Beta-secretase inhibitors and methods of use

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 9/48 (2006.01) A61K 38/04 (2006.01) A61P 25/28 (2006.01) C07D 207/16 (2006.01) C07D 213/30 (2006.01) C07D 213/40 (2006.01) C07D 215/14 (2006.01) C07D 215/36 (2006.01) C07D 215/54 (2006.01) C07D 307/14 (2006.01) C07D 307/16 (2006.01) C07D 307/20 (2006.01) C07D 307/93 (2006.01) C07D 493/04 (2006.01) C07D 521/00 (2006.01) C07K 5/00 (2006.01) C07K 5/10 (2006.01) C07K 7/00 (2006.01) C07K 7/06 (2006.01) C30B 29/58 (2006.01)

Patent

CA 2464736

Compounds inhibit memapsin 2 .beta.-secretase activity and selectively inhibit memapsin 2 .beta.-secretase activity relative to memapsin 1 .beta.-secretase activity. The compounds are employed in methods to inhibit memapsin 2 .beta.- secretase activity, in the treatment of Alzheimer's disease, in the inhibition of hydrolysis of a .beta.-secretase site of a .beta.-amyloid precursor protein and to decrease .beta.-amyloid protein in in vitro samples and in mammals. Proteins of memapsin 2 associated with compounds of the invention are crystallized.

L'invention concerne des composés qui inhibent l'activité de .beta.-sécrétase de la mémapsine 2 et inhibent de manière sélective l'activité de .beta.-sécrétase de la mémapsine 2 par rapport à l'activité de bêta-sécrétase de la mémapsine 1. Lesdits composés sont employés dans des procédés pour inhiber l'activité de .beta.-sécrétase de la mémapsine 2, dans le traitement de la maladie d'Alzheimer, dans l'inhibition de l'hydrolyse du site de .beta.-sécrétase d'une protéine précurseur .beta.-amyloïde et pour diminuer la concentration de la protéine .beta.-amyloïde dans des échantillonsin vitro et chez les mammifères. Des protéines de mémapsine 2 associées auxdits composés sont cristallisées.

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