US4027009A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Compositions and methods for depressing blood serum cholesterol
Assignee: Merck and Co Inc
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Filing: 1974-04-23
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Granted: 1977-05-31
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Expires: 1994-04-23
Abstract
Abstract The invention disclosed herein relates to novel unit dosage compositions comprising 0.1 to 10.0 grams of quaternary poly[(alkylimino)alkylene] linear polymers free from cross-linking, which compositions are valuable as bile acid binding agents; and the invention also relates to the method of binding bile acids by orally administering such compositions.
Inventors
- 👤 Nathaniel Grier
- 👤 Merwin F. Hoover
- 👤 Jesse W. Huff
- 👤 Gunther W. Kuron
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 22:49
CPC Classifications
C; C08; C08G; C08G73/00; C08G73/02; C08G73/0206; C08G73/0213; C08G73/0226; A; A61; A61K; A61K31/00; A61K31/74; A61K31/785
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
170 words
A method for lowering mammalian blood serum cholesterol levels and binding bile acids in the gastrointestinal tract comprising orally administering an effective bile acid binding dose of a polymer having linear backbone which is neither branched nor crosslinked of the structure: ##STR6## wherein Q is (CH 2 ) x and W is (CH 2 ) y and, when x is the integer 2, y is an integer of from 4 to 8 inclusive, and when x is an integer of from 3 to 8 inclusive, y is an integer of from 3 to 8 inclusive; or Q and W are C 3 to C 8 hydroxy substituted straight or branched chain alkylene groups wherein the hydroxy substituent is on a carbon atom other than one bonded directly to nitrogen; R is C 1 to C 4 alkyl; Z is a physiologically acceptable anion; T 1 and T 2 are terminal groups, and n is an integer within a range such that molecular weight of the polymer is 1,500 to 70,000.
Claim 2
Independent Claim
170 words
A method for lowering mammalian blood serum cholesterol levels and binding bile acids in the gastrointestinal tract comprising orally administering an effective bile acid binding dose of a polymer having linear backbone which is neither branched nor crosslinked of the structure: ##STR6## wherein Q is (CH 2 ) x and W is (CH 2 ) y and, when x is the integer 2, y is an integer of from 4 to 8 inclusive, and when x is an integer of from 3 to 8 inclusive, y is an integer of from 3 to 8 inclusive; or Q and W are C 3 to C 8 hydroxy substituted straight or branched chain alkylene groups wherein the hydroxy substituent is on a carbon atom other than one bonded directly to nitrogen; R is C 1 to C 4 alkyl; Z is a physiologically acceptable anion; T 1 and T 2 are terminal groups, and n is an integer within a range such that molecular weight of the polymer is 1,500 to 70,000.
Claim 3
Dependent Claim
26 words
A method according to claim 1 where said physiologically acceptable anion 2 is chloride, bromide, iodide, carbonate, acetate, ascorbate, palmitate, stearate, benzoate, nicotinate, salicylate or hydroxycitrate.
Claim 4
Dependent Claim
27 words
A method according to claim 1 in which each R is methyl and Q is (CH 2 ) x and W is (CH 2 ) y .
Claim 5
Dependent Claim
11 words
A method according to claim 1 in which Z is halide.
Claim 6
Dependent Claim
11 words
A method according to claim 1 in which Z is ascorbate.
Claim 7
Dependent Claim
18 words
A method according to claim 3 in which x is 3, y is 3, and Z is chloride.
Claim 8
Dependent Claim
174 words
A composition for binding bile acid in the gastrointestinal tract of mammals comprising in unit does form from 0.1 to 10.0 grams of a polymer having linear backbone which is neither branched nor crosslinked of the structure: ##STR7## wherein Q is (CH 2 ) x and W is (CH 2 ) y and, when x is the integer 2, y is an integer of from 4 to 8 inclusive, and when x is an integer of from 3 to 8 inclusive, y is an integer of from 3 to 8 inclusive; or Q and W are C 3 to C 8 hydroxy substituted straight or branched chain alkylene groups wherein the hydroxy substituent is on a carbon atom other than one bonded directly to nitrogen; R is C 1 to C 4 alkyl; Z is a physiologically acceptable anion; T 1 and T 2 are terminal groups; and n is an integer within a range such that molecular weight of the polymer is 1,500 to 70,000, and a said non-toxic physiologically acceptable pharmaceutical carrier.
Claim 9
Dependent Claim
174 words
A composition for binding bile acid in the gastrointestinal tract of mammals comprising in unit does form from 0.1 to 10.0 grams of a polymer having linear backbone which is neither branched nor crosslinked of the structure: ##STR7## wherein Q is (CH 2 ) x and W is (CH 2 ) y and, when x is the integer 2, y is an integer of from 4 to 8 inclusive, and when x is an integer of from 3 to 8 inclusive, y is an integer of from 3 to 8 inclusive; or Q and W are C 3 to C 8 hydroxy substituted straight or branched chain alkylene groups wherein the hydroxy substituent is on a carbon atom other than one bonded directly to nitrogen; R is C 1 to C 4 alkyl; Z is a physiologically acceptable anion; T 1 and T 2 are terminal groups; and n is an integer within a range such that molecular weight of the polymer is 1,500 to 70,000, and a said non-toxic physiologically acceptable pharmaceutical carrier.
Claim 10
Dependent Claim
27 words
A composition according to claim 7 in which each R is methyl and Q is (CH 2 ) x and W is (CH 2 ) y .
Claim 11
Dependent Claim
11 words
A composition according to claim 7 in which Z is halide.
Claim 12
Dependent Claim
37 words
A composition according to claim 7 in which each R is methyl, Q is (CH 2 ) x , W is (CH 2 ) y , X is 3, Y is 3, and each Z is chloride.
Claim 13
Dependent Claim
10 words
A composition according to claim 8 wherein Z is 3-trifluoromethylphenoxy-(4-chlorophenyl)acetate.
Claim 14
Dependent Claim
10 words
A composition according to claim 8 wherein Z is 2-(p-chlorophenoxy)-2-methylpropionate.
Claim 15
Dependent Claim
10 words
A composition according to claim 8 wherein Z is ascorbate.
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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) | 1980-05-30 | 1980-11-29 | 1981-05-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-05-30 | 1984-11-29 | 1985-05-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-05-30 | 1988-11-29 | 1989-05-31 | $7700.00 | Window Closed / Lapsed |