Novel .gamma.-secretase inhibitor

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/062 (2006.01) A61K 38/00 (2006.01) A61P 1/18 (2006.01) A61P 3/10 (2006.01) A61P 21/02 (2006.01) A61P 25/00 (2006.01) A61P 25/08 (2006.01) A61P 25/28 (2006.01) A61P 43/00 (2006.01) C07C 323/59 (2006.01) C07K 5/065 (2006.01) C07K 5/08 (2006.01) C12N 9/99 (2006.01) A61K 38/55 (2006.01)

Patent

CA 2695877

It is intended to provide a novel compound that has an excellent .gamma.-secretase inhibitory effect and specifically inhibits A.beta. production. The present invention provides a compound of the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a linear or branched alkyl group having 1 to 4 carbon atoms or a phenyl group; R2 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more phenyl or halogenophenyl groups; R3 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more hydroxyl groups; R4 represents a linear or branched alkyl group having 1 to 4 carbon atoms; and the symbol "*" represents a chiral center. (see formula 1)

L'invention concerne un nouveau composé ayant une excellente activité d'inhibition de la ?-sécrétase et inhibant spécifiquement la production d'Aß. Elle concerne spécifiquement un composé représenté par la formule (1) ci-dessous ou l'un de ses sels pharmaceutiquement acceptables. (Dans la formule (1), R1 représente un groupe alkyle linéaire ou ramifié contenant 1-4 atomes de carbone ou un groupe phényle ; R2 représente un groupe alkyle linéaire ou ramifié contenant 1-4 atomes de carbone qui peut être substitué par un ou plusieurs groupes phényle ou halogénophényle ; R3 représente un groupe alkyle linéaire ou ramifié contenant 1-4 atomes de carbone ou un groupe qui peut être substitué par un ou plusieurs groupes hydroxy ; R4 représente un groupe alkyle linéaire ou ramifié contenant 1-4 atomes de carbone ; et * représente un centre chiral.)

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