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US4551475A Expired / Lapsed US ⏱️ 0.0 years remaining

Pharmaceutical preparations for topical application which contain salts of alkanecarboxylic acids

Assignee: Novartis Corp
•
Filing: 1983-07-27
•
Granted: 1985-11-05
•
Expires: 2003-07-27
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Abstract

Abstract The invention relates to pharmaceutical preparations for topical application which contain salts of alkanecarboxylic acids, in particular compounds of the formula ##STR1## wherein R 1 is a group of the formula ##STR2## wherein X 1 and X 2 are hydrogen and X 3 is isobutyl, or X 1 and X 3 are hydrogen and X 2 is benzoyl, or X 1 is hydrogen, X 2 is chlorine, and X 3 is 3-pyrrolin-1-yl, or X 1 is hydrogen, X 2 is a group of the formula --CH═CH--C(OCH 3 )═CH--X 4 , and X 3 together with X 4 are a bond, and R 2 is methyl, or X 2 and X 3 are hydrogen and X 1 is 2,6-dichloroanilino, and R 2 is hydrogen, or R 1 is a group of the formula ##STR3## wherein X 5 is the common bond with the methine group in formula I, X 6 and X 7 are hydrogen, X 8 is p-methylbenzoyl, Y is a nitrogen atom, and X 9 is a methyl group, or X 5 is a methyl group, X 6 is a common bond with the methine group in formula I, X 7 is a group of the formula --CH═C(OCH 3 )--CH═CH--X 10 , X 8 together with X 10 are a bond, Y is a nitrogen atom and X 9 is p-chlorobenzoyl, or X 5 is a methyl group, X 6 is the common bond with the methine group in formula I, X 7 is a group of the formula --CH═C(F)--CH═CH--X 11 , X 8 together with X 11 are a bond, Y is a carbon atom and X 9 is (p-methanesulfinylphenyl)methylene, and R 2 is hydrogen, and each of R 3 , R 4 and R 5 independently is hydrogen, an aliphatic radical, or two of R 3 , R 4 and R 5 together are a bivalent aliphatic radical, unsubstituted or substituted or interrupted by aza, oxa or thia, with the proviso that at least one of R 3 , R 4 and R 5 is different from hydrogen, optionally in the form of an isomer, together with conventional carriers and/or excipients for topical application. The invention also relates to the production of these preparations and also to novel compounds of the formula I and a process for their production. The compounds of the formula I are suitable for use an anti-inflammatory agents and/or analgesics for topical application.

Inventors

  • 👤 Theodor Eckert

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-31 04:21
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/02; C07D295/027; A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K31/205; C07C; C07C57/00; C07C57/30; C07C57/52; C07C57/58; C07C59/00; C07C59/40; C07C59/58; C07C59/64; C07C59/76; C07C59/84; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/26; C07D209/28

