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US4078073A Expired / Lapsed US ⏱️ 0.0 years remaining

N-tricyclic derivatives of azetidine

Assignee: Pfizer Italia SRL
•
Filing: 1976-11-02
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Granted: 1978-03-07
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Expires: 1996-11-02
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Abstract

Abstract Novel N-tricyclic derivatives of azetidine of the formula: ##STR1## wherein A is a --CH 2 --O-- or an --O--CH 2 group, and the remaining substituents being defined in the specification are disclosed. An illustrative compound is 1-[11-(6,11-dihydro-dibenzo [b,e] oxepinyl)]-3-methylamino-azetidine. The compounds are useful for their anti-depressant, anti-convulsant and anxiolytic activities.

Inventors

  • 👤 Piero Melloni
  • 👤 Arturo Della Torre
  • 👤 Francesco Lauria
  • 👤 Norina Passerini
  • 👤 Alessandro Rossi
  • 👤 Raffaele Tommasini

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 13:11
CPC Classifications
C; C07; C07D; C07D205/00; C07D205/02; C07D205/04

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 81 words
A compound of formula: ##STR15## wherein: n 1 is zero or 1 R 5 and R 6 each independently represent hydrogen or C 1 -C 6 alkyl; and one of the Y groups is hydrogen and the other is hydrogen, halogen, C 1 -C 6 alkoxy, trifluoromethyl or methylsulphonyl, provided that, when n 1 is zero, the ##STR16## radical is exclusively bound to the carbon atom in the 3-position of the azetidine radical, and the salts thereof with pharmaceutically acceptable acids.
Claim 2
Dependent Claim 81 words
A compound of formula: ##STR15## wherein: n 1 is zero or 1 R 5 and R 6 each independently represent hydrogen or C 1 -C 6 alkyl; and one of the Y groups is hydrogen and the other is hydrogen, halogen, C 1 -C 6 alkoxy, trifluoromethyl or methylsulphonyl, provided that, when n 1 is zero, the ##STR16## radical is exclusively bound to the carbon atom in the 3-position of the azetidine radical, and the salts thereof with pharmaceutically acceptable acids.
Claim 3
Dependent Claim 6 words
1-[11-(6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 4
Dependent Claim 6 words
1-[11-(2-chloro-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 5
Dependent Claim 6 words
1-[11-(9-chloro-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 6
Dependent Claim 6 words
1-[11-(2-trifluoromethyl-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 7
Dependent Claim 6 words
1-[11-(9-trifluoromethyl-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 8
Dependent Claim 6 words
1-[11-(2-methoxy-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 9
Dependent Claim 6 words
1-[11-(9-methoxy-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 10
Dependent Claim 6 words
1-[11-(2-methylsulphonyl-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 11
Dependent Claim 6 words
1-[11-(9-methylsulphonyl-6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, as claimed in claim 1.
Claim 12
Dependent Claim 6 words
1-[11-(6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylaminomethyl-azetidine, as claimed in claim 1.
Claim 13
Dependent Claim 6 words
1-[11-(6,11-dihydro-dibenzo[b,e]oxepinyl)]-2-methylamino-methyl-azetidine, as claimed in claim 1.
Claim 14
Independent Claim 29 words
A method of treating central nervous system depression consisting essentially of administering to a person suffering therefrom an effective amount of compound 1-[11-(6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, and the pharmaceutically acceptable salts thereof.
Claim 15
Independent Claim 29 words
A method of treating central nervous system depression consisting essentially of administering to a person suffering therefrom an effective amount of compound 1-[11-(6,11-dihydro-dibenzo[b,e]oxepinyl)]-3-methylamino-azetidine, and the pharmaceutically acceptable salts thereof.
Claim 16
Dependent Claim 20 words
The method of claim 13 wherein from 20 to 50 mg. of the compound is administered 2-4 times a day.
Claim 17
Dependent Claim 26 words
An anti-convulsant pharmaceutical composition containing, as the active ingredient thereof, an effective amount of a compound of claim 1, together with a suitable carrier or diluent.
Claim 18
Dependent Claim 22 words
A method of treating convulsions consisting of administering to a person suffering therefrom an effective amount of a compound of claim 1.

References Cited (Backward Citations)

US3509176A Cited
US3991103A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-03-06 1981-09-05 1982-03-07 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-03-06 1985-09-05 1986-03-07 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-03-06 1989-09-05 1990-03-07 $7700.00 Window Closed / Lapsed

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