US4089953A
Expired / Lapsed
US
⏱️ 0.0 years remaining
1,5-Benzodiazocines
Assignee: DDSA Pharmaceuticals Ltd
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Filing: 1975-10-15
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Granted: 1978-05-16
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Expires: 1995-10-15
Abstract
Abstract 1,5-Benzodiazocines of the general formula ##STR1## their 5N-oxides, and acid addition salts thereof. In the above formula R 1 =H, Halogen, CF 3 , --CN, --NO, C 1-6 alkyl, C 1-6 alkoxy or C 1-6 alkylthio; R 2 =H, C 1-6 alkyl or furyl; R 3 =H, C 1-6 alkyl, hydroxy-(C 1-6 alkyl), C 2-6 alkenyl or benzyl; and R 4 =phenyl, (C 1-6 alkyl)-phenyl, nitrophenyl, halophenyl or pyridyl. Also the production of such compounds from compounds of the benzodiazepine series.
Inventors
- 👤 Umakant Devdas Shenoy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 08:39
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/70; C07D239/72; C07D239/74; C07D239/76; C07D243/00; C07D243/06; C07D243/10; C07D243/14; C07D243/16; C07D243/18; C07D243/20; C07D245/00; C07D245/04; C07D245/06
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
86 words
A 1,5-Benzodiazepine derivative of the general formula ##STR9## wherein R 1 represents chlorine, a trifluoromethyl, cyano or nitro all in the 8 position; R 2 represents a hydrogen atom or a lower alkyl group; R 3 represents a hydrogen atom, a lower alkyl group, a hydroxy group, a lower alkenyl group or a benzyl group; and A represents a grouping of the general formula ##STR10## in which R 4 represents a phenyl, (lower alkyl) phenyl, nitrophenyl or halophenyl; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
86 words
A 1,5-Benzodiazepine derivative of the general formula ##STR9## wherein R 1 represents chlorine, a trifluoromethyl, cyano or nitro all in the 8 position; R 2 represents a hydrogen atom or a lower alkyl group; R 3 represents a hydrogen atom, a lower alkyl group, a hydroxy group, a lower alkenyl group or a benzyl group; and A represents a grouping of the general formula ##STR10## in which R 4 represents a phenyl, (lower alkyl) phenyl, nitrophenyl or halophenyl; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
16 words
A compound according to claim 1 wherein R 3 is methyl and R 4 is phenyl.
Claim 4
Dependent Claim
1 words
8-chloro-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide.
Claim 5
Dependent Claim
1 words
8-chloro-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide.
Claim 6
Dependent Claim
10 words
8-chloro-4-methyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide or a solvate thereof with methanol, ethanol or isopropanol.
Claim 7
Dependent Claim
10 words
8-chloro-4-methyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide or a solvate thereof with methanol, ethanol or isopropanol.
Claim 8
Dependent Claim
1 words
8-chloro-4-ethyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide.
Claim 9
Dependent Claim
1 words
8-chloro-4-ethyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide.
Claim 10
Dependent Claim
1 words
8-chloro-4-propyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide.
Claim 11
Dependent Claim
1 words
8-chloro-4-propyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide.
Claim 12
Dependent Claim
18 words
An acid addition salt of a compound of claim 1 with a pharmaceutically acceptable inorganic or organic acid.
Claim 13
Dependent Claim
2 words
8-chloro-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 14
Dependent Claim
2 words
8-chloro-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 15
Dependent Claim
2 words
8-chloro-4-methyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 16
Dependent Claim
2 words
8-chloro-4-methyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 17
Dependent Claim
2 words
8-chloro-4-ethyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 18
Dependent Claim
2 words
8-chloro-4-ethyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 19
Dependent Claim
2 words
8-chloro-4-pyropyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 20
Dependent Claim
2 words
8-chloro-4-pyropyl-2-methylamino-6-phenyl-1,5-benzodiazocine-5-oxide hydrochloride.
Claim 21
Dependent Claim
6 words
A solvate according to claim 4.
Claim 22
Dependent Claim
31 words
A tranquilizing, sedative or hypnosis-inducing composition comprising a tranquilizing, sedative, or hypnosis-inducing amount of at least one compound according to claim 1 in admixture with a pharmacologically acceptable diluent or carrier.
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) | 1981-05-15 | 1981-11-14 | 1982-05-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-05-15 | 1985-11-14 | 1986-05-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-05-15 | 1989-11-14 | 1990-05-16 | $7700.00 | Window Closed / Lapsed |