EP0201742A2
Expired / Lapsed
EP
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N-Acylpyrrolidine derivatives, processes for preparing them, pharmaceutical composition and use
Assignee: Suntory Ltd
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Filing: 1986-04-16
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Granted: —
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Expires: 2006-04-16
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
- 👤 Masayuki Saitoh
- 👤 Masaki Hashimoto
- 👤 Naoki Higuchi
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 11:04
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; A; A61; A61P; A61P25/00; A61P25/28; A61P43/00; C07D207/08
Claims Analysis
Total Claims: 3
Claim 1
Independent Claim
249 words
A process of producing N-acylpyrrolidine derivatives of the general formula (I): wherein R is hydrogen atom, a lower alkyl group or phenyl group, R 3 is a lower alkyloxycarbonyl group, hydroxymethyl groap or formyl group, when R 1 is hydrogen atom, R 2 is a substituted or unsubstituted phenyloxy group or phenylcarbonyl group or a substituted phenyl group, and when R 1 is a lower alkyl group or phenyl group, R 2 is a substituted or unsubstituted phenyl group, a lower alkyl group, an aralkyl group of 7 to 10 carbon atoms or hydroxy group; or R 1 and R 2 together form a benzylidene group which is unsubstituted or substituted on its aromatic moiety, and n is an integer of 0 to 5, which comprises condensing a carboxylic acid, or a chloride or anhydride thereof of the formula: or wherein R 1 1 R 2 and n have meanings as defined above, with proline, proline alkylester or salt thereof of the formula: wherein R 4 is hydrogen atom or a lower alkyl group, to give a compound of the formula (I) in which R 3 represents -COOR 4 (wherein R 4 is hydrogen atom or a lower alkyl group), and if necessary the formed compound is then reduced to give a compound of the formula (I) in which R 3 represents -CH 2 OH, and if necessary the compound thus obtained is then oxidized to give a compound of the formula (I) in which R 3 represents -CHO.
Claim 2
Dependent Claim
249 words
A process of producing N-acylpyrrolidine derivatives of the general formula (I): wherein R is hydrogen atom, a lower alkyl group or phenyl group, R 3 is a lower alkyloxycarbonyl group, hydroxymethyl groap or formyl group, when R 1 is hydrogen atom, R 2 is a substituted or unsubstituted phenyloxy group or phenylcarbonyl group or a substituted phenyl group, and when R 1 is a lower alkyl group or phenyl group, R 2 is a substituted or unsubstituted phenyl group, a lower alkyl group, an aralkyl group of 7 to 10 carbon atoms or hydroxy group; or R 1 and R 2 together form a benzylidene group which is unsubstituted or substituted on its aromatic moiety, and n is an integer of 0 to 5, which comprises condensing a carboxylic acid, or a chloride or anhydride thereof of the formula: or wherein R 1 1 R 2 and n have meanings as defined above, with proline, proline alkylester or salt thereof of the formula: wherein R 4 is hydrogen atom or a lower alkyl group, to give a compound of the formula (I) in which R 3 represents -COOR 4 (wherein R 4 is hydrogen atom or a lower alkyl group), and if necessary the formed compound is then reduced to give a compound of the formula (I) in which R 3 represents -CH 2 OH, and if necessary the compound thus obtained is then oxidized to give a compound of the formula (I) in which R 3 represents -CHO.
Claim 3
Dependent Claim
26 words
Use of at least one of the products of claim 1 for the preparation of a medicament having anti-prolyl endopeptidase activity for the treatment of amnesia.
References Cited (Backward Citations)
No citation records indexed.
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