900800-07-9

Upstream product

• 900800-06-8 [(1S,2S)-1-(3-allyl-benzyl)-3-chloro-2-hydroxy-propyl]-carbamic acid tert-butyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1391538-82-1 C₁₅H₂₀BrNO₃ 
• 72824-04-5 2-Allyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 1446478-57-4 C₁₃H₁₆BrNO 
• 1446478-56-3 C₁₀H₉BrO₂ 

Downstream Products

• 939442-46-3 C₃₂H₄₂N₂O₃ 
• 939408-09-0 C₄₁H₄₆N₄O₄ 
• 939442-47-4 C₃₃H₄₄N₂O₃ 
• 939442-27-0 C₃₄H₄₆N₂O₃ 
• 1446478-45-0 C₃₅H₄₉N₃O₃ 
• 939408-10-3 C₃₆H₄₂BrN₃O₄ 
• 1446478-58-5 C₃₂H₄₄N₂O₄ 
• 900800-08-0 [(1S,2R)-1-(3-allyl-benzyl)-2-hydroxy-3-(3-isopropyl-benzylamino)-propyl]-carbamic acid tert-butyl ester 
• 943925-61-9 {(1S,2R)-1-(3-allyl-benzyl)-2-hydroxy-3-[1-(3-isopropyl-phenyl)-cyclopropylamino]-propyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity

We describe a systematic study of how macrocyclization in the P 1-P3 region of hydroxyethylamine-based inhibitors of β-site amyloid precursor protein (APP)-cleaving enzyme (BACE1) modulates in vitro activity. This study reveals that in a number of instances macrocyclization of bis-terminal dienes leads to improved potency toward BACE1 and selectivity against cathepsin D (CatD), as well as greater amyloid β-peptide (Aβ)-lowering activity in HEK293T cells stably expressing APPSW. However, for several closely related analogs the benefits of macrocyclization are attenuated by the effects of other structural features in different regions of the molecules. X-ray crystal structures of three of these novel macrocyclic inhibitors bound to BACE1 revealed their binding conformations and interactions with the enzyme.

Macrocyclic Compounds Useful as Bace Inhibitors

The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS

The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.