Claims for Patent: 4,452,808
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Summary 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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