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US3678036A Expired / Lapsed US ⏱️ 0.0 years remaining

2-substituted amino-1,4-benzodiazepine

Assignee: F Hoffmann La Roche AG
•
Filing: 1968-09-20
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Granted: 1972-07-18
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Expires: 1988-09-20
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Abstract

Abstract 1,4-Benzodiazepines bearing in position-2, either a disubstituted amino group or an GROUP WHEREIN R is lower alkylene and R6 and R7 are either lower alkyl or together with the nitrogen atom form a heterocyclic moiety or an NH-R-phenyl grouping wherein R is as above and certain 4-oxides thereof. Such compounds are useful as muscle relaxants, sedatives and anticonvulsants.

Inventors

  • 👤 Giles Allan Archer
  • 👤 Leo Henryk Sternbach

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-30 09:19
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/02; C07D403/04; A; A61; A61K; A61K31/00

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 53 words
A compound as defined in clam 1 wherein R4 is halogen and is joined to the benzodiazepine nucleus in position-7; R2 and R5 are both hydrogen, R3 is hydrogen and halogen and R6 and R7 is taken together with the nitrogen atom and represents piperidine, i.e., 7-halo-5-(R3-phenyl)-2-piperidino-3H-1,4-benzodiazepine wherein R3 is hydrogen and halogen.
Claim 2
Dependent Claim 17 words
A compound as in claim 2 wherein the 7-halo-group is a 7-chloro group and R3 is hydrogen.
Claim 3
Dependent Claim 38 words
A compound as in claim 1 wherein R4 is halogen, and is joined to the benzodiazepine nucleus in position-7, R2 and R5 are both hydrogen, R3 is hydrogen and halogen, and R6 and R7 are both lower alkyl.
Claim 4
Dependent Claim 18 words
A compound as defined in claim 4 wherein R4 is chlorine and R3 is hydrogen, i.e., 7-chloro-2-dilower alkyl-amino-5-phenyl-3H-1,4-benzodiazepine.
Claim 5
Dependent Claim 25 words
A compound as defined in claim 5 wherein R4 is chloro and R6 and R7 are both methyl, i.e., a compound of the formula 7-chloro-2-dimethylamino-5-phenyl-3H-1,4-benzodiazepine.
Claim 6
Dependent Claim 12 words
A compound selected from the group consisting of compounds of the formula:
Claim 7
Dependent Claim 51 words
A compound as defined in claim 7 wherein R2, R3 and R5 are all hydrogen; R4 is halogen and is joined to the benzodiazepine nucleus in position-7; R is lower alkylene and R6 and R7 are both lower alkyl, i.e., a compound of the formula 7-halo-2-( Beta -dilower alkylamino lower alkyleneamino)-5-phenyl-3H-1,4-benzodiazepine.
Claim 8
Dependent Claim 45 words
A compound as in claim 7 wherein R2, R3 and R5 are all hydrogen; R4 is chlorine and is joined to the 7-position of the benzodiazepine; R is ethylene and R6 and R7 are both ethyl, i.e., a compound of the formula 7-chloro-2-( Beta -diethyl-aminoethylamino)-5-phenyl-3H-1,4-benzodiazepine.
Claim 9
Dependent Claim 12 words
A compound selected from the group consisting of compounds of the formula:
Claim 10
Dependent Claim 38 words
A compound as defined in claim 10 wherein R2, R3 and R5 are all hydrogen; R4 is chlorine and is joined to the benzodiazepine nucleus in position-7 and R is ethylene, i.e., a compound of the formula 7-chloro-2-phenethylamino-5-phenyl-3H-1,4-benzodiazepine.
Claim 11
Dependent Claim 13 words
A compound selected from the group consisting of compounds having the formula of
Claim 12
Dependent Claim 19 words
7-R1-5-(R2phenyl)-2-pyrrolidino-3H-1,4-benzodiazepine 4-oxide wherein R1 and R2 are selected from the group consisting of hydrogen, lower alkyl, halogen and trifluoromethyl.
Claim 13
Dependent Claim 2 words
7-chloro-5-phenyl-2-pyrrolidino-3H-1,4-benzodiazepine 4-oxide.
Claim 14
Dependent Claim 13 words
A member selected from the group consisting of the compound of the formula

References Cited (Backward Citations)

US3419545A Cited
US3462419A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1975-07-18 1976-01-17 1976-07-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1979-07-18 1980-01-17 1980-07-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1983-07-18 1984-01-17 1984-07-18 $7700.00 Window Closed / Lapsed

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