Patent US4258058A successfully refreshed from Google Patents.
US4258058A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Phenoxyalkylcarboxylic acid compounds and thrombocyte-aggregation inhibition
Assignee: Roche Diagnostics GmbH
•
Filing: 1979-02-26
•
Granted: 1981-03-24
•
Expires: 1999-02-26
Abstract
Abstract Phenoxyalkylcarboxylic acid compounds of the formula <IMAGE> wherein R is hydrogen or lower alkyl R1 is alkyl or aryl, aralkyl or aralkenyl radical, the aryl moiety of which can be substituted one or more times by halogen, hydroxyl, trifluoromethyl or lower alkyl, alkoxy or acyl R2 and R3 are individually selected from hydrogen or lower alkyl, and n is 0, 1, 2 or 3 and the physiologically acceptable salts, esters and amides thereof; are outstandingly effective in inhibiting thrombocyte aggregation.
Inventors
- 👤 Ernst-Christian Witte
- 👤 Hans P. Wolff
- 👤 Max Thiel
- 👤 Karlheinz Stegmeier
- 👤 Egon Roesch
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 06:12
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/44; C07D209/48; A; A61; A61P; A61P3/00; A61P3/06; A61P7/00; A61P7/02
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
123 words
Phenoxyalkylcarboxylic acid compound of the formula ##STR10## wherein R is hydrogen or lower alkyl of up to 6 carbon atoms R 1 is aryl, aralkyl or aralkenyl wherein the aryl moiety contains from 6 to 14 carbon atoms, and the alkyl or alkenyl moiety contains up to 5 carbon atoms and wherein said aralkyl and aralkenyl is optionally substituted with at least one substituent selected from halogen, hydroxyl, trifluoromethyl, alkyl or alkoxy of up to 5 carbon atoms, and alkanoyl of up to 5 carbon atoms R 2 and R 3 are individually selected from hydrogen or lower alkyl of up to 6 carbon atoms, and n is 0, 1, 2 or 3 or the physiologically acceptable salt or lower alkyl ester thereof.
Claim 2
Dependent Claim
123 words
Phenoxyalkylcarboxylic acid compound of the formula ##STR10## wherein R is hydrogen or lower alkyl of up to 6 carbon atoms R 1 is aryl, aralkyl or aralkenyl wherein the aryl moiety contains from 6 to 14 carbon atoms, and the alkyl or alkenyl moiety contains up to 5 carbon atoms and wherein said aralkyl and aralkenyl is optionally substituted with at least one substituent selected from halogen, hydroxyl, trifluoromethyl, alkyl or alkoxy of up to 5 carbon atoms, and alkanoyl of up to 5 carbon atoms R 2 and R 3 are individually selected from hydrogen or lower alkyl of up to 6 carbon atoms, and n is 0, 1, 2 or 3 or the physiologically acceptable salt or lower alkyl ester thereof.
Claim 3
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein R is hydrogen.
Claim 4
Dependent Claim
39 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein R 1 is aryl, aralkyl or aralkenyl wherein the aryl moiety contains from 6 to 14 carbon atoms, and the alkyl or alkenyl moiety contains up to 5 carbon atoms.
Claim 5
Dependent Claim
49 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein R 1 is substituted aryl, aralkyl or aralkenyl wherein the substituent is on the aryl moiety and is selected from halogen, hydroxyl, trifluoromethyl, alkyl or alkoxy of up to 5 carbon atoms and alkanoyl of up to 5 carbon atoms.
Claim 6
Dependent Claim
18 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein one of R 2 and R 3 is hydrogen.
Claim 7
Dependent Claim
24 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein one of R 2 and R 3 is alkyl of up to 6 carbon atoms.
Claim 8
Dependent Claim
18 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein both of R 2 and R 3 are hydrogen.
Claim 9
Dependent Claim
24 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein both of R 2 and R 3 are alkyl of up to 6 carbon atoms.
Claim 10
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein n is 0.
Claim 11
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein n is 1.
Claim 12
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein n is 2.
Claim 13
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 wherein n is 3.
Claim 14
Dependent Claim
11 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 4-[2-(phenylsulfonylamino)-ethyl]-phenoxyacetic acid.
Claim 15
Dependent Claim
12 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 4-[2-(phenylsulfonylamino)-ethyl]-phenoxyacetic acid-isopropyl ester.
Claim 16
Dependent Claim
11 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 4-[2-(4-fluorophenylsulfonylamino)-ethyl]-phenoxyacetic acid.
Claim 17
Dependent Claim
11 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 4-[2-(1-naphthalenesulfonylamino)-ethyl]-phenoxyacetic acid.
Claim 18
Dependent Claim
11 words
Phenoxyalkylcarboxylic acid compound as claimed in claim 1 designated 4-[3-(phenylsulfonylamino)-propyl]-phenoxyacetic acid.
Claim 19
Dependent Claim
25 words
Composition for inhibiting thrombocyte aggregation which composition comprises a pharmacologically acceptable carrier and, in effective amounts, a phenoxyalkylcarboxylic acid compound as claimed in claim 1.
Claim 20
Dependent Claim
28 words
Method for inhibiting thrombocyte aggregation in an afflicted host which method comprises administering to such host effective amounts of a phenoxyalkylcarboxylic acid compound as claimed in claim 1.
Claim 21
Dependent Claim
27 words
Method as claimed in 19 wherein said phenoxyalkylcarboxylic acid compound is selected from 4-[2-(phenylsulfonylamino)-ethyl]-phenoxyacetic acid 4-[2-(phenylsulfonylamino)-ethyl]-phenoxyacetic acid-isopropyl ester 4-[2-(4-fluorophenylsulfonylamino)-ethyl]-phenoxyacetic acid 4-[2-(1-naphthalenesulfonylamino)-ethyl]-phenoxyacetic acid 4-[2-phenylsulfonylamino)-ethyl]-phenoxyacetic acid-(2-ethoxycarbonylethylamide), and 4-[3-(phenylsulfonylamino)-propyl]-phenoxyacetic acid.
References Cited (Backward Citations)
US3364249A
Cited
US3402198A
Cited
US3652646A
Cited
US3549689A
Cited
US3629320A
Cited
US3720709A
Cited
US4112236A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-03-23 | 1984-09-22 | 1985-03-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-03-23 | 1988-09-22 | 1989-03-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-03-23 | 1992-09-22 | 1993-03-24 | $7700.00 | Window Closed / Lapsed |