US4452808A
Expired / Lapsed
US
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4-Aminoalkyl-2(3H)-indolones
Assignee: SmithKline Beecham Corp
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Filing: 1982-12-07
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Granted: 1984-06-05
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Expires: 2002-12-07
Abstract
Abstract A series of new chemical compounds which are 4-aminoalkyl-2(3H)-indolones has been demonstrated to be D2-agonists useful for treating hypertension. A representative compound of the series is 4-di-n-propylaminoethyl-2(3H)-indolone.
Inventors
- 👤 Gregory Gallagher, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 15:43
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/02; C07D403/12; A; A61; A61P; A61P43/00; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/32; C07D209/34; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/582
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
59 words
A compound of the structural formula: ##STR4## in which: R is amino, C 1-6 -lower alkylamino, di-(C 1-6 -lower alkyl)amino, allylamino, diallylamino, N-(C 1-6 -lower alkyl)-N-allylamino, benzylamino, dibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethyl amino or di-(4-hydroxyphenethyl)amino, and R 1 , R 2 and R 3 are, each, hydrogen or C 1-4 -lower alkyl; or a pharmaceutically acceptable, acid addition salt thereof.
Claim 2
Dependent Claim
59 words
A compound of the structural formula: ##STR4## in which: R is amino, C 1-6 -lower alkylamino, di-(C 1-6 -lower alkyl)amino, allylamino, diallylamino, N-(C 1-6 -lower alkyl)-N-allylamino, benzylamino, dibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethyl amino or di-(4-hydroxyphenethyl)amino, and R 1 , R 2 and R 3 are, each, hydrogen or C 1-4 -lower alkyl; or a pharmaceutically acceptable, acid addition salt thereof.
Claim 3
Dependent Claim
28 words
The compound of claim 1 in which R 1 , R 2 and R 3 are hydrogen, n is 2 and R is amino, di-n-propylamino, n-propyl-n-butylamino or 4-hydroxyphenethylamino.
Claim 4
Dependent Claim
15 words
The compound of claim 1 being 4-(2-di-n-propylaminoethyl)-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.
Claim 5
Dependent Claim
11 words
The compound of claim 1 being 4-(2-di-n-propylaminoethyl)-2(3H)-indolone as the free base.
Claim 6
Dependent Claim
8 words
The compound of claim 1 being 4-(2-di-n-propylaminoethyl)-2(3H)-indolone hydrochloride.
Claim 7
Dependent Claim
15 words
The compound of claim 1 being 4-(2-aminoethyl)-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.
Claim 8
Dependent Claim
15 words
The compound of claim 1 being 4-(4-hydroxyphenethylaminoethyl-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.
Claim 9
Dependent Claim
82 words
A pharmaceutical composition having D 2 receptor agonist activity comprising a nontoxic, agonist quantity of a compound of the structural formula: ##STR5## in which: R is amino, C 1-6 -lower alkylamino, di-(C 1-6 -lower alkyl)amino, allylamino, diallylamino, N-(C 1-6 -lower alkyl)-N-allylamino, benzylamino, bibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethylamino or di-(4-hydroxyphenethyl)amino, and R 1 , R 2 and R 3 are each hydrogen or C 1-4 -lower alkyl; or a pharmaceutically acceptable acid addition salt thereof, in dosage unit form, combined with a pharmaceutical carrier.
Claim 10
Dependent Claim
82 words
A pharmaceutical composition having D 2 receptor agonist activity comprising a nontoxic, agonist quantity of a compound of the structural formula: ##STR5## in which: R is amino, C 1-6 -lower alkylamino, di-(C 1-6 -lower alkyl)amino, allylamino, diallylamino, N-(C 1-6 -lower alkyl)-N-allylamino, benzylamino, bibenzylamino, phenethylamino, diphenethylamino, 4-hydroxyphenethylamino or di-(4-hydroxyphenethyl)amino, and R 1 , R 2 and R 3 are each hydrogen or C 1-4 -lower alkyl; or a pharmaceutically acceptable acid addition salt thereof, in dosage unit form, combined with a pharmaceutical carrier.
Claim 11
Dependent Claim
22 words
The composition of claim 8 in which the D 2 -agonist compound is 4-(2-di-n-propylaminoethyl)-2(3H)-indolone or a pharmaceutically acceptable, acid addition salt thereof.
Claim 12
Dependent Claim
15 words
The composition of claim 8 in which the D 2 -agonist compound is 4-(2-di-n-propylaminoethyl)-2(3H)-indolone hydrochloride.
Claim 13
Dependent Claim
16 words
The composition of claim 8 in dosage unit form adapted for use as an antihypertensive composition.
Claim 14
Dependent Claim
25 words
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.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-06-05 | 1987-12-05 | 1988-06-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-06-05 | 1991-12-05 | 1992-06-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-06-05 | 1995-12-05 | 1996-06-05 | $7700.00 | Window Closed / Lapsed |