUP CONSISTING OF (I) THE SOLID COPOLYMER OF DEXTRAN AND EPICHLOROHYDRIN HAVING FROM 10-35 PERCENT OF ITS WEIGHT OF HYDROXYL GROUPS, BASED UPON THE DRY SUBSTANCE, FROM 6-50 PERCENT OF SAID HYDROXYL GROUPS HAVING BEEN REPLACED BY GROUPS OF THE FORMULA RYO- IN WHICH Y IS AN ALKYLENE GROUP HAVING AT LEAST ONE BUT LESS THAN THREE CARBON ATOMS AND R IS A DIALKYLAMINO GROUP HAVING AT LEAST TWO BUT LESS THAN FIVE CARBON ATOMS, SAID COPOLYMER HAVING AN ION EXCHANGE CAPACITY OF 2-6 MILLIEQUIVALENTS PER GRAM OF DRY COMPOUND (II) THE SOLID COPOLYMER OF TETRAETHAYLENE PENTAMINE AND EPICHLOROHYDRIN WHICH HAS BEEN BROUGHT TO A PH OF APPROXIMATELY 4 AND THEN DRIED, AND (III) A SOLID STYRENE-DIVINYLBENZENE COPOLYMER CONTAINING NOT MORE THAN 5 PERCENT BY WEIGHT OF DIVINYL-BENZENE INTO WHICH MORE TERNARY ALKYLAMMONIUM GROUPS CONTAINING NOT MORE THAN 10 CARBON ATOMS HAVE BEEN INTRODUCED, WHICH COPOLYMER HAS AN EQUIVALENT WEIGHT, BASED UPON THE AMMONIUM GROUPS OF LESS THAN 500, SAID ANION EXCHANGE RESINS BEING ADMINISTERED IN AN OVERALL DAILY AMOUNT OF 3 TO 50 GRAMS.
Claim 2
Independent Claim 252 words
A METHOD OF TREATING PATIENTS SUFFERING FROM HYPERCHOLESTEREMIA WHICH COMPRISES THE DAILY ORAL ADMINISTRATION THERETO OF A HYPOCHOLESTEREMIC EFFECTIVE AMOUNT OF A COMPOSITION COMPRISING (A) A COMPOUND SELECTED FROM THE GROUP CONSISTING OF PARA-CHLOROPHENOXYISOBUTYRIC ACID, THE ETHYL ESTER O SAID ACID AND SALTS OF SAID ACID WITH PHARMACOLOGICALLY ACCEPTABLE METALS AND (B) A PHARMACOLOGICALLY ACCEPTABLE GRADE OF A SOLID NON-TOXIC ANION EXCHANGE RESIN IN THE WEIGHT RATIO OF 1:2 TO 1:20, SAID RESIN BEING SELECTED FROM THE GROUP CONSISTING OF (I) THE SOLID COPOLYMER OF DEXTRAN AND EPICHLOROHYDRIN HAVING FROM 10-35 PERCENT OF ITS WEIGHT OF HYDROXYL GROUPS, BASED UPON THE DRY SUBSTANCE, FROM 6-50 PERCENT OF SAID HYDROXYL GROUPS HAVING BEEN REPLACED BY GROUPS OF THE FORMULA RYO- IN WHICH Y IS AN ALKYLENE GROUP HAVING AT LEAST ONE BUT LESS THAN THREE CARBON ATOMS AND R IS A DIALKYLAMINO GROUP HAVING AT LEAST TWO BUT LESS THAN FIVE CARBON ATOMS, SAID COPOLYMER HAVING AN ION EXCHANGE CAPACITY OF 2-6 MILLIEQUIVALENTS PER GRAM OF DRY COMPOUND (II) THE SOLID COPOLYMER OF TETRAETHAYLENE PENTAMINE AND EPICHLOROHYDRIN WHICH HAS BEEN BROUGHT TO A PH OF APPROXIMATELY 4 AND THEN DRIED, AND (III) A SOLID STYRENE-DIVINYLBENZENE COPOLYMER CONTAINING NOT MORE THAN 5 PERCENT BY WEIGHT OF DIVINYL-BENZENE INTO WHICH MORE TERNARY ALKYLAMMONIUM GROUPS CONTAINING NOT MORE THAN 10 CARBON ATOMS HAVE BEEN INTRODUCED, WHICH COPOLYMER HAS AN EQUIVALENT WEIGHT, BASED UPON THE AMMONIUM GROUPS OF LESS THAN 500, SAID ANION EXCHANGE RESINS BEING ADMINISTERED IN AN OVERALL DAILY AMOUNT OF 3 TO 50 GRAMS.
Claim 3
Dependent Claim 24 words
The method of claim 1 in which the weight ratio of said compound to said anion exchange resins is 1:3 to 1:15 by weight.
Claim 4
Dependent Claim 23 words
The method of claim 1 in which the weight ratio of said compound to said anion exchange resin is substantially 1:10 by weight.
Claim 5
Dependent Claim 28 words
The method of claim 1 in which a patient receives of said compound and said anion exchange resin a total weight of 3.0 to 50.0 grams per day.
Claim 6
Dependent Claim 28 words
The method of claim 1 in which a patient receives of said compound and said anion exchange resin a total weight of 10.0 to 25.0 grams per day.
Claim 7
Dependent Claim 12 words
The method of claim 1 in which said compound is ethyl para-chlorophenoxyisobutyrate.
Claim 8
Dependent Claim 12 words
The method of claim 1 in which said compound is aluminium para-chlorophenoxyisobutyrate.
Claim 9
Dependent Claim 218 words
