US3962440A
Expired / Lapsed
US
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Quinoxaline compounds as hypnotic agents
Assignee: Eli Lilly and Co
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Filing: 1973-12-26
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Granted: 1976-06-08
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Expires: 1993-12-26
Abstract
Abstract The present invention is concerned with the use of certain quinoxaline compounds as hypnotic agents.
Inventors
- 👤 Roger L. St. Clair
- 👤 Thomas D. Thibault
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 07:22
CPC Classifications
C; C07; C07D; C07D241/00; C07D241/36; C07D241/38; C07D241/40; C07D241/44
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
161 words
A method for causing a hypnotic effect in a warm-blooded animal which comprises administering to a warm-blooded animal suffering from insomnia an effective amount of an active agent selected from the group consisting of a compound of the formula ##SPC14## wherein n represents 0, 1, or 2; each R independently represents 1. loweralkyl of C 1 -C 4 , 2. loweralkoxy of C 1 -C 4 , 3. loweralkylthio of C 1 -C 4 , 4. cyclopropyl, 5. bromo, 6. chloro, 7. fluoro, 8. nitro, 9. cyano, 10. fluoroalkyl of C 1 -C 2 , 11. amino, or 12. amino mono or disubstituted with loweralkyl of C 1 -C 4 , each independently selected; subject to the limitation that R can represent bromo or chloro only when n represents 2 and one R represents a moiety other than bromo or chloro; and R 1 represents 1. H or 2. methyl; and a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 2
Independent Claim
161 words
A method for causing a hypnotic effect in a warm-blooded animal which comprises administering to a warm-blooded animal suffering from insomnia an effective amount of an active agent selected from the group consisting of a compound of the formula ##SPC14## wherein n represents 0, 1, or 2; each R independently represents 1. loweralkyl of C 1 -C 4 , 2. loweralkoxy of C 1 -C 4 , 3. loweralkylthio of C 1 -C 4 , 4. cyclopropyl, 5. bromo, 6. chloro, 7. fluoro, 8. nitro, 9. cyano, 10. fluoroalkyl of C 1 -C 2 , 11. amino, or 12. amino mono or disubstituted with loweralkyl of C 1 -C 4 , each independently selected; subject to the limitation that R can represent bromo or chloro only when n represents 2 and one R represents a moiety other than bromo or chloro; and R 1 represents 1. H or 2. methyl; and a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 3
Dependent Claim
13 words
The method of claim 1 wherein the warm-blooded animal is a human being.
Claim 4
Dependent Claim
23 words
The method of claim 2 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 5
Dependent Claim
12 words
The method of claim 3 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione.
Claim 6
Dependent Claim
14 words
The method of claim 3 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione monopotassium salt.
Claim 7
Dependent Claim
23 words
The method of claim 2 wherein the active agent is 6-methyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 8
Dependent Claim
23 words
The method of claim 2 wherein the active agent is 6-ethyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 9
Dependent Claim
23 words
The method of claim 2 wherein the active agent is 5-methyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 10
Dependent Claim
23 words
The method of claim 2 wherein the active agent is 2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 11
Independent Claim
92 words
A method for causing a hypnotic effect in a warm-blooded animal which comprises administering to a warm-blooded animal in which it is desired to induce sleep an effective amount of an active agent selected from the group consisting of a compound of the formula ##SPC15## wherein n represents 0, 1, or 2; each R independently represents 1. loweralkyl of C 1 -C 4 , 2. loweralkoxy of C 1 -C 4 , 3. loweralkylthio of C 1 -C 4 , 4. cyclopropyl, 5. bromo, 6. chloro, 7. fluoro, 8. nitro, 9. cyano,
Claim 12
Independent Claim
92 words
A method for causing a hypnotic effect in a warm-blooded animal which comprises administering to a warm-blooded animal in which it is desired to induce sleep an effective amount of an active agent selected from the group consisting of a compound of the formula ##SPC15## wherein n represents 0, 1, or 2; each R independently represents 1. loweralkyl of C 1 -C 4 , 2. loweralkoxy of C 1 -C 4 , 3. loweralkylthio of C 1 -C 4 , 4. cyclopropyl, 5. bromo, 6. chloro, 7. fluoro, 8. nitro, 9. cyano,
Claim 13
Dependent Claim
73 words
fluoroalkyl of C 1 -C 2 , 11. amino, or 12. amino mono or disubstituted with loweralkyl of C 1 -C 4 , each independently selected; subject to the limitation that R can represent bromo or chloro only when n represents 2 and one R represents a moiety other than bromo or chloro; and R 1 represents 1. H or 2. methyl; and a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 14
Dependent Claim
73 words
fluoroalkyl of C 1 -C 2 , 11. amino, or 12. amino mono or disubstituted with loweralkyl of C 1 -C 4 , each independently selected; subject to the limitation that R can represent bromo or chloro only when n represents 2 and one R represents a moiety other than bromo or chloro; and R 1 represents 1. H or 2. methyl; and a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 15
Dependent Claim
13 words
The method of claim 10 wherein the warm-blooded animal is a human being.
