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US4432985A Expired / Lapsed US ⏱️ 0.0 years remaining

N-alkylated carboxylic acid derivatives as anti-convulsant agents

Assignee: Abbott Laboratories
•
Filing: 1982-03-15
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Granted: 1984-02-21
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Expires: 2002-03-15
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Abstract

Abstract Described are compounds of the formula ##STR1## wherein R is hydrogen or loweralkyl; R 1 is --OR 2 or --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl; n is 0 or 1; R 4 and R 5 independently of one another denote loweralkyl or together form a 5 or 6 membered cycloalkyl substituted by hydrogen or loweralkyl, and together with the nitrogen atom, form a ring; and pharmaceutically acceptable salts thereof and their use as anticonvulsant agents in a method of controlling convulsions or seizures.

Inventors

  • 👤 Alex M. Nadzan
  • 👤 George R. Granneman

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-28 07:59
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/16; C07D295/20; C07D295/215; A; A61; A61K; A61K31/00; A61K31/16; A61K31/17; A61K31/185; A61K31/19; A61K31/195; C07D295/04; C07D295/14; C07D295/145; C07D295/15

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 55 words
A compound of the formula ##STR5## wherein R 1 is --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl, R 4 and R 5 together with the nitrogen atom form a 5 or 6 membered saturated ring substituted by loweralkyl, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 55 words
A compound of the formula ##STR5## wherein R 1 is --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl, R 4 and R 5 together with the nitrogen atom form a 5 or 6 membered saturated ring substituted by loweralkyl, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 6 words
The compound of claim 1: [1-(3,5-dimethylpiperidinyl)]carboxamide.
Claim 4
Dependent Claim 6 words
The compound of claim 1: 1-(3,4-dimethylpyrrolidinyl)carboxamide.
Claim 5
Dependent Claim 73 words
A pharmaceutical composition useful as an anticonvulsant which comprises an effective amount of a compound of the formula ##STR6## wherein R 1 is --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl; R 4 and R 5 together with the nitrogen atom form a 5 or 6 membered saturated ring substituted by loweralkyl; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim 73 words
A pharmaceutical composition useful as an anticonvulsant which comprises an effective amount of a compound of the formula ##STR6## wherein R 1 is --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl; R 4 and R 5 together with the nitrogen atom form a 5 or 6 membered saturated ring substituted by loweralkyl; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 7
Dependent Claim 10 words
The composition of claim 4 wherein the compound is: [1-(3,5-dimethylpiperidinyl)]carboxamide.
Claim 8
Dependent Claim 10 words
The composition of claim 4 wherein the compound is: 1-(3,4-dimethylpyrrolidinyl)carboxamide.
Claim 9
Independent Claim 100 words
A method of controlling convulsions or seizures comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of the formula ##STR7## wherein R is hydrogen or loweralkyl; R 1 is --OR 2 or --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl; n is 0 or 1; R 4 and R 5 independently of one another denote loweralkyl or together with the nitrogen atom form a 5 or 6 membered saturated ring which may be substituted by loweralkyl; or a pharmaceutically acceptable salt thereof.
Claim 10
Independent Claim 100 words
A method of controlling convulsions or seizures comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of the formula ##STR7## wherein R is hydrogen or loweralkyl; R 1 is --OR 2 or --NR 2 R 3 wherein R 2 and R 3 independently of one another denote hydrogen or loweralkyl; n is 0 or 1; R 4 and R 5 independently of one another denote loweralkyl or together with the nitrogen atom form a 5 or 6 membered saturated ring which may be substituted by loweralkyl; or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim 47 words
The method of claim 7 wherein R is hydrogen or loweralkyl, R 1 is OR 2 wherein R 2 is hydrogen, or --NR 2 R 3 wherein R 2 and R 3 are both hydrogen, n is 0 or 1, R 4 and R 5 are loweralkyl.
Claim 12
Dependent Claim 29 words
The method of claim 8 wherein R is hydrogen, R 1 is OR 2 wherein R 2 is hydrogen, n is 1, R 4 and R 5 are n-propyl.
Claim 13
Dependent Claim 29 words
The method of claim 8 wherein R is butyl, R 1 is --OR 2 wherein R 2 is hydrogen, n is 1, R 4 and R 5 are n-propyl.
Claim 14
Dependent Claim 32 words
The method of claim 8 wherein R 1 is --NR 2 R 3 wherein R 2 and R 3 are both hydrogen, n is 0, R 4 and R 5 are n-propyl.
Claim 15
Dependent Claim 11 words
The method of claim 7 wherein the compound is 2-[1-(3,5-dimethylpiperidinyl)]acetic acid.
Claim 16
Dependent Claim 11 words
The method of claim 7 wherein the compound is 2-[1-(3,4-dimethylpyrrolidinyl)]acetic acid.
Claim 17
Dependent Claim 10 words
The method of claim 7 wherein the compound is [1-(3,5-dimethylpiperidinyl)]carboxamide.
Claim 18
Dependent Claim 10 words
The method of claim 7 wherein the compound is 1-(3,4-dimethylpyrrolidinyl)carboxamide.

References Cited (Backward Citations)

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-02-20 1987-08-22 1988-02-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-02-20 1991-08-22 1992-02-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-02-20 1995-08-22 1996-02-21 $7700.00 Window Closed / Lapsed

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