US3973024A
Expired / Lapsed
US
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Analgesic and anti-inflammatory anilino-phenylacetic acid-(2,3 or 4 pyridyl)-methyl esters and derivatives
Assignee: Novartis Corp
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Filing: 1975-04-28
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Granted: 1976-08-03
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Expires: 1995-04-28
Abstract
Abstract Basic esters and acid addition salts thereof of substituted o-anilino-phenylacetic acids with pyridinols or pyridine-alkanols have anti-inflammatory and analgesic activity; they are active ingredients of pharmaceutical compositions and can be used for the relief and removal of pain as well as for the treatment of rheumatic, arthritic and other inflammatory complaints; an illustrative example is [o-(2,6-Dichloro-anilino)-phenyl]-acetic acid (2-pyridyl)-methyl ester.
Inventors
- 👤 Georges Haas
- 👤 Alfred Sallmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 19:21
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/63; C07D213/65; A; A61; A61K; A61K8/00; A61K8/18; A61K8/30; A61K8/49; A61K8/4906; A61K8/4926; A61Q; A61Q17/00; A61Q17/04; C07D213/24; C07D213/28; C07D213/30
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
143 words
A pharmaceutical anti-inflammatory and analgesic preparation, comprising an anti-inflammatory and analgesically effective amount of an ester of the formula ##SPC5## in which R 1 represents lower alkyl, lower alkoxy, halogen up to and including atomic number 35 or trifluoromethyl, R 2 represents hydrogen or a substituent corresponding to the definition of R 1 , R 3 represents hydrogen, lower alkyl, lower alkoxy, halogen up to and including atomic number 35, R 4 represents hydrogen, lower alkyl, lower alkoxy, halogen up to and including atomic number 35 or trifluoromethyl, R 5 represents hydrogen, lower alkyl or benzyl, A represents a direct bond, lower alkylene or lower alkylidene and Py represents unsubstituted, lower alkyl-substituted or lower alkoxy-substituted pyridyl, wherein "lower" denotes said straight-chain radicals with up to 4 carbon atoms; the N-oxide or a pharmacologically tolerable acid addition salt thereof, together with a pharmaceutical excipient.
Claim 2
Dependent Claim
143 words
A pharmaceutical anti-inflammatory and analgesic preparation, comprising an anti-inflammatory and analgesically effective amount of an ester of the formula ##SPC5## in which R 1 represents lower alkyl, lower alkoxy, halogen up to and including atomic number 35 or trifluoromethyl, R 2 represents hydrogen or a substituent corresponding to the definition of R 1 , R 3 represents hydrogen, lower alkyl, lower alkoxy, halogen up to and including atomic number 35, R 4 represents hydrogen, lower alkyl, lower alkoxy, halogen up to and including atomic number 35 or trifluoromethyl, R 5 represents hydrogen, lower alkyl or benzyl, A represents a direct bond, lower alkylene or lower alkylidene and Py represents unsubstituted, lower alkyl-substituted or lower alkoxy-substituted pyridyl, wherein "lower" denotes said straight-chain radicals with up to 4 carbon atoms; the N-oxide or a pharmacologically tolerable acid addition salt thereof, together with a pharmaceutical excipient.
Claim 3
Dependent Claim
86 words
A composition as claimed in claim 1, wherein R 1 is in the 2-position of the anilino group and has the meaning chlorine or methyl, R 2 is in the 3- or 6-position and is hydrogen, chlorine or methyl, R 3 denotes hydrogen or, if R 2 is in the 6-position, also denotes a 3-methyl group, each of R 4 and R 5 represents hydrogen, A is a direct bond or methylene, ethylene, ethylidene, 1,2- or 1,3-propylene or 1,1-propylidene and Py is 2-, 3- or 4-pyridyl.
Claim 4
Dependent Claim
16 words
A composition as claimed in claim 1, in which the ester is [o-(2,6-dichloro-anilino)-phenyl]-acetic acid (2-pyridyl)-methyl ester.
Claim 5
Dependent Claim
24 words
A composition as claimed in claim 1, in which the ester is [o-(3-methyl-(2,6-dichloro-anilino)-phenyl]-acetic acid (2-pyridyl)-methyl ester or a pharmacologically tolerable acid addition salt thereof.
Claim 6
Dependent Claim
24 words
A composition as claimed in claim 1, in which the ester is [o-(2,6-dichloro-anilino)-phenyl]-acetic acid (3-pyridyl)-methyl ester or a pharmacologically tolerable acid addition salt thereof.
Claim 7
Dependent Claim
24 words
A composition as claimed in claim 1, in which the ester is [o-(2,6-dichloro-anilino)-phenyl]-acetic acid (4-pyridyl)-methyl ester or a pharmacologically tolerable acid addition salt thereof.
Claim 8
Dependent Claim
24 words
A composition as claimed in claim 1, in which the ester is [o-(2,6-dichloro-anilino)-phenyl]-acetic acid 2-(2-pyridyl)-ethyl ester or a pharmacologically tolerable acid addition salt thereof.
Claim 9
Dependent Claim
23 words
A composition as claimed in claim 1, in which the ester is [o-(2,6-dichloro-anilino)-phenyl]-acetic acid-3-pyridyl ester or a pharmacologically tolerable acid addition salt thereof.
Claim 10
Dependent Claim
30 words
A method for producing an anti-inflammatory effect in a mammal in need thereof, which comprises administering to said mammal an anti-inflammatory effective amount of a composition claimed in claim 1.
Claim 11
Dependent Claim
31 words
A method for producing an analgesic effect in a mammal in need thereof, which comprises administering to said mammal an analgesically effective amount of a composition as claimed in claim 1.
References Cited (Backward Citations)
US3557129A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-08-03 | 1980-02-02 | 1980-08-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-08-03 | 1984-02-02 | 1984-08-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-08-03 | 1988-02-02 | 1988-08-03 | $7700.00 | Window Closed / Lapsed |