US4554284A
Expired / Lapsed
US
⏱️ 0.0 years remaining
7-(2-Aminoethyl)-1,3-benzthia- or oxa-zol-2(3H)-ones
Assignee: SmithKline Beecham Corp
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Filing: 1984-09-12
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Granted: 1985-11-19
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Expires: 2004-09-12
Abstract
Abstract Certain aminoethyl substituted 1,3-benzthiazol- and 1,3-benzoxazol-2(3H)-ones are D 2 -dopamine agonists. These compounds are prepared by reacting an appropriate o-aminophenol or thiophenol with phosgene.
Inventors
- 👤 Orum D. Stringer
- 👤 Joseph Weinstock
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 14:29
CPC Classifications
C; C07; C07D; C07D263/00; C07D263/52; C07D263/54; C07D263/58; A; A61; A61P; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07D277/00; C07D277/60; C07D277/62; C07D277/68
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
62 words
A chemical compound of the formula: ##STR4## in which: X is --S--or --O--; R 1 and R 2 are, each, hydrogen, C 1-6 -alkyl, allyl, benzyl, phenethyl, methoxyphenethyl or hydroxyphenethyl; and R 3 and R 4 are, each, hydroxy, hydrogen, halo, C 1-3 -alkyl or C 1-3 -alkoxy, a pharmaceutically acceptable, acid addition salt thereof or an O-C 2-6 -alkanoyl derivative thereof.
Claim 2
Dependent Claim
62 words
A chemical compound of the formula: ##STR4## in which: X is --S--or --O--; R 1 and R 2 are, each, hydrogen, C 1-6 -alkyl, allyl, benzyl, phenethyl, methoxyphenethyl or hydroxyphenethyl; and R 3 and R 4 are, each, hydroxy, hydrogen, halo, C 1-3 -alkyl or C 1-3 -alkoxy, a pharmaceutically acceptable, acid addition salt thereof or an O-C 2-6 -alkanoyl derivative thereof.
Claim 3
Dependent Claim
15 words
The compound of claim 1 in which R 1 and R 2 are both n-propyl.
Claim 4
Dependent Claim
10 words
The compound of claim 1 in which X is --S--.
Claim 5
Dependent Claim
21 words
The compound of claim 1 in which X is --S--, R 3 is hydrogen and R 4 is 4-hydroxy or hydrogen.
Claim 6
Dependent Claim
15 words
The compound of claim 1 being 4-hydroxy-7-[2-(di-n-propylamino)ethyl]-1,3-benzthiazol-2(3H)-one or a pharmaceutically acceptable, acid addition salt thereof.
Claim 7
Dependent Claim
8 words
The compound of claim 1 being 4-hydroxy-7-[2-(di-n-propylamino)ethyl]-1,3-benzthiazol-2(3H)-one hydrobromide.
Claim 8
Dependent Claim
15 words
The compound of claim 1 being 4-hydroxy-7-[2-(di-n-propylamino)ethyl-1,3-benzoxazol-2(3H)-one or a pharmaceutically acceptable, acid addition salt thereof.
Claim 9
Dependent Claim
15 words
The compound of claim 1 being 7-[2-(di-n-propylamino)ethyl]-1,3-benzthiazol-2(3H)-one or a pharmaceutically acceptable, acid addition salt thereof.
Claim 10
Dependent Claim
15 words
The compound of claim 1 being 7-[2-(n-propylamino)ethyl]-1,3-benzthiazol-2(3H)-one or a pharmaceutically acceptable, acid addition salt thereof.
Claim 11
Dependent Claim
26 words
A pharmaceutical composition having D 2 -agonistic activity comprising an effective therefor but nontoxic quantity of a compound of claim 1 combined with a pharmaceutical carrier.
Claim 12
Dependent Claim
20 words
The composition of claim 10 in which the composition is for oral administration and is effective for treatment of hypertension.
Claim 13
Dependent Claim
30 words
The composition of claim 10 in which the compound is 4-hydroxy-7-[2-(di-n-propylamino)ethyl]-1,3-benzthiazol-2(3H)-one or a pharmaceutically acceptable, acid addition salt thereof and the D 2 -agonistic activity is manifested in anti-hypertensive activity.
Claim 14
Dependent Claim
32 words
The method of inducing D 2 -agonistic activity in a patient in need thereof comprising administering internally to said patient a D 2 -agonistic, nontoxic quantity of a compound of claim 1.
Claim 15
Dependent Claim
16 words
The method of claim 13 in which the patient is hypertensive and the administration is oral.
References Cited (Backward Citations)
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1988-11-18 | 1989-05-20 | 1989-11-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-11-18 | 1993-05-20 | 1993-11-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-11-18 | 1997-05-20 | 1997-11-19 | $7700.00 | Window Closed / Lapsed |