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Claims for Patent: 4,452,808

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Claims for Patent: 4,452,808

Title: 4-Aminoalkyl-2(3H)-indolones
Abstract:A series of new chemical compounds which are 4-aminoalkyl-2(3H)-indolones has been demonstrated to be D.sub.2 -agonists useful for treating hypertension. A representative compound of the series is 4-di-n-propylaminoethyl-2(3H)-indolone.
Inventor(s): Gallagher, Jr.; Gregory (Collegeville, PA)
Assignee: Smithkline Beckman Corporation (Philadelphia, PA)
Application Number:06/447,564
Patent Claims: 1. A compound of the structural formula: ##STR4## in which: R is amino, C.sub.1-6 -lower alkylamino, di-(C.sub.1-6 -lower alkyl)amino, allylamino, diallylamino, N-(C.sub.1-6 -lower alkyl)-N-allylamino, benzylamino, dibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethyl amino or di-(4-hydroxyphenethyl)amino, and

R.sup.1, R.sup.2 and R.sup.3 are, each, hydrogen or C.sub.1-4 -lower alkyl; or a pharmaceutically acceptable, acid addition salt thereof.

2. The compound of claim 1 in which R.sup.1, R.sup.2 and R.sup.3 are hydrogen, n is 2 and R is amino, di-n-propylamino, n-propyl-n-butylamino or 4-hydroxyphenethylamino.

3. The compound of claim 1 being 4-(2-di-n-propylaminoethyl)-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.

4. The compound of claim 1 being 4-(2-di-n-propylaminoethyl)-2(3H)-indolone as the free base.

5. The compound of claim 1 being 4-(2-di-n-propylaminoethyl)-2(3H)-indolone hydrochloride.

6. The compound of claim 1 being 4-(2-aminoethyl)-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.

7. The compound of claim 1 being 4-(4-hydroxyphenethylaminoethyl-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.

8. A pharmaceutical composition having D.sub.2 receptor agonist activity comprising a nontoxic, agonist quantity of a compound of the structural formula: ##STR5## in which: R is amino, C.sub.1-6 -lower alkylamino, di-(C.sub.1-6 -lower alkyl)amino, allylamino, diallylamino, N-(C.sub.1-6 -lower alkyl)-N-allylamino, benzylamino, bibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethylamino or di-(4-hydroxyphenethyl)amino, and

R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or C.sub.1-4 -lower alkyl; or a pharmaceutically acceptable acid addition salt thereof, in dosage unit form, combined with a pharmaceutical carrier.

9. The composition of claim 8 in which the D.sub.2 -agonist compound is 4-(2-di-n-propylaminoethyl)-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.

10. The composition of claim 8 in which the D.sub.2 -agonist compound is 4-(2-di-n-propylaminoethyl)-2(3H)-indolone hydrochloride.

11. The composition of claim 8 in dosage unit form adapted for use as an antihypertensive composition.

12. The composition of claim 8 in which the quantity per dosage unit is selected from the range of 50-500 mg base weight of said compound.
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