A pharmaceutical composition useful for the treatment of hypercholesteremia comprising, an effective amount of an admixture (a) a compound selected from the group consisting of para-chlorophenoxyisobutyric acid, the ethyl ester of said acid and salts of said acid with pharmacologically acceptable metals and (b) a pharmacologically acceptable grade of a solid non-tOxic anion exchange resin in the weight ratio of 1:2 to 1:20, with resin being selected from the group consisting of (i) the solid copolymer of dextran and epichlorohydrin having from 10-35 percent of its weight of hydroxyl groups, based upon the dry substance, from 6-50 percent of said hydroxyl groups having been replaced by groups of the formula RYO- in which Y is an alkylene group having at least one but less than three carbon atoms and R is a dialkylamino group having at least two but less than five carbon atoms, said copolymer having an ion exchange capacity of 2- 6 milliequivalents per gram of dry compound (ii) the solid copolymer of tetraethylene pentamine and epichlorohydrin which has been brought to a pH of approximately 4 and then dried, and (iii) a solid styrene-divinylbenzene copolymer into which quaternary alkyl-ammonium groups containing not more than 10 carbon atoms have been introduced, which copolymer has an equivalent weight, based upon the ammonium groups of less than 500.
Claim 10
Dependent Claim 218 words
A pharmaceutical composition useful for the treatment of hypercholesteremia comprising, an effective amount of an admixture (a) a compound selected from the group consisting of para-chlorophenoxyisobutyric acid, the ethyl ester of said acid and salts of said acid with pharmacologically acceptable metals and (b) a pharmacologically acceptable grade of a solid non-tOxic anion exchange resin in the weight ratio of 1:2 to 1:20, with resin being selected from the group consisting of (i) the solid copolymer of dextran and epichlorohydrin having from 10-35 percent of its weight of hydroxyl groups, based upon the dry substance, from 6-50 percent of said hydroxyl groups having been replaced by groups of the formula RYO- in which Y is an alkylene group having at least one but less than three carbon atoms and R is a dialkylamino group having at least two but less than five carbon atoms, said copolymer having an ion exchange capacity of 2- 6 milliequivalents per gram of dry compound (ii) the solid copolymer of tetraethylene pentamine and epichlorohydrin which has been brought to a pH of approximately 4 and then dried, and (iii) a solid styrene-divinylbenzene copolymer into which quaternary alkyl-ammonium groups containing not more than 10 carbon atoms have been introduced, which copolymer has an equivalent weight, based upon the ammonium groups of less than 500.
Claim 11
Dependent Claim 25 words
The composition of claim 8 in which said compound and said anion exchange resin are respectively present in the weight ratios of 1:3 to 1:15.
Claim 12
Dependent Claim 24 words
The composition of claim 8 in which said compound and said anion exchange resin are respectively present in the weight ratios of substantially 1:10.
Claim 13
Dependent Claim 12 words
The composition of claim 8 in which said compound is ethyl para-chlorophenoxyisobutyrate.
Claim 14
Dependent Claim 12 words
The composition of claim 8 in which said compound is aluminium para-chlorophenoxyisobutyrate.

References Cited (Backward Citations)

GB860303A Cited
US3042667A Cited
US3277025A Cited
US3308020A Cited
US3383281A Cited
US3627872A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1977-11-04 1978-05-06 1978-11-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1981-11-04 1982-05-06 1982-11-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1985-11-04 1986-05-06 1986-11-05 $7700.00 Window Closed / Lapsed

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