US4153728A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Phenoxyalkylcarboxylic acid compounds and therapeutic compositions
Assignee: Roche Diagnostics GmbH
•
Filing: 1976-10-18
•
Granted: 1979-05-08
•
Expires: 1996-10-18
Abstract
Abstract Novel phenoxyalkylcarboxylic acid compounds of the formula <IMAGE> (I) wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms; N IS 1 OR 2 AND R1, R2 and R3 are hydrogen or lower alkyl; and the pharmacologically compatible salts thereof; have been found to be outstandingly effective in lowering the serum lipid level and the cholesterol level in mammals without inducing undesired side effects and to possess excellent thrombocyte-aggregation inhibiting activity.
Inventors
- 👤 Hans P. Wolff
- 👤 Ernst-Christian Witte
- 👤 Max Thiel
- 👤 Harald Stork
- 👤 Egon Roesch
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 00:45
CPC Classifications
C; C07; C07C; C07C229/00; C07C229/02; C07C229/34; C07C229/36; A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K31/21; A61K31/215; A61K31/22; C07C235/00; C07C235/02; C07C235/32; C07C235/42; C07C235/44; C07C2601/00; C07C2601/12; C07C2601/14
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
63 words
Phenoxyalkylcarboxylic acid compound of the formula: ##STR6## wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms; n is 1 or 2 and R 1 , r 2 and R 3 , which can be the same or different, are hydrogen atoms or lower alkyl; and the pharmacologically compatible salts thereof.
Claim 2
Dependent Claim
63 words
Phenoxyalkylcarboxylic acid compound of the formula: ##STR6## wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms; n is 1 or 2 and R 1 , r 2 and R 3 , which can be the same or different, are hydrogen atoms or lower alkyl; and the pharmacologically compatible salts thereof.
Claim 3
Dependent Claim
14 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein B is a valency bond.
Claim 4
Dependent Claim
20 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein B is a hydrocarbon radical of up to 3 carbon atoms.
Claim 5
Dependent Claim
18 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein B is alkylene of up to 3 carbon atoms.
Claim 6
Dependent Claim
18 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein B is alkenylene of up to 3 carbon atoms.
Claim 7
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein n is 1.
Claim 8
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein n is 2.
Claim 9
Dependent Claim
23 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein at least one of R 1 , R 2 and R 3 is hydrogen.
Claim 10
Dependent Claim
24 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein at least one of R 1 , R 2 and R 3 is lower alkyl.
Claim 11
Dependent Claim
11 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 2-{4-(2-[3-(3,5-di-tert.-butyl-4-hydroxyphenyl)-propionylamino]-ethyl)-phenoxy}-2-methylpropionic acid.
Claim 12
Dependent Claim
11 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 2-{4-[2-(3,5-di-tert.-butyl-4-hydroxyphenyl-α-methylacetamino)-ethyl]-phenoxy}-2-methylpropionic acid.
Claim 13
Dependent Claim
11 words
Phenylalkylcarboxylic acid compound as claimed in claim 1 designated 2-{4-[2-{3-(3,5-di-tert.-butyl-4-hydroxyphenyl)-acryloylamino}-ethyl]-phenoxy}-2-methylpropionic acid.
Claim 14
Dependent Claim
11 words
Phenylalkylcarboxylic acid compound as claimed in claim 1 designated 2-{4-[3-(3,5-di-tert.-butyl-4-hydroxyphenyl)-propionylaminomethyl]-phenoxy}-2-methylpropionic acid.
Claim 15
Dependent Claim
11 words
Phenylalkylcarboxylic acid compound as claimed in claim 1 designated 2-{4-[2-(3,5-di-tert.-butyl-4-hydroxybenzoylamino)-ethyl]-phenoxy}-acetic acid.
Claim 16
Dependent Claim
36 words
Therapeutic compositions for lowering the serum lipid and/or cholesterol level and for inhibiting thrombocyte aggregation in mammals comprising a pharmocologically acceptable carrier and, in therapeutically effective amounts, a phenoxyalkylcarboxylic acid compound as claimed in claim 1.
Claim 17
Dependent Claim
34 words
Method for lowering the serum lipid and/or cholesterol level and for inhibiting thrombocyte aggregation in mammals which method comprises administering thereto an effective amount of a phenoxyalkylcarboxylic acid compound as claimed in claim 1.
Claim 18
Dependent Claim
20 words
Method as claimed in claim 16 wherein said compound is applied at a dosage of about 30 mg/kg per day.
Claim 19
Dependent Claim
29 words
Method as claimed in claim 16 wherein said compound is at least one selected from the group consisting of: 2-{4-(2-[3-(3,5-di-tert.-butyl-4-hydroxyphenyl)-propionylamino]-ethyl)-phenoxy}-2-methylpropionic acid 2-{4-[2-(3,5-di-tert.-butyl-4-hydroxyphenyl-α-methylacetamino)-ethyl]-phenoxy}-2-methylpropionic acid 2-{4-[2-{3-(3,5-di-tert.-butyl-4-hydroxyphenyl)-acryloylamino}-ethyl]-phenoxy}-2-methylpropionic acid 2-{4-[3-(3,5-di-tert.-butyl-4-hydroxyphenyl)-propionylaminomethyl]-phenoxy}-2-methylpropionic acid 2-{4-[2-(3,5-di-tert.-butyl-4-hydroxybenzoylamino)-ethyl]-phenoxy}-acetic acid.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-05-07 | 1982-11-06 | 1983-05-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-05-07 | 1986-11-06 | 1987-05-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-05-07 | 1990-11-06 | 1991-05-08 | $7700.00 | Window Closed / Lapsed |