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METHODS FOR THE IMPROVEMENT OF COGNITION WITH FUNCTIONAL ANTAGONISTS OF THE GLYCINE NMDA RECEPTOR COMPLEX.CM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.0678021.A1
Fecha publicacion
25/10/1995
Numero solicitud
EP19940906547

En detalle

Resumen

The use of a compound possessing functional antagonist properties at the NMDA receptor complex through a specific action at the associated strychnine-insensitive glycine site to improve cognition in normal humans and to treat cognitive deficits resulting from chronic neuronal degeneration, acute brain injury, hypoxia, or other neurological disorders is provided. In particular, the compounds possessing functional antagonist properties comprise 1-aminocyclopropanecarboxylic acid, and its pharmaceutically acceptable esters, salts, and acid addition salts or 7-chlorokynurenic acid, and its pharmaceutically acceptable esters, amides, salts, ethers, and acid addition salts.

Reivindicaciones

1. Use of a compound having the formula: <img class="EMIRef" id="588191205-ib0003" /> where A is -CO<2>H, or a pharmaceutically acceptable ester, amide, or salt thereof; and X is -NR<1>R<2> or a pharmaceutically acceptable acid addition salt thereof, and where R<1> and R<2> are independently selected from hydrogen or lower alkyl, optionally substituted with halogen, hydroxyl, alkoxy, oxo, mercapto, aryl, or amino, or R<1> and R<2> together with the nitrogen to which they are attached form a substituted 5-membered or 6-membered heterocycle which can also contain another heteroatom selected from oxygen, sulfur or nitrogen, which is a partial agonist for the strychnine-insensitive glycine site of the NMDA receptor due to a specific interaction with the receptor, and which acts as a functional antagonist of the strychnine-insensitive glycine site of the NMDA receptor complex by reducing or antagonizing the effects of glutamate or NMDA, in the preparation of a medicament for either improving or enhancing memory or cognition. 2. Use of a compound as claimed in claim 1, characterised in that the compound possessing partial agonist properties is selected from 1-aminocyclopropanecarboxylic acid or a pharmaceutically-acceptable salt, amide, and ester thereof. 3. Use of a compound as claimed in claim 2, characterised in that the compound possessing partial agonist properties is 1-aminocyclopropanecarboxylic acid.

Etiquetas

Inventores
Skolnick PhilTrullas RamonFaiman Claudia PViu EugeniaPhil SkolnickRamon TrullasClaudia P FaimanEugenia ViuSkolnickPhilTrullasRamonFaimanClaudia P.ViuEugenia
Solicitantes
Us Gov Health & Human ServConsejo Superior de Investigaciones CientíficasThe Government of the United States of America As Represented By the Secretary of the Department of Health and Human ServicesUs HealthThe Government of the United States of America, As RepresentedSecretary of the Department of Health and Human Services (TheThe Government of the United States of America As Represented By the Secretary of the Department of Health and Human Services, BethesdaConsejo Superior de Investigaciones Cientificas, MadridUs ArmyThe United States of America As Represented By the Department of Health & Human ServicesThe Government of the United States of America, As
Clasificacion ipc
A61K 31/ 16 A IA61K 31/ 195 A IA61K 31/ 19 A IA61K 31/ 21 A IA61K 31/ 47 A IA61K 45/ 00 A IA61P 25/ 00 A IA61P 25/ 08 A IA61P 25/ 28 A IA61P 43/ 00 A IC07C 229/ 48 A IC07C 237/ 24 A IC07D 215/ 48 A I
Clasificacion cpc
4C031/MA014C084/AA174C084/MA174C084/MA234C084/MA354C084/MA364C084/MA374C084/MA434C084/MA444C084/MA524C084/MA554C084/MA654C084/MA664C084/ZA0224C084/ZA0624C084/ZA1524C084/ZA1624C084/ZA1824C084/ZA8924C084/ZC4224C086/AA014C086/AA024C086/BA034C086/BB034C086/BC074C086/BC174C086/BC294C086/CB054C086/ZA024C086/ZA064C086/ZA154C086/ZA164C206/AA014C206/AA024C206/DA134C206/DB114C206/DB414C206/FA294C206/GA064C206/GA214C206/JA524C206/KA014C206/MA144C206/ZA024C206/ZA054C206/ZA064C206/ZA154C206/ZA164C206/ZC424H006/AA034H006/AB214H006/BJ204H006/BJ304H006/BT224H006/BU42A61K31/16A61K31/19A61K31/21A61K31/47A61K45/00A61P25/00A61P25/08A61P25/28A61P43/00&111C07C229/48C07D215/48514/531514/557
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