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US4053615A Expired / Lapsed US ⏱️ 0.0 years remaining

Phthalimidopiperidines and anti-convulsant compositions thereof

Assignee: John Wyeth and Brother Ltd
•
Filing: 1976-01-21
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Granted: 1977-10-11
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Expires: 1996-01-21
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Abstract

Abstract Phthalimidopiperidines of the formula ##STR1## are described where R 1 is hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, phenyl(lower)alkyl, pyridyl(lower)alkyl, furyl(lower)alkyl or thienyl(lower)alkyl and R 2 and R 3 are hydrogen or various substituents. The compounds are useful pharmaceutically, particularly as anti-convulsants, and also in some cases as anti-arrhythmic agents and anti-inflammatory agents, and in some cases useful as intermediates for the preparation of 4-aminoquinoline derivatives having anti-malarial activity.

Inventors

  • 👤 John Terence Arnott Boyle
  • 👤 John Christopher Saunders

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 19:58
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/04

Claims Analysis

Total Claims: 23
Claim 1
Independent Claim 64 words
A compound selected from those having the formula ##STR11## and their pharmaceutically acceptable acid addition salts, wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, phenyl(lower)alkyl, pyridyl(lower)alkyl, furyl(lower)alkyl and thienyl(lower)alkyl, and R 2 and R 3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, nitro, amino and di(lower alkyl)amino.
Claim 2
Dependent Claim 64 words
A compound selected from those having the formula ##STR11## and their pharmaceutically acceptable acid addition salts, wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, phenyl(lower)alkyl, pyridyl(lower)alkyl, furyl(lower)alkyl and thienyl(lower)alkyl, and R 2 and R 3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, nitro, amino and di(lower alkyl)amino.
Claim 3
Dependent Claim 35 words
A compound selected from those having the formula ##STR12## and their pharmaceutically acceptable acid addition salts, wherein R 1 is selected from lower alkyl and benzyl and R 2 is selected from nitro and amino.
Claim 4
Dependent Claim 35 words
A compound selected from those having the formula ##STR12## and their pharmaceutically acceptable acid addition salts, wherein R 1 is selected from lower alkyl and benzyl and R 2 is selected from nitro and amino.
Claim 5
Dependent Claim 18 words
A compound as defined in claim 1, which is 1-benzyl-4-phthalimidopiperidine or a pharmaceutically acceptable acid addition salt thereof,
Claim 6
Dependent Claim 18 words
A compound as defined in claim 1, which is 4-phthalimido-piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim 18 words
A compound as defined in claim 1, which is 1-ethyl-3-phthalimido-piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim 18 words
A compound as defined in claim 2, which is 1ethyl-3-(4nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim 18 words
A compound as defined in claim 1, which is 1ethyl-3-(3-nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim 18 words
A compound as defined in claim 2, which is 3-(4-aminophthalimido)-1-ethylpiperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim 18 words
A compound as defined in claim 1, which is 3-(3-aminophthalimido)-1-ethylpiperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Dependent Claim 18 words
A compound as defined in claim 2, which is 4-(4-aminophthalimido)-1-n-butylpiperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 13
Dependent Claim 18 words
A compound as defined in claim 1, which is 1-cyclohexyl-4-(4nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 14
Dependent Claim 18 words
A compound as defined in claim 2, which is 1-n-butyl-4-(4-nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 15
Dependent Claim 19 words
A compound as defined in claim 1, which is 4-(4nitrophthalimido)-1-(3-pyridylmethyl) piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 16
Dependent Claim 18 words
A compound as defined in claim 1, which is 4-(4-chlorophthalimido)-1-(2-phenethyl)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 17
Dependent Claim 18 words
A compound as defined in claim 2, which is 1-benzyl-4(4-nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 18
Dependent Claim 18 words
A compound as defined in claim 2, which is 4-(4-aminophthalimido)-1-benzylpiperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 19
Dependent Claim 18 words
A compound as defined in claim 1, which is 4-(4-nitrophthalimido)-1-(2-phenylethyl)-piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 20
Dependent Claim 18 words
A compound as defined in claim 1, which is 1-ethyl-4-phthalimido-piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 21
Dependent Claim 18 words
A compound as defined in claim 1, which is 1-ethyl-4-(4-nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 22
Dependent Claim 18 words
A compound as defined in claim 1, which is 4-(4-nitrophthalimido)piperidine or a pharmaceutically acceptable acid addition salt thereof.
Claim 23
Dependent Claim 21 words
An anti-convulsant composition comprising an anti-convulsantly effective amount of a compound as claimed in claim 1 and a pharmaceutically tolerable carrier.

References Cited (Backward Citations)

US3316276A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-10-10 1981-04-11 1981-10-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-10-10 1985-04-11 1985-10-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-10-10 1989-04-11 1989-10-11 $7700.00 Window Closed / Lapsed

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