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US4405622A Expired / Lapsed US ⏱️ 0.0 years remaining

[1-(1,4-Benzodioxan-2-yl)-4-(4-aminopyrimidin-2-yl]piperazines useful as anti-depressants

Assignee: Syntex USA LLC
•
Filing: 1980-10-16
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Granted: 1983-09-20
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Expires: 2000-10-16
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Abstract

Abstract Novel [1-(1,4-benzodioxan-2-yl)-4-(4-aminopyrimidin-2-yl]piperazines having the general formula <IMAGE> (I) wherein: R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2 and the pharmaceutically acceptable acid addition salts thereof are useful as anti-depressants.

Inventors

  • 👤 Arthur F. Kluge

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 15:36
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/12; C07D319/00; C07D319/10; C07D319/14; C07D319/16; C07D319/20

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 89 words
A composition for reducing, inhibiting or preventing depression in humans which comprises an effective amount of a compound of the formula ##STR8## or the pharmaceutically acceptable acid addition salts thereof wherein: R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2, in admixture with at least one pharmaceutically acceptable excipient.
Claim 2
Dependent Claim 89 words
A composition for reducing, inhibiting or preventing depression in humans which comprises an effective amount of a compound of the formula ##STR8## or the pharmaceutically acceptable acid addition salts thereof wherein: R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2, in admixture with at least one pharmaceutically acceptable excipient.
Claim 3
Independent Claim 90 words
A method for preventing, inhibiting or reducing depression in humans, which comprises administering to a subject in need of such treatment an effective amount of, or a pharmaceutical composition containing an effective amount of, a compound of the formula ##STR9## wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2.
Claim 4
Independent Claim 90 words
A method for preventing, inhibiting or reducing depression in humans, which comprises administering to a subject in need of such treatment an effective amount of, or a pharmaceutical composition containing an effective amount of, a compound of the formula ##STR9## wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2.
Claim 5
Dependent Claim 64 words
A compound having the formula ##STR10## and the pharmaceutically acceptable acid addition salts thereof wherein: R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2.
Claim 6
Dependent Claim 64 words
A compound having the formula ##STR10## and the pharmaceutically acceptable acid addition salts thereof wherein: R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2.
Claim 7
Dependent Claim 19 words
The compound of claim 1 and the pharmaceutically acceptable acid addition salts thereof wherein X and Y are hydrogen.
Claim 8
Dependent Claim 33 words
The compound of claim 1 and the pharmaceutically acceptable acid addition salts thereof wherein R 1 and R 2 are hydrogen; and R 3 and R 4 are independently hydrogen or lower alkyl.
Claim 9
Dependent Claim 19 words
The compound of claim 3 and the pharmaceutically acceptable acid addition salts thereof wherein X and Y are hydrogen.
Claim 10
Dependent Claim 24 words
The compound of claim 4, wherein R 3 and R 4 are hydrogen and n=0, [1-(1,4-benzodioxan-2-yl)-4-(4-aminopyrimidin-2yl)]-piperazine, and the pharmaceutically acceptable acid addition salts thereof.
Claim 11
Dependent Claim 24 words
The compound of claim 4 wherein R 3 and R 4 are hydrogen, and n=1; [1-(1,4-benzodioxan-2-yl-methyl)-4-(4-aminopyrimidin-2-yl)]piperazine and the pharmaceutically acceptable acid addition salts thereof.
Claim 12
Dependent Claim 24 words
The compound of claim 4, wherein R 3 and R 4 are hydrogen and n=2, [1-[2-(1,4-benzodioxan-2-yl)-ethyl]-4-(4-aminopyrimidin-2-yl)]-piperazine, and the pharmaceutically acceptable acid addition salts thereof.

References Cited (Backward Citations)

CA731147A Cited
US2979511A Cited
US3360529A Cited
US3829441A Cited
GB1094982A Cited
BE643853A Cited
US3944549A Cited
US3959283A Cited
BE837386A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-09-19 1987-03-21 1987-09-20 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-09-19 1991-03-21 1991-09-20 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-09-19 1995-03-21 1995-09-20 $7700.00 Window Closed / Lapsed

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