Macrocyclic beta-secretase inhibitors

Details Macrocyclic beta-secretase inhibitors Macrocyclic beta-secretase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 413/06 (2006.01) A61K 31/00 (2006.01) A61P 25/28 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2575340

Disclosed are novel compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula (I) and at least one compound selected from the group consisting of -secretase inhibitors other than those of formula (I), HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non- steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

Cette invention a pour objet de nouveaux composés de formule (I), ou de sel ou de solvate pharmaceutiquement acceptables, au sein de laquelle R1, R2, R3, n et X sont identiques à la définition fournie par leurs caractéristiques techniques. En outre, cette invention a également pour objet des compositions pharmaceutiques comprenant ces mêmes composés de formule (I). De plus, cette invention porte sur les procédés de traitement d~une affection cognitive ou neurodégénérative, impliquant l~administration, à un patient I, d~un traitement contenant au moins un composé de formule (I) et au moins un composé sélectionné dans le groupe composé d~inhibiteurs de secrétase autres que ceux de formule (I), d~inhibiteurs d~HMG-CoA réductase, d~inhibiteurs de gamma-secrétase, d~agents anti-inflammatoires non stéroïdiens, d~antagonistes récepteurs de N-méthyl-D-aspartate, d~inhibiteurs de cholinestérase et d~anticorps anti-amyloïdes.

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