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 218 words
A pharmaceutical preparation for topical application which contains an antiinflammatory and analgesically effective amount of a compound of the formula ##STR15## wherein R 1 is a group of the formula ##STR16## wherein X 1 is hydrogen, X 2 is chlorine, and X 3 is 3-pyrrolin-1-yl, and R 2 methyl, or X 2 and X 3 are hydrogen and X 1 is 2,6-dichloroanilino, and R 2 is hydrogen, and each of R 3 , R 4 and R 5 independently is lower alkyl containing up to and including 4 carbon atoms, or hydroxy-lower alkyl containing up to and including 4 carbon atoms, hydroxy-lower alkyl containing up to and including 4 carbon atoms to or one of the others is lower alkyl containing up to and including 4 carbon atoms, and the third is oligo-hydroxy-lower alkyl, or two of R 3 , R 4 and R 5 are hydrogen and the other is lower alkyl containing up to and including 4 carbon atoms, hydroxy-lower alkyl containing up to and including 4 carbon atoms, oligo-hydroxy-lower alkyl containing up to and including 4 carbon atoms, amino-lower alkyl containing up to and including 4 carbon atoms, or a group of the formula ##STR17## wherein alk is lower alkylene containing up to and including 4 carbon atoms, together with pharmaceutically acceptable carriers and excipients.
Claim 2
Dependent Claim 218 words
A pharmaceutical preparation for topical application which contains an antiinflammatory and analgesically effective amount of a compound of the formula ##STR15## wherein R 1 is a group of the formula ##STR16## wherein X 1 is hydrogen, X 2 is chlorine, and X 3 is 3-pyrrolin-1-yl, and R 2 methyl, or X 2 and X 3 are hydrogen and X 1 is 2,6-dichloroanilino, and R 2 is hydrogen, and each of R 3 , R 4 and R 5 independently is lower alkyl containing up to and including 4 carbon atoms, or hydroxy-lower alkyl containing up to and including 4 carbon atoms, hydroxy-lower alkyl containing up to and including 4 carbon atoms to or one of the others is lower alkyl containing up to and including 4 carbon atoms, and the third is oligo-hydroxy-lower alkyl, or two of R 3 , R 4 and R 5 are hydrogen and the other is lower alkyl containing up to and including 4 carbon atoms, hydroxy-lower alkyl containing up to and including 4 carbon atoms, oligo-hydroxy-lower alkyl containing up to and including 4 carbon atoms, amino-lower alkyl containing up to and including 4 carbon atoms, or a group of the formula ##STR17## wherein alk is lower alkylene containing up to and including 4 carbon atoms, together with pharmaceutically acceptable carriers and excipients.
Claim 3
Dependent Claim 79 words
A pharmaceutical preparation for topical application according to claim 1, which contains a compound of the formula I, wherein each of R 3 , R 4 , and R 5 is independently hydroxy-lower alkyl containing up to and including 4 carbon atoms, or one of R 3 , R 4 and R 5 is hydrogen and the others are lower alkyl containing up to and including 4 carbon atoms, hydroxy-lower alkyl containing up to and including 4 carbon atoms.
Claim 4
Dependent Claim 47 words
A pharmaceutical preparation for topical application according to claim 1, which contains a compound of the formula I, wherein R 1 is a group of the formula (IIa), in which X 1 is 2,6-dichloroanilino and X 2 and X 3 are hydrogen, and R 2 is hydrogen.
Claim 5
Dependent Claim 10 words
A pharmaceutical preparation according to claim 1 which contains diethylammonium-2-(2,6-dichloroanilino)phenylacetate.
Claim 6
Dependent Claim 13 words
A pharmaceutical preparation for topical application according to claim 1 which contains tris-(hydroxymethyl)methylammonium-2-(2,6-dichloroanilino)phenylacetate.
Claim 7
Dependent Claim 13 words
A pharmaceutical preparation for topical application according to claim 1 which contains triethanolammonium-(2,6-dichloroanilino)phenylacetate.
Claim 8
Dependent Claim 13 words
A pharmaceutical preparation for topical application according to claim 1 which contains diethanolammonium-2-(2,6-dichloroanilino)phenylacetate.
Claim 9
Dependent Claim 13 words
A pharmaceutical preparation for topical application according to claim 1 which contains diisopropanolammonium-2-(2,6-dichloroanilino)phenylacetate.
Claim 10
Dependent Claim 13 words
A pharmaceutical preparation for topical application according to claim 1 which contains N-methyl-D-glucammonium-2-(2,6-dichloroanilino)phenylacetate.
Claim 11
Dependent Claim 33 words
A pharmaceutical preparation for topical application according to claim 1 comprising about 0.5% to 5% by weight of a compound of the formula I according to any one of claims 1 to 9.

References Cited (Backward Citations)

US514839A Cited
GB1211134A Cited
US3896157A Cited
US4048330A Cited
US3592902A Cited
USB514839I5 Cited
US3936528A Cited
GB1467528A Cited
CA1095077A Cited
US4346105A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-11-04 1989-05-06 1989-11-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-11-04 1993-05-06 1993-11-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-11-04 1997-05-06 1997-11-05 $7700.00 Window Closed / Lapsed

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