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Claims for Patent: 3,862,321

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Claims for Patent: 3,862,321

Title: ACYL XYLIDIDE LOCAL ANAESTHETICS
Abstract:The 2-alkyl-2-alkylamino-2',6'-acetoxylidide compounds are useful as long lasting local anaesthetics.
Inventor(s): Adams; Herbert John Frederich (Worcester, MA), Kronberg; George Herbert (Worcester, MA), Takman; Bertil Herbert (Worcester, MA)
Assignee: Astra Pharmaceutical Products, Inc. (Worcester, MA)
Application Number:05/447,680
Patent Claims: 1. A local anesthetic composition comprising (a) as its active ingredient a compound having the structural formula ##SPC13##

wherein R.sup.1 is ethyl, propyl or butyl; R.sup.2 and R.sup.3 are each separately selected from the group consisting of methyl, ethyl, propyl and butyl; R.sup.2 together with R.sup.3 is tetramethylene; the total sum of carbon atoms in R.sup.1, R.sup.2 and R.sup.3 is at least six; or a pharmaceutically acceptable salt thereof in an effective amount sufficient to provide local anesthetic effect, together with (b) a nontoxic pharmaceutically acceptable carrier.

2. The composition as defined by claim 1 wherein the active ingredient is 2-diethylamino-2',6'-n-butyroxylidide.

3. The composition as defined by claim 1 wherein the active ingredient is 2-(N-ethyl-n-propylamino)-2',6'-n-butyroxylidide.

4. The composition as defined by claim 1 wherein the active ingredient is 2-diethylamino-2',6'-n-valeroxylidide.

5. The composition as defined by claim 1 wherein the active ingredient is 2-pyrrolidino-2',6'-n-butyroxylidide.

6. The composition as defined by claim 1 wherein the active ingredient is 2-(N-ethyl-n-butylamino)-2',6'-n-butyroxylidide.

7. The composition as defined by claim 1 wherein the active ingredient is 2-dimethylamino-2',6'-caproylxylidide.

8. The composition as defined by claim 1 wherein the active ingredient is 2-pyrrolidino-2',6'-n-valeroxylidide.

9. A method of inducing local anesthesia in animals, which comprises applying to the area of the body to be anesthetized a locally anesthetizing amount of a compound having the structural formula ##SPC14##

wherein R.sup.1 is ethyl, propyl or butyl; R.sup.2 and R.sup.3 are each separately selected from the group consisting of methyl, ethyl, propyl and butyl; R.sup.2 together with R.sup.3 is tetramethylene; the total sum of carbon atoms in R.sup.1, R.sup.2 and R.sup.3 is at least six; or a pharmaceutically acceptable salt thereof.

10. The method as defined by claim 9 wherein said compound is 2-diethylamino-2',6'-n-butyroxylidide.

11. The method as defined by claim 9 wherein said compound is 2-(N-ethyl-n-propylamino)-2',6'-n-butyroxylidide.

12. The method as defined by claim 9 wherein said compound is 2-diethylamino-2',6'-n-valeroxylidide.

13. The method as defined by claim 9 wherein said compound is 2-pyrrolidino-2',6'-n-butyroxylidide.

14. The method as defined by claim 9 wherein said compound is 2-(N-ethyl-n-butylamino)-2',6'-butyroxylidide.

15. The method as defined by claim 9 wherein said compound is 2-dimethylamino-2',6'-caproylxylidide.

16. The method as defined by claim 9 wherein said compound is 2-pyrrolidino-2',6'-n-valeroxylidide.
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