Claim 16
Dependent Claim
23 words
The method of claim 11 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 17
Dependent Claim
12 words
The method of claim 12 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione.
Claim 18
Dependent Claim
14 words
The method of claim 12 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione monopotassium salt.
Claim 19
Dependent Claim
23 words
The method of claim 11 wherein the active agent is 6-methyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 20
Dependent Claim
23 words
The method of claim 11 wherein the active agent is 6-ethyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 21
Dependent Claim
23 words
The method of claim 11 wherein the active agent is 5-methyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 22
Dependent Claim
23 words
The method of claim 11 wherein the active agent is 2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 23
Dependent Claim
178 words
A pharmaceutical formulation in dosage unit form adapted for administration to obtain a hypnotic effect, comprising per dosage unit, a hypnotically-effective non-toxic amount within the range from about 10 to about 1000 milligrams of at least one active agent selected from the group consisting of a compound of the formula ##SPC16## wherein n represents 0, 1, or 2; each R independently represents 1. loweralkyl of C 1 -C 4 , 2. loweralkoxy of C 1 -C 4 , 3. loweralkylthio of C 1 -C 4 , 4. cyclopropyl, 5. bromo, 6. chloro, 7. fluoro, 8. nitro, 9. cyano, 10. fluoroalkyl of C 1 -C 2 , 11. amino, or 12. amino mono or disubstituted with loweralkyl of C 1 -C 4 , each independently selected; subject to the limitation that R can represent bromo or chloro only when n represents 2 and one R represents a moiety other than bromo or chloro; and R 1 represents 1. H or 2. methyl; and a pharmaceutically acceptable alkali metal or alkaline earth metal salt and a pharmaceutically acceptable carrier therefor.
Claim 24
Dependent Claim
178 words
A pharmaceutical formulation in dosage unit form adapted for administration to obtain a hypnotic effect, comprising per dosage unit, a hypnotically-effective non-toxic amount within the range from about 10 to about 1000 milligrams of at least one active agent selected from the group consisting of a compound of the formula ##SPC16## wherein n represents 0, 1, or 2; each R independently represents 1. loweralkyl of C 1 -C 4 , 2. loweralkoxy of C 1 -C 4 , 3. loweralkylthio of C 1 -C 4 , 4. cyclopropyl, 5. bromo, 6. chloro, 7. fluoro, 8. nitro, 9. cyano, 10. fluoroalkyl of C 1 -C 2 , 11. amino, or 12. amino mono or disubstituted with loweralkyl of C 1 -C 4 , each independently selected; subject to the limitation that R can represent bromo or chloro only when n represents 2 and one R represents a moiety other than bromo or chloro; and R 1 represents 1. H or 2. methyl; and a pharmaceutically acceptable alkali metal or alkaline earth metal salt and a pharmaceutically acceptable carrier therefor.
Claim 25
Dependent Claim
23 words
The formulation of claim 19 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione or a pharmaceutically acceptable alkali metal or alkaline earth metal salt.
Claim 26
Dependent Claim
12 words
The formulation of claim 20 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione.
Claim 27
Dependent Claim
14 words
The formulation of claim 20 wherein the active agent is 6-trifluoromethyl-2(1H), 3(4H)-quinoxalinedione monopotassium salt.
References Cited (Backward Citations)
US3133056A
Cited
US3594418A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-06-08 | 1979-12-08 | 1980-06-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-06-08 | 1983-12-08 | 1984-06-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-06-08 | 1987-12-08 | 1988-06-08 | $7700.00 | Window Closed / Lapsed |