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Details for Patent: 3,978,116

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Details for Patent: 3,978,116

Title: 2-Naphthyl acetic acid derivatives and compositions and methods thereof
Abstract:2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.
Inventor(s): Fried; John H. (Palo Alto, CA), Harrison; Ian T. (Palo Alto, CA)
Assignee: Syntex Corporation (Panama, PM)
Filing Date:Mar 17, 1975
Application Number:05/559,357
Claims:1. The compounds of the formulas: ##SPC9##

wherein one of R.sup.1 and R.sup.2 is hydrogen and the other is difluoromethyl, fluoro, or chloro; or

R.sup.1 and R.sup.2 taken together are alkylidene, halomethylene, or ethylene;

R.sup.3 is trifluoromethyl, difluoromethoxy, alkoxymethyloxy, alkylthio, difluoromethylthio, alkoxymethylthio or alkylthiomethylthio;

R.sup.4 is cycloalkyl, hydroxymethyl, alkoxymethyl, trifluoromethyl, vinyl, ethynyl, alkoxymethyloxy, alkylthiomethylthio, difluoromethoxy, alkoxymethylthio, alkylthiomethyloxy, difluoromethylthio, formyl, carboxy, acetyl, or aryl;

each of R.sup.5 (at position 4, 7, or 8) and R.sup.6 (at position 1, 4, 7, or 8) is alkyl, trifluoromethyl, fluoro, chloro, hydroxy, alkoxy, difluoromethoxy, alkoxymethyloxy, alkylthiomethyloxy, alkylthio, difluoromethylthio, alkoxymethylthio or alkylthiomethylthio; provided that R.sup.5 (when at position 7) is other than alkyl;

R.sup.7 is alkyl, cycloalkyl, hydroxymethyl, alkoxymethyl, trifluoromethyl, vinyl, ethynyl, fluoro, chloro, hydroxy, alkoxy, difluoromethoxy, alkoxymethyloxy, alkylthiomethyloxy, alkylthio, difluoromethylthio, alkoxymethylthio or alkylthiomethylthio, formyl, carboxy, acetyl, or aryl;

each of R.sup.8 and R.sup.9 (at position 1, 4, 7, or 8) is alkyl, fluoro, chloro, hydroxy, alkoxy, difluoromethoxy, alkoxymethyloxy, alkylthiomethyloxy, alkylthio, difluoromethylthio, alkoxymethylthio or alkylthiomethylthio; provided that when one of R.sup.8 and R.sup.9 is hydroxy, alkoxy, difluoromethoxy, alkoxymethyloxy, alkylthiomethyloxy, alkylthio, difluoromethylthio, alkoxymethylthio or alkylthiomethylthio, the other is the identical group or alkyl, fluoro, or chloro;

one of R.sup.10 and R.sup.11 is hydrogen, the other being methyl, ethyl, difluoromethyl, fluoro, or chloro; or

R.sup.10 and R.sup.11 taken together are alkylidene, halomethylene, or ethylene; provided that when one of R.sup.10 or R.sup.11 is methyl or ethyl, R.sup.6 (when at position 1 or 7) is other than alkyl.

2. The compounds according to claim 1 wherein one of R.sup.1 and R.sup.2 is hydrogen and the other is difluoromethyl, fluoro, or chloro; or

R.sup.1 and R.sup.2 taken together are methylene or difluoromethylene;

R.sup.3 is difluoromethoxy, methoxymethyloxy, methylthio, difluoromethylthio, or methoxymethylthio;

R.sup.4 is cyclopropyl, vinyl, ethynyl, trifluoromethyl, difluoromethoxy, methoxymethyloxy, ethoxymethyloxy, n-propoxymethyloxy, difluoromethylthio, or methoxymethylthio;

each of R.sup.5 (at position 4, 7, or 8), R.sup.6 (at position 1, 4, 7, or 8), R.sup.8 and R.sup.9 (at position 1, 4, 7, or 8) is fluoro, chloro, methyl, ethyl, isopropyl, methoxy, methoxymethyloxy, difluoromethoxy, methylthio, difluoromethylthio, or methoxymethylthio; provided that R.sup.5 (when at position 7) is other than methyl, ethyl, or isopropyl; provided that when one of R.sup.8 or R.sup.9 is methoxy, methoxymethyloxy, difluoromethoxy, methylthio, difluoromethylthio, or methoxymethylthio, the other is the identical group or fluoro, chloro, methyl, ethyl, or isopropyl;

R.sup.7 is methyl, ethyl, isopropyl, cyclopropyl, trifluoromethyl, vinyl, ethynyl, fluoro, chloro, methoxy, methoxymethyloxy, difluoromethoxy, methylthio, methoxymethylthio, or difluoromethylthio;

one of R.sup.10 and R.sup.11 is hydrogen, the other being methyl or difluoromethyl; or

R.sup.10 and R.sup.11 taken together are methylene or difluoromethylene; provided that when one of R.sup.10 and R.sup.11 is methyl or ethyl, R.sup.6 (when at position 1 or 7) is other than methyl, ethyl, or isopropyl.

3. The compound of formula XIV according to claim 1 wherein R.sup.7 is methyl; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

4. The compound of formula XIV according to claim 1 wherein R.sup.7 is ethyl; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

5. The compound of formula XIV according to claim 1 wherein R.sup.7 is trifluoromethyl; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

6. The compound of formula XIV according to claim 1 wherein R.sup.7 is fluoro; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

7. The compound of formula XIV according to claim 1 wherein R.sup.7 is chloro; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

8. The compound of formula XIV according to claim 1 wherein R.sup.7 is methoxy; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

9. The compound of formula XIV according to claim 1 wherein R.sup.7 is difluoromethoxy; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

10. The compound of formula XIV according to claim 1 wherein R.sup.7 is methoxymethyloxy; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

11. The compound of formula XIV according to claim 1 wherein R.sup.7 is methylthio; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

12. The compound of formula XIV according to claim 1 wherein R.sup.7 is difluoromethylthio; one of R.sup.10 and R.sup.11 is hydrogen and the other is methyl.

13. The compound of formula XIV according to claim 1 wherein R.sup.7 is methoxy; one of R.sup.10 and R.sup.11 is hydrogen and the other is difluoromethyl.
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