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Details for Patent: 4,588,740

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Details for Patent: 4,588,740

Title: Pharmaceutical methods using 4-aminoalkyl-2(3H)-indolones
Abstract:A series of pharmaceutical compositions which contain 4-aminoalkyl-2(3H)-indolones has been demonstrated to have D.sub.2 -agonist activity useful for treating congestive heart failure and hypertension. A representative ingredient of the compositions is 4-di-n-propylaminoethyl-2(3H)-indolone or a salt thereof.
Inventor(s): Gallagher, Jr.; Gregory (Jeffersonville, PA)
Assignee: SmithKline Beckman Corporation (Philadelphia, PA)
Filing Date:Apr 05, 1984
Application Number:06/597,006
Claims:1. The method of treating hypertension, angina pectoris, congestive heart failure or kidney dysfunction by inducing D.sub.2 -receptor agonist activity comprising administering orally, rectally or parenterally to a patient subject to one of these abnormal conditions a nontoxic, active therefor quantity of a compound of the structural formula; ##STR4## in which: R is, each, hydrogen, lower alkyl, benzyl, allyl, phenethyl or 4-hydroxyphenethyl;

R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or C.sub.1-4 -lower alkyl; and

n is 1, 2 or 3; or a pharmaceutically acceptable acid addition salt thereof, in dosage unit form, combined with a pharmaceutical carrier.

2. The method of claim 1 in which the compound is 4-(2-di-n-propylaminoethyl)-2(3H)-indolone or a pharmaceutically active acid addition salt thereof.

3. The method of claim 1 in which the compound is 4-(2-di-n-propylaminoethyl)-2(3H)-indolone hydrochloride.

4. The method of claim 8 in which the compound is 4-[N-n-propyl-N-(4-hydroxyphenethyl)-2-aminoethyl]-2-(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.

5. The method of claim 1 in which the compound is administered orally or parenterally from 1 to 5 times daily in the form of a dosage unit containing a quantity of the compound selected from the range of 50-500 mg.

6. The method of claim 5 in which a quantity selected from 75-250 mg per dosage unit is administered from 1-5 times daily.

7. The method of claim 1 in which R.sup.1, R.sup.2 and R.sup.3 are each hydrogen.

8. The method of claim 6 in which the patient is hypertensive.

9. The method of claim 6 in which the patient has angina pectoris.

10. The method of claim 6 in which the patient has the symptoms of congestive heart failure.

11. 4-[N-n-Propyl-N-(4-hydroxyphenethyl)-2-aminoethyl]-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.

12. The compound of claim 11 as the hydrochloride salt.

13. The compound of claim 11 as the methanesulfonic acid salt.
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