1215864-46-2

Upstream product

• 1215864-24-6 2′-bromo-7′-methoxyspiro[1,3-oxazole-4,9′-xanthen]-2-amine 
• 17933-03-8 m-tolylboronic acid 
• 1215864-23-5 2-bromo-7-methoxy-9-methylene-9H-xanthene 
• 65193-10-4 2-bromo-7-methoxy-9H-xanthen-9-one 
• 1215864-17-7 2-(4-bromophenoxy)-5-methoxybenzoic acid 
• 22921-68-2 2-bromo-5-methoxy-benzoic acid 

Relevant academic research and scientific papers

Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and cns penetrable BACE inhibitors for the treatment of alzheimers disease

A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity against the structurally related aspartyl protease cathepsin D. Our efforts resulted in the identification of a potent, orally bioavailable CNS penetrant compound that exhibited in vivo efficacy. A single oral dose of compound 11a resulted in a significant reduction of CNS Aβ40 in naive rats.

SPIRO-TETRACYCLIC RING COMPOUNDS AS BETASECRETASE MODULATORS AND METHODS OF USE

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula (I).