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Claims for Patent: 4,387,103

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Claims for Patent: 4,387,103

Title: Method for treatment or prophylaxis of cardiac disorders
Abstract:A method for the treatment of prophylaxis of cardiac disorders in a mammal, comprising administering to such mammal a short-acting .beta.-blocking compound of the formula: ##STR1## wherein R may be lower alkyl, aryl, or aralkyl; n may be an integer from 0 to about 10; x may be an integer from 1 to 3; Ar may be substituted or unsubstituted aromatic; R.sub.1 may be lower alkyl, or aralkyl; and pharmaceutically accepted salts thereof. Novel compounds possessing short-acting .beta.-adrenergic blocking activity are also disclosed.
Inventor(s): Erhardt; Paul W. (Mundelein, IL), Borgman; Robert J. (Mundelein, IL), O'Donnell; John P. (Morgantown, WV)
Assignee: American Hospital Supply Corporation (Evanston, IL)
Application Number:06/211,345
Patent Claims: 1. A method for the treatment or prophylaxis of cardiac disorders in a mammal, comprising administering by intravenous infusion into a mammal having a critical cardiac illness a .beta.-blocking ester compound of the formula ##STR21## wherein R is lower alkyl or alkenyl of from 1 to about 5 carbon atoms; n is an integer of from 0 to about 3; x is 1 or 2, provided that when x is 2, different occurrences of the ##STR22## group may be the same or different; R.sub.1 is lower alkyl or aralkyl; and Ar is phenyl or naphthyl optionally additionally substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, alkylamino, hydroxy, lower hydroxyalkyl, or cyano; or a pharmaceutically acceptable salt thereof; which .beta.-blocking ester compound is rapidly inactivated in vivo; wherein said .beta.-blocking ester compound is intravenously infused at a rate sufficient to establish an effective .beta.-blockade in said mammal, and said infusion is then terminated to effect a rapid recovery of said mammal from the .beta.-blocking effects of said compound.

2. The method of claim 1, wherein Ar is phenyl.

3. The method of claim 2, wherein x is 1 and the ##STR23## group is in the ortho position with respect to the ##STR24## group.

4. The method of claim 2, wherein n is 2, x is 1 and the ##STR25## group is in the para position with respect to the ##STR26## group.

5. The method of claim 3, wherein n is 0.

6. The method of claim 4, wherein R is a lower alkyl or alkenyl group having from 1 to about 3 carbon atoms, and the optional aromatic substituents are lower alkoxy of from 1 to about 5 carbon atoms, lower alkyl of from 1 to about 5 carbon atoms, halogen or cyano.

7. The method of claim 6, wherein the halogen is fluorine.

8. The method of claim 6, wherein R is methyl or ethyl.

9. The method of claim 6, wherein R is methyl.

10. The method of claim 6, wherein R.sub.1 is lower alkyl of from 1 to about 5 carbon atoms or aralkyl wherein the alkyl portion contains from 1 to about 5 carbon atoms and the aryl portion contains about 6 to 10 carbon atoms.

11. The method of claim 9, wherein R.sub.1 is lower alkyl of from 1 to about 5 carbon atoms or aralkyl wherein the alkyl portion contains from 1 to about 5 carbon atoms and the aryl portion contains from 6 to about 10 carbon atoms.

12. The method of claim 10, wherein R.sub.1 is isopropyl, t-butyl, or 3,4-dimethoxyphenethyl.

13. The method of claim 11, wherein R.sub.1 is isopropyl, t-butyl, or 3,4-dimethoxyphenethyl.

14. The method of claim 13, wherein no optional substituents are on the phenyl group.

15. The method of claim 14, wherein R.sub.1 is isopropyl.

16. The method of claim 2, wherein x is 2, R is methyl or ethyl and R.sub.1 is isopropyl, t-butyl or 3,4-dimethoxyphenethyl.

17. The method of claim 3, wherein R is lower alkyl or alkenyl having from 1 to about 3 carbon atoms and R.sub.1 is isopropyl, t-butyl and 3,4-dimethoxyphenethyl.

18. The method of claim 5, wherein R is methyl and R.sub.1 is isopropyl.

19. The method of claim 5, wherein R is methyl and R.sub.1 is t-butyl.

20. The method of claim 1, 4, 5, 6, 8, 9, 10, 11, 15 or 16, wherein the .beta.-blocking ester compound is intravenously infused at a rate of from about 0.001 to about 100 mg. of compound per kg. of body weight of said mammal per hour.

21. The method of claim 1, 4, 5, 6, 8, 9, 10, 11, 15 or 36, wherein the .beta.-blocking ester compound is intravenously infused at a rate of from about 0.01 to about 10 mg. of compound per kg. of body weight of said mammal per hour.
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