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EP0172458A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Novel biologically active compound having anti-prolyl endopeptidase activity

Assignee: Suntory Ltd
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Filing: 1985-07-30
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Granted: —
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Expires: 2005-07-30
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Abstract

Abstract A novel compound that exhibits inhibitory activity against prolyl endopeptidase and a method for chemical synthesis of said compound, as well as its use as a prolyl endopeptidase inhibitor and an anti-amnesic agent that contains said compound as the active ingredient are provided.

Inventors

  • 👤 Takaharu Tanaka
  • 👤 Naoki Higuchi
  • 👤 Masayuki Saito
  • 👤 Masaki Hashimoto

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-30 16:06
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/08; A; A61; A61P; A61P25/00; A61P25/28; A61P43/00; C07D207/10; C07D207/16

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 28 words
An N-acylpyrrolidine derivative of formula (I): (wherein n is a number of 1 to 4; R is a lower alkyl ester group, -CH 2 0H or aldehyde group).
Claim 2
Dependent Claim 28 words
An N-acylpyrrolidine derivative of formula (I): (wherein n is a number of 1 to 4; R is a lower alkyl ester group, -CH 2 0H or aldehyde group).
Claim 3
Dependent Claim 59 words
A process for producing an N-acylpyrrolidine derivative of formula (II): (wherein n is a number of 1 to 4; R' is a lower alkyl group) by reacting a carboxylic acid, a carboxylic anhydride or a carboxylic acid chloride of the formula: or (wherein n is a number of 1 to 4) with a p roline lower alkyl ester hydrochloride.
Claim 4
Dependent Claim 59 words
A process for producing an N-acylpyrrolidine derivative of formula (II): (wherein n is a number of 1 to 4; R' is a lower alkyl group) by reacting a carboxylic acid, a carboxylic anhydride or a carboxylic acid chloride of the formula: or (wherein n is a number of 1 to 4) with a p roline lower alkyl ester hydrochloride.
Claim 5
Dependent Claim 101 words
A process for producing an N-acylpyrrolidine derivative of formula (IV): (wherein n is a number of 1 to 4) by first reacting a carboxylic acid, a carboxylic anhydride or a carboxylic acid chloride of the formula: or (wherein n is a number of 1 to 4) with a proline lower alkyl ester hydrochloride so as to obtain an N-acylpyrrolidine derivative of formula (II): (wherein n is a number of 1 to 4; R' is a lower alkyl group), reducing said derivative to a compound of formula (III): (wherein n is a number of 1 to 4), and oxidizing said compound (III).
Claim 6
Dependent Claim 101 words
A process for producing an N-acylpyrrolidine derivative of formula (IV): (wherein n is a number of 1 to 4) by first reacting a carboxylic acid, a carboxylic anhydride or a carboxylic acid chloride of the formula: or (wherein n is a number of 1 to 4) with a proline lower alkyl ester hydrochloride so as to obtain an N-acylpyrrolidine derivative of formula (II): (wherein n is a number of 1 to 4; R' is a lower alkyl group), reducing said derivative to a compound of formula (III): (wherein n is a number of 1 to 4), and oxidizing said compound (III).
Claim 7
Dependent Claim 33 words
A prolyl endopeptidase inhibitor comprising an N-acylpyrrolidine derivative of formula (I): (wherein n is a number of 1 to 4; R is a lower alkyl ester group, -CH 2 0H or aldehyde group).
Claim 8
Dependent Claim 33 words
A prolyl endopeptidase inhibitor comprising an N-acylpyrrolidine derivative of formula (I): (wherein n is a number of 1 to 4; R is a lower alkyl ester group, -CH 2 0H or aldehyde group).
Claim 9
Dependent Claim 36 words
An anti-amnesic agent containing as the active ingredient an N-acylpyrrolidine derivative of formula (I): (wherein n is a number of 1 to 4; R is a lower alkyl ester group, -CH 2 OH or aldehyde group).
Claim 10
Dependent Claim 36 words
An anti-amnesic agent containing as the active ingredient an N-acylpyrrolidine derivative of formula (I): (wherein n is a number of 1 to 4; R is a lower alkyl ester group, -CH 2 OH or aldehyde group